-
1
-
-
60449094498
-
Heart disease and stroke statistics-2009 update: a report from the American Heart Association Statistics Committee and Stroke Statistics Subcommittee
-
Lloyd-Jones, D., Adams, R., Carnethon, M., De Simone, G., Ferguson, T.B., Flegal, K., Ford, E., Furie, K., Go, A., Greenlund, K., Haase, N., Hailpern, S., Ho, M., Howard, V., Kissela, B., Kittner, S., Lackland, D., Lisabeth, L., Marelli, A., McDermott, M., Meigs, J., Mozaffarian, D., Nichol, G., Odonnell, C., Roger, V., Rosamond, W., Sacco, R., Sorlie, P., Stafford, R., Steinberger, J., Thom, T., Wasserthiel-Smoller, S., Wong, N., Wylie-Rosett, J., and Hong, Y. (2009) Heart disease and stroke statistics-2009 update: a report from the American Heart Association Statistics Committee and Stroke Statistics Subcommittee. Circulation, 119, e21-e181.
-
(2009)
Circulation
, vol.119
, pp. e21-e181
-
-
Lloyd-Jones, D.1
Adams, R.2
Carnethon, M.3
De Simone, G.4
Ferguson, T.B.5
Flegal, K.6
Ford, E.7
Furie, K.8
Go, A.9
Greenlund, K.10
Haase, N.11
Hailpern, S.12
Ho, M.13
Howard, V.14
Kissela, B.15
Kittner, S.16
Lackland, D.17
Lisabeth, L.18
Marelli, A.19
McDermott, M.20
Meigs, J.21
Mozaffarian, D.22
Nichol, G.23
Odonnell, C.24
Roger, V.25
Rosamond, W.26
Sacco, R.27
Sorlie, P.28
Stafford, R.29
Steinberger, J.30
Thom, T.31
Wasserthiel-Smoller, S.32
Wong, N.33
Wylie-Rosett, J.34
Hong, Y.35
more..
-
2
-
-
17244364283
-
Proteases universally recognize beta strands in their active sites
-
Tyndall, J.D.A., Nall, T., and Fairlie, D.P. (2005) Proteases universally recognize beta strands in their active sites. Chemical Reviews, 105, 973-999.
-
(2005)
Chemical Reviews
, vol.105
, pp. 973-999
-
-
Tyndall, J.D.A.1
Nall, T.2
Fairlie, D.P.3
-
3
-
-
0028961335
-
SCOP: a structural classification of proteins database for the investigation of sequences and structures
-
Murzin, A.G., Brenner, S.E., Hubbard, T., and Chothia, C. (1995) SCOP: a structural classification of proteins database for the investigation of sequences and structures. Journal of Molecular Biology, 247, 536-541.
-
(1995)
Journal of Molecular Biology
, vol.247
, pp. 536-541
-
-
Murzin, A.G.1
Brenner, S.E.2
Hubbard, T.3
Chothia, C.4
-
4
-
-
0036690114
-
Drugs targeting the renin-angiotensin-aldosterone system
-
Zaman, M.A., Oparil, S., and Calhoun, D.A. (2002) Drugs targeting the renin-angiotensin-aldosterone system. Nature Reviews. Drug Discovery, 1, 621-636.
-
(2002)
Nature Reviews. Drug Discovery
, vol.1
, pp. 621-636
-
-
Zaman, M.A.1
Oparil, S.2
Calhoun, D.A.3
-
6
-
-
0346895374
-
Therapeutic potential of renin inhibitors in the management of cardiovascular disorders
-
Stanton, A. (2003) Therapeutic potential of renin inhibitors in the management of cardiovascular disorders. American Journal of Cardiovascular Drugs, 3, 389-394.
-
(2003)
American Journal of Cardiovascular Drugs
, vol.3
, pp. 389-394
-
-
Stanton, A.1
-
7
-
-
0028096969
-
Expression of components of the RAS during prolonged blockade at different levels in primates
-
Samani, N.J., Cumin, F., Kelly, M., and Wood, J.M. (1994) Expression of components of the RAS during prolonged blockade at different levels in primates. The American Journal of Physiology, 267, E612-E619.
-
(1994)
The American Journal of Physiology
, vol.267
, pp. E612-E619
-
-
Samani, N.J.1
Cumin, F.2
Kelly, M.3
Wood, J.M.4
-
8
-
-
33846160571
-
Aspartic proteases in drug discovery
-
Eder, J., Hommel, U., Cumin, F., Martoglio, B., and Gerhartz, B. (2007) Aspartic proteases in drug discovery. Current Pharmaceutical Design, 13, 271-285.
-
(2007)
Current Pharmaceutical Design
, vol.13
, pp. 271-285
-
-
Eder, J.1
Hommel, U.2
Cumin, F.3
Martoglio, B.4
Gerhartz, B.5
-
9
-
-
0019782878
-
The amino terminal amino acid sequence of human angiotensinogen
-
Tewksbury, D.A., Dart, R.A., and Travis, J. (1981) The amino terminal amino acid sequence of human angiotensinogen. Biochemical and Biophysical Research Communications, 99, 1311-1320.
-
(1981)
Biochemical and Biophysical Research Communications
, vol.99
, pp. 1311-1320
-
-
Tewksbury, D.A.1
Dart, R.A.2
Travis, J.3
-
10
-
-
0030293795
-
Angiotensinogen: molecular biology, biochemistry and physiology
-
Morgan, L., Pipkin, F.B., and Kalsheker, N. (1996) Angiotensinogen: molecular biology, biochemistry and physiology. The International Journal of Biochemistry & Cell Biology, 28, 1211-1222.
-
(1996)
The International Journal of Biochemistry & Cell Biology
, vol.28
, pp. 1211-1222
-
-
Morgan, L.1
Pipkin, F.B.2
Kalsheker, N.3
-
11
-
-
0023434194
-
Binding of a reduced peptide inhibitor to the aspartic proteinase from Rhizopus chinensis: implications for a mechanism of action
-
Suguna, K., Padlan, E.A., Smith, C.W., Carlson, W.D., and Davies, D.R. (1987) Binding of a reduced peptide inhibitor to the aspartic proteinase from Rhizopus chinensis: implications for a mechanism of action. Proceedings of the National Academy of Sciences of the United States of America, 84, 7009-7011.
-
(1987)
Proceedings of the National Academy of Sciences of the United States of America
, vol.84
, pp. 7009-7011
-
-
Suguna, K.1
Padlan, E.A.2
Smith, C.W.3
Carlson, W.D.4
Davies, D.R.5
-
13
-
-
0024438910
-
High-resolution X-ray diffraction study of the complex between endothiapepsin and an oligopeptide inhibitor: the analysis of the inhibitor binding and description of the rigid body shift in the enzyme
-
Sali, A., Veerapandian, B., Cooper, J.B., Foundling, S.I., Hoover, D.J., and Blundell, T.L. (1989) High-resolution X-ray diffraction study of the complex between endothiapepsin and an oligopeptide inhibitor: the analysis of the inhibitor binding and description of the rigid body shift in the enzyme. The EMBO Journal, 8, 2179-2180.
-
(1989)
The EMBO Journal
, vol.8
, pp. 2179-2180
-
-
Sali, A.1
Veerapandian, B.2
Cooper, J.B.3
Foundling, S.I.4
Hoover, D.J.5
Blundell, T.L.6
-
14
-
-
0026005186
-
Human immunodeficiency virus-1 protease
-
Use ofpH rate studies and solvent kinetic isotope effects to elucidate details of chemical mechanism
-
Hyland, L.J., Tomaszek, T.A., Jr., and Meek, T.D. (1991) Human immunodeficiency virus-1 protease. 2. Use ofpH rate studies and solvent kinetic isotope effects to elucidate details of chemical mechanism. Biochemistry, 30, 8454-8461.
-
(1991)
Biochemistry
, vol.30
, pp. 8454-8461
-
-
Hyland, L.J.1
Tomaszek, T.A.2
Meek, T.D.3
-
15
-
-
0029080864
-
Thermodynamic mapping of the inhibitor site of the aspartic protease endothiapepsin
-
Gomez, J. and Freire, E. (1995) Thermodynamic mapping of the inhibitor site of the aspartic protease endothiapepsin. Journal of Molecular Biology, 252, 337-340.
-
(1995)
Journal of Molecular Biology
, vol.252
, pp. 337-340
-
-
Gomez, J.1
Freire, E.2
-
16
-
-
0029757151
-
Solution NMR evidence that the HIV-1 protease catalytic aspartyl groups have different ionization states in the complex formed with the asymmetric drug KNI-272
-
Wang, Y.-X., Freedberg, D.I., Yamazaki, T., Wingfield, P.T., Stahl, S.J., Kaufman, J.D., Kiso, Y., and Torchia, D.A. (1996) Solution NMR evidence that the HIV-1 protease catalytic aspartyl groups have different ionization states in the complex formed with the asymmetric drug KNI-272. Biochemistry, 35, 9945-9950.
-
(1996)
Biochemistry
, vol.35
, pp. 9945-9950
-
-
Wang, Y.-X.1
Freedberg, D.I.2
Yamazaki, T.3
Wingfield, P.T.4
Stahl, S.J.5
Kaufman, J.D.6
Kiso, Y.7
Torchia, D.A.8
-
17
-
-
0029863567
-
Inhibition and catalytic mechanism of HIV-1 aspartic protease
-
Silva, A.M., Cachau, R.E., Sham, H.L., and Erickson, J.W. (1996) Inhibition and catalytic mechanism of HIV-1 aspartic protease. Journal of Molecular Biology, 255, 321-330.
-
(1996)
Journal of Molecular Biology
, vol.255
, pp. 321-330
-
-
Silva, A.M.1
Cachau, R.E.2
Sham, H.L.3
Erickson, J.W.4
-
18
-
-
0029859529
-
Ionization states of the catalytic residues in HIV-1 protease
-
Smith, R., Brereton, I.M., Chai, R.Y., and Kent, S.B.H. (1996) Ionization states of the catalytic residues in HIV-1 protease. Nature Structural Biology, 3, 946-950.
-
(1996)
Nature Structural Biology
, vol.3
, pp. 946-950
-
-
Smith, R.1
Brereton, I.M.2
Chai, R.Y.3
Kent, S.B.H.4
-
19
-
-
0031423107
-
Dissection of the pH dependence of inhibitor binding energetics for an aspartic protease: direct measurement of the protonation states of the catalytic aspartic acid residues
-
Xie, D.,Gulnik, S., Collins, L.,Gustchina, E., Suvorov, L., and Erickson, J.W. (1997) Dissection of the pH dependence of inhibitor binding energetics for an aspartic protease: direct measurement of the protonation states of the catalytic aspartic acid residues. Biochemistry, 36, 16166-16172.
-
(1997)
Biochemistry
, vol.36
, pp. 16166-16172
-
-
Xie, D.1
Gulnik, S.2
Collins, L.3
Gustchina, E.4
Suvorov, L.5
Erickson, J.W.6
-
20
-
-
0034778987
-
Follow the protons: a low-barrier hydrogen bond unifies the mechanisms of the aspartic proteases
-
Northrop, D.B. (2001) Follow the protons: a low-barrier hydrogen bond unifies the mechanisms of the aspartic proteases. Accounts of Chemical Research, 34, 790-797.
-
(2001)
Accounts of Chemical Research
, vol.34
, pp. 790-797
-
-
Northrop, D.B.1
-
21
-
-
4744338363
-
Modeling the protonation states of the catalytic aspartates in beta-secretase
-
Rajamani, R. and Reynolds, C.H. (2004) Modeling the protonation states of the catalytic aspartates in beta-secretase. Journal of Medicinal Chemistry, 47, 5159-5166.
-
(2004)
Journal of Medicinal Chemistry
, vol.47
, pp. 5159-5166
-
-
Rajamani, R.1
Reynolds, C.H.2
-
22
-
-
0347694970
-
Determination of the active site protonation state of beta-secretase from molecular dynamics simulation and docking experiment: implications for structure-based inhibitor design
-
Park, H. and Lee, S. (2003) Determination of the active site protonation state of beta-secretase from molecular dynamics simulation and docking experiment: implications for structure-based inhibitor design. Journal of the American Chemical Society, 125, 16416-16422.
