-
1
-
-
0031027901
-
Molecular basis of HIV-1 protease drug resistance: Structural analysis of mutant proteases complexed with cyclic urea inhibitors
-
P.J. Ala E.E. Huston R.M. Klabe D.D. McCabe J.L. Duke C.J. Rizzo B.D. Korant R.J. DeLoskey P.Y. Lam C.N. Hodge C.H. Chang Molecular basis of HIV-1 protease drug resistance: Structural analysis of mutant proteases complexed with cyclic urea inhibitors Biochemistry 36 1997 1573 1580
-
(1997)
Biochemistry
, vol.36
, pp. 1573-1580
-
-
Ala, P.J.1
Huston, E.E.2
Klabe, R.M.3
McCabe, D.D.4
Duke, J.L.5
Rizzo, C.J.6
Korant, B.D.7
DeLoskey, R.J.8
Lam, P.Y.9
Hodge, C.N.10
Chang, C.H.11
-
2
-
-
15444345861
-
Molecular recognition of cyclic urea HIV-1 protease inhibitors
-
R. Ala R. DeLoskey E. Huston P. Jadhav P. Lam C. Eyermann C. Hodge M. Schadt F. Lewandowski P. Weber D. McCabe J. Duke C. Chang Molecular recognition of cyclic urea HIV-1 protease inhibitors J. Biol. Chem. 273 1998 12325 12331
-
(1998)
J. Biol. Chem.
, vol.273
, pp. 12325-12331
-
-
Ala, R.1
DeLoskey, R.2
Huston, E.3
Jadhav, P.4
Lam, P.5
Eyermann, C.6
Hodge, C.7
Schadt, M.8
Lewandowski, F.9
Weber, P.10
McCabe, D.11
Duke, J.12
Chang, C.13
-
3
-
-
0029644939
-
Structure of HIV-1 protease with KNI-272, a tight-binding transition-state analog containing allophenylnorstatine
-
E.T. Baldwin T.N. Bhat S. Gulnik B. Liu I.A. Topol Y. Kiso T. Mimoto H. Mitsuya J.W. Erickson Structure of HIV-1 protease with KNI-272, a tight-binding transition-state analog containing allophenylnorstatine Structure 3 1995 581 590
-
(1995)
Structure
, vol.3
, pp. 581-590
-
-
Baldwin, E.T.1
Bhat, T.N.2
Gulnik, S.3
Liu, B.4
Topol, I.A.5
Kiso, Y.6
Mimoto, T.7
Mitsuya, H.8
Erickson, J.W.9
-
5
-
-
0030007802
-
Natural variation in HIV-1 protease, Gag p7 and p6, and protease cleavage sites within gag/polpolyproteins: Amino acid substitutions in the absence of protease inhibitors in mothers and children infected by human immunodeficiency virus type 1
-
K.A. Barrie E.E. Perez S.L. Lamers W.G. Farmerie B.M. Dunn J.W. Sleasman M.M. Goodenow Natural variation in HIV-1 protease, Gag p7 and p6, and protease cleavage sites within gag/polpolyproteins: Amino acid substitutions in the absence of protease inhibitors in mothers and children infected by human immunodeficiency virus type 1 Virology 219 1996 407 416
-
(1996)
Virology
, vol.219
, pp. 407-416
-
-
Barrie, K.A.1
Perez, E.E.2
Lamers, S.L.3
Farmerie, W.G.4
Dunn, B.M.5
Sleasman, J.W.6
Goodenow, M.M.7
-
6
-
-
0030895312
-
Protease inhibitors in patients with HIV disease. Clinically important pharmacokinetic considerations
-
M. Barry S. Gibvons D. Back F. Mulcahy Protease inhibitors in patients with HIV disease. Clinically important pharmacokinetic considerations Clin. Pharmacokinet. 32 1997 194 209
-
(1997)
Clin. Pharmacokinet.
, vol.32
, pp. 194-209
-
-
Barry, M.1
Gibvons, S.2
Back, D.3
Mulcahy, F.4
-
8
-
-
0031724008
-
Resistance to human immunodeficiency virus type 1 protease inhibitors
-
D. Boden M. Markowitz Resistance to human immunodeficiency virus type 1 protease inhibitors Antimicrob. Agents Chemother. 42 1998 2775 2783
-
(1998)
Antimicrob. Agents Chemother.
, vol.42
, pp. 2775-2783
-
-
Boden, D.1
Markowitz, M.2
-
9
-
-
0031849665
-
In vitro selection and characterization of human immunodeficiency virus type 1 variants with increased resistance to ABT-378, a novel protease inhibitor
-
A. Carrillo K.D. Stewart H.L. Sham D.W. Norbeck W.E. Kohlbrenner J.M. Leonard D.J. Kempf A. Molla In vitro selection and characterization of human immunodeficiency virus type 1 variants with increased resistance to ABT-378, a novel protease inhibitor J. Virol. 72 1998 7532 7541
-
(1998)
J. Virol.
, vol.72
, pp. 7532-7541
-
-
Carrillo, A.1
Stewart, K.D.2
Sham, H.L.3
Norbeck, D.W.4
Kohlbrenner, W.E.5
Leonard, J.M.6
Kempf, D.J.7
Molla, A.8
-
10
-
-
0029131607
-
Three-dimensional structure of a mutant HIV-1 protease displaying cross-resistance to all protease inhibitors in clinical trials
-
Z. Chen Y. Li H.B. Schock D. Hall E. Chen L.C. Kuo Three-dimensional structure of a mutant HIV-1 protease displaying cross-resistance to all protease inhibitors in clinical trials J. Biol. Chem. 270 1995 21433 21436
-
(1995)
J. Biol. Chem.
, vol.270
, pp. 21433-21436
-
-
Chen, Z.1
Li, Y.2
Schock, H.B.3
Hall, D.4
Chen, E.5
Kuo, L.C.6
-
11
-
-
0025641617
-
Stability and activity of human immunodeficiency virus protease: Comparison of the natural dimer with a homologous, single-chain tethered dimer
-
Y.-S.E. Cheng F.H. Yin S. Foundling D. Blomstrom C.A. Kettner Stability and activity of human immunodeficiency virus protease: Comparison of the natural dimer with a homologous, single-chain tethered dimer Proc. Natl. Acad. Sci. U.S.A. 87 1990 9660 9664
-
(1990)
, pp. 9660-9664
-
-
Cheng, Y.-S.E.1
Yin, F.H.2
Foundling, S.3
Blomstrom, D.4
Kettner, C.A.5
-
12
-
-
0028952146
-
HIV population dynamics in vivo: Implications for genetic variation, pathogenesis and therapy
-
J.M. Coffin HIV population dynamics in vivo : Implications for genetic variation, pathogenesis and therapy Science 267 1995 483 489
-
(1995)
Science
, vol.267
, pp. 483-489
-
-
Coffin, J.M.1
-
13
-
-
85119552453
-
-
J.M. Coffin S.H. Hughes H.E. Varmus Retroviruses 1997 Cold Spring Harbor Lab. Press Cold Spring Harbor, NY
-
(1997)
-
-
-
14
-
-
0028958868
-
Flap opening in HIV-1 protease simulated by ‘activated’ molecular dynamics
-
J.R. Collins S.K. Burt J.W. Erickson Flap opening in HIV-1 protease simulated by ‘activated’ molecular dynamics Nat. Struct. Biol. 2 1995 334 338
-
(1995)
Nat. Struct. Biol.
, vol.2
, pp. 334-338
-
-
Collins, J.R.1
Burt, S.K.2
Erickson, J.W.3
-
15
-
-
0028943992
-
In vivo emergence of HIV-1 variants resistant to multiple protease inhibitors
-
J.H. Condra W.A. Schleif O.M. Blahy L.J. Gabryelski D.J. Graham J.C. Quintero A. Rhodes H.L. Robbins E. Roth M. Shivaprakash D. Titus T. Yang H. Teppler K.E. Squires P.J. Deutsch E.A. Emini In vivo emergence of HIV-1 variants resistant to multiple protease inhibitors Nature (London) 374 1995 569 571
-
(1995)
Nature (London)
, vol.374
, pp. 569-571
-
-
Condra, J.H.1
Schleif, W.A.2
Blahy, O.M.3
Gabryelski, L.J.4
Graham, D.J.5
Quintero, J.C.6
Rhodes, A.7
Robbins, H.L.8
Roth, E.9
Shivaprakash, M.10
Titus, D.11
Yang, T.12
Teppler, H.13
Squires, K.E.14
Deutsch, P.J.15
Emini, E.A.16
-
16
-
-
10344263394
-
Genetic correlates of in vivo viral resistance to indinavir, a human immunodeficiency virus type 1 protease inhibitor
-
J.H. Condra D.J. Holder W.A. Schleif O.M. Blahy R.M. Danovich L.J. Gabryelski D.J. Graham D. Laird J.C. Quintero A. Rhodes H.L. Robbins E. Roth M. Shivaprakash T. Yang J.A. Chodakewitz P.J. Deutsch R.Y. Leavitt F.E. Massari J.W. Mellors K.E. Squires R.T. Steigbigel H. Teppler E.A. Emini Genetic correlates of in vivo viral resistance to indinavir, a human immunodeficiency virus type 1 protease inhibitor J. Virol. 70 1996 8270 8276
-
(1996)
J. Virol.
, vol.70
, pp. 8270-8276
-
-
Condra, J.H.1
Holder, D.J.2
Schleif, W.A.3
Blahy, O.M.4
Danovich, R.M.5
Gabryelski, L.J.6
Graham, D.J.7
Laird, D.8
Quintero, J.C.9
Rhodes, A.10
Robbins, H.L.11
Roth, E.12
Shivaprakash, M.13
Yang, T.14
Chodakewitz, J.A.15
Deutsch, P.J.16
Leavitt, R.Y.17
Massari, F.E.18
Mellors, J.W.19
Squires, K.E.20
Steigbigel, R.T.21
Teppler, H.22
Emini, E.A.23
more..
-
17
-
-
0030858617
-
pol gene diversity of five human immunodeficiency virus type 1 subtypes: Evidence for naturally occurring mutations that contribute to drug resistance, limited recombination patterns, and common ancestry for subtypes B and D
-
M. Cornelissen R. van den Burg F. Zorgdrager V. Lukashov J. Goudsmit pol gene diversity of five human immunodeficiency virus type 1 subtypes: Evidence for naturally occurring mutations that contribute to drug resistance, limited recombination patterns, and common ancestry for subtypes B and D J. Virol. 71 1997 6348 6358
-
(1997)
J. Virol.
, vol.71
, pp. 6348-6358
-
-
Cornelissen, M.1
van den Burg, R.2
Zorgdrager, F.3
Lukashov, V.4
Goudsmit, J.5
-
18
-
-
0031015475
-
Impaired fitness of human immunodeficiency virus type 1 variants with high-level resistance to protease inhibitors
-
G. Croteau L. Doyon D. Thibeault G. McKercher L. Pilote D. Lamarre Impaired fitness of human immunodeficiency virus type 1 variants with high-level resistance to protease inhibitors J. Virol. 71 1997 1089 1096
-
(1997)
J. Virol.
, vol.71
, pp. 1089-1096
-
-
Croteau, G.1
Doyon, L.2
Thibeault, D.3
McKercher, G.4
Pilote, L.5
Lamarre, D.6
-
19
-
-
0029002115
-
Stability of dimeric retroviral proteases
-
P.L. Darke Stability of dimeric retroviral proteases L.C. Kuo J.A. Shafer Methods in Enzymology Vol. 241 1994 Academic Press San Diego, CA 104 127
-
(1994)
, pp. 104-127
-
-
Darke, P.L.1
-
21
-
-
0025290527
-
The structure and function of the aspartic proteinases
-
D.R. Davies The structure and function of the aspartic proteinases Annu. Rev. Biophys. Biomol. Struct. 19 1990 189 215
-
(1990)
Annu. Rev. Biophys. Biomol. Struct.