-
(2003)
Journal of the American Chemical Society
, vol.125
, pp. 16416-16422
-
-
Park, H.1
Lee, S.2
-
23
-
-
15744387343
-
Evolutionarily conserved functional mechanics across pepsin-like and retroviral aspartic proteases
-
Cascella, M., Micheletti, C., Rothlisberger, U., and Carloni, P. (2005) Evolutionarily conserved functional mechanics across pepsin-like and retroviral aspartic proteases. Journal of the American Chemical Society, 127, 3734-3742.
-
(2005)
Journal of the American Chemical Society
, vol.127
, pp. 3734-3742
-
-
Cascella, M.1
Micheletti, C.2
Rothlisberger, U.3
Carloni, P.4
-
24
-
-
26444552906
-
Functional plasticity in the substrate binding site of beta-secretase
-
Gorfe, A.A. and Caflisch, A. (2005) Functional plasticity in the substrate binding site of beta-secretase. Structure (London, England: 1993), 13, 1487-1498.
-
(2005)
Structure (London, England: 1993)
, vol.13
, pp. 1487-1498
-
-
Gorfe, A.A.1
Caflisch, A.2
-
25
-
-
0024538619
-
Structure of recombinant human renin, a target for cardiovascular-active drugs, at 2.5 A resolution
-
Sielecki, A.R., Hayakawa, K., Fujinaga, M., Murphy, M.E.P., Fraser, M., Muir, A.K., Carilli, C.T., Lewicki, J.A., Baxter, J.D., and James, M.N.G. (1989) Structure of recombinant human renin, a target for cardiovascular-active drugs, at 2.5 A resolution. Science, 243, 1346-1350.
-
(1989)
Science
, vol.243
, pp. 1346-1350
-
-
Sielecki, A.R.1
Hayakawa, K.2
Fujinaga, M.3
Murphy, M.E.P.4
Fraser, M.5
Muir, A.K.6
Carilli, C.T.7
Lewicki, J.A.8
Baxter, J.D.9
James, M.N.G.10
-
26
-
-
0026683982
-
X-ray analyses of peptide-inhibitor complexes define the structural basis of specificity for human and mouse renins
-
Dhanaraj, V., Dealwis, C.G., Frazao, C., Badasso, M., Sibanda, B.L., Tickle, I.J., Cooper, J.B., Driessen, H.P.C., Newman, M., Aguilar, C.,Wood, S.P., Blundell,T.L., Hobart, P.M., Geoghegan, K.F., Ammirati, M.J., Danley, D.E., Oconnor, B.A., and Hoover, D.J. (1992) X-ray analyses of peptide-inhibitor complexes define the structural basis of specificity for human and mouse renins. Nature, 357, 466-470.
-
(1992)
Nature
, vol.357
, pp. 466-470
-
-
Dhanaraj, V.1
Dealwis, C.G.2
Frazao, C.3
Badasso, M.4
Sibanda, B.L.5
Tickle, I.J.6
Cooper, J.B.7
Driessen, H.P.C.8
Newman, M.9
Aguilar, C.10
Wood, S.P.11
Blundell, T.L.12
Hobart, P.M.13
Geoghegan, K.F.14
Ammirati, M.J.15
Danley, D.E.16
Oconnor, B.A.17
Hoover, D.J.18
-
27
-
-
0027050188
-
Direct observation by X-ray analysis of the tetrahedral 'intermediate' of aspartic proteinases
-
Veerapandian, B., Cooper, J.B., Sali, A., Blundell,T.L., Rosati, R.L., Dominy, B.W., Damon, D.B., and Hoover, D.J. (1992) Direct observation by X-ray analysis of the tetrahedral 'intermediate' of aspartic proteinases. Protein Science: A Publication of the Protein Society, 1, 322-330.
-
(1992)
Protein Science: A Publication of the Protein Society
, vol.1
, pp. 322-330
-
-
Veerapandian, B.1
Cooper, J.B.2
Sali, A.3
Blundell, T.L.4
Rosati, R.L.5
Dominy, B.W.6
Damon, D.B.7
Hoover, D.J.8
-
28
-
-
44949239669
-
The catalytic mechanism of an aspartic proteinase explored with neutron and X-ray diffraction
-
Coates, L., Tuan, H.-F., Tomanicek, S., Kovalevsky, A., Mustyakimov, M., Erskine, P., and Cooper, J. (2008) The catalytic mechanism of an aspartic proteinase explored with neutron and X-ray diffraction. Journal of the American Chemical Society, 130, 7235-7237.
-
(2008)
Journal of the American Chemical Society
, vol.130
, pp. 7235-7237
-
-
Coates, L.1
Tuan, H.-F.2
Tomanicek, S.3
Kovalevsky, A.4
Mustyakimov, M.5
Erskine, P.6
Cooper, J.7
-
29
-
-
0029268976
-
Enzymic characterization of purified recombinant human renin
-
Pilote, L., McKercher, G., Thibeault, D., and Lamarre, D. (1995) Enzymic characterization of purified recombinant human renin. Biochemistry and Cell Biology, 73, 163-170.
-
(1995)
Biochemistry and Cell Biology
, vol.73
, pp. 163-170
-
-
Pilote, L.1
McKercher, G.2
Thibeault, D.3
Lamarre, D.4
-
30
-
-
0033141673
-
Tyrosine-83 of human renin contributes to biphasic pH dependence of the renin-angiotensinogen reaction
-
Nasir, U.M., Suzuki, F., Nagai, T., Nakagawa, T., and Nakamura, Y. (1999) Tyrosine-83 of human renin contributes to biphasic pH dependence of the renin-angiotensinogen reaction. Bioscience, Biotechnology, and Biochemistry, 63, 1143-1150.
-
(1999)
Bioscience, Biotechnology, and Biochemistry
, vol.63
, pp. 1143-1150
-
-
Nasir, U.M.1
Suzuki, F.2
Nagai, T.3
Nakagawa, T.4
Nakamura, Y.5
-
31
-
-
0031989626
-
Two peaks in pH dependence of renin-angiotensinogen reaction
-
Nasir, U.M., Takahashi, K., Nagai, T., Nakagawa, T., Suzuki, F., and Nakamura, Y. (1998) Two peaks in pH dependence of renin-angiotensinogen reaction. Bioscience, Biotechnology, and Biochemistry, 62, 338-340.
-
(1998)
Bioscience, Biotechnology, and Biochemistry
, vol.62
, pp. 338-340
-
-
Nasir, U.M.1
Takahashi, K.2
Nagai, T.3
Nakagawa, T.4
Suzuki, F.5
Nakamura, Y.6
-
32
-
-
0037085353
-
Substrate and inhibitor profile of BACE (beta-secretase) and comparison with other mammalian aspartic proteases
-
Gruninger-Leitch, F., Schlatter, D., Kung, E., Nelbock, P., and Dobeli, H. (2002) Substrate and inhibitor profile of BACE (beta-secretase) and comparison with other mammalian aspartic proteases. The Journal of Biological Chemistry, 277, 4687-4693.
-
(2002)
The Journal of Biological Chemistry
, vol.277
, pp. 4687-4693
-
-
Gruninger-Leitch, F.1
Schlatter, D.2
Kung, E.3
Nelbock, P.4
Dobeli, H.5
-
33
-
-
0019351886
-
The enzymic digestion of elastin at acidic pH
-
Collins, J.F. and Fine, R. (1981) The enzymic digestion of elastin at acidic pH. Biochimica et Biophysica Acta, 657, 295-303.
-
(1981)
Biochimica et Biophysica Acta
, vol.657
, pp. 295-303
-
-
Collins, J.F.1
Fine, R.2
-
34
-
-
0026323860
-
The crystal structures of recombinant glycosylated human renin alone and in complex with a transition state analog inhibitor
-
Rahuel, J., Priestle, J., and Gruetter, M.G. (1991) The crystal structures of recombinant glycosylated human renin alone and in complex with a transition state analog inhibitor. Journal of Structural Biology, 107, 227-230.
-
(1991)
Journal of Structural Biology
, vol.107
, pp. 227-230
-
-
Rahuel, J.1
Priestle, J.2
Gruetter, M.G.3
-
35
-
-
0033941893
-
Structurebased drug design: the discovery of novel nonpeptide orally active inhibitors of human renin
-
Rahuel, J., Rasetti, V., Maibaum, J., Rueger, H., Goschke, R., Cohen, N.C., Stutz, S., Cumin, F., Fuhrer, W., Wood, J.M., and Grutter, M.G. (2000) Structurebased drug design: the discovery of novel nonpeptide orally active inhibitors of human renin. Chemistry & Biology, 7, 493-504.
-
(2000)
Chemistry & Biology
, vol.7
, pp. 493-504
-
-
Rahuel, J.1
Rasetti, V.2
Maibaum, J.3
Rueger, H.4
Goschke, R.5
Cohen, N.C.6
Stutz, S.7
Cumin, F.8
Fuhrer, W.9
Wood, J.M.10
Grutter, M.G.11
-
36
-
-
9644295730
-
The discovery and preparation of disubstituted novel amino-arylpiperidine-based renin inhibitors
-
Cody, W.L., Holsworth, D.D., Powell, N.A., Jalaie, M., Zhang, E., Wang, W., Samas, B., Bryant, J., Ostroski, R., Ryan, M.J., and Edmunds, J.J. (2005) The discovery and preparation of disubstituted novel amino-arylpiperidine-based renin inhibitors. Bioorganic & Medicinal Chemistry, 13, 59-68.
-
(2005)
Bioorganic & Medicinal Chemistry
, vol.13
, pp. 59-68
-
-
Cody, W.L.1
Holsworth, D.D.2
Powell, N.A.3
Jalaie, M.4
Zhang, E.5
Wang, W.6
Samas, B.7
Bryant, J.8
Ostroski, R.9
Ryan, M.J.10
Edmunds, J.J.11
-
37
-
-
0033577692
-
Substituted piperidines: highly potent renin inhibitors due to induced fit adaptation of the active site
-
Vieira, E., Binggeli, A., Breu, V., Bur, D., Fischli, W., Guller, R., Hirth, G., Marki, H.P.,Muller, M., Oefner, C., Scalone, M., Stadler, H., Wilhelm, M., and Wostl, W. (1999) Substituted piperidines: highly potent renin inhibitors due to induced fit adaptation of the active site. Bioorganic & Medicinal Chemistry Letters, 9, 1397-1402.
-
(1999)
Bioorganic & Medicinal Chemistry Letters
, vol.9
, pp. 1397-1402
-
-
Vieira, E.1
Binggeli, A.2
Breu, V.3
Bur, D.4
Fischli, W.5
Guller, R.6
Hirth, G.7
Marki, H.P.8
Muller, M.9
Oefner, C.10
Scalone, M.11
Stadler, H.12
Wilhelm, M.13
Wostl, W.14
-
38
-
-
0003694381
-
Piperidine-renin inhibitors compounds with improved physicochemical properties
-
Guller, R., Binggeli, A., Breu, V., Bur, D., Fischli, W., Hirth, G., Jenny, C., Kansy, M., Montavon, F.,Muller, M., Oefner, C., Stadler, H., Vieira, E., Wilhelm, M., Wostl, W., and Marki, H.P. (1999) Piperidine-renin inhibitors compounds with improved physicochemical properties. Bioorganic & Medicinal Chemistry Letters, 9, 1403-1408.
-
(1999)
Bioorganic & Medicinal Chemistry Letters
, vol.9
, pp. 1403-1408
-
-
Guller, R.1
Binggeli, A.2
Breu, V.3
Bur, D.4
Fischli, W.5
Hirth, G.6
Jenny, C.7
Kansy, M.8
Montavon, F.9
Muller, M.10
Oefner, C.11
Stadler, H.12
Vieira, E.13
Wilhelm, M.14
Wostl, W.15
Marki, H.P.16
-
39
-
-
0033102135
-
Renin inhibition by substituted piperidines: a novel paradigm for the inhibition of monomeric aspartic proteinases
-
Oefner, C., Binggeli, A., Breu, V., Bur, D., Clozel, J.P., Darcy, A., Dorn, A., Fischli, W., Gruninger, F., Guller, R., Hirth, G., Marki, H.P., Mathews, S., Muller, M., Ridley, R.G., Stadler, H., Vieira, E., Wilhelm, M., Winkler, F.K., and Wostl, W. (1999) Renin inhibition by substituted piperidines: a novel paradigm for the inhibition of monomeric aspartic proteinases? Chemistry & Biology, 6, 127-131.
-
(1999)
Chemistry & Biology
, vol.6
, pp. 127-131
-
-
Oefner, C.1
Binggeli, A.2
Breu, V.3
Bur, D.4
Clozel, J.P.5
Darcy, A.6
Dorn, A.7
Fischli, W.8
Gruninger, F.9
Guller, R.10
Hirth, G.11
Marki, H.P.12
Mathews, S.13
Muller, M.14
Ridley, R.G.15
Stadler, H.16
Vieira, E.17
Wilhelm, M.18
Winkler, F.K.19
Wostl, W.20
more..
-
40
-
-
0035273245
-
Piperidine renin inhibitors: from leads to drug candidates
-
Marki, H.P., Binggeli, A., Bittner, B., Bohner-Lang, V., Breu, V., Bur, D., Coassolo, P., Clozel, J.P., Darcy, A., Doebeli, H., Fischli, W., Funk, C., Foricher, J., Giller, T., Gruninger, F., Guenzi, A., Guller, R., Hartung, T., Hirth, G., Jenny, C., Kansy, M., Klinkhammer, U., Lave, T., Lohri, B., Luft, F.C., Mervaala, E.M., Muller, D.N., Muller, M., Montavon, F., Oefner, C., Qiu, C., Reichel, A., Sanwald-Ducray, P., Scalone, M., Schleimer, M., Schmid, R., Stadler, H., Treiber, A., Valdenaire, O., Vieira, E.,Waldmeier, P.,Wiegand-Chou, R., Wilhelm, M.,Wostl, W., Zell, M., and Zell, R. (2001) Piperidine renin inhibitors: from leads to drug candidates. Farmaco (Societa Chimica Italiana: 1989), 56, 21-27.
-
(2001)
Farmaco (Societa Chimica Italiana: 1989)
, vol.56
, pp. 21-27
-
-
Marki, H.P.1
Binggeli, A.2
Bittner, B.3
Bohner-Lang, V.4
Breu, V.5
Bur, D.6
Coassolo, P.7
Clozel, J.P.8
Darcy, A.9
Doebeli, H.10
Fischli, W.11
Funk, C.12
Foricher, J.13
Giller, T.14
Gruninger, F.15
Guenzi, A.16
Guller, R.17
Hartung, T.18
Hirth, G.19
Jenny, C.20
Kansy, M.21
Klinkhammer, U.22
Lave, T.23
Lohri, B.24
Luft, F.C.25
Mervaala, E.M.26
Muller, D.N.27
Muller, M.28
Montavon, F.29
Oefner, C.30
Qiu, C.31
Reichel, A.32
Sanwald-Ducray, P.33
Scalone, M.34
Schleimer, M.35
Schmid, R.36
Stadler, H.37
Treiber, A.38
Valdenaire, O.39
Vieira, E.40
Waldmeier, P.41
Wiegand-Chou, R.42
Wilhelm, M.43
Wostl, W.44
Zell, M.45
Zell, R.46
more..
-
41
-
-
33644967829
-
Ketopiperazine-based renin inhibitors: optimization of the 'C' ring
-
Holsworth, D.D., Cai, C., Cheng, X.-M., Cody, W.L., Downing, D.M., Erasga, N., Lee, C., Powell, N.A., Edmunds, J.J., Stier, M., Jalaie, M., Zhang, E., McConnell, P., Ryan, M.J., Bryant, J., Li, T., Kasani, A., Hall, E., Subedi, R., Rahim, M., and Maiti, S. (2006) Ketopiperazine-based renin inhibitors: optimization of the 'C' ring. Bioorganic & Medicinal Chemistry Letters, 16, 2500-2504.
-
(2006)
Bioorganic & Medicinal Chemistry Letters
, vol.16
, pp. 2500-2504
-
-
Holsworth, D.D.1
Cai, C.2
Cheng, X.-M.3
Cody, W.L.4
Downing, D.M.5
Erasga, N.6
Lee, C.7
Powell, N.A.8
Edmunds, J.J.9
Stier, M.10
Jalaie, M.11
Zhang, E.12
McConnell, P.13
Ryan, M.J.14
Bryant, J.15
Li, T.16
Kasani, A.17
Hall, E.18
Subedi, R.19
Rahim, M.20
Maiti, S.21
more..
-
42
-
-
17144388295
-
Equipotent activity in both enantiomers of a series of ketopiperazine-based renin inhibitors
-
Powell, N.A., Clay, E.H., Holsworth, D.D., Bryant, J.W., Ryan, M.J., Jalaie, M., Zhang, E., and Edmunds, J.J. (2005) Equipotent activity in both enantiomers of a series of ketopiperazine-based renin inhibitors. Bioorganic & Medicinal Chemistry Letters, 15, 2371-2374.
-
(2005)
Bioorganic & Medicinal Chemistry Letters
, vol.15
, pp. 2371-2374
-
-
Powell, N.A.1
Clay, E.H.2
Holsworth, D.D.3
Bryant, J.W.4
Ryan, M.J.5
Jalaie, M.6
Zhang, E.7
Edmunds, J.J.8
-
43
-
-
38849188537
-
Cloning, characterization and site-directed mutagenesis of canine renin
-
Bukhtiyarov, Y., Zecher, M., Panemangalore, R., Wu, Z., Bruno, J.G., Yuan, J., Xu, Z., Dillard, L.W., McGeehan, G.M., Harrison, R.K., and Scott, B.B. (2007) Cloning, characterization and site-directed mutagenesis of canine renin. Journal of Biochemistry, 142, 671-680.
-
(2007)
Journal of Biochemistry
, vol.142
, pp. 671-680
-
-
Bukhtiyarov, Y.1
Zecher, M.2
Panemangalore, R.3
Wu, Z.4
Bruno, J.G.5
Yuan, J.6
Xu, Z.7
Dillard, L.W.8
McGeehan, G.M.9
Harrison, R.K.10
Scott, B.B.11
-
44
-
-
0020541678
-
Novel renin inhibitors containing the amino acid statine
-
Boger, J., Lohr, N.S., Ulm, E.H., Poe, M., Blaine, E.H., Fanelli, G.M., Lin, T.Y., Payne, L.S., Schorn, T.W., LaMont, B.I., Vassil, T.C., Stabilito, I.I., and Veber, D.F. (1983) Novel renin inhibitors containing the amino acid statine. Nature, 303, 81-91.
-
(1983)
Nature
, vol.303
, pp. 81-91
-
-
Boger, J.1
Lohr, N.S.2
Ulm, E.H.3
Poe, M.4
Blaine, E.H.5
Fanelli, G.M.6
Lin, T.Y.7
Payne, L.S.8
Schorn, T.W.9
LaMont, B.I.10
Vassil, T.C.11
Stabilito, I.I.12
Veber, D.F.13
-
45
-
-
0026753520
-
Species specificity of renin kinetics in transgenic rats harboring the human renin and angiotensinogen genes
-
Ganten, D., Wagner, J., Zeh, K., Bader, M., Michel, J.B., Paul, M., Zimmermann, F., Ruf, P., Hilgenfeldt, U., and Ganten, U. (1992) Species specificity of renin kinetics in transgenic rats harboring the human renin and angiotensinogen genes. Proceedings of the National Academy of Sciences of the United States of America, 89, 7806-7811.
-
(1992)
Proceedings of the National Academy of Sciences of the United States of America
, vol.89
, pp. 7806-7811
-
-
Ganten, D.1
Wagner, J.2
Zeh, K.3
Bader, M.4
Michel, J.B.5
Paul, M.6
Zimmermann, F.7
Ruf, P.8
Hilgenfeldt, U.9
Ganten, U.10
-
46
-
-
85026154669
-
High human renin hypertension in transgenic rats
-
Bohlender, J., Fukamizu, A., Lippoldt, A., Nomura, T., Dietz, R., Menard, J., Murakami, K., Luft, F.C., and Ganten, D. (1997) High human renin hypertension in transgenic rats. Hypertension, 29, 428-434.
-
(1997)
Hypertension
, vol.29
, pp. 428-434
-
-
Bohlender, J.1
Fukamizu, A.2
Lippoldt, A.3
Nomura, T.4
Dietz, R.5
Menard, J.6
Murakami, K.7
Luft, F.C.8
Ganten, D.9
-
47
-
-
0029866957
-
Human renin-dependent hypertension in rats transgenic for human angiotensinogen
-
Bohlender, J., Menard, J., Wagner, J., Luft, F.C., and Ganten, D. (1996)Human renin-dependent hypertension in rats transgenic for human angiotensinogen. Hypertension, 27, 535-541.
-
(1996)
Hypertension
, vol.27
, pp. 535-541
-
-
Bohlender, J.1
Menard, J.2
Wagner, J.3
Luft, F.C.4
Ganten, D.5
-
48
-
-
0027190950
-
Chimeric renin-angiotensin system demonstrates sustained increase in blood pressure of transgenic mice carrying both human renin and human angiotensinogen genes
-
Fukamizu, A., Sugimura, K., Takimoto, E., Sugiyama, F., Seo, S.M., Takahashi, S., Hatae, T., Kawijara, N., Yagami, K., and Murakami, K. (1993) Chimeric renin-angiotensin system demonstrates sustained increase in blood pressure of transgenic mice carrying both human renin and human angiotensinogen genes. The Journal of Biological Chemistry, 268, 11617.
-
(1993)
The Journal of Biological Chemistry
, vol.268
, pp. 11617
-
-
Fukamizu, A.1
Sugimura, K.2
Takimoto, E.3
Sugiyama, F.4
Seo, S.M.5
Takahashi, S.6
Hatae, T.7
Kawijara, N.8
Yagami, K.9
Murakami, K.10
-
49
-
-
0032617112
-
Hypertension-induced end-organ damage: a new transgenic approach to an old problem
-
Luft, F.C., Mervaala, E., Muller, D.N., Gross, V., Schmidt, F., Park, J.K., Schmitz, C., Lippoldt, A., Breu, V., Dechend, R., Dragun, D., Schneider, W., Ganten, D., and Haller, H. (1999) Hypertension-induced end-organ damage: a new transgenic approach to an old problem. Hypertension, 33, 212-218.
-
(1999)
Hypertension
, vol.33
, pp. 212-218
-
-
Luft, F.C.1
Mervaala, E.2
Muller, D.N.3
Gross, V.4
Schmidt, F.5
Park, J.K.6
Schmitz, C.7
Lippoldt, A.8
Breu, V.9
Dechend, R.10
Dragun, D.11
Schneider, W.12
Ganten, D.13
Haller, H.14
-
50
-
-
0014401555
-
Peptide inhibitors of the renin-angiotensin system
-
Kokubu, T., Ueda, E., Fujimoto, S., Hiwada, K., and Kato, A. (1968) Peptide inhibitors of the renin-angiotensin system. Nature, 217, 456-460.
-
(1968)
Nature
, vol.217
, pp. 456-460
-
-
Kokubu, T.1
Ueda, E.2
Fujimoto, S.3
Hiwada, K.4
Kato, A.5
-
51
-
-
0348019883
-
Specific inhibition of renin by an angiotensinogen analog: studies in sodium depletion and renindependent hypertension
-
Burton, J., Cody, R.J., Jr., Herd, J.A., and Haber, E. (1980) Specific inhibition of renin by an angiotensinogen analog: studies in sodium depletion and renindependent hypertension. Proceedings of the National Academy of Sciences of the United States of America, 77, 5476-5481.
-
(1980)
Proceedings of the National Academy of Sciences of the United States of America
, vol.77
, pp. 5476-5481
-
-
Burton, J.1
Cody, R.J.2
Herd, J.A.3
Haber, E.4
-
52
-
-
0022357221
-
New class of inhibitors specific for human renin
-
Part A, Theory and Practice
-
Papaioannou, S., Hansen, D., Jr., Babler, M., Yang, P.C., Bittner, S., Miller, A., and Clare, M. (1985) New class of inhibitors specific for human renin. Clinical and Experimental Hypertension. Part A, Theory and Practice, A7, 1243-1250.
-
(1985)
Clinical and Experimental Hypertension
, vol.7
, pp. 1243-1250
-
-
Papaioannou, S.1
Hansen, D.2
Babler, M.3
Yang, P.C.4
Bittner, S.5
Miller, A.6
Clare, M.7
-
53
-
-
0019256202
-
A substrate analog inhibitor of renin that is effective in vivo
-
Cody, R.J., Burton, J., Evin, G., Poulsen, K., Herd, J.A., and Haber, E. (1980) A substrate analog inhibitor of renin that is effective in vivo. Biochemical and Biophysical Research Communications, 97, 230-240.