, vol.19
, pp. 189-215
-
-
Davies, D.R.1
-
22
-
-
0026579208
-
The HIV-1 protease as a therapeutic target for AIDS
-
C. Debouck The HIV-1 protease as a therapeutic target for AIDS AIDS Res. Hum. Retroviruses 8 1992 153 164
-
(1992)
AIDS Res. Hum. Retroviruses
, vol.8
, pp. 153-164
-
-
Debouck, C.1
-
23
-
-
0023477907
-
Human immunodeficiency virus protease expressed in Escherichia coli exhibits autoprocessing and specific maturation of the gag precursor
-
C. Debouck J.G. Gorniak J.E. Strickler T.D. Meek B.W. Metcalf M. Rosenberg Human immunodeficiency virus protease expressed in Escherichia coli exhibits autoprocessing and specific maturation of the gag precursor Proc. Natl. Acad. Sci. U.S.A. 84 1987 8903 8906
-
(1987)
, pp. 8903-8906
-
-
Debouck, C.1
Gorniak, J.G.2
Strickler, J.E.3
Meek, T.D.4
Metcalf, B.W.5
Rosenberg, M.6
-
25
-
-
0027969994
-
L-735,524: The design of a potent and orally bioavailable HIV protease inhibitor
-
B.D. Dorsey R.B. Levin S.L. McDaniel J.P. Vacca J.P. Guare P.L. Darke J.A. Zugay E. Emini W.A. Schleif J.C. Quintero J.H. Lin I.-W. Chen M.K. Holloway P.M.D. Fitzgerald M.G. Axel D. Ostovic P.S. Anderson J.R. Huff L-735,524: The design of a potent and orally bioavailable HIV protease inhibitor J. Med. Chem. 37 1994 3443 3451
-
(1994)
J. Med. Chem.
, vol.37
, pp. 3443-3451
-
-
Dorsey, B.D.1
Levin, R.B.2
McDaniel, S.L.3
Vacca, J.P.4
Guare, J.P.5
Darke, P.L.6
Zugay, J.A.7
Emini, E.8
Schleif, W.A.9
Quintero, J.C.10
Lin, J.H.11
Chen, I.-W.12
Holloway, M.K.13
Fitzgerald, P.M.D.14
Axel, M.G.15
Ostovic, D.16
Anderson, P.S.17
Huff, J.R.18
-
26
-
-
0029899093
-
Second locus involved in human immunodeficiency virus type 1 resistance to protease inhibitors
-
L. Doyon G. Croteau D. Thibeault F. Poulin L. Pilote D. Lamarre Second locus involved in human immunodeficiency virus type 1 resistance to protease inhibitors J. Virol. 70 1996 3763 3769
-
(1996)
J. Virol.
, vol.70
, pp. 3763-3769
-
-
Doyon, L.1
Croteau, G.2
Thibeault, D.3
Poulin, F.4
Pilote, L.5
Lamarre, D.6
-
27
-
-
0029001259
-
Subsite preferences of retroviral proteinases
-
B.M. Dunn A. Gustchina A. Wlodawer J. Kay Subsite preferences of retroviral proteinases L.C. Kuo J.A. Shafer Methods of Enzymology Vol. 241 1994 Academic Press San Diego, CA 254 278
-
(1994)
, pp. 254-278
-
-
Dunn, B.M.1
Gustchina, A.2
Wlodawer, A.3
Kay, J.4
-
28
-
-
0031950370
-
Genotypic changes in human immunodeficiency virus type 1 associated with loss of suppression of plasma viral RNA levels in subjects treated with ritonavir (norvir) monotherapy
-
P. Eastman J. Mittler R. Kelso C. Gee E. Boyer J. Kolberg M. Urdea J. Leonard D. Norbeck H. Mo M. Markowitz Genotypic changes in human immunodeficiency virus type 1 associated with loss of suppression of plasma viral RNA levels in subjects treated with ritonavir (norvir) monotherapy J. Virol. 72 1998 5154 5164
-
(1998)
J. Virol.
, vol.72
, pp. 5154-5164
-
-
Eastman, P.1
Mittler, J.2
Kelso, R.3
Gee, C.4
Boyer, E.5
Kolberg, J.6
Urdea, M.7
Leonard, J.8
Norbeck, D.9
Mo, H.10
Markowitz, M.11
-
29
-
-
0024992935
-
Design, activity, and 2.8 Å crystal structure of a C2 symmetric inhibitor complexed to HIV-1 protease
-
2 symmetric inhibitor complexed to HIV-1 protease Science 249 1990 527 533
-
(1990)
Science
, vol.249
, pp. 527-533
-
-
Erickson, J.1
Neidhart, D.J.2
vanDrie, J.3
Kempf, D.J.4
Wang, X.C.5
Norbeck, D.W.6
Plattner, J.J.7
Rittenhouse, J.W.8
Turon, M.9
Wideburg, N.10
Kohlbrenner, W.E.11
Simmer, R.12
Helfrich, R.13
Paul, D.A.14
Knigge, M.15
-
30
-
-
0029157399
-
The not-so-great escape
-
J.W. Erickson The not-so-great escape Nat. Struct. Biol. 2 1995 523 529
-
(1995)
Nat. Struct. Biol.
, vol.2
, pp. 523-529
-
-
Erickson, J.W.1
-
32
-
-
0001928313
-
HIV protease as a target for the design of antiviral agents for AIDS
-
J.W. Erickson M.E. Eissenstat HIV protease as a target for the design of antiviral agents for AIDS B. Dunn Proteases of Infectious Agents 1999 Academic Press San Diego, CA 1 60
-
(1999)
, pp. 1-60
-
-
Erickson, J.W.1
Eissenstat, M.E.2
-
33
-
-
0000131149
-
Protease inhibitors: Resistance, cross-resistance, fitness and the choice of initial and salvage therapies
-
J.W. Erickson S.V. Gulnik M. Markowitz Protease inhibitors: Resistance, cross-resistance, fitness and the choice of initial and salvage therapies AIDS 13 Suppl A 1999 S189 S204
-
(1999)
AIDS
, vol.13
, Issue.Suppl A
, pp. S189-S204
-
-
Erickson, J.W.1
Gulnik, S.V.2
Markowitz, M.3
-
34
-
-
0030870159
-
Kinetic properties of saquinavir-resistant mutants of human immunodeficiency virus type 1 protease and their implications in drug resistance in vivo
-
J. Ermolieff X. Lin J. Tang Kinetic properties of saquinavir-resistant mutants of human immunodeficiency virus type 1 protease and their implications in drug resistance in vivo Biochemistry 36 1997 12364 12370
-
(1997)
Biochemistry
, vol.36
, pp. 12364-12370
-
-
Ermolieff, J.1
Lin, X.2
Tang, J.3
-
35
-
-
0026047763
-
Determination of the relative binding free energies of peptide inhibitors to the HIV-1 protease
-
D.M. Ferguson R.J. Radmer P.A. Kollman Determination of the relative binding free energies of peptide inhibitors to the HIV-1 protease J. Med. Chem. 34 1991 2654 2659
-
(1991)
J. Med. Chem.
, vol.34
, pp. 2654-2659
-
-
Ferguson, D.M.1
Radmer, R.J.2
Kollman, P.A.3
-
36
-
-
0032580479
-
HIV-protease inhibitors
-
C. Flexner HIV-protease inhibitors N. Engl. J. Med. 338 1998 1281 1292
-
(1998)
N. Engl. J. Med.
, vol.338
, pp. 1281-1292
-
-
Flexner, C.1
-
37
-
-
27244462844
-
Isothermal titration calorimetry. Direct thermodynamic characterization of biological molecular interactions
-
E. Freire O.L. Mayorga M. Straume Isothermal titration calorimetry. Direct thermodynamic characterization of biological molecular interactions Anal. Chem. 62 1990 950A 959A
-
(1990)
Anal. Chem.
, vol.62
, pp. 950A-959A
-
-
Freire, E.1
Mayorga, O.L.2
Straume, M.3
-
39
-
-
0026787837
-
Use of protein unfolding studies to determine the conformational and dimeric stabilities of HIV-1 and SIV protease
-
S. Grant I. Deckman J. Culp M. Minnich I. Brooks P. Hensley C. Debouck T. Meek Use of protein unfolding studies to determine the conformational and dimeric stabilities of HIV-1 and SIV protease Biochemistry 31 1992 9491 9501
-
(1992)
Biochemistry
, vol.31
, pp. 9491-9501
-
-
Grant, S.1
Deckman, I.2
Culp, J.3
Minnich, M.4
Brooks, I.5
Hensley, P.6
Debouck, C.7
Meek, T.8
-
40
-
-
0026721254
-
Different requirements for productive interaction between the active site of HIV-1 proteinase and substrates containing -hydrophobic∗ hydrophobic- or -aromatic∗pro- cleavage sites
-
∗pro- cleavage sites Biochemistry 31 1992 5193 5200
-
(1992)
Biochemistry
, vol.31
, pp. 5193-5200
-
-
Griffiths, J.T.1
Phylip, L.H.2
Konvalinka, J.3
Strop, P.4
Gustchina, A.5
Wlodawer, A.6
Davenport, R.J.7
Briggs, R.8
Dunn, B.M.9
Kay, J.10
-
41
-
-
0029151345
-
Kinetic characterization and cross-resistance patterns of HIV-1 protease mutants selected under drug pressure
-
S.V. Gulnik L.I. Suvorov B. Liu B. Yu B. Anderson H. Mitsuya J.W. Erickson Kinetic characterization and cross-resistance patterns of HIV-1 protease mutants selected under drug pressure Biochemistry 34 1995 9282 9287
-
(1995)
Biochemistry
, vol.34
, pp. 9282-9287
-
-
Gulnik, S.V.1
Suvorov, L.I.2
Liu, B.3
Yu, B.4
Anderson, B.5
Mitsuya, H.6
Erickson, J.W.7
-
42
-
-
0001917813
-
Mutation in retroviral genes associated with drug resistance
-
J. Hammond B.A. Larder R.F. Schinazi J.W. Mellors Mutation in retroviral genes associated with drug resistance B. Korber B. Foley T. Leither F. McCutchan B. Hahn J.W. Mellors G. Myers C. Kuiken Human Retroviruses and AIDS 1997 III 207-III-249 Los Alamos, NM
-
(1997)
, pp. III-207-III-249
-
-
Hammond, J.1
Larder, B.A.2
Schinazi, R.F.3
Mellors, J.W.4
-
43
-
-
0027181741
-
Prediction of the protonation state of the active site aspartyl residues in HIV-1 protease-inhibitor complexes via molecular dynamics simulation
-
W.E. Harte Jr. D.L. Beveridge Prediction of the protonation state of the active site aspartyl residues in HIV-1 protease-inhibitor complexes via molecular dynamics simulation J. Am. Chem. Soc. 115 1993 3883 3886
-
(1993)
J. Am. Chem. Soc.
, vol.115
, pp. 3883-3886
-
-
Harte, W.E.1
Beveridge, D.L.2
-
44
-
-
0028709492
-
Assay methods for retroviral proteases
-
C.U.T. Hellen Assay methods for retroviral proteases L.C. Kuo J.A. Shafer Methods of Enzymology Vol. 241 1994 Academic Press San Diego, CA 46 58
-
(1994)
, pp. 46-58
-
-
Hellen, C.U.T.1
-
46
-
-
0008547476
-
Patterns of cross-resistance among protease inhibitors in over 1500 clinical HIV-1 isolates. Comparison of genotypic and phenotypic resistance profiles
-
K. Hertogs S. Kemp S. Bloor V. Miller S. Staszewski J. Mellors C. van den Eynde F. Peeters B. Larder R. Pauwels Patterns of cross-resistance among protease inhibitors in over 1500 clinical HIV-1 isolates. Comparison of genotypic and phenotypic resistance profiles Int. Workshop HIV Drug Resist. Treat. Strategies, 2nd 24–27 June, 1998, Lake Maggiore, Italy 1998 49 Abstract 70
-
(1998)
, pp. 49
-
-
Hertogs, K.1
Kemp, S.2
Bloor, S.3
Miller, V.4
Staszewski, S.5
Mellors, J.6
van den Eynde, C.7
Peeters, F.8
Larder, B.9
Pauwels, R.10
-
47
-
-
0028014288
-
Characterization of human immunodeficiency virus type 1 variants with increased resistance to a C2-symmetric protease inhibitor
-
2-symmetric protease inhibitor J. Virol. 68 1994 2016 2020
-
(1994)
J. Virol.
, vol.68
, pp. 2016-2020
-
-
Ho, D.D.1
Toyoshima, T.2
Mo, H.3
Kempf, D.J.4
Norbeck, D.5
Chen, C.-M.6
Wideburg, N.E.7
Burt, S.K.8
Erickson, J.W.9
Singh, M.K.10
-
48
-
-
0030113025
-
Improved cyclic urea inhibitors of the HIV-1 protease: Synthesis, potency, resistance profile, human pharmacokinetics and X-ray crystal structure of DMP 450
-
C.N. Hodge P.E. Aldrich L.T. Bacheler C.H. Chang C.J. Eyermann S. Garber M. Grubb D.A. Jackson P.K. Jadhav B. Korant P.Y. Lam M.B. Maurin J.L. Meek M.J. Otto M.M. Rayner C. Reid T.R. Sharpe L. Shum D.L. Winslow S. Erickson-Viitanen Improved cyclic urea inhibitors of the HIV-1 protease: Synthesis, potency, resistance profile, human pharmacokinetics and X-ray crystal structure of DMP 450 Chem. Biol. 3 1996 301 314
-
(1996)
Chem. Biol.
, vol.3
, pp. 301-314
-
-
Hodge, C.N.1
Aldrich, P.E.2
Bacheler, L.T.3
Chang, C.H.4
Eyermann, C.J.5
Garber, S.6
Grubb, M.7
Jackson, D.A.8
Jadhav, P.K.9
Korant, B.10
Lam, P.Y.11
Maurin, M.B.12
Meek, J.L.13
Otto, M.J.14
Rayner, M.M.15
Reid, C.16
Sharpe, T.R.17
Shum, L.18
Winslow, D.L.19
Erickson-Viitanen, S.20
more..
-
49
-
-
0029795041
-
Human immunodeficiency virus protease ligand specificity conferred by residues outside of the active site cavity
-
S.S. Hoog E.M. Towler B. Zhao M.L. Doyle C. Debouck S.S. Abdel-Meguid Human immunodeficiency virus protease ligand specificity conferred by residues outside of the active site cavity Biochemistry 35 1996 10279 10286
-
(1996)
Biochemistry
, vol.35
, pp. 10279-10286
-
-
Hoog, S.S.1
Towler, E.M.2
Zhao, B.3
Doyle, M.L.4
Debouck, C.5
Abdel-Meguid, S.S.6
-
51
-
-
0026005186
-
Human immunodeficiency virus-1 protease. 2. Use of pH rate studies and solvent kinetic isotope effects to elucidate details of chemical mechanism
-
L.J. Hyland T.A. Tomaszek Jr. T.D. Meek Human immunodeficiency virus-1 protease. 2. Use of pH rate studies and solvent kinetic isotope effects to elucidate details of chemical mechanism Biochemistry 30 1991 8454 8463
-
(1991)
Biochemistry
, vol.30
, pp. 8454-8463
-
-
Hyland, L.J.1
Tomaszek, T.A.2
Meek, T.D.3
-
52
-
-
0026325601
-
Kinetic studies of human immunodeficiency virus type 1 protease and its active-site hydrogen vond mutant A28S
-
E. Ido H.P. Han F.J. Kezdy J. Tang Kinetic studies of human immunodeficiency virus type 1 protease and its active-site hydrogen vond mutant A28S J. Biol. Chem. 266 1991 24359 24366
-
(1991)
J. Biol. Chem.
, vol.266
, pp. 24359-24366
-
-
Ido, E.1
Han, H.P.2
Kezdy, F.J.3
Tang, J.4
-
53
-
-
0029824426
-
In vivo resistance to a human immunodeficiency virus type 1 proteinase inhibitor: Mutations, kinetics, and frequencies
-
H. Jacobsen M. Hanggi M. Ott I.B. Duncan S. Owen M. Andreoni S. Vella J. Mous In vivo resistance to a human immunodeficiency virus type 1 proteinase inhibitor: Mutations, kinetics, and frequencies J. Infect. Dis. 173 1996 1379 1387
-
(1996)
J. Infect. Dis.
, vol.173
, pp. 1379-1387
-
-
Jacobsen, H.1
Hanggi, M.2
Ott, M.3
Duncan, I.B.4
Owen, S.5
Andreoni, M.6
Vella, S.7
Mous, J.8
-
54
-
-
0031022510
-
Cyclic urea amides: HIV-1 protease inhibitors with low nanomolar potency against both wild type and protease inhibitor resistant mutants of HIV
-
P.K. Jadhav P. Ala F.J. Woerner C.H. Chang S.S. Garber E.D. Anton L.T. Bacheler Cyclic urea amides: HIV-1 protease inhibitors with low nanomolar potency against both wild type and protease inhibitor resistant mutants of HIV J. Med. Chem. 40 1997 181 191
-
(1997)
J. Med. Chem.
, vol.40
, pp. 181-191
-
-
Jadhav, P.K.1
Ala, P.2
Woerner, F.J.3
Chang, C.H.4
Garber, S.S.5
Anton, E.D.6
Bacheler, L.T.7
-
55
-
-
0026640529
-
Activity and dimerization of human immunodeficiency virus protease as a function of solvent composition and enzyme concentration
-
S. Jordan J. Zugay P. Darke L. Kuo Activity and dimerization of human immunodeficiency virus protease as a function of solvent composition and enzyme concentration J. Biol. Chem. 267 1992 20028 20032
-
(1992)
J. Biol. Chem.
, vol.267
, pp. 20028-20032
-
-
Jordan, S.1
Zugay, J.2
Darke, P.3
Kuo, L.4
-
56
-
-
14444281534
-
Viracept (nelfinavir mesylate, AG1343): A potent, orally bioavailable inhibitor of HIV-1 protease
-
S.W. Kaldor V.J. Kalish J.F. Davies 2nd B.V. Shetty J.E. Fritz K. Appelt J.A. Burgess K.M. Campanale N.Y. Chirgadze D.K. Clawson B.A. Dressman S.D. Hatch D.A. Khalil M.B. Kosa P.P. Lubbehusen M.A. Muesing A.K. Patick S.H. Reich K.S. Su J.H. Tatlock Viracept (nelfinavir mesylate, AG1343): A potent, orally bioavailable inhibitor of HIV-1 protease J. Med. Chem. 40 1997 3979 3985
-
(1997)
J. Med. Chem.
, vol.40
, pp. 3979-3985
-
-
Kaldor, S.W.1
Kalish, V.J.2
Davies, J.F.3
Shetty, B.V.4
Fritz, J.E.5
Appelt, K.6
Burgess, J.A.7
Campanale, K.M.8
Chirgadze, N.Y.9
Clawson, D.K.10
Dressman, B.A.11
Hatch, S.D.12
Khalil, D.A.13
Kosa, M.B.14
Lubbehusen, P.P.15
Muesing, M.A.16
Patick, A.K.17
Reich, S.H.18
Su, K.S.19
Tatlock, J.H.20
more..
-
57
-
-
0025828543
-
Human immunodeficiency virus type 1 Gag proteins are processed in two cellular compartments
-
A.H. Kaplan R. Swanstrom Human immunodeficiency virus type 1 Gag proteins are processed in two cellular compartments Proc. Natl. Acad. Sci. U.S.A. 88 1991 4528 4532
-
(1991)
, pp. 4528-4532
-
-
Kaplan, A.H.1
Swanstrom, R.2
-
58
-
-
0027158754
-
Partial inhibition of the human immunodeficiency virus type 1 protease results in aberrant virus assembly and the formation of noninfectious particles
-
A.H. Kaplan J.A. Zack M. Knigge D.A. Paul D.J. Kempf D.W. Norbeck R. Swanstrom Partial inhibition of the human immunodeficiency virus type 1 protease results in aberrant virus assembly and the formation of noninfectious particles J. Virol. 67 1993 4050
-
(1993)
J. Virol.
, vol.67
, pp. 4050
-
-
Kaplan, A.H.1
Zack, J.A.2
Knigge, M.3
Paul, D.A.4
Kempf, D.J.5
Norbeck, D.W.6
Swanstrom, R.7
-
59
-
-
0027932364
-
The activity of the protease of human immunodeficiency virus type 1 is initiated at the membrane of infected cells before the release of viral proteins and is required for release to occur with maximum efficiency
-
A.H. Kaplan M. Manchester R. Swanstrom The activity of the protease of human immunodeficiency virus type 1 is initiated at the membrane of infected cells before the release of viral proteins and is required for release to occur with maximum efficiency J. Virol. 68 1994 6782 6786
-
(1994)
J. Virol.
, vol.68
, pp. 6782-6786
-
-
Kaplan, A.H.1
Manchester, M.2
Swanstrom, R.3
-
60
-
-
0028286025
-
Selection of multiple human immunodeficiency virus type 1 variants that encode viral proteases with decreased sensitivity to an inhibitor of the viral protease
-
A.H. Kaplan S.F. Michael R.S. Wehbie M.F. Knigge D.A. Paul L. Everitt D.J. Kempf D.W. Norbeck J.W. Erickson R. Swanstrom Selection of multiple human immunodeficiency virus type 1 variants that encode viral proteases with decreased sensitivity to an inhibitor of the viral protease Proc. Natl. Acad. Sci. U.S.A. 91 1994 5597 5601
-
(1994)
, pp. 5597-5601
-
-
Kaplan, A.H.1
Michael, S.F.2
Wehbie, R.S.3
Knigge, M.F.4
Paul, D.A.5
Everitt, L.6
Kempf, D.J.7
Norbeck, D.W.8
Erickson, J.W.9
Swanstrom, R.10
-
61
-
-
0023199453
-
Inhibition of retroviral protease activity by an aspartyl proteinase inhibitor
-
I. Katoh T. Yasunaga Y. Ikawa Y. Yoshinaka Inhibition of retroviral protease activity by an aspartyl proteinase inhibitor Nature (London) 329 1987 654 656
-
(1987)
Nature (London)
, vol.329
, pp. 654-656
-
-
Katoh, I.1
Yasunaga, T.2
Ikawa, Y.3
Yoshinaka, Y.4
-
62
-
-
0028968902
-
ABT-538 is a potent inhibitor of human immunodeficiency virus protease and as high oral bioavailability in humans
-
D.J. Kempf K.C. Marsh J.F. Denissen E. McDonald S. Vasavanonda C.A. Flentge B.E. Green L. Fino C.H. Park X.P. Kong ABT-538 is a potent inhibitor of human immunodeficiency virus protease and as high oral bioavailability in humans Proc. Natl. Acad. Sci. U.S.A. 92 1995 2484 2488
-
(1995)
, pp. 2484-2488
-
-
Kempf, D.J.1
Marsh, K.C.2
Denissen, J.F.3
McDonald, E.4
Vasavanonda, S.5
Flentge, C.A.6
Green, B.E.7
Fino, L.8
Park, C.H.9
Kong, X.P.10
-
63
-
-
15144357022
-
The duration of viral suppression during protease inhibitor therapy for HIV-1 infection is predicted by plasma HIV-1 RNA at the nadir
-
D.J. Kempf R.A. Rode Y. Xu E. Sun M.E. Heath-Chiozzi J. Valdes A.J. Japour S. Danner C. Boucher A. Molla J.M. Leonard The duration of viral suppression during protease inhibitor therapy for HIV-1 infection is predicted by plasma HIV-1 RNA at the nadir AIDS 12 1998 F9 F14
-
(1998)
AIDS
, vol.12
, pp. F9-F14
-
-
Kempf, D.J.1
Rode, R.A.2
Xu, Y.3
Sun, E.4
Heath-Chiozzi, M.E.5
Valdes, J.6
Japour, A.J.7
Danner, S.8
Boucher, C.9
Molla, A.10
Leonard, J.M.11
-
64
-
-
0029794741
-
New series of potent, orally bioavailable, non-peptidic cyclic sulfones as HIV-1 protease inhibitors
-
C.U. Kim L.R. McGee S.H. Krawczyk E. Harwood Y. Harada S. Swaminathan N. Bischofberger M.S. Chen J.M. Cherrington S.F. Xiong L. Griffin K.C. Cundy A. Lee B. Yu S. Gulnik J.W. Erickson New series of potent, orally bioavailable, non-peptidic cyclic sulfones as HIV-1 protease inhibitors J. Med. Chem. 39 1996 3431 3434
-
(1996)