-
(1980)
Biochemical and Biophysical Research Communications
, vol.97
, pp. 230-240
-
-
Cody, R.J.1
Burton, J.2
Evin, G.3
Poulsen, K.4
Herd, J.A.5
Haber, E.6
-
54
-
-
0002903441
-
Analog approaches to the structure of the transition state in enzyme reactions
-
Wolfenden, R. (1972) Analog approaches to the structure of the transition state in enzyme reactions. Accounts of Chemical Research, 5, 10-18.
-
(1972)
Accounts of Chemical Research
, vol.5
, pp. 10-18
-
-
Wolfenden, R.1
-
56
-
-
0029436599
-
Renin Inhibitors
-
Rosenberg, S.H. (1995) Renin Inhibitors, Elsevier Science, vol. 32, pp. 37-114.
-
(1995)
Elsevier Science
, vol.32
, pp. 37-114
-
-
Rosenberg, S.H.1
-
57
-
-
0014784381
-
Pepstatin, a new pepsin inhibitor produced by actinomycetes
-
Umezawa, H., Aoyagi, T., Morishima, H., Matsuzaki, M., Hamada, M., and Takeuchi, T. (1970) Pepstatin, a new pepsin inhibitor produced by actinomycetes. The Journal of Antibiotics, 23, 259-260.
-
(1970)
The Journal of Antibiotics
, vol.23
, pp. 259-260
-
-
Umezawa, H.1
Aoyagi, T.2
Morishima, H.3
Matsuzaki, M.4
Hamada, M.5
Takeuchi, T.6
-
58
-
-
0022472377
-
Design and synthesis of a potent and specific renin inhibitor with a prolonged duration of action in vivo
-
Thaisrivongs, S., Pals, D.T.,Harris, D.W., Kati, W.M., and Turner, S.R. (1986) Design and synthesis of a potent and specific renin inhibitor with a prolonged duration of action in vivo. Journal of Medicinal Chemistry, 29, 2088-2090.
-
(1986)
Journal of Medicinal Chemistry
, vol.29
, pp. 2088-2090
-
-
Thaisrivongs, S.1
Pals, D.T.2
Harris, D.W.3
Kati, W.M.4
Turner, S.R.5
-
59
-
-
0028964620
-
Terlakiren: an orally active renin inhibitor in the guinea pig
-
Mangiapane, M.L., Wester, R.T., Holt, W.F., Ellery, S.S., Simpson, K.A., Schelhorn, T.M., Smith, A.H., Purcell, I.M., and Murphy, W.R. (1995) Terlakiren: an orally active renin inhibitor in the guinea pig. Drug Development Research, 34, 361-368.
-
(1995)
Drug Development Research
, vol.34
, pp. 361-368
-
-
Mangiapane, M.L.1
Wester, R.T.2
Holt, W.F.3
Ellery, S.S.4
Simpson, K.A.5
Schelhorn, T.M.6
Smith, A.H.7
Purcell, I.M.8
Murphy, W.R.9
-
60
-
-
0022379041
-
Dipeptide glycols: a new class of renin inhibitors
-
Hanson, G.J., Baran, J.S., Lindberg, T., Walsh, G.M., Papaioannou, S.E., Babler, M., Bittner, S.E., Yang, P.C., and Dal Corobbo, M. (1985) Dipeptide glycols: a new class of renin inhibitors. Biochemical and Biophysical Research Communications, 132, 155-160.
-
(1985)
Biochemical and Biophysical Research Communications
, vol.132
, pp. 155-160
-
-
Hanson, G.J.1
Baran, J.S.2
Lindberg, T.3
Walsh, G.M.4
Papaioannou, S.E.5
Babler, M.6
Bittner, S.E.7
Yang, P.C.8
Dal Corobbo, M.9
-
61
-
-
0023849663
-
Renin inhibitors
-
FEBS Letters
-
Kleinert, H.D., Luly, J.R., Marcotte, P.A., Perun, T.J., Plattner, J.J., and Stein, H. (1988) Renin inhibitors. Improvements in the stability and biological activity of small peptides containing novel Leu-Val replacements. FEBS Letters, 230, 38-42.
-
(1988)
Improvements in the stability and biological activity of small peptides containing novel Leu-Val replacements
, vol.230
, pp. 38-42
-
-
Kleinert, H.D.1
Luly, J.R.2
Marcotte, P.A.3
Perun, T.J.4
Plattner, J.J.5
Stein, H.6
-
62
-
-
0023676335
-
Synthesis and biological activity of some transition-state inhibitors of human renin
-
Buehlmayer, P., Caselli, A., Fuhrer, W., Goeschke, R., Rasetti, V., Rueger, H., Stanton, J.L., Criscione, L., and Wood, J.M. (1988) Synthesis and biological activity of some transition-state inhibitors of human renin. Journal of Medicinal Chemistry, 31, 1839-1846.
-
(1988)
Journal of Medicinal Chemistry
, vol.31
, pp. 1839-1846
-
-
Buehlmayer, P.1
Caselli, A.2
Fuhrer, W.3
Goeschke, R.4
Rasetti, V.5
Rueger, H.6
Stanton, J.L.7
Criscione, L.8
Wood, J.M.9
-
63
-
-
0024340317
-
CGP 38 560: orally active, low-molecular-weight renin inhibitor with high potency and specificity
-
Wood, J.M., Criscione, L., De Gasparo, M., Buhlmayer, P., Rueger, H., Stanton, J.L., Jupp, R.A., and Kay, J. (1989) CGP 38 560: orally active, low-molecular-weight renin inhibitor with high potency and specificity. Journal of Cardiovascular Pharmacology, 14, 221-226.
-
(1989)
Journal of Cardiovascular Pharmacology
, vol.14
, pp. 221-226
-
-
Wood, J.M.1
Criscione, L.2
De Gasparo, M.3
Buhlmayer, P.4
Rueger, H.5
Stanton, J.L.6
Jupp, R.A.7
Kay, J.8
-
64
-
-
0022409744
-
Renin inhibitors
-
Syntheses of subnanomolar, competitive, transitionstate analog inhibitors containing a novel analog of statine
-
Boger, J., Payne, L.S., Perlow, D.S., Lohr, N.S., Poe, M., Blaine, E.H., Ulm, E.H., Schorn, T.W., LaMont, B.I., Lin, T.-Y., Kawai, M., Rich, D.H., and Veber, D.F. (1985) Renin inhibitors. Syntheses of subnanomolar, competitive, transitionstate analog inhibitors containing a novel analog of statine. Journal of Medicinal Chemistry, 28, 1779-1790.
-
(1985)
Journal of Medicinal Chemistry
, vol.28
, pp. 1779-1790
-
-
Boger, J.1
Payne, L.S.2
Perlow, D.S.3
Lohr, N.S.4
Poe, M.5
Blaine, E.H.6
Ulm, E.H.7
Schorn, T.W.8
LaMont, B.I.9
Lin, T.-Y.10
Kawai, M.11
Rich, D.H.12
Veber, D.F.13
-
65
-
-
0025607164
-
Pharmacokinetics and tissue distribution of the renin inhibitor N-(2-(R)-benzyl-3-tert-butyl-sulfonyl-propionyl)-His-Cha(c)Val-N-butylamine in marmosets
-
Cumin, F., Schnell, C., Richert, P., Raschdorf, F., Probst, A., Schmid, K., Wood, J.M., and De Gasparo, M. (1990) Pharmacokinetics and tissue distribution of the renin inhibitor N-(2-(R)-benzyl-3-tert-butyl-sulfonyl-propionyl)-His-Cha(c)Val-N-butylamine in marmosets. Drug Metabolism and Disposition: The Biological Fate of Chemicals, 18, 831-835.
-
(1990)
Drug Metabolism and Disposition: The Biological Fate of Chemicals
, vol.18
, pp. 831-835
-
-
Cumin, F.1
Schnell, C.2
Richert, P.3
Raschdorf, F.4
Probst, A.5
Schmid, K.6
Wood, J.M.7
De Gasparo, M.8
-
66
-
-
0024368885
-
Pharmacological investigations of a new renin inhibitor in normal sodium-unrestricted volunteers
-
De Gasparo, M., Cumin, F., Nussberger, J., Guyenne, T.T., Wood, J.M., and Menard, J. (1989) Pharmacological investigations of a new renin inhibitor in normal sodium-unrestricted volunteers. British Journal of Clinical Pharmacology, 27, 587-596.
-
(1989)
British Journal of Clinical Pharmacology
, vol.27
, pp. 587-596
-
-
De Gasparo, M.1
Cumin, F.2
Nussberger, J.3
Guyenne, T.T.4
Wood, J.M.5
Menard, J.6
-
67
-
-
0027479677
-
Discovery of remikiren as the first orally active renin inhibitor
-
Clozel, J.P. and Fischli, W. (1993) Discovery of remikiren as the first orally active renin inhibitor. Arzneimittel-Forschung, 43, 260-270.
-
(1993)
Arzneimittel-Forschung
, vol.43
, pp. 260-270
-
-
Clozel, J.P.1
Fischli, W.2
-
68
-
-
0025738927
-
Ro 42-5892 is a potent orally active renin inhibitor in primates
-
Fischli, W., Clozel, J.P., El Amrani, K., Wostl, W., Neidhart, W., Stadler, H., and Branca, Q. (1991) Ro 42-5892 is a potent orally active renin inhibitor in primates. Hypertension, 18, 22-31.
-
(1991)
Hypertension
, vol.18
, pp. 22-31
-
-
Fischli, W.1
Clozel, J.P.2
El Amrani, K.3
Wostl, W.4
Neidhart, W.5
Stadler, H.6
Branca, Q.7
-
69
-
-
0027245555
-
Comparative effects of three different potent renin inhibitors in primates
-
Clozel, J.P. and Fischli, W. (1993) Comparative effects of three different potent renin inhibitors in primates. Hypertension, 22, 9-17.
-
(1993)
Hypertension
, vol.22
, pp. 9-17
-
-
Clozel, J.P.1
Fischli, W.2
-
70
-
-
0029929451
-
Pharmacokinetics of remikiren, a potent orally active inhibitor of human renin, in rat, dog and primates
-
Coassolo, P., Fischli,W., Clozel, J.P., and Chou, R.C. (1996) Pharmacokinetics of remikiren, a potent orally active inhibitor of human renin, in rat, dog and primates. Xenobiotica; the Fate of Foreign Compounds in Biological Systems, 26, 333-340.
-
(1996)
Xenobiotica; the Fate of Foreign Compounds in Biological Systems
, vol.26
, pp. 333-340
-
-
Coassolo, P.1
Fischli, W.2
Clozel, J.P.3
Chou, R.C.4
-
71
-
-
0029969207
-
Excretion and metabolism of remikiren, a potent orally active inhibitor of primate renin
-
Jauch, R., Schmid, P., Fischli, W., Meister, W., Maurer, R., and Wendt, G. (1996) Excretion and metabolism of remikiren, a potent orally active inhibitor of primate renin. Xenobiotica; the Fate of Foreign Compounds in Biological Systems, 26, 285-290.
-
(1996)
Xenobiotica; the Fate of Foreign Compounds in Biological Systems
, vol.26
, pp. 285-290
-
-
Jauch, R.1
Schmid, P.2
Fischli, W.3
Meister, W.4
Maurer, R.5
Wendt, G.6
-
72
-
-
0030005173
-
Distribution of remikiren, a potent orally active inhibitor of human renin, in laboratory animals
-
Richter, W.F., Whitby, B.R., and Chou, R.C. (1996) Distribution of remikiren, a potent orally active inhibitor of human renin, in laboratory animals. Xenobiotica; the Fate of Foreign Compounds in Biological Systems, 26, 243-250.
-
(1996)
Xenobiotica; the Fate of Foreign Compounds in Biological Systems
, vol.26
, pp. 243-250
-
-
Richter, W.F.1
Whitby, B.R.2
Chou, R.C.3
-
73
-
-
0027246493
-
Hemodynamics, biochemical effects, and pharmacokinetics of the renin inhibitor remikiren in healthy human subjects
-
Kleinbloesem, C.H., Weber, C., Fahrner, E., Dellenbach, M., Welker, H., Schroter, V., and Belz, G.G. (1993) Hemodynamics, biochemical effects, and pharmacokinetics of the renin inhibitor remikiren in healthy human subjects. Clinical Pharmacology and Therapeutics, 53, 585-591.
-
(1993)
Clinical Pharmacology and Therapeutics
, vol.53
, pp. 585-591
-
-
Kleinbloesem, C.H.1
Weber, C.2
Fahrner, E.3
Dellenbach, M.4
Welker, H.5
Schroter, V.6
Belz, G.G.7
-
74
-
-
0025938930
-
Effect of the renin response during renin inhibition: oral Ro 42-5892 in normal humans
-
Camenzind, E., Nussberger, J., Juillerat, L., Munafo, A., Fischli, W., Coassolo, P., Van Brummelen, P., Kelinbloesem, C.H., Waeber, B., and Brunner, H.R. (1991) Effect of the renin response during renin inhibition: oral Ro 42-5892 in normal humans. Journal of Cardiovascular Pharmacology, 18, 299-307.
-
(1991)
Journal of Cardiovascular Pharmacology
, vol.18
, pp. 299-307
-
-
Camenzind, E.1
Nussberger, J.2
Juillerat, L.3
Munafo, A.4
Fischli, W.5
Coassolo, P.6
Van Brummelen, P.7
Kelinbloesem, C.H.8
Waeber, B.9
Brunner, H.R.10
-
75
-
-
0026560294
-
Blood pressure control by the renin-angiotensin system in normotensive subjects
-
Kiowski,W., Linder, L., Kleinbloesem, C., van Brummelen, P., and Buhler, F.R. (1992) Blood pressure control by the renin-angiotensin system in normotensive subjects. Assessment by angiotensin converting enzyme and renin inhibition. Circulation, 85, 1-8.
-
(1992)
Assessment by angiotensin converting enzyme and renin inhibition. Circulation
, vol.85
, pp. 1-8
-
-
Kiowski, W.1
Linder, L.2
Kleinbloesem, C.3
van Brummelen, P.4
Buhler, F.R.5
-
76
-
-
0028210554
-
Blood pressure effects of acute intravenous renin or oral angiotensin converting enzyme inhibition in essential hypertension
-
Azizi, M., Guyene, T.T., Chatellier, G., and Menard, J. (1994) Blood pressure effects of acute intravenous renin or oral angiotensin converting enzyme inhibition in essential hypertension. Journal of Hypertension, 12, 419-420.
-
(1994)
Journal of Hypertension
, vol.12
, pp. 419-420
-
-
Azizi, M.1
Guyene, T.T.2
Chatellier, G.3
Menard, J.4
-
77
-
-
0027235991
-
Comparison of blood pressure and angiotensin responses to the renin inhibitor Ro 42-5892 and the angiotensin converting enzyme inhibitor enalapril in essential hypertension
-
van den Meiracker, A.H., Admiraal, P.J., Derkx, F.H., Kleinbloesem, C., Man int Veld, A.J., van Brummelen, P., Mulder, P., and Schalekamp, M.A. (1993) Comparison of blood pressure and angiotensin responses to the renin inhibitor Ro 42-5892 and the angiotensin converting enzyme inhibitor enalapril in essential hypertension. Journal of Hypertension, 11, 831-841.
-
(1993)
Journal of Hypertension
, vol.11
, pp. 831-841
-
-
van den Meiracker, A.H.1
Admiraal, P.J.2
Derkx, F.H.3
Kleinbloesem, C.4
Man int Veld, A.J.5
van Brummelen, P.6
Mulder, P.7
Schalekamp, M.A.8
-
78
-
-
0027381605
-
Efficacy and tolerability of the renin inhibitor Ro 42-5892 in patients with hypertension
-
Rongen, G.A., Lenders, J.W., Kleinbloesem, C.H., Weber, C., Welker, H., Fahrner, E., Pozenel, H., Woittiez, A.J., Haug, G., and Buchmann, M.S. (1993) Efficacy and tolerability of the renin inhibitor Ro 42-5892 in patients with hypertension. Clinical Pharmacology and Therapeutics, 54, 567-571.
-
(1993)
Clinical Pharmacology and Therapeutics
, vol.54
, pp. 567-571
-
-
Rongen, G.A.1
Lenders, J.W.2
Kleinbloesem, C.H.3
Weber, C.4
Welker, H.5
Fahrner, E.6
Pozenel, H.7
Woittiez, A.J.8
Haug, G.9
Buchmann, M.S.10
-
79
-
-
0028136988
-
Ciprokiren (Ro 44-9375)
-
Fischli, W., Clozel, J.P., Breu, V., Buchmann, S., Mathews, S., Stadler, H., Vieira, E., and Wostl, W. (1994) Ciprokiren (Ro 44-9375). A renin inhibitor with increasing effects on chronic treatment. Hypertension, 24, 163-170.
-
(1994)
A renin inhibitor with increasing effects on chronic treatment. Hypertension
, vol.24
, pp. 163-170
-
-
Fischli, W.1
Clozel, J.P.2
Breu, V.3
Buchmann, S.4
Mathews, S.5
Stadler, H.6
Vieira, E.7
Wostl, W.8
-
80
-
-
0023731219
-
Effects of the renin inhibitor A-64662 in monkeys and rats with varying baseline plasma renin activity
-
Kleinert, H.D., Martin, D., Chekal, M.A., Kadam, J., Luly, J.R., Plattner, J.J., Perun, T.J., and Luther, R.R. (1988) Effects of the renin inhibitor A-64662 in monkeys and rats with varying baseline plasma renin activity. Hypertension, 11, 613-621.
-
(1988)
Hypertension
, vol.11
, pp. 613-621
-
-
Kleinert, H.D.1
Martin, D.2
Chekal, M.A.3
Kadam, J.4
Luly, J.R.5
Plattner, J.J.6
Perun, T.J.7
Luther, R.R.8
-
81
-
-
0024369806
-
Hemodynamic and humoral effects of the new renin inhibitor enalkiren in normal humans
-
Delabays, A., Nussberger, J., Porchet, M., Waeber, B., Hoyos, P., Boger, R., Glassman, H., Kleinert, H.D., Luther, R., and Brunner, H.R. (1989)Hemodynamic and humoral effects of the new renin inhibitor enalkiren in normal humans. Hypertension, 13, 941-951.
-
(1989)
Hypertension
, vol.13
, pp. 941-951
-
-
Delabays, A.1
Nussberger, J.2
Porchet, M.3
Waeber, B.4
Hoyos, P.5
Boger, R.6
Glassman, H.7
Kleinert, H.D.8
Luther, R.9
Brunner, H.R.10
-
82
-
-
0025855012
-
Renal and endocrine responses to a renin inhibitor, enalkiren, in normal humans
-
Cordero, P., Fisher, N.D., Moore, T.J., Gleason, R., Williams, G.H., and Hollenberg, N.K. (1991) Renal and endocrine responses to a renin inhibitor, enalkiren, in normal humans. Hypertension, 17, 510-511.
-
(1991)
Hypertension
, vol.17
, pp. 510-511
-
-
Cordero, P.1
Fisher, N.D.2
Moore, T.J.3
Gleason, R.4
Williams, G.H.5
Hollenberg, N.K.6
-
83
-
-
0025375432
-
Prolonged duration of blood pressure response to enalkiren, the novel dipeptide renin inhibitor, in essential hypertension
-
Boger, R.S., Glassman, H.N.,Cavanaugh, J.H., Schmitz, P.J., Lamm, J., Moyse, D., Cohen, A., Kleinert, H.D., and Luther, R.R. (1990) Prolonged duration of blood pressure response to enalkiren, the novel dipeptide renin inhibitor, in essential hypertension. Hypertension, 15, 835-841.
-
(1990)
Hypertension
, vol.15
, pp. 835-841
-
-
Boger, R.S.1
Glassman, H.N.2
Cavanaugh, J.H.3
Schmitz, P.J.4
Lamm, J.5
Moyse, D.6
Cohen, A.7
Kleinert, H.D.8
Luther, R.R.9
-
84
-
-
0025302484
-
Assessment of renin dependency of hypertension with a dipeptide renin inhibitor
-
Weber, M.A., Neutel, J.M., Essinger, I., Glassman, H.N., Boger, R.S., and Luther, R. (1990) Assessment of renin dependency of hypertension with a dipeptide renin inhibitor. Circulation, 81, 1768-1770.
-
(1990)
Circulation
, vol.81
, pp. 1768-1770
-
-
Weber, M.A.1
Neutel, J.M.2
Essinger, I.3
Glassman, H.N.4
Boger, R.S.5
Luther, R.6
-
85
-
-
0025060409
-
Effects of a novel renin inhibitor in patients with essential hypertension
-
Bursztyn, M., Gavras, I., Tifft, C.P., Luther, R., Boger, R., and Gavras, H. (1990) Effects of a novel renin inhibitor in patients with essential hypertension. Journal of Cardiovascular Pharmacology, 15, 493-500.
-
(1990)
Journal of Cardiovascular Pharmacology
, vol.15
, pp. 493-500
-
-
Bursztyn, M.1
Gavras, I.2
Tifft, C.P.3
Luther, R.4
Boger, R.5
Gavras, H.6
-
86
-
-
0025147729
-
Clinical pharmacology of enalkiren, a novel, dipeptide renin inhibitor
-
Glassman, H.N., Kleinert, H.D., Boger, R.S., Moyse, D.M., Griffiths, A.N., and Luther, R.R. (1990) Clinical pharmacology of enalkiren, a novel, dipeptide renin inhibitor. Journal of Cardiovascular Pharmacology, 16. (Suppl. 4), S76-S81.
-
(1990)
Journal of Cardiovascular Pharmacology
, vol.16
, Issue.4
, pp. S76-S81
-
-
Glassman, H.N.1
Kleinert, H.D.2
Boger, R.S.3
Moyse, D.M.4
Griffiths, A.N.5
Luther, R.R.6
-
87
-
-
0026740226
-
C-terminal modifications of nonpeptide renin inhibitors: improved oral bioavailability via modification of physicochemical properties
-
Boyd, S.A., Fung, A.K., Baker, W.R., Mantei, R.A., Armiger, Y.L., Stein, H.H., Cohen, J., Egan, D.A., Barlow, J.L., and Klinghofer, V. (1992) C-terminal modifications of nonpeptide renin inhibitors: improved oral bioavailability via modification of physicochemical properties. Journal ofMedicinal Chemistry, 35, 1735-1740.
-
(1992)
Journal ofMedicinal Chemistry
, vol.35
, pp. 1735-1740
-
-
Boyd, S.A.1
Fung, A.K.2
Baker, W.R.3
Mantei, R.A.4
Armiger, Y.L.5
Stein, H.H.6
Cohen, J.7
Egan, D.A.8
Barlow, J.L.9
Klinghofer, V.10
-
88
-
-
0026698259
-
Discovery of a peptide-based renin inhibitor with oral bioavailability and efficacy
-
Kleinert, H.D., Rosenberg, S.H., Baker, W.R., Stein, H.H., Klinghofer, V., Barlow, J., Spina, K., Polakowski, J., Kovar, P., Cohen, J., and Denissen, J. (1992) Discovery of a peptide-based renin inhibitor with oral bioavailability and efficacy. Science, 257, 1940-1950.
-
(1992)
Science
, vol.257
, pp. 1940-1950
-
-
Kleinert, H.D.1
Rosenberg, S.H.2
Baker, W.R.3
Stein, H.H.4
Klinghofer, V.5
Barlow, J.6
Spina, K.7
Polakowski, J.8
Kovar, P.9
Cohen, J.10
Denissen, J.11
-
89
-
-
0027396090
-
Studies directed toward the design of orally active renin inhibitors
-
Some factors influencing the absorption of small peptides
-
Rosenberg, S.H., Spina, K.P., Woods, K.W., Polakowski, J., Martin, D.L., Yao, Z., Stein, H.H., Cohen, J., Barlow, J.L., Egan, D.A., Tricarico, K.A., Baker, W.R., and Kleinert, H.D. (1993) Studies directed toward the design of orally active renin inhibitors. 1. Some factors influencing the absorption of small peptides. Journal of Medicinal Chemistry, 36, 449-450.