J. Med. Chem.
, vol.39
, pp. 3431-3434
-
-
Kim, C.U.1
McGee, L.R.2
Krawczyk, S.H.3
Harwood, E.4
Harada, Y.5
Swaminathan, S.6
Bischofberger, N.7
Chen, M.S.8
Cherrington, J.M.9
Xiong, S.F.10
Griffin, L.11
Cundy, K.C.12
Lee, A.13
Yu, B.14
Gulnik, S.15
Erickson, J.W.16
-
66
-
-
0032537482
-
Resistance to HIV protease inhibitors: A comparison of enzyme inhibition and antiviral potency
-
R.M. Klabe L.T. Bacheler P.J. Ala S. Erickson-Viitanen J.L. Meek Resistance to HIV protease inhibitors: A comparison of enzyme inhibition and antiviral potency Biochemistry 37 1998 8735 8742
-
(1998)
Biochemistry
, vol.37
, pp. 8735-8742
-
-
Klabe, R.M.1
Bacheler, L.T.2
Ala, P.J.3
Erickson-Viitanen, S.4
Meek, J.L.5
-
68
-
-
0025358371
-
Sub-site preferences of the aspartic proteinase from the human immunodeficiency virus, HIV-1
-
J. Konvalinnka P. Strop J. Velek V. Cerna V. Kostka L.H. Phylip A.D. Richards B.M. Dunn J. Kay Sub-site preferences of the aspartic proteinase from the human immunodeficiency virus, HIV-1 FEBS Lett. 268 1990 35 38
-
(1990)
FEBS Lett.
, vol.268
, pp. 35-38
-
-
Konvalinnka, J.1
Strop, P.2
Velek, J.3
Cerna, V.4
Kostka, V.5
Phylip, L.H.6
Richards, A.D.7
Dunn, B.M.8
Kay, J.9
-
69
-
-
0026600844
-
An engineered retroviral proteinase from myeloblastosis associated virus acquires pH dependence and substrate specificity of the HIV-1 proteinase
-
J. Konvalinka M. Horejsi M. Andreansky P. Novek I. Pichova I. Blaha M. Fabry J. Sedlacek S. Foundling P. Strop An engineered retroviral proteinase from myeloblastosis associated virus acquires pH dependence and substrate specificity of the HIV-1 proteinase EMBO J. 11 1992 1141 1144
-
(1992)
EMBO J.
, vol.11
, pp. 1141-1144
-
-
Konvalinka, J.1
Horejsi, M.2
Andreansky, M.3
Novek, P.4
Pichova, I.5
Blaha, I.6
Fabry, M.7
Sedlacek, J.8
Foundling, S.9
Strop, P.10
-
70
-
-
0030825663
-
The HIV protease and therapies for AIDS
-
B.D. Korant C.J. Rizzo The HIV protease and therapies for AIDS Adv. Exp. Med. Biol. 421 1997 279 284
-
(1997)
Adv. Exp. Med. Biol.
, vol.421
, pp. 279-284
-
-
Korant, B.D.1
Rizzo, C.J.2
-
72
-
-
0026757343
-
Human immunodeficiency virus type 1 Gag-protease fusion proteins are enzymatically active
-
M. Kotler G. Arad S. Hughes Human immunodeficiency virus type 1 Gag-protease fusion proteins are enzymatically active J. Virol. 66 1992 6781 6783
-
(1992)
J. Virol.
, vol.66
, pp. 6781-6783
-
-
Kotler, M.1
Arad, G.2
Hughes, S.3
-
73
-
-
0030740060
-
Human immunodeficiency virus type 1 (HIV-1) protein Vif inhibits the activity of HIV-1 protease in bacteria and in vitro
-
M. Kotler M. Simm Y.S. Zhao P. Sova W. Chao S.F. Ohnona R. Roller C. Krachmarov M.J. Potash D.J. Volsky Human immunodeficiency virus type 1 (HIV-1) protein Vif inhibits the activity of HIV-1 protease in bacteria and in vitro J. Virol. 71 1997 5774 5781
-
(1997)
J. Virol.
, vol.71
, pp. 5774-5781
-
-
Kotler, M.1
Simm, M.2
Zhao, Y.S.3
Sova, P.4
Chao, W.5
Ohnona, S.F.6
Roller, R.7
Krachmarov, C.8
Potash, M.J.9
Volsky, D.J.10
-
74
-
-
15844378825
-
Extensive polymorphisms observed in HIV-1 clade B protease gene using high-density oligonucleotide arrays
-
M.J. Kozal N. Shah N. Shen R. Yang R. Fucini T.C. Merigan D.D. Richman D. Morris E. Hubbell M. Chee T.R. Gingeras Extensive polymorphisms observed in HIV-1 clade B protease gene using high-density oligonucleotide arrays Nat. Med. 2 1996 753 759
-
(1996)
Nat. Med.
, vol.2
, pp. 753-759
-
-
Kozal, M.J.1
Shah, N.2
Shen, N.3
Yang, R.4
Fucini, R.5
Merigan, T.C.6
Richman, D.D.7
Morris, D.8
Hubbell, E.9
Chee, M.10
Gingeras, T.R.11
-
75
-
-
0028693604
-
Synthetic approaches to continuous assays of retro-viral proteases
-
G.A. Krafft G.T. Wang Synthetic approaches to continuous assays of retro-viral proteases L.C. Kuo J.A. Shafer Methods in Enzymology Vol. 241 1994 Academic Press San Diego, CA 70 86
-
(1994)
, pp. 70-86
-
-
Krafft, G.A.1
Wang, G.T.2
-
77
-
-
0029013585
-
The spacer peptide between human immonodeficiency virus capsid and nucleocapsid proteins is essential for ordered assembly and viral infectivity
-
H.-G. Kräusslich M. Fäcke A.-M. Heuser J. Konvalinka H. Sentgraf The spacer peptide between human immonodeficiency virus capsid and nucleocapsid proteins is essential for ordered assembly and viral infectivity J. Virol. 69 1995 3407 3419
-
(1995)
J. Virol.
, vol.69
, pp. 3407-3419
-
-
Kräusslich, H.-G.1
Fäcke, M.2
Heuser, A.-M.3
Konvalinka, J.4
Sentgraf, H.5
-
79
-
-
0030266484
-
Sensing the heat: The application of isothermal titration calorimetry to the thermodynamic studies of biomolecular interactions
-
J. Ladbury B. Chowdhry Sensing the heat: The application of isothermal titration calorimetry to the thermodynamic studies of biomolecular interactions Chem. Biol. 3 1996 791 801
-
(1996)
Chem. Biol.
, vol.3
, pp. 791-801
-
-
Ladbury, J.1
Chowdhry, B.2
-
80
-
-
0028057975
-
Rational design of potent, bioavailable, nonpeptide cyclic ureas as HIV protease inhibitors
-
P.Y.S. Lam P.K. Jadhav C.J. Eyermann C.N. Hodge Y. Ru L.T. Bacheler J.L. Meek M.J. Otto M.M. Rayner Y.N. Wong C.-H. Chang P.C. Weber D.A. Jackson T.R. Sharpe S. Erickson-Viitanen Rational design of potent, bioavailable, nonpeptide cyclic ureas as HIV protease inhibitors Science 263 1994 380 384
-
(1994)
Science
, vol.263
, pp. 380-384
-
-
Lam, P.Y.S.1
Jadhav, P.K.2
Eyermann, C.J.3
Hodge, C.N.4
Ru, Y.5
Bacheler, L.T.6
Meek, J.L.7
Otto, M.J.8
Rayner, M.M.9
Wong, Y.N.10
Chang, C.-H.11
Weber, P.C.12
Jackson, D.A.13
Sharpe, T.R.14
Erickson-Viitanen, S.15
-
81
-
-
20244373125
-
X-ray analysis of HIV-1 proteinase at 2.7Å resolution confirms structural homology among retroviral enzymes
-
R. Lapatto T. Blundell A. Hemmings J. Overington A. Wilderspin S. Wood J.R. Merson P.J. Whittle D.E. Danley K.F. Geoghegan S.J. Hawrylik S.E. Lee K. Scheld P.M. Hobart X-ray analysis of HIV-1 proteinase at 2.7Å resolution confirms structural homology among retroviral enzymes Nature (London) 342 1989 299 302
-
(1989)
Nature (London)
, vol.342
, pp. 299-302
-
-
Lapatto, R.1
Blundell, T.2
Hemmings, A.3
Overington, J.4
Wilderspin, A.5
Wood, S.6
Merson, J.R.7
Whittle, P.J.8
Danley, D.E.9
Geoghegan, K.F.10
Hawrylik, S.J.11
Lee, S.E.12
Scheld, K.13
Hobart, P.M.14
-
82
-
-
9044230526
-
In vivo sequence diversity of the protease of human immunodeficiency virus type 1: Presence of protease inhibitor-resistant variants in untreated subjects
-
W.J. Lech G. Wang Y.L. Yang Y. Chee K. Dorman D. McCrae L.C. Lazzeroni J.W. Erickson J.S. Sinsheimer A.H. Kaplan In vivo sequence diversity of the protease of human immunodeficiency virus type 1: Presence of protease inhibitor-resistant variants in untreated subjects J. Virol. 70 1996 2038 2043
-
(1996)
J. Virol.
, vol.70
, pp. 2038-2043
-
-
Lech, W.J.1
Wang, G.2
Yang, Y.L.3
Chee, Y.4
Dorman, K.5
McCrae, D.6
Lazzeroni, L.C.7
Erickson, J.W.8
Sinsheimer, J.S.9
Kaplan, A.H.10
-
83
-
-
0029872085
-
Design, synthesis, and characterization of dipeptide isostere containing cis-epoxide for the irreversible inactivation of HIV protease
-
C.S. Lee N. Choy C. Park H. Choi Y.C. Son S. Kim J.H. Ok H. Yoon S.C. Kim Design, synthesis, and characterization of dipeptide isostere containing cis-epoxide for the irreversible inactivation of HIV protease Bioorg. Med. Chem. Lett. 6 1996 589 594
-
(1996)
Bioorg. Med. Chem. Lett.
, vol.6
, pp. 589-594
-
-
Lee, C.S.1
Choy, N.2
Park, C.3
Choi, H.4
Son, Y.C.5
Kim, S.6
Ok, J.H.7
Yoon, H.8
Kim, S.C.9
-
84
-
-
0032574705
-
Molecular basis of resistance to HIV-1 protease inhibition: A plausible hypothesis
-
I. Luque M. Todd J. Gomez N. Semo E. Freire Molecular basis of resistance to HIV-1 protease inhibition: A plausible hypothesis Biochemistry 37 1998 5791 5797
-
(1998)
Biochemistry
, vol.37
, pp. 5791-5797
-
-
Luque, I.1
Todd, M.2
Gomez, J.3
Semo, N.4
Freire, E.5
-
85
-
-
0031846317
-
Resistance-associated loss of viral fitness in human immunodeficiency virus type 1: Phenotypic analysis of protease and gag coevolution in protease inhibitor-treated patients
-
F. Mammano C. Petit F. Clavel Resistance-associated loss of viral fitness in human immunodeficiency virus type 1: Phenotypic analysis of protease and gag coevolution in protease inhibitor-treated patients J. Virol. 72 1998 7632 7637
-
(1998)
J. Virol.
, vol.72
, pp. 7632-7637
-
-
Mammano, F.1
Petit, C.2
Clavel, F.3
-
86
-
-
0028854676
-
Selection and analysis of human immunodeficiency virus type 1 variants with increased resistance to ABT-538, a novel protease inhibitor
-
M. Markowitz H. Mo D.J. Kempf D.W. Norbeck T.N. Bhat J.W. Erickson D.D. Ho Selection and analysis of human immunodeficiency virus type 1 variants with increased resistance to ABT-538, a novel protease inhibitor J. Virol. 69 1995 701 706
-
(1995)
J. Virol.
, vol.69
, pp. 701-706
-
-
Markowitz, M.1
Mo, H.2
Kempf, D.J.3
Norbeck, D.W.4
Bhat, T.N.5
Erickson, J.W.6
Ho, D.D.7
-
87
-
-
0032928065
-
Replicative fitness of protease inhibitor resistant mutants of human immunodeficiency virus type 1
-
J. Martinez-Picado A. Savara L. Sutton R. D'Aquila Replicative fitness of protease inhibitor resistant mutants of human immunodeficiency virus type 1 J. Virol. 73 1999 3744 3752
-
(1999)
J. Virol.
, vol.73
, pp. 3744-3752
-
-
Martinez-Picado, J.1
Savara, A.2
Sutton, L.3
D'Aquila, R.4
-
88
-
-
0030468331
-
Human immunodeficiency virus. Mutations in the viral protease that confer resistance to saquinavir increase the dissociation rate constant of the protease-saquinavir complex
-
B. Maschera G. Darby G. Palu L.L. Wright M. Tisdale R. Myers E.D. Blair E.S. Furfine Human immunodeficiency virus. Mutations in the viral protease that confer resistance to saquinavir increase the dissociation rate constant of the protease-saquinavir complex J. Biol. Chem. 271 1996 33231 33235
-
(1996)
J. Biol. Chem.
, vol.271
, pp. 33231-33235
-
-
Maschera, B.1
Darby, G.2
Palu, G.3
Wright, L.L.4
Tisdale, M.5
Myers, R.6
Blair, E.D.7
Furfine, E.S.8
-
89
-
-
0025099016
-
A synthetic HIV-1 protease inhibitor with antiviral activity arrests HIV-like particle maturation
-
T.J. McQuade A.G. Tomasselli L. Liu V. Karacostas B. Moss T.K. Sawyer R.L. Heinrikson W.G. Tarpley A synthetic HIV-1 protease inhibitor with antiviral activity arrests HIV-like particle maturation Science 247 1990 454 456
-
(1990)
Science
, vol.247
, pp. 454-456
-
-
McQuade, T.J.1
Tomasselli, A.G.2
Liu, L.3
Karacostas, V.4
Moss, B.5
Sawyer, T.K.6
Heinrikson, R.L.7
Tarpley, W.G.8
-
90
-
-
0000004753
-
Human immunodeficiency virus 1 protease expressed in Escherichia coli behaves as a dimeric aspartic protease
-
T.D. Meek B.D. Dayton B.W. Metcalf G.B. Dreyer J.E. Strickler J.G. Gorniak M. Rosenberg M.L. Moore V.W. Magaard C. Debouck Human immunodeficiency virus 1 protease expressed in Escherichia coli behaves as a dimeric aspartic protease Proc. Natl. Acad. Sci. U.S.A. 86 1989 1841 1845
-
(1989)
, pp. 1841-1845
-
-
Meek, T.D.1
Dayton, B.D.2
Metcalf, B.W.3
Dreyer, G.B.4
Strickler, J.E.5
Gorniak, J.G.6
Rosenberg, M.7
Moore, M.L.8
Magaard, V.W.9
Debouck, C.10
-
91
-
-
0028717766
-
Use of steady state kinetic methods to elucidate the kinetic and chemical mechanisms of retroviral proteases
-
T.D. Meek E.J. Rodriguez T.S. Angeles Use of steady state kinetic methods to elucidate the kinetic and chemical mechanisms of retroviral proteases L.C. Kuo J.A. Shafer Methods in Enzymology Vol. 241 1994 Academic Press San Diego, CA 127 156
-
(1994)
, pp. 127-156
-
-
Meek, T.D.1
Rodriguez, E.J.2
Angeles, T.S.3
-
92
-
-
0028105957
-
The HIV-1 protease as enzyme and substrate: Mutagenesis of autolysis sites and generation of a stable mutant with retained kinetic properties
-
A.M. Mildner D.J. Rothrock J.W. Leone C.A. vannow J.M. Lull I.M. Reardon J.L. Sarcich W.J. Howe C.-S.C. Tomich C.W. Smith R.L. Heinrikson A.G. Tomasselli The HIV-1 protease as enzyme and substrate: Mutagenesis of autolysis sites and generation of a stable mutant with retained kinetic properties Biochemistry 33 1994 9405 9413
-
(1994)
Biochemistry
, vol.33
, pp. 9405-9413
-
-
Mildner, A.M.1
Rothrock, D.J.2
Leone, J.W.3
vannow, C.A.4
Lull, J.M.5
Reardon, I.M.6
Sarcich, J.L.7
Howe, W.J.8
Tomich, C.-S.C.9
Smith, C.W.10
Heinrikson, R.L.11
Tomasselli, A.G.12
-
93
-
-
15444377672
-
Ordered accumulation of mutations in HIV protease confers resistance to ritonavir
-
A. Molla M. Korneyeva Q. Gao S. Vasavanonda P.J. Schipper H.M. Mo M. Markowitz T. Chernyavskiy P. Niu N. Lyons A. Hsu G.R. Granneman D.D. Ho C.A. Boucher J.M. Leonard D.W. Norbeck D.J. Kempf Ordered accumulation of mutations in HIV protease confers resistance to ritonavir Nat Med. 2 1996 760 766
-
(1996)
Nat Med.
, vol.2
, pp. 760-766
-
-
Molla, A.1
Korneyeva, M.2
Gao, Q.3
Vasavanonda, S.4
Schipper, P.J.5
Mo, H.M.6
Markowitz, M.7
Chernyavskiy, T.8
Niu, P.9
Lyons, N.10
Hsu, A.11
Granneman, G.R.12
Ho, D.D.13
Boucher, C.A.14
Leonard, J.M.15
Norbeck, D.W.16
Kempf, D.J.17
-
95
-
-
0029964107
-
Current knowledge and future prospects for the use of HIV protease inhibitors
-
G. Moyle B. Gazzard Current knowledge and future prospects for the use of HIV protease inhibitors Drugs 51 1996 701 712
-
(1996)
Drugs
, vol.51
, pp. 701-712
-
-
Moyle, G.1
Gazzard, B.2
-
96
-
-
0026756702
-
Thermodynamics of structural stability and cooperative folding behavior in proteins
-
K.P. Murphy E. Freire Thermodynamics of structural stability and cooperative folding behavior in proteins Adv. Protein Chem. 43 1992 313 361
-
(1992)
Adv. Protein Chem.
, vol.43
, pp. 313-361
-
-
Murphy, K.P.1
Freire, E.2
-
97
-
-
0024555898
-
Three-dimensional structure of aspartyl protease from human immunodeficiency virus HIV-1
-
M.A. Navia P.M.D. Fitzgerald B.M. McKeever C.-T. Leu J.C. Heimbach W.K. Herber I.S. Sigal P.L. Darke J.P. Springer Three-dimensional structure of aspartyl protease from human immunodeficiency virus HIV-1 Nature (London) 337 1989 615 620
-
(1989)
Nature (London)
, vol.337
, pp. 615-620
-
-
Navia, M.A.1
Fitzgerald, P.M.D.2
McKeever, B.M.3
Leu, C.-T.4
Heimbach, J.C.5
Herber, W.K.6
Sigal, I.S.7
Darke, P.L.8
Springer, J.P.9
-
100
-
-
0029897059
-
Saquinavir. A review of its pharmacology and clinical potential in the management of HIV infection
-
S. Noble D. Faulds Saquinavir. A review of its pharmacology and clinical potential in the management of HIV infection Drugs 52 1996 93 112
-
(1996)
Drugs
, vol.52
, pp. 93-112
-
-
Noble, S.1
Faulds, D.2
-
101
-
-
0028046926
-
Determination of kinetic rate constants for the binding of inhibitors to HIV-1 protease and for the association and dissociation of active homodimer
-
C.A. Pargellis M.M. Morelock E.T. Graham P. Kinkade S. Pav K. Lubbe D. Lamarre P.C. Anderson Determination of kinetic rate constants for the binding of inhibitors to HIV-1 protease and for the association and dissociation of active homodimer Biochemistry 33 1994 12527 12534
-
(1994)
Biochemistry
, vol.33
, pp. 12527-12534
-
-
Pargellis, C.A.1
Morelock, M.M.2
Graham, E.T.3
Kinkade, P.4
Pav, S.5
Lubbe, K.6
Lamarre, D.7
Anderson, P.C.8
-
102
-
-
0029125661
-
Rational design of irreversible, pseudo-C2-symmetric HIV-1 protease inhibitors
-
2-symmetric HIV-1 protease inhibitors Bioorg. Med. Chem. Lett. 5 1995 1843 1848
-
(1995)
Bioorg. Med. Chem. Lett.