-
(1993)
Journal of Medicinal Chemistry
, vol.36
, pp. 449-450
-
-
Rosenberg, S.H.1
Spina, K.P.2
Woods, K.W.3
Polakowski, J.4
Martin, D.L.5
Yao, Z.6
Stein, H.H.7
Cohen, J.8
Barlow, J.L.9
Egan, D.A.10
Tricarico, K.A.11
Baker, W.R.12
Kleinert, H.D.13
-
90
-
-
0027535899
-
Studies directed toward the design of orally active renin inhibitors
-
Development of the efficacious, bioavailable renin inhibitor (2S)-2-benzyl-3-[[(1-methylpiperazin-4-yl)sulfonyl]propionyl]-3-thiazol-4-yl-lalanine amide of (2S,3R,4S)-2-amino-1-cyclohexyl-3,4-dihydroxy-6-methylheptane (A-72517)
-
Rosenberg, S.H., Spina, K.P., Condon, S.L., Polakowski, J., Yao, Z., Kovar, P., Stein, H.H., Cohen, J., Barlow, J.L., Klinghofer, V., Egan, D.A., Tricarico, K.A., Perun, T.J., Baker, W.R., and Kleinert, H.D. (1993) Studies directed toward the design of orally active renin inhibitors. 2. Development of the efficacious, bioavailable renin inhibitor (2S)-2-benzyl-3-[[(1-methylpiperazin-4-yl)sulfonyl]propionyl]-3-thiazol-4-yl-lalanine amide of (2S,3R,4S)-2-amino-1-cyclohexyl-3,4-dihydroxy-6-methylheptane (A-72517). Journal of Medicinal Chemistry, 36, 460-467.
-
(1993)
Journal of Medicinal Chemistry
, vol.36
, pp. 460-467
-
-
Rosenberg, S.H.1
Spina, K.P.2
Condon, S.L.3
Polakowski, J.4
Yao, Z.5
Kovar, P.6
Stein, H.H.7
Cohen, J.8
Barlow, J.L.9
Klinghofer, V.10
Egan, D.A.11
Tricarico, K.A.12
Perun, T.J.13
Baker, W.R.14
Kleinert, H.D.15
-
91
-
-
0028895715
-
Dose-dependent effects of the renin inhibitor zankiren HCl after a single oral dose in mildly sodium-depleted normotensive subjects
-
Menard, J., Boger, R.S., Moyse, D.M., Guyene, T.T., Glassman, H.N., and Kleinert, H.D. (1995) Dose-dependent effects of the renin inhibitor zankiren HCl after a single oral dose in mildly sodium-depleted normotensive subjects. Circulation, 91, 330-340.
-
(1995)
Circulation
, vol.91
, pp. 330-340
-
-
Menard, J.1
Boger, R.S.2
Moyse, D.M.3
Guyene, T.T.4
Glassman, H.N.5
Kleinert, H.D.6
-
92
-
-
0026625690
-
Structure-activity relationships of a series of 2-amino-4-thiazole-containing renin inhibitors
-
Patt,W.C.,Hamilton, H.W., Taylor, M.D., Ryan, M.J., Taylor, D.G., Jr., Connolly, C.J.C., Doherty, A.M., Klutchko, S.R., Sircar, I., Steinbaugh, B.A., Batley, B.L., Painchaud, C.A., Rapundalo, S.T., Michniewicz, B.M., and Olson, S.C. (1992) Structure-activity relationships of a series of 2-amino-4-thiazole-containing renin inhibitors. Journal of Medicinal Chemistry, 35, 2562-2570.
-
(1992)
Journal of Medicinal Chemistry
, vol.35
, pp. 2562-2570
-
-
Patt, W.C.1
Hamilton, H.W.2
Taylor, M.D.3
Ryan, M.J.4
Taylor, D.G.5
Connolly, C.J.C.6
Doherty, A.M.7
Klutchko, S.R.8
Sircar, I.9
Steinbaugh, B.A.10
Batley, B.L.11
Painchaud, C.A.12
Rapundalo, S.T.13
Michniewicz, B.M.14
Olson, S.C.15
-
93
-
-
0002924501
-
A novel orally active renin inhibitor containing 2-amino-4-thiazolyl-alanine at P2 with a long duration of action in a primate model of hypertension
-
Patt, W.C., Hamilton, H.W., Ryan, M.J., Painchaud, C.A., Taylor, M.D., Rapundalo, S.T., Batley, B.L., Connolly, C.J.C., and Taylor, D.G., Jr. (1992) A novel orally active renin inhibitor containing 2-amino-4-thiazolyl-alanine at P2 with a long duration of action in a primate model of hypertension. Medicinal Chemistry Research, 2, 10-15.
-
(1992)
Medicinal Chemistry Research
, vol.2
, pp. 10-15
-
-
Patt, W.C.1
Hamilton, H.W.2
Ryan, M.J.3
Painchaud, C.A.4
Taylor, M.D.5
Rapundalo, S.T.6
Batley, B.L.7
Connolly, C.J.C.8
Taylor, D.G.9
-
94
-
-
26744435258
-
Absorption, biotransformation and excretion of the renin inhibitor, CI-992, and its P1-P10 isostere in the bile-duct-cannulated (BDC) rat
-
Stewart, B.H., Lu, R.H.H., and Chan, O.H. (1992) Absorption, biotransformation and excretion of the renin inhibitor, CI-992, and its P1-P10 isostere in the bile-duct-cannulated (BDC) rat. Pharmaceutical Research, 9, S295.
-
(1992)
Pharmaceutical Research
, vol.9
, pp. S295
-
-
Stewart, B.H.1
Lu, R.H.H.2
Chan, O.H.3
-
95
-
-
0028904424
-
Evaluation of physicochemical parameters important to the oral bioavailability of peptide-like compounds: implications for the synthesis of renin inhibitors
-
Hamilton, H.W., Steinbaugh, B.A., Stewart, B.H., Chan, O.H., Schmid, H.L., Schroeder, R., Ryan, M.J., Keiser, J., Taylor, M.D., Blankley, C.J., Kaltenbronn, J.S., Wright, J., and Hicks, J. (1995) Evaluation of physicochemical parameters important to the oral bioavailability of peptide-like compounds: implications for the synthesis of renin inhibitors. Journal of Medicinal Chemistry, 38, 1446-1455.
-
(1995)
Journal of Medicinal Chemistry
, vol.38
, pp. 1446-1455
-
-
Hamilton, H.W.1
Steinbaugh, B.A.2
Stewart, B.H.3
Chan, O.H.4
Schmid, H.L.5
Schroeder, R.6
Ryan, M.J.7
Keiser, J.8
Taylor, M.D.9
Blankley, C.J.10
Kaltenbronn, J.S.11
Wright, J.12
Hicks, J.13
-
96
-
-
0026058492
-
1,2,4-Triazolo[4,3-a]pyrazine derivatives with human renin inhibitory activity
-
Synthesis and biological properties of aminodeoxystatine and difluorostatone derivatives
-
Bradbury, R.H. and Rivett, J.E. (1991) 1,2,4-Triazolo[4,3-a]pyrazine derivatives with human renin inhibitory activity. 3. Synthesis and biological properties of aminodeoxystatine and difluorostatone derivatives. Journal of Medicinal Chemistry, 34, 151-157.
-
(1991)
Journal of Medicinal Chemistry
, vol.34
, pp. 151-157
-
-
Bradbury, R.H.1
Rivett, J.E.2
-
97
-
-
0033010183
-
Discovery of non-peptidic P2-P3 butanediamide renin inhibitors with high oral efficacy
-
Simoneau, B., Lavallee, P., Anderson, P.C., Bailey, M., Bantle, G., Berthiaume, S., Chabot, C., Fazal, G., Halmos, T., Ogilvie, W.W., Poupart, M.-A., Thavonekham, B., Xin, Z., Thibeault, D., Bolger, G., Panzenbeck, M., Winquist, R., and Jung, G.L. (1999) Discovery of non-peptidic P2-P3 butanediamide renin inhibitors with high oral efficacy. Bioorganic & Medicinal Chemistry, 7, 489-508.
-
(1999)
Bioorganic & Medicinal Chemistry
, vol.7
, pp. 489-508
-
-
Simoneau, B.1
Lavallee, P.2
Anderson, P.C.3
Bailey, M.4
Bantle, G.5
Berthiaume, S.6
Chabot, C.7
Fazal, G.8
Halmos, T.9
Ogilvie, W.W.10
Poupart, M.-A.11
Thavonekham, B.12
Xin, Z.13
Thibeault, D.14
Bolger, G.15
Panzenbeck, M.16
Winquist, R.17
Jung, G.L.18
-
98
-
-
0027762522
-
Diol sulfonamides: a potent and novel class of inhibitors of human renin
-
Poss, M.A., Reid, J.A., Free, C.A., Rogers, W.L.,Weber, H., Ryono, D.E., Dejneka,T., DeForrest, J.M., Waldron, T.L., Brittain, R.J., Weller, H.N., Cimarusti, M.P., and Petrillo, E.W. (1993) Diol sulfonamides: a potent and novel class of inhibitors of human renin. Bioorganic & Medicinal Chemistry Letters, 3, 2739-2740.
-
(1993)
Bioorganic & Medicinal Chemistry Letters
, vol.3
, pp. 2739-2740
-
-
Poss, M.A.1
Reid, J.A.2
Free, C.A.3
Rogers, W.L.4
Weber, H.5
Ryono, D.E.6
Dejneka, T.7
DeForrest, J.M.8
Waldron, T.L.9
Brittain, R.J.10
Weller, H.N.11
Cimarusti, M.P.12
Petrillo, E.W.13
-
99
-
-
0024338931
-
Azido glycols: potent, low molecular weight renin inhibitors containing an unusual post scissile site residue
-
Rosenberg, S.H., Woods, K.W., Kleinert, H.D., Stein, H., Nellans, H.N., Hoffman, D.J., Spanton, S.G., Pyter, R.A., Cohen, J., Egan, D.A., Plattner, J.J., and Perun, T.J. (1989) Azido glycols: potent, low molecular weight renin inhibitors containing an unusual post scissile site residue. Journal of Medicinal Chemistry, 32, 1371-1378.
-
(1989)
Journal of Medicinal Chemistry
, vol.32
, pp. 1371-1378
-
-
Rosenberg, S.H.1
Woods, K.W.2
Kleinert, H.D.3
Stein, H.4
Nellans, H.N.5
Hoffman, D.J.6
Spanton, S.G.7
Pyter, R.A.8
Cohen, J.9
Egan, D.A.10
Plattner, J.J.11
Perun, T.J.12
-
100
-
-
0029156258
-
Design and synthesis of renin inhibitors: incorporation of transition-state isostere side chains that span from the S1 to the S3 binding pockets and examination of P3-modified renin inhibitors
-
Plummer, M.S., Shahripour, A., Kaltenbronn, J.S., Lunney, E.A., Steinbaugh, B.A., Hamby, J.M., Hamilton, H.W., Sawyer, T.K., Humblet, C., Doherty, A.M., Taylor, M.D., Hingorani, G., Batley, B.L., and Rapundalo, S.T. (1995) Design and synthesis of renin inhibitors: incorporation of transition-state isostere side chains that span from the S1 to the S3 binding pockets and examination of P3-modified renin inhibitors. Journal of Medicinal Chemistry, 38, 2893-2905.
-
(1995)
Journal of Medicinal Chemistry
, vol.38
, pp. 2893-2905
-
-
Plummer, M.S.1
Shahripour, A.2
Kaltenbronn, J.S.3
Lunney, E.A.4
Steinbaugh, B.A.5
Hamby, J.M.6
Hamilton, H.W.7
Sawyer, T.K.8
Humblet, C.9
Doherty, A.M.10
Taylor, M.D.11
Hingorani, G.12
Batley, B.L.13
Rapundalo, S.T.14
-
101
-
-
0027934039
-
Design and synthesis of a prototypical non-peptidic inhibitor model for the enzyme renin
-
Hanessian, S. and Raghavan, S. (1994) Design and synthesis of a prototypical non-peptidic inhibitor model for the enzyme renin. Bioorganic & Medicinal Chemistry Letters, 4, 1697-1700.
-
(1994)
Bioorganic & Medicinal Chemistry Letters
, vol.4
, pp. 1697-1700
-
-
Hanessian, S.1
Raghavan, S.2
-
102
-
-
0030576323
-
Bioactive hydroxyethylene dipeptide isosteres with hydrophobic (P3-P1)-moieties
-
A novel strategy towards small non-peptide renin inhibitors
-
Rasetti, V., Cohen, N.C., Rueeger, H., Goeschke, R., Maibaum, J., Cumin, F., Fuhere, W., and Wood, J.M. (1996) Bioactive hydroxyethylene dipeptide isosteres with hydrophobic (P3-P1)-moieties. A novel strategy towards small non-peptide renin inhibitors. Bioorganic & Medicinal Chemistry Letters, 6, 1589-1594.