, vol.5
, pp. 1843-1848
-
-
Park, C.1
Koh, S.J.2
Son, Y.C.3
Choi, H.4
Lee, C.S.5
Cho, N.6
Moon, K.Y.7
Jung, W.H.8
Kim, S.C.9
Yoon, H.10
-
103
-
-
0029092503
-
In vitro selection and characterization of human immunodeficiency virus type 1 (HIV-1) isolates with reduced sensitivity to hydroxyethylamino sulfonamide inhibitors of HIV-1 aspartyl protease
-
J.A. Partaledis K. Yamaguchi M. Tisdale E.E. Blair C. Falcione B. Maschera R.E. Myers S. Pazhanisamy O. Futer A.B. Cullinan C.M. Stuver R.A. Byrn D.J. Livingston In vitro selection and characterization of human immunodeficiency virus type 1 (HIV-1) isolates with reduced sensitivity to hydroxyethylamino sulfonamide inhibitors of HIV-1 aspartyl protease J. Virol. 69 1995 5228 5235
-
(1995)
J. Virol.
, vol.69
, pp. 5228-5235
-
-
Partaledis, J.A.1
Yamaguchi, K.2
Tisdale, M.3
Blair, E.E.4
Falcione, C.5
Maschera, B.6
Myers, R.E.7
Pazhanisamy, S.8
Futer, O.9
Cullinan, A.B.10
Stuver, C.M.11
Byrn, R.A.12
Livingston, D.J.13
-
104
-
-
0028949246
-
Characterization of a human immunodeficiency virus type 1 variant with reduced sensitivity to an aminodiol protease inhibitor
-
A.K. Patick R. Rose J. Greytok C.M. Bechtold M.A. Hermsmeier P.T. Chen J.C. Barrish R. Zahler R.J. Colonno P.-E. Lin Characterization of a human immunodeficiency virus type 1 variant with reduced sensitivity to an aminodiol protease inhibitor J. Virol. 69 1995 2148 2152
-
(1995)
J. Virol.
, vol.69
, pp. 2148-2152
-
-
Patick, A.K.1
Rose, R.2
Greytok, J.3
Bechtold, C.M.4
Hermsmeier, M.A.5
Chen, P.T.6
Barrish, J.C.7
Zahler, R.8
Colonno, R.J.9
Lin, P.-E.10
-
105
-
-
13344275873
-
Antiviral and resistance studies of AG1343, an orally bioavailable inhibitor of human immunodeficiency virus protease
-
A.K. Patick H. Mo M. Markowitz K. Appelt B. Wu L. Musick V. Kalish S. Kaldor S. Reich D. Ho S. Webber Antiviral and resistance studies of AG1343, an orally bioavailable inhibitor of human immunodeficiency virus protease Antimicrob. Agents Chemother. 40 1996 292 297
-
(1996)
Antimicrob. Agents Chemother.
, vol.40
, pp. 292-297
-
-
Patick, A.K.1
Mo, H.2
Markowitz, M.3
Appelt, K.4
Wu, B.5
Musick, L.6
Kalish, V.7
Kaldor, S.8
Reich, S.9
Ho, D.10
Webber, S.11
-
107
-
-
0023189868
-
A structural model for the retroviral proteases
-
L.H. Pearl W.R. Taylor A structural model for the retroviral proteases Nature (London) 329 1987 351 354
-
(1987)
Nature (London)
, vol.329
, pp. 351-354
-
-
Pearl, L.H.1
Taylor, W.R.2
-
108
-
-
0027971621
-
The p2 domain of human immunodeficiency virus type 1 Gag regulates sequential proteolytic processing and is required to produce fully infectio virions
-
S. Pettit M. Moody R. Wehbie A. Kaplan P. Nantermet C. Klein R. Swantstrom The p2 domain of human immunodeficiency virus type 1 Gag regulates sequential proteolytic processing and is required to produce fully infectio virions J. Virol. 68 1994 8017 8027
-
(1994)
J. Virol.
, vol.68
, pp. 8017-8027
-
-
Pettit, S.1
Moody, M.2
Wehbie, R.3
Kaplan, A.4
Nantermet, P.5
Klein, C.6
Swantstrom, R.7
-
109
-
-
0025005515
-
Hydrolysis of synthetic chromogenic substrates by HIV-1 and HIV-2 proteinases
-
L.H. Phylip A.D. Richards J. Kay J. Konvalinka P. Strop I. Bláha J. Velek V. Kostka A.J. Ritchie A.V. Broadhurst W.G. Farmerie P.E. Scarborough B.M. Dunn Hydrolysis of synthetic chromogenic substrates by HIV-1 and HIV-2 proteinases Biochem. Biophys. Res. Commun. 171 1990 439 444
-
(1990)
Biochem. Biophys. Res. Commun.
, vol.171
, pp. 439-444
-
-
Phylip, L.H.1
Richards, A.D.2
Kay, J.3
Konvalinka, J.4
Strop, P.5
Bláha, I.6
Velek, J.7
Kostka, V.8
Ritchie, A.J.9
Broadhurst, A.V.10
Farmerie, W.G.11
Scarborough, P.E.12
Dunn, B.M.13
-
110
-
-
0028070285
-
Substrate-dependent mechanisms in the catalysis of human immunodeficiency virus protease
-
L. Polgár Z. Szeltner I. Boros Substrate-dependent mechanisms in the catalysis of human immunodeficiency virus protease Biochemistry 33 1994 9351 9357
-
(1994)
Biochemistry
, vol.33
, pp. 9351-9357
-
-
Polgár, L.1
Szeltner, Z.2
Boros, I.3
-
111
-
-
0026345896
-
A cumulative specificity model for proteases from human immunodeficiency virus types 1 and 2, inferred from statistical analysis of an extended substrate data base
-
R.A. Poorman A.G. Tomasselli R.L. Heinrikson F.J. Kézdy A cumulative specificity model for proteases from human immunodeficiency virus types 1 and 2, inferred from statistical analysis of an extended substrate data base J. Biol. Chem. 266 1991 14554 14561
-
(1991)
J. Biol. Chem.
, vol.266
, pp. 14554-14561
-
-
Poorman, R.A.1
Tomasselli, A.G.2
Heinrikson, R.L.3
Kézdy, F.J.4
-
112
-
-
0028846290
-
HIV protease inhibitors possessing a novel, high affinity and achiral P1/P2 ligand with unique pattern of in vitro resistance. Importance of conformationally-restricted template in the design of enzyme inhibitors
-
J.V. Prasad E.A. Lunney D. Ferguson P.J. Tummino R.J. Rubin E.L. Reyner B.H. Stewart R.J. Guttendorf J.M. Domagala L.I. Suvorov S.V. Gulnik I.A. Topol T.N. Bhat J.W. Erickson HIV protease inhibitors possessing a novel, high affinity and achiral P1/P2 ligand with unique pattern of in vitro resistance. Importance of conformationally-restricted template in the design of enzyme inhibitors J. Am. Chem. Soc. 117 1995 11070 11074
-
(1995)
J. Am. Chem. Soc.
, vol.117
, pp. 11070-11074
-
-
Prasad, J.V.1
Lunney, E.A.2
Ferguson, D.3
Tummino, P.J.4
Rubin, R.J.5
Reyner, E.L.6
Stewart, B.H.7
Guttendorf, R.J.8
Domagala, J.M.9
Suvorov, L.I.10
Gulnik, S.V.11
Topol, I.A.12
Bhat, T.N.13
Erickson, J.W.14
-
113
-
-
0342854936
-
Nonpeptidic potent HIV-1 protease inhibitors
-
J.V. Prasad E.A. Lunney K.S. Para P.J. Tummino D. Ferguson D. Hupe J.M. Domagala J.W. Erickson Nonpeptidic potent HIV-1 protease inhibitors Drug Des. Discovery 13 1996 15 28
-
(1996)
Drug Des. Discovery
, vol.13
, pp. 15-28
-
-
Prasad, J.V.1
Lunney, E.A.2
Para, K.S.3
Tummino, P.J.4
Ferguson, D.5
Hupe, D.6
Domagala, J.M.7
Erickson, J.W.8
-
115
-
-
0025274362
-
Sensitive, soluble chromogenic substrates for HIV-1 proteinase
-
A.D. Richards L.H. Phylip W.G. Farmerie P.E. Scarborough A. Alverez B.M. Dunn P.-H. Hirel J. Konvalinka L. Pavlickova V. Kostka J. Kay Sensitive, soluble chromogenic substrates for HIV-1 proteinase J. Biol. Chem. 265 1990 7733 7736
-
(1990)
J. Biol. Chem.
, vol.265
, pp. 7733-7736
-
-
Richards, A.D.1
Phylip, L.H.2
Farmerie, W.G.3
Scarborough, P.E.4
Alverez, A.5
Dunn, B.M.6
Hirel, P.-H.7
Konvalinka, J.8
Pavlickova, L.9
Kostka, V.10
Kay, J.11
-
116
-
-
0029563229
-
Development of drug resistance to HIV-1 protease inhibitors
-
T. Ridky J. Leis Development of drug resistance to HIV-1 protease inhibitors J. Biol. Chem. 270 1995 29621 29623
-
(1995)
J. Biol. Chem.
, vol.270
, pp. 29621-29623
-
-
Ridky, T.1
Leis, J.2
-
117
-
-
0032578505
-
Drug-resistant HIV-1 proteases identify enzyme residues important for substrate selection and catalytic rate
-
T.W. Ridky A. Kikonyogo J. Leis S. Gulnik T. Copeland J. Erickson A. Wlodawer I. Kurinov R.W. Harrison I.T. Weber Drug-resistant HIV-1 proteases identify enzyme residues important for substrate selection and catalytic rate Biochemistry 37 1998 13835 13845
-
(1998)
Biochemistry
, vol.37
, pp. 13835-13845
-
-
Ridky, T.W.1
Kikonyogo, A.2
Leis, J.3
Gulnik, S.4
Copeland, T.5
Erickson, J.6
Wlodawer, A.7
Kurinov, I.8
Harrison, R.W.9
Weber, I.T.10
-
118
-
-
0025854741
-
Processing of the precursor of NF-kappa B by the HIV-1 protease during acute infection
-
Y. Riviere V. Blank P. Kourilsky A. Israel Processing of the precursor of NF-kappa B by the HIV-1 protease during acute infection Nature (London) 350 1991 625 626
-
(1991)
Nature (London)
, vol.350
, pp. 625-626
-
-
Riviere, Y.1
Blank, V.2
Kourilsky, P.3
Israel, A.4
-
119
-
-
0032568248
-
Resistance and cross-resistance with saquinavir and other HIV protease inhibitors: Theory and practice
-
N.A. Roberts J.C. Craig J. Sheldon Resistance and cross-resistance with saquinavir and other HIV protease inhibitors: Theory and practice AIDS 12 1998 453 460
-
(1998)
AIDS
, vol.12
, pp. 453-460
-
-
Roberts, N.A.1
Craig, J.C.2
Sheldon, J.3
-
120
-
-
0025268321
-
Rational design of peptide-based HIV proteinase inhibitors
-
N.A. Roberts J.A. Martin D. Kinchington A.V. Broadhurst J.C. Craig I.B. Duncan S.A. Galpin B.K. Handa J. Kay A. Kröhn R.W. Lambert J.H. Merrett J.S. Mills K.E.B. Parkes S. Redshaw A.J. Ritchie D.L. Taylor G.J. Thomas P.J. Machin Rational design of peptide-based HIV proteinase inhibitors Science 248 1990 358 361
-
(1990)
Science
, vol.248
, pp. 358-361
-
-
Roberts, N.A.1
Martin, J.A.2
Kinchington, D.3
Broadhurst, A.V.4
Craig, J.C.5
Duncan, I.B.6
Galpin, S.A.7
Handa, B.K.8
Kay, J.9
Kröhn, A.10
Lambert, R.W.11
Merrett, J.H.12
Mills, J.S.13
Parkes, K.E.B.14
Redshaw, S.15
Ritchie, A.J.16
Taylor, D.L.17
Thomas, G.J.18
Machin, P.J.19
-
121
-
-
0027263501
-
Regulation of autoproteolysis of the HIV-1 and HIV-2 proteases with engineered amino acid substitutions
-
J.R. Rose R. Salto C.S. Craik Regulation of autoproteolysis of the HIV-1 and HIV-2 proteases with engineered amino acid substitutions J. Biol. Chem. 268 1993 11939 11945
-
(1993)
J. Biol. Chem.
, vol.268
, pp. 11939-11945
-
-
Rose, J.R.1
Salto, R.2
Craik, C.S.3
-
122
-
-
0028969065
-
Defining the level of human immunodeficiency virus type 1 (HIV-1) protease activity required for HIV-1 particle maturation and infectivity
-
J.R. Rose L.M. Babe C.S. Craik Defining the level of human immunodeficiency virus type 1 (HIV-1) protease activity required for HIV-1 particle maturation and infectivity J. Virol. 69 1994 2751 2758
-
(1994)
J. Virol.
, vol.69
, pp. 2751-2758
-
-
Rose, J.R.1
Babe, L.M.2
Craik, C.S.3
-
123
-
-
0032562224
-
Domain flexibility in retroviral proteases: Structural implications for drug resistant mutations
-
R. Rose C. Craik R. Stroud Domain flexibility in retroviral proteases: Structural implications for drug resistant mutations Biochemistry 37 1998 2606 2621
-
(1998)
Biochemistry
, vol.37
, pp. 2606-2621
-
-
Rose, R.1
Craik, C.2
Stroud, R.3
-
124
-
-
0029869305
-
Human immunodeficiency virus type 1 viral background plays a major role in development of resistance to protease inhibitors
-
R.E. Rose Y.F. Gong J.A. Greytok C.M. Bechtold B.J. Terry B.S. Robinson M. Alam R.J. Colonno P.F. Lin Human immunodeficiency virus type 1 viral background plays a major role in development of resistance to protease inhibitors Proc. Natl. Acad. Sci. U.S.A. 93 1996 1648 1653
-
(1996)
, pp. 1648-1653
-
-
Rose, R.E.1
Gong, Y.F.2
Greytok, J.A.3
Bechtold, C.M.4
Terry, B.J.5
Robinson, B.S.6
Alam, M.7
Colonno, R.J.8
Lin, P.F.9
-
125
-
-
0014211618
-
On the size of the active site in proteases. I. Papain
-
I. Schechter A. Berger On the size of the active site in proteases. I. Papain Biochem. Biophys. Res. Commun. 27 1967 157 162
-
(1967)
Biochem. Biophys. Res. Commun.
, vol.27
, pp. 157-162
-
-
Schechter, I.1
Berger, A.2
-
126
-
-
0029731556
-
Mutational anatomy of an HIV-1 protease variant conferring cross-resistance to protease inhibitors in clinical trials. Compensatory modulations of binding and activity
-
H.B. Schock V.M. Garsky L.C. Kuo Mutational anatomy of an HIV-1 protease variant conferring cross-resistance to protease inhibitors in clinical trials. Compensatory modulations of binding and activity J. Biol. Chem. 271 1996 31957 31963
-
(1996)
J. Biol. Chem.
, vol.271
, pp. 31957-31963
-
-
Schock, H.B.1
Garsky, V.M.2
Kuo, L.C.3
-
127
-
-
19244375366
-
The inhibition of human immunodeficiency virus proteases by ‘interface peptides’
-
H.J. Schramm J. Boetzel J. Buttner E. Fritsche W. Gohring E. Jaeger S. Konig O. Thumfart T. Wenger N.E. Nagel W. Schramm The inhibition of human immunodeficiency virus proteases by ‘interface peptides’ Antiviral Res. 30 1996 155 170
-
(1996)
Antiviral Res.
, vol.30
, pp. 155-170
-
-
Schramm, H.J.1
Boetzel, J.2
Buttner, J.3
Fritsche, E.4
Gohring, W.5
Jaeger, E.6
Konig, S.7
Thumfart, O.8
Wenger, T.9
Nagel, N.E.10
Schramm, W.11
-
128
-
-
0001650127
-
Human immunodeficiency virus has an aspartic-type protease that can be inhibited by pepstatin A
-
S. Seelmeier H. Schmidt V. Turk K. von der Helm Human immunodeficiency virus has an aspartic-type protease that can be inhibited by pepstatin A Proc. Natl. Acad. Sci. U.S.A. 85 1988 6612 6616
-
(1988)
, pp. 6612-6616
-
-
Seelmeier, S.1
Schmidt, H.2
Turk, V.3
von der Helm, K.4
-
129
-
-
0032103187
-
Multiple concurrent reverse transcriptase and protease mutations and multidrug resistance of HIV-1 isolates from heavily treated patients
-
R.W. Shafer M.A. Winters S. Palmer T.C. Merigan Multiple concurrent reverse transcriptase and protease mutations and multidrug resistance of HIV-1 isolates from heavily treated patients Ann. Intern. Med. 128 1998 906 911
-
(1998)
Ann. Intern. Med.
, vol.128
, pp. 906-911
-
-
Shafer, R.W.1
Winters, M.A.2
Palmer, S.3
Merigan, T.C.4
-
130
-
-
0027529843
-
Cleavage of human and mouse cytoskeletal and sarcomeric proteins by human immunodeficiency virus type 1 protease: Actin, desmin, myosin, and tropomyosin
-
R.L. Shoeman B. Sachse E. Honer E. Mothes M. Kaufmann P. Traub Cleavage of human and mouse cytoskeletal and sarcomeric proteins by human immunodeficiency virus type 1 protease: Actin, desmin, myosin, and tropomyosin Am. J. Pathol. 142 1993 221 230
-
(1993)
Am. J. Pathol.
, vol.142
, pp. 221-230
-
-
Shoeman, R.L.1
Sachse, B.2
Honer, E.3
Mothes, E.4
Kaufmann, M.5
Traub, P.6
-
132
-
-
0031035963
-
A mutation in human immunodeficiency virus type 1 protease at position 88, located outside the active site, confers resistance to the hydroxyethylurea inhibitor SC-55389A
-
M.L. Smidt K.E. Potts S.P. Tucker L. Blystone T.R. Stiebel Jr. W.C. Stallings J.J. McDonald D. Pillay D.D. Richamn M.L. Bryant A mutation in human immunodeficiency virus type 1 protease at position 88, located outside the active site, confers resistance to the hydroxyethylurea inhibitor SC-55389A Antimicrob. Agents Chemother. 31 1997 515 522
-
(1997)
Antimicrob. Agents Chemother.
, vol.31
, pp. 515-522
-
-
Smidt, M.L.1
Potts, K.E.2
Tucker, S.P.3
Blystone, L.4
Stiebel, T.R.5
Stallings, W.C.6
McDonald, J.J.7
Pillay, D.8
Richamn, D.D.9
Bryant, M.L.10
-
134
-
-
0029778343
-
The cleavage of host cell proteins by HIV-1 protease
-
J. Snasel I. Pichova The cleavage of host cell proteins by HIV-1 protease Folia Biol. 42 1996 227 230
-
(1996)
Folia Biol.
, vol.42
, pp. 227-230
-
-
Snasel, J.1
Pichova, I.2
-
135
-
-
0028708269
-
Expression systems for retroviral proteases
-
J. Stebbins C. Debouck Expression systems for retroviral proteases L.C. Kuo J.A. Shafer Methods in Enzymology Vol. 241 1994 Academic Press San Diego, CA 3 16
-
(1994)
, pp. 3-16
-
-
Stebbins, J.1
Debouck, C.2
-
136
-
-
0024457366
-
Characterization and autoprocessing of precursor and mature forms of human immunodefiency virus type 1 (HIV 1) protease purified from Escherichia coli
-
J.E. Strickler J. Gorniak B. Dayton T. Meek M. Moore V. Magaard J. Malinowski C. Debouck Characterization and autoprocessing of precursor and mature forms of human immunodefiency virus type 1 (HIV 1) protease purified from Escherichia coli Proteins 6 1989 139 154
-
(1989)
Proteins
, vol.6
, pp. 139-154
-
-
Strickler, J.E.1
Gorniak, J.2
Dayton, B.3
Meek, T.4
Moore, M.5
Magaard, V.6
Malinowski, J.7
Debouck, C.8
-
137
-
-
0029753776
-
Rate-determining steps in HIV-1 protease catalysis. The hydrolysis of the most specific substrate
-
Z. Szeltner L. Polgár Rate-determining steps in HIV-1 protease catalysis. The hydrolysis of the most specific substrate J. Biol. Chem. 271 1996 32180 32184
-
(1996)
J. Biol. Chem.
, vol.271
, pp. 32180-32184
-
-
Szeltner, Z.1
Polgár, L.2
-
138
-
-
0029005035
-
A kinetic model for comparing proteolytic processing activity and inhibitor resistance potential of mutant HIV-1 proteases
-
J. Tang J.A. Hartsuck A kinetic model for comparing proteolytic processing activity and inhibitor resistance potential of mutant HIV-1 proteases FEBS Lett. 367 1995 112 116
-
(1995)
FEBS Lett.
, vol.367
, pp. 112-116
-
-
Tang, J.1
Hartsuck, J.A.2
-
140
-
-
0032475454
-
Calculation of relative binding free energies of peptidic inhibitors to HIV-1 protease and its I84V mutant
-
G.J. Tawa I. Topol S. Burt J.W. Erickson Calculation of relative binding free energies of peptidic inhibitors to HIV-1 protease and its I84V mutant J. Am. Chem. Soc. 120 1998 8856 8863
-
(1998)
J. Am. Chem. Soc.
, vol.120
, pp. 8856-8863
-
-
Tawa, G.J.1
Topol, I.2
Burt, S.3
Erickson, J.W.4
-
141
-
-
0029909674
-
Structure-based design of HIV protease inhibitors: Sulfonamide-containing 5,6-dihydro-4-hydroxy-2-pyrones as non-peptidic inhibitors
-
S. Thaisrivongs H.I. Skulnick S.R. Turner J.W. Strohbach R.A. Tommasi P.D. Johnson P.A. Aristoff T.M. Judge R.B. Gammill J.K. Morris K.R. Romines R.A. Chrusciel R.R. Hinshaw K.T. Chong W.G. Tarpley S.M. Poppe D.E. Slade J.C. Lynn M.M. Horng P.K. Tomich E.P. Seest L.A. Dolak W.J. Howe G.M. Howard Structure-based design of HIV protease inhibitors: Sulfonamide-containing 5,6-dihydro-4-hydroxy-2-pyrones as non-peptidic inhibitors J. Med. Chem. 39 1996 4349 4353
-
(1996)
J. Med. Chem.
, vol.39
, pp. 4349-4353
-
-
Thaisrivongs, S.1
Skulnick, H.I.2
Turner, S.R.3
Strohbach, J.W.4
Tommasi, R.A.5
Johnson, P.D.6
Aristoff, P.A.7
Judge, T.M.8
Gammill, R.B.9
Morris, J.K.10
Romines, K.R.11
Chrusciel, R.A.12
Hinshaw, R.R.13
Chong, K.T.14
Tarpley, W.G.15
Poppe, S.M.16
Slade, D.E.17
Lynn, J.C.18
Horng, M.M.19
Tomich, P.K.20
Seest, E.P.21
Dolak, L.A.22
Howe, W.J.23
Howard, G.M.24
more..