-
(1996)
Bioorganic & Medicinal Chemistry Letters
, vol.6
, pp. 1589-1594
-
-
Rasetti, V.1
Cohen, N.C.2
Rueeger, H.3
Goeschke, R.4
Maibaum, J.5
Cumin, F.6
Fuhere, W.7
Wood, J.M.8
-
103
-
-
0028886572
-
Rational design, synthesis, and X-ray structure of renin inhibitors with extended P1 side-chains
-
Lefker, B.A., Hada, W.A., Wright, A.S., Martin, W.H., Stock, I.A., Schulte, G.K., Pandit, J., Danley, D.E., Ammirati, M.J., and Sneddon, S.F. (1995) Rational design, synthesis, and X-ray structure of renin inhibitors with extended P1 side-chains. Bioorganic & Medicinal Chemistry Letters, 5, 2623-2630.
-
(1995)
Bioorganic & Medicinal Chemistry Letters
, vol.5
, pp. 2623-2630
-
-
Lefker, B.A.1
Hada, W.A.2
Wright, A.S.3
Martin, W.H.4
Stock, I.A.5
Schulte, G.K.6
Pandit, J.7
Danley, D.E.8
Ammirati, M.J.9
Sneddon, S.F.10
-
104
-
-
0141608479
-
Design and synthesis of novel 2,7-dialkyl substituted 5(S)-amino-4(S)-hydroxy-8-phenyloctanecarboxamides as in vitro potent peptidomimetic inhibitors of human renin
-
Goschke, R., Cohen, N.C., Wood, J.M., and Maibaum, J. (1997) Design and synthesis of novel 2,7-dialkyl substituted 5(S)-amino-4(S)-hydroxy-8-phenyloctanecarboxamides as in vitro potent peptidomimetic inhibitors of human renin. Bioorganic & Medicinal Chemistry Letters, 7, 2735-2740.
-
(1997)
Bioorganic & Medicinal Chemistry Letters
, vol.7
, pp. 2735-2740
-
-
Goschke, R.1
Cohen, N.C.2
Wood, J.M.3
Maibaum, J.4
-
105
-
-
0028512575
-
Renin inhibitor SC-51106 complexed with human renin: discovery of a new binding site adjacent to P3
-
Hanson, G.J., Clare, M., Summers, N.L., Lim, L.W., Neidhart, D.J., Shieh, H.S., and Stevens, A.M. (1994) Renin inhibitor SC-51106 complexed with human renin: discovery of a new binding site adjacent to P3. Bioorganic & Medicinal Chemistry, 2, 909-918.
-
(1994)
Bioorganic & Medicinal Chemistry
, vol.2
, pp. 909-918
-
-
Hanson, G.J.1
Clare, M.2
Summers, N.L.3
Lim, L.W.4
Neidhart, D.J.5
Shieh, H.S.6
Stevens, A.M.7
-
106
-
-
66349100410
-
Design and optimization of renin inhibitors: orally bioavailable alkyl amines
-
Tice, C.M., Xu, Z., Yuan, J., Simpson, R.D., Cacatian, S.T., Flaherty, P.T., Zhao, W., Guo, J., Ishchenko, A., Singh, S.B., Wu, Z., Scott, B.B., Bukhtiyarov, Y., Berbaum, J., Mason, J., Panemangalore, R., Cappiello, M.G., Mueller, D., Harrison, R.K., McGeehan, G.M., Dillard, L.W., Baldwin, J.J., and Claremon, D.A. (2009) Design and optimization of renin inhibitors: orally bioavailable alkyl amines. Bioorganic & Medicinal Chemistry Letters, 19, 3541-3545.
-
(2009)
Bioorganic & Medicinal Chemistry Letters
, vol.19
, pp. 3541-3545
-
-
Tice, C.M.1
Xu, Z.2
Yuan, J.3
Simpson, R.D.4
Cacatian, S.T.5
Flaherty, P.T.6
Zhao, W.7
Guo, J.8
Ishchenko, A.9
Singh, S.B.10
Wu, Z.11
Scott, B.B.12
Bukhtiyarov, Y.13
Berbaum, J.14
Mason, J.15
Panemangalore, R.16
Cappiello, M.G.17
Mueller, D.18
Harrison, R.K.19
McGeehan, G.M.20
Dillard, L.W.21
Baldwin, J.J.22
Claremon, D.A.23
more..
-
107
-
-
34848888592
-
Novel 2,7-dialkyl-substituted 5(S)-amino-4(S)-hydroxy-8-phenyloctanecarboxamide transition state peptidomimetics are potent and orally active inhibitors of human renin
-
Goschke, R., Stutz, S., Rasetti, V., Cohen, N.C., Rahuel, J., Rigollier, P., Baum, H.P., Forgiarini, P., Schnell, C.R., Wagner, T., Gruetter, M.G., Fuhrer, W., Schilling, W., Cumin, F., Wood, J.M., and Maibaum, J. (2007) Novel 2,7-dialkyl-substituted 5(S)-amino-4(S)-hydroxy-8-phenyloctanecarboxamide transition state peptidomimetics are potent and orally active inhibitors of human renin. Journal of Medicinal Chemistry, 50, 4818-4831.
-
(2007)
Journal of Medicinal Chemistry
, vol.50
, pp. 4818-4831
-
-
Goschke, R.1
Stutz, S.2
Rasetti, V.3
Cohen, N.C.4
Rahuel, J.5
Rigollier, P.6
Baum, H.P.7
Forgiarini, P.8
Schnell, C.R.9
Wagner, T.10
Gruetter, M.G.11
Fuhrer, W.12
Schilling, W.13
Cumin, F.14
Wood, J.M.15
Maibaum, J.16
-
108
-
-
34848869297
-
Structural modification of the P20 position of 2,7-dialkyl-substituted 5(S)-amino-4(S)-hydroxy-8-phenyloctanecarboxamides: the discovery of aliskiren, a potent nonpeptide human renin inhibitor active after once daily dosing in marmosets
-
Maibaum, J., Stutz, S., Goschke, R., Rigollier, P., Yamaguchi, Y., Cumin, F., Rahuel, J., Baum, H.P., Cohen, N.C., Schnell, C.R., Fuhrer,W., Gruetter, M.G., Schilling, W., and Wood, J.M. (2007) Structural modification of the P20 position of 2,7-dialkyl-substituted 5(S)-amino-4(S)-hydroxy-8-phenyloctanecarboxamides: the discovery of aliskiren, a potent nonpeptide human renin inhibitor active after once daily dosing in marmosets. Journal ofMedicinal Chemistry, 50, 4832-4844.
-
(2007)
Journal ofMedicinal Chemistry
, vol.50
, pp. 4832-4844
-
-
Maibaum, J.1
Stutz, S.2
Goschke, R.3
Rigollier, P.4
Yamaguchi, Y.5
Cumin, F.6
Rahuel, J.7
Baum, H.P.8
Cohen, N.C.9
Schnell, C.R.10
Fuhrer, W.11
Gruetter, M.G.12
Schilling, W.13
Wood, J.M.14
-
109
-
-
14044271546
-
Aliskiren, a novel, orally effective renin inhibitor, lowers blood pressure in marmosets and spontaneously hypertensive rats
-
Wood, J.M., Schnell, C.R., Cumin, F., Menard, J., and Webb, R.L. (2005) Aliskiren, a novel, orally effective renin inhibitor, lowers blood pressure in marmosets and spontaneously hypertensive rats. Journal of Hypertension, 23, 417-426.
-
(2005)
Journal of Hypertension
, vol.23
, pp. 417-426
-
-
Wood, J.M.1
Schnell, C.R.2
Cumin, F.3
Menard, J.4
Webb, R.L.5
-
110
-
-
34547972201
-
Low-dose renin inhibitor and low-dose AT1-receptor blocker therapy ameliorate target-organ damage in rats harbouring human renin and angiotensinogen genes
-
Dechend, R., Shagdarsuren, E., Gratze, P., Fiebeler, A., Pilz, B., Meiners, S., Derer, W., Feldman, D.L., Webb, R., and Muller, D.N. (2007) Low-dose renin inhibitor and low-dose AT1-receptor blocker therapy ameliorate target-organ damage in rats harbouring human renin and angiotensinogen genes. Journal of the renin-angiotensin-aldosterone system, 8, 81-84.
-
(2007)
Journal of the renin-angiotensin-aldosterone system
, vol.8
, pp. 81-84
-
-
Dechend, R.1
Shagdarsuren, E.2
Gratze, P.3
Fiebeler, A.4
Pilz, B.5
Meiners, S.6
Derer, W.7
Feldman, D.L.8
Webb, R.9
Muller, D.N.10
-
111
-
-
25444454353
-
Aliskiren, a human renin inhibitor, ameliorates cardiac and renal damage in doubletransgenic rats
-
Pilz, B., Shagdarsuren, E., Wellner, M., Fiebeler, A., Dechend, R., Gratze, P., Meiners, S., Feldman, D.L., Webb, R.L., Garrelds, I.M., Danser, A.H.J., Luft, F.C., and Mueller, D.N. (2005) Aliskiren, a human renin inhibitor, ameliorates cardiac and renal damage in doubletransgenic rats. Hypertension, 46, 569-576.
-
(2005)
Hypertension
, vol.46
, pp. 569-576
-
-
Pilz, B.1
Shagdarsuren, E.2
Wellner, M.3
Fiebeler, A.4
Dechend, R.5
Gratze, P.6
Meiners, S.7
Feldman, D.L.8
Webb, R.L.9
Garrelds, I.M.10
Danser, A.H.J.11
Luft, F.C.12
Mueller, D.N.13
-
112
-
-
34848907212
-
Aliskiren, a novel renin inhibitor, is renoprotective in a model of advanced diabetic nephropathy in rats
-
Kelly, D.J., Zhang, Y., Moe, G., Naik, G., and Gilbert, R.E. (2007) Aliskiren, a novel renin inhibitor, is renoprotective in a model of advanced diabetic nephropathy in rats. Diabetologia, 50, 2398-2404.
-
(2007)
Diabetologia
, vol.50
, pp. 2398-2404
-
-
Kelly, D.J.1
Zhang, Y.2
Moe, G.3
Naik, G.4
Gilbert, R.E.5
-
113
-
-
34848903955
-
Aliskiren
-
Siragy, H.M., Kar, S., and Kirkpatrick, P. (2007) Aliskiren. Nature Reviews. Drug Discovery, 6, 779-780.
-
(2007)
Nature Reviews. Drug Discovery
, vol.6
, pp. 779-780
-
-
Siragy, H.M.1
Kar, S.2
Kirkpatrick, P.3
-
114
-
-
42949109643
-
Aliskiren: the first renin inhibitor for clinical treatment
-
Jensen, C.,Herold, P., and Brunner, H.R. (2008) Aliskiren: the first renin inhibitor for clinical treatment. Nature Reviews. Drug Discovery, 7, 399-410.
-
(2008)
Nature Reviews. Drug Discovery
, vol.7
, pp. 399-410
-
-
Jensen, C.1
Herold, P.2
Brunner, H.R.3
-
115
-
-
34547221695
-
Absorption, distribution, metabolism, and elimination of the direct renin inhibitor aliskiren in healthy volunteers
-
Waldmeier, F., Glaenzel, U., Wirz, B., Oberer, L., Schmid, D., Seiberling, M., Valencia, J., Riviere, G.-J., End, P., and Vaidyanathan, S. (2007) Absorption, distribution, metabolism, and elimination of the direct renin inhibitor aliskiren in healthy volunteers. Drug Metabolism and Disposition: The Biological Fate of Chemicals, 35, 1418-1428.
-
(2007)
Drug Metabolism and Disposition: The Biological Fate of Chemicals
, vol.35
, pp. 1418-1428
-
-
Waldmeier, F.1
Glaenzel, U.2
Wirz, B.3
Oberer, L.4
Schmid, D.5
Seiberling, M.6
Valencia, J.7
Riviere, G.-J.8
End, P.9
Vaidyanathan, S.10
-
116
-
-
47049089844
-
Clinical pharmacokinetics and pharmacodynamics of aliskiren
-
Vaidyanathan, S., Jarugula, V., Dieterich Hans, A., Howard, D., and Dole William, P. (2008) Clinical pharmacokinetics and pharmacodynamics of aliskiren. Clinical Pharmacokinetics, 47, 515-521.
-
(2008)
Clinical Pharmacokinetics
, vol.47
, pp. 515-521
-
-
Vaidyanathan, S.1
Jarugula, V.2
Dieterich Hans, A.3
Howard, D.4
Dole William, P.5
-
117
-
-
70249111167
-
Aliskiren: the next innovation in renin-angiotensin-aldosterone system blockade
-
Duprez, D.A. (2009) Aliskiren: the next innovation in renin-angiotensin-aldosterone system blockade. Aging Health, 5, 269-279.
-
(2009)
Aging Health
, vol.5
, pp. 269-279
-
-
Duprez, D.A.1
-
118
-
-
67849128863
-
Blood pressure lowering efficacy of renin inhibitors for primary hypertension: a cochrane systematic review
-
Musini, V.M., Fortin, P.M., Bassett, K., and Wright, J.M. (2009) Blood pressure lowering efficacy of renin inhibitors for primary hypertension: a cochrane systematic review. Journal of Human Hypertension, 23, 495-502.
-
(2009)
Journal of Human Hypertension
, vol.23
, pp. 495-502
-
-
Musini, V.M.1
Fortin, P.M.2
Bassett, K.3
Wright, J.M.4
-
119
-
-
67650495757
-
Managing cardiovascular and renal risk: the potential of direct renin inhibition
-
Sever, P.S.,Gradman, A.H., and Azizi, M. (2009) Managing cardiovascular and renal risk: the potential of direct renin inhibition. Journal of the Renin-Angiotensin-Aldosterone System, 10, 65-76.
-
(2009)
Journal of the Renin-Angiotensin-Aldosterone System
, vol.10
, pp. 65-76
-
-
Sever, P.S.1
Gradman, A.H.2
Azizi, M.3
-
120
-
-
67651087348
-
The P1 N-isopropyl motif bearing hydroxyethylene dipeptide isostere analogues of aliskiren are in vitro potent inhibitors of the human aspartyl protease renin
-
Yamaguchi, Y., Menear, K., Cohen, N.-C., Mah, R., Cumin, F., Schnell, C., Wood, J.M., and Maibaum, J. (2009) The P1 N-isopropyl motif bearing hydroxyethylene dipeptide isostere analogues of aliskiren are in vitro potent inhibitors of the human aspartyl protease renin. Bioorganic & Medicinal Chemistry Letters, 19, 4863-4867.
-
(2009)
Bioorganic & Medicinal Chemistry Letters
, vol.19
, pp. 4863-4867
-
-
Yamaguchi, Y.1
Menear, K.2
Cohen, N.-C.3
Mah, R.4
Cumin, F.5
Schnell, C.6
Wood, J.M.7
Maibaum, J.8
-
121
-
-
0036354363
-
Preformulation approaches to improve the oral bioavailability of two novel piperidine renin inhibitors in dog
-
Bittner, B., Chou, R., Schleimer, M., Morgenroth, B., Zell, M., and Lave, T. (2002) Preformulation approaches to improve the oral bioavailability of two novel piperidine renin inhibitors in dog. Arzneimittel-Forschung, 52, 593-599.
-
(2002)
Arzneimittel-Forschung
, vol.52
, pp. 593-599
-
-
Bittner, B.1
Chou, R.2
Schleimer, M.3
Morgenroth, B.4
Zell, M.5
Lave, T.6
-
122
-
-
56149092172
-
A nonpeptide
-
piperidine renin inhibitor provides renal and cardiac protection in double-transgenic mice expressing human renin and angiotensinogen genes
-
Major, T.C., Olszewski, B., Rosebury, W., Okerberg, C., Carlson, T., Ostroski, R., Schroeder, R., Kowala, M.C., and Leadley, R. (2008) A nonpeptide. piperidine renin inhibitor provides renal and cardiac protection in double-transgenic mice expressing human renin and angiotensinogen genes. Cardiovascular Drugs and Therapy, 22, 469-478.
-
(2008)
Cardiovascular Drugs and Therapy
, vol.22
, pp. 469-478
-
-
Major, T.C.1
Olszewski, B.2
Rosebury, W.3
Okerberg, C.4
Carlson, T.5
Ostroski, R.6
Schroeder, R.7
Kowala, M.C.8
Leadley, R.9
-
123
-
-
20044391231
-
Discovery of novel non-peptidic ketopiperazine-based renin inhibitors
-
Holsworth, D.D., Powell, N.A., Downing, D.M., Cai, C., Cody, W.L., Ryan, J.M., Ostroski, R., Jalaie, M., Bryant, J.W., and Edmunds, J.J. (2005) Discovery of novel non-peptidic ketopiperazine-based renin inhibitors. Bioorganic & Medicinal Chemistry, 13, 2657-2664.
-
(2005)
Bioorganic & Medicinal Chemistry
, vol.13
, pp. 2657-2664
-
-
Holsworth, D.D.1
Powell, N.A.2
Downing, D.M.3
Cai, C.4
Cody, W.L.5
Ryan, J.M.6
Ostroski, R.7
Jalaie, M.8
Bryant, J.W.9
Edmunds, J.J.10
-
124
-
-
25144441809
-
Benzyl ether structure-activity relationships in a series of ketopiperazine-based renin inhibitors
-
Powell, N.A., Clay, E.H., Holsworth, D.D., Bryant, J.W., Ryan, M.J., Jalaie, M., and Edmunds, J.J. (2005) Benzyl ether structure-activity relationships in a series of ketopiperazine-based renin inhibitors. Bioorganic & Medicinal Chemistry Letters, 15, 4713-4716.
-
(2005)
Bioorganic & Medicinal Chemistry Letters
, vol.15
, pp. 4713-4716
-
-
Powell, N.A.1
Clay, E.H.2
Holsworth, D.D.3
Bryant, J.W.4
Ryan, M.J.5
Jalaie, M.6
Edmunds, J.J.7
-
125
-
-
67549146537
-
Design and preparation of potent, nonpeptidic, bioavailable renin inhibitors
-
Bezencon, O., Bur, D.,Weller, T., Richard-Bildstein, S., Remen, L., Sifferlen, T., Corminboeuf, O., Grisostomi, C., Boss, C., Prade, L., Delahaye, S., Treiber, A., Strickner, P., Binkert, C., Hess, P., Steiner, B., and Fischli, W. (2009) Design and preparation of potent, nonpeptidic, bioavailable renin inhibitors. Journal ofMedicinal Chemistry, 52, 3689-3702.
-
(2009)
Journal ofMedicinal Chemistry
, vol.52
, pp. 3689-3702
-
-
Bezencon, O.1
Bur, D.2
Weller, T.3
Richard-Bildstein, S.4
Remen, L.5
Sifferlen, T.6
Corminboeuf, O.7
Grisostomi, C.8
Boss, C.9
Prade, L.10
Delahaye, S.11
Treiber, A.12
Strickner, P.13
Binkert, C.14
Hess, P.15
Steiner, B.16
Fischli, W.17
-
126
-
-
85017429153
-
Discovery of trisubstituted triazines as potent renin inhibitors
-
DC, August p. MEDI-188
-
Donofrio, A., Coppo, F., Squire, M., Burton, G., Semus, S., Hubbard, J., and Rivero, R. (2009) Discovery of trisubstituted triazines as potent renin inhibitors. Abstract of Papers presented at 238th ACS National Meeting, Washington, DC, August 16-20, 2009, p. MEDI-188.
-
(2009)
Abstract of Papers presented at 238th ACS National Meeting, Washington
, pp. 16-20
-
-
Donofrio, A.1
Coppo, F.2
Squire, M.3
Burton, G.4
Semus, S.5
Hubbard, J.6
Rivero, R.7
-
127
-
-
46849092364
-
Recent advances in the discovery of non-peptidic direct renin inhibitors as antihypertensives: new patent applications in years 2000-2008
-
Yokokawa, F. and Maibaum, J. (2008) Recent advances in the discovery of non-peptidic direct renin inhibitors as antihypertensives: new patent applications in years 2000-2008. Expert Opinion on Therapeutic Patents, 18, 581-602.
-
(2008)
Expert Opinion on Therapeutic Patents
, vol.18
, pp. 581-602
-
-
Yokokawa, F.1
Maibaum, J.2
-
128
-
-
34250218617
-
Discovery of 6-ethyl-2,4-diaminopyrimidine-based small molecule renin inhibitors
-
Holsworth, D.D., Jalaie, M., Belliotti, T., Cai, C., Collard, W., Ferreira, S., Powell, N.A., Stier, M., Zhang, E., McConnell, P., Mochalkin, I., Ryan, M.J., Bryant, J., Li, T., Kasani, A., Subedi, R., Maiti, S.N., and Edmunds, J.J. (2007) Discovery of 6-ethyl-2,4-diaminopyrimidine-based small molecule renin inhibitors. Bioorganic & Medicinal Chemistry Letters, 17, 3575-3580.
-
(2007)
Bioorganic & Medicinal Chemistry Letters
, vol.17
, pp. 3575-3580
-
-
Holsworth, D.D.1
Jalaie, M.2
Belliotti, T.3
Cai, C.4
Collard, W.5
Ferreira, S.6
Powell, N.A.7
Stier, M.8
Zhang, E.9
McConnell, P.10
Mochalkin, I.11
Ryan, M.J.12
Bryant, J.13
Li, T.14
Kasani, A.15
Subedi, R.16
Maiti, S.N.17
Edmunds, J.J.18
-
129
-
-
33947636525
-
Application of fragment screening by X-ray crystallography to the discovery of aminopyridines as inhibitors of betasecretase
-
Congreve, M., Aharony, D., Albert, J., Callaghan, O., Campbell, J., Carr, R.A.E., Chessari, G., Cowan, S., Edwards, P.D., Frederickson, M., McMenamin, R., Murray, C.W., Patel, S., and Wallis, N. (2007) Application of fragment screening by X-ray crystallography to the discovery of aminopyridines as inhibitors of betasecretase. Journal of Medicinal Chemistry, 50, 1124-1132.
-
(2007)
Journal of Medicinal Chemistry
, vol.50
, pp. 1124-1132
-
-
Congreve, M.1
Aharony, D.2
Albert, J.3
Callaghan, O.4
Campbell, J.5
Carr, R.A.E.6
Chessari, G.7
Cowan, S.8
Edwards, P.D.9
Frederickson, M.10
McMenamin, R.11
Murray, C.W.12
Patel, S.13
Wallis, N.14
-
130
-
-
34447293062
-
Rational design of 6-(2,4-diaminopyrimidinyl)-1,4-benzoxazin-3-ones as small molecule renin inhibitors
-
Powell, N.A., Ciske, F.L., Cai, C., Holsworth, D.D., Mennen, K., Van Huis, C.A., Jalaie, M., Day, J., Mastronardi, M., McConnell, P., Mochalkin, I., Zhang, E., Ryan, M.J., Bryant, J., Collard, W., Ferreira, S., Gu, C., Collins, R., and Edmunds, J.J. (2007) Rational design of 6-(2,4-diaminopyrimidinyl)-1,4-benzoxazin-3-ones as small molecule renin inhibitors. Bioorganic & Medicinal Chemistry, 15, 5912-5949.
-
(2007)
Bioorganic & Medicinal Chemistry
, vol.15
, pp. 5912-5949
-
-
Powell, N.A.1
Ciske, F.L.2
Cai, C.3
Holsworth, D.D.4
Mennen, K.5
Van Huis, C.A.6
Jalaie, M.7
Day, J.8
Mastronardi, M.9
McConnell, P.10
Mochalkin, I.11
Zhang, E.12
Ryan, M.J.13
Bryant, J.14
Collard, W.15
Ferreira, S.16
Gu, C.17
Collins, R.18
Edmunds, J.J.19
-
131
-
-
33947658802
-
Identification of hot spots within druggable binding regions by computational solvent mapping of proteins
-
Landon, M.R., Lancia, D.R., Jr., Yu, J., Thiel, S.C., and Vajda, S. (2007) Identification of hot spots within druggable binding regions by computational solvent mapping of proteins. Journal of Medicinal Chemistry, 50, 1231-1240.
-
(2007)
Journal of Medicinal Chemistry
, vol.50
, pp. 1231-1240
-
-
Landon, M.R.1
Lancia, D.R.2
Yu, J.3
Thiel, S.C.4
Vajda, S.5
-
132
-
-
34250221934
-
Renin Inhibitors in Antihypertensive Drugs
-
(eds P.A. Uan Zweiten and W.J. Greenlee)
-
Rosenberg, S.H., and Boyd, S.A. (1997) Renin Inhibitors in Antihypertensive Drugs (eds P.A. Uan Zweiten and W.J. Greenlee) Harwood Academic Publishers, pp. 77-111.
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(1997)
Harwood Academic Publishers
, pp. 77-111
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Rosenberg, S.H.1
Boyd, S.A.2
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