-
142
-
-
0032561137
-
The structural stability of the HIV-1 protease
-
M.J. Todd N. Semo E. Freire The structural stability of the HIV-1 protease J. Mol. Biol. 283 1998 475 488
-
(1998)
J. Mol. Biol.
, vol.283
, pp. 475-488
-
-
Todd, M.J.1
Semo, N.2
Freire, E.3
-
143
-
-
36849159719
-
Retroviral protease-like sequence in the yeast transposon Ty1
-
H. Toh M. Ono K. Saigo T. Miyata Retroviral protease-like sequence in the yeast transposon Ty1 Nature (London) 315 1985 691 692
-
(1985)
Nature (London)
, vol.315
, pp. 691-692
-
-
Toh, H.1
Ono, M.2
Saigo, K.3
Miyata, T.4
-
144
-
-
0029052114
-
Specificity of retroviral proteases: An analysis of viral and nonviral protein substrates
-
A.G. Tomasselli R.L. Heinrikson Specificity of retroviral proteases: An analysis of viral and nonviral protein substrates L.C. Kuo J.A. Shafer Methods in Enzymology Vol. 241 1994 Academic Press San Diego, CA 279 301
-
(1994)
, pp. 279-301
-
-
Tomasselli, A.G.1
Heinrikson, R.L.2
-
145
-
-
0025858972
-
Calcium-free calmodulin is a substrate of proteases from human immunodeficiency viruses 1 and 2
-
A.G. Tomasselli W.J. Howe J.O. Hui T.K. Sawyer I.M. Reardon D.L. DeCamp C.S. Craik R.L. Heinrikson Calcium-free calmodulin is a substrate of proteases from human immunodeficiency viruses 1 and 2 Proteins 10 1991 1 9
-
(1991)
Proteins
, vol.10
, pp. 1-9
-
-
Tomasselli, A.G.1
Howe, W.J.2
Hui, J.O.3
Sawyer, T.K.4
Reardon, I.M.5
DeCamp, D.L.6
Craik, C.S.7
Heinrikson, R.L.8
-
146
-
-
0026327505
-
Actin, troponin C, Alzheimer amyloid precursor protein and pro-interleukin 1β as substrates of the protease from human immunodeficiency virus
-
A.G. Tomasselli J.O. Hui L. Adams J. Chosay D. Lowery B. Greenberg A. Yem M.R. Deibel H. Zürcher-Neely R.L. Heinrikson Actin, troponin C, Alzheimer amyloid precursor protein and pro-interleukin 1β as substrates of the protease from human immunodeficiency virus J. Biol. Chem. 266 1991 14548 14553
-
(1991)
J. Biol. Chem.
, vol.266
, pp. 14548-14553
-
-
Tomasselli, A.G.1
Hui, J.O.2
Adams, L.3
Chosay, J.4
Lowery, D.5
Greenberg, B.6
Yem, A.7
Deibel, M.R.8
Zürcher-Neely, H.9
Heinrikson, R.L.10
-
148
-
-
0028693381
-
Design of tight-binding human immunodeficiency virus type 1 protease inhibitors
-
J.P. Vacca Design of tight-binding human immunodeficiency virus type 1 protease inhibitors L.C. Kuo J.A. Shafer Methods in Enzymology Vol. 241 1994 Academic Press San Diego, CA 311 334
-
(1994)
, pp. 311-334
-
-
Vacca, J.P.1
-
149
-
-
0030849517
-
Clinically effective HIV-1 protease inhibitors
-
J.P. Vacca J.H. Condra Clinically effective HIV-1 protease inhibitors Drug Des. Discovery 2 1997 261 272
-
(1997)
Drug Des. Discovery
, vol.2
, pp. 261-272
-
-
Vacca, J.P.1
Condra, J.H.2
-
150
-
-
0028222149
-
L-735, 524: An orally bioavailable human immunodeficiency virus type 1 protease inhibitor
-
J.P. Vacca B.D. Dorsey W.A. Schleif R.B. Levin S.L. McDaniel P.L. Darke J. Zugai J.C. Quintero O.M. Blahy E. Roth V.V. Sardana A.J. Schlabach P.I. Graham J.H. Condra L. Gotlib M.K. Holloway J. Lin I.-W. Chen K. Vastag D. Ostovic P.S. Anderson E.A. Emini J.R. Huff L-735, 524: An orally bioavailable human immunodeficiency virus type 1 protease inhibitor Proc. Natl. Acad. Sci. U.S.A. 91 1994 4096 4100
-
(1994)
, pp. 4096-4100
-
-
Vacca, J.P.1
Dorsey, B.D.2
Schleif, W.A.3
Levin, R.B.4
McDaniel, S.L.5
Darke, P.L.6
Zugai, J.7
Quintero, J.C.8
Blahy, O.M.9
Roth, E.10
Sardana, V.V.11
Schlabach, A.J.12
Graham, P.I.13
Condra, J.H.14
Gotlib, L.15
Holloway, M.K.16
Lin, J.17
Chen, I.-W.18
Vastag, K.19
Ostovic, D.20
Anderson, P.S.21
Emini, E.A.22
Huff, J.R.23
more..
-
151
-
-
0030419901
-
Proteolytic processing and particle maturation
-
V.M. Vogt Proteolytic processing and particle maturation Curr. Top. Microbiol. Immunol. 214 1996 95 131
-
(1996)
Curr. Top. Microbiol. Immunol.
, vol.214
, pp. 95-131
-
-
Vogt, V.M.1
-
152
-
-
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
-
Y.X. Wang D.I. Freedberg T. Yamazaki P.T. Wingfield S.J. Stahl J.D. Kaufman Y. Kiso D.A. Torchia 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 1996 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
-
153
-
-
0028986487
-
Targeting HIV-1 protease: A test of drug-design methodologies
-
M.L. West D.P. Fairlie Targeting HIV-1 protease: A test of drug-design methodologies Trends Pharmacol. Sci. 16 1995 67 75
-
(1995)
Trends Pharmacol. Sci.
, vol.16
, pp. 67-75
-
-
West, M.L.1
Fairlie, D.P.2
-
155
-
-
0344243836
-
HIV protease inhibitors
-
D.L. Winslow M.J. Otto HIV protease inhibitors AIDS 9 Suppl. A 1995 S183 S192
-
(1995)
AIDS
, vol.9
, Issue.Suppl. A
, pp. S183-S192
-
-
Winslow, D.L.1
Otto, M.J.2
-
156
-
-
0031949563
-
Human immunodeficiency virus type 1 protease genotypes and in vitro protease inhibitor susceptibilities of isolates from individuals who were switched to other protease inhibitors after long-term saquinavir treatment
-
M.A. Winters J.M. Schapiro J. Lawrence T.C. Merigan Human immunodeficiency virus type 1 protease genotypes and in vitro protease inhibitor susceptibilities of isolates from individuals who were switched to other protease inhibitors after long-term saquinavir treatment J. Virol. 72 1998 5303 5306
-
(1998)
J. Virol.
, vol.72
, pp. 5303-5306
-
-
Winters, M.A.1
Schapiro, J.M.2
Lawrence, J.3
Merigan, T.C.4
-
157
-
-
0027218692
-
Structure-based inhibitors of HIV-1 protease
-
A. Wlodawer J.W. Erickson Structure-based inhibitors of HIV-1 protease Annu. Rev. Biochem. 62 1993 543 585
-
(1993)
Annu. Rev. Biochem.
, vol.62
, pp. 543-585
-
-
Wlodawer, A.1
Erickson, J.W.2
-
158
-
-
0031804609
-
Inhibitors of HIV-1 protease: A major success of structure-assisted drug design
-
A. Wlodawer J. vondrasek Inhibitors of HIV-1 protease: A major success of structure-assisted drug design Annu. Rev. Biophys. Biomol. Struct. 27 1998 249 284
-
(1998)
Annu. Rev. Biophys. Biomol. Struct.
, vol.27
, pp. 249-284
-
-
Wlodawer, A.1
vondrasek, J.2
-
159
-
-
0024412506
-
Conserved folding in retroviral proteases: Crystal structure of a synthetic HIV-1 protease
-
A. Wlodawer M. Miller M. Jaskólski B.K. Sathyanarayana E. Baldwin I.T. Weber L.M. Selk L. Clawson J. Schneider S.B.H. Kent Conserved folding in retroviral proteases: Crystal structure of a synthetic HIV-1 protease Science 245 1989 616 621
-
(1989)
Science
, vol.245
, pp. 616-621
-
-
Wlodawer, A.1
Miller, M.2
Jaskólski, M.3
Sathyanarayana, B.K.4
Baldwin, E.5
Weber, I.T.6
Selk, L.M.7
Clawson, L.8
Schneider, J.9
Kent, S.B.H.10
-
161
-
-
0032771020
-
Drug resistant mutations can affect dimer stability of HIV-1 protease at neutral pH
-
D. Xie S. Gulnik E. Gustchina B. Yu W. Shao W. Qoronfleh A. Nathan J.W. Erickson Drug resistant mutations can affect dimer stability of HIV-1 protease at neutral pH Protein Sci. 8 1999 1702 1707
-
(1999)
Protein Sci.
, vol.8
, pp. 1702-1707
-
-
Xie, D.1
Gulnik, S.2
Gustchina, E.3
Yu, B.4
Shao, W.5
Qoronfleh, W.6
Nathan, A.7
Erickson, J.W.8
-
163
-
-
0028114966
-
NMR and X-ray evidence that the HIV protease catalytic aspartyl groups are protonated in the complex formed by the protease and a non-peptide cyclic urea-based inhibitor
-
T. Yamazaki L. Nicholson D. Torchia P. Wingfield S. Stahl J. Kaufman C. Eyermann N. Hodge P. Lam Y. Ru P. Jadhav C.-H. Chang P. Weber NMR and X-ray evidence that the HIV protease catalytic aspartyl groups are protonated in the complex formed by the protease and a non-peptide cyclic urea-based inhibitor J. Am. Chem. Soc. 116 1994 10791 10792
-
(1994)
J. Am. Chem. Soc.
, vol.116
, pp. 10791-10792
-
-
Yamazaki, T.1
Nicholson, L.2
Torchia, D.3
Wingfield, P.4
Stahl, S.5
Kaufman, J.6
Eyermann, C.7
Hodge, N.8
Lam, P.9
Ru, Y.10
Jadhav, P.11
Chang, C.-H.12
Weber, P.13
-
164
-
-
0030018856
-
Irreversiible inhibition of the HIV-1 protease: Targeting alkylating agents to the catalytic aspartate groups
-
Z. Yu P. Caldera F. McPhee J.J. De Voss P.R. Jones A.L. Burlingame I.D. Kuntz C.S. Craik P.R. Ortiz de Montellano Irreversiible inhibition of the HIV-1 protease: Targeting alkylating agents to the catalytic aspartate groups J. Am. Chem. Soc. 118 1996 5846 5856
-
(1996)
J. Am. Chem. Soc.
, vol.118
, pp. 5846-5856
-
-
Yu, Z.1
Caldera, P.2
McPhee, F.3
De Voss, J.J.4
Jones, P.R.5
Burlingame, A.L.6
Kuntz, I.D.7
Craik, C.S.8
Ortiz de Montellano, P.R.9
-
165
-
-
0031946007
-
Loss of viral fitness associated with multiple Gag and Gag-Pol processing defects in human immunodeficiency virus type 1 variants selected for resistance to protease inhibitors in vivo
-
V. Zennou F. Mammano S. Paulous D. Mathez F. Clavel Loss of viral fitness associated with multiple Gag and Gag-Pol processing defects in human immunodeficiency virus type 1 variants selected for resistance to protease inhibitors in vivo J. Virol. 72 1998 3300 3306
-
(1998)
J. Virol.
, vol.72
, pp. 3300-3306
-
-
Zennou, V.1
Mammano, F.2
Paulous, S.3
Mathez, D.4
Clavel, F.5
-
166
-
-
0030769354
-
Drug resistance during indinavir therapy is caused by mutations in the protease gene and in its Gag substrate cleavage sites
-
Y.M. Zhang H. Imamichi T. Imamichi H.C. Lane J. Falloon M.B. Vasudevachari N.P. Salzman Drug resistance during indinavir therapy is caused by mutations in the protease gene and in its Gag substrate cleavage sites J. Virol. 71 1997 6662 6670
-
(1997)
J. Virol.
, vol.71
, pp. 6662-6670
-
-
Zhang, Y.M.1
Imamichi, H.2
Imamichi, T.3
Lane, H.C.4
Falloon, J.5
Vasudevachari, M.B.6
Salzman, N.P.7
|