SCOPUS 정보 검색 플랫폼

Bioorganic and Medicinal Chemistry Letters

Volumn 22, Issue 2, 2012, Pages 1049-1054

Structure-based library design and the discovery of a potent and selective mast cell β-tryptase inhibitor as an oral therapeutic agent

(15) Liang, Guyan a Aldous, Suzanne b Merriman, Gregory a Levell, Julian f Pribish, James c Cairns, Jennifer a Chen, Xin a Maignan, Sebastien d Mathieu, Magali d Tsay, Joseph b Sides, Keith b Rebello, Sam f Whitely, Brian g Morize, Isabelle a Pauls, Henry W e

a Sanofi Pharmaceuticals (United States)

b Fibrosis and Wound Repair (United States)

c Oncology (United States)

d SANOFI (France)

e PRINCESS MARGARET HOSPITAL (Canada)

f Norvartis Institute for BioMedical Research (United States)

g BRISTOL MYERS SQUIBB (United States)

Author keywords

Asthma; Benzylamine; COPD; Inhibitor; Molecular modeling; Serine protease; Structure based drug design; Tryptase; X ray

Indexed keywords

BETA TRYPTASE; SERINE PROTEINASE; TRYPSIN; TRYPTASE; TRYPTASE INHIBITOR; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ARTICLE; COMBINATORIAL LIBRARY; COMPUTER MODEL; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG DESIGN; DRUG POTENCY; DRUG STRUCTURE; MAST CELL; MAXIMUM PLASMA CONCENTRATION; NONHUMAN; RAT; TIME TO MAXIMUM PLASMA CONCENTRATION;

ADMINISTRATION, ORAL; ANIMALS; COMBINATORIAL CHEMISTRY TECHNIQUES; CRYSTALLOGRAPHY, X-RAY; DOSE-RESPONSE RELATIONSHIP, DRUG; ENZYME INHIBITORS; HUMANS; MAST CELLS; MODELS, MOLECULAR; MOLECULAR STRUCTURE; RATS; RECOMBINANT PROTEINS; SMALL MOLECULE LIBRARIES; STRUCTURE-ACTIVITY RELATIONSHIP; TRYPTASES;

EID: 84855678999 PISSN: 0960894X EISSN: 14643405 Source Type: Journal
DOI: 10.1016/j.bmcl.2011.11.119 Document Type: Article

Times cited : (19)

References (31)

1
- 0025455517
- E.K. Tam, and G.H. Caughey Am. J. Respir. Cell Mol. Biol. 3 1990 27
- (1990) Am. J. Respir. Cell Mol. Biol. , vol.3 , pp. 27
- Tam, E.K.¹ Caughey, G.H.²

2
- 0029905642
- J.M. Clark, W.R. Moore, and R.D. Tanaka Drugs Future 21 1996 811
- (1996) Drugs Future , vol.21 , pp. 811
- Clark, J.M.¹ Moore, W.R.² Tanaka, R.D.³

3
- 0035013541
- M.T. Krishna, A. Chauhan, L. Little, K. Sampson, R. Hawksworth, T. Mant, R. Djukanovic, T. Lee, and S. Holgate J. Allergy Clin. Immunol. 107 2001 1039
- (2001) J. Allergy Clin. Immunol. , vol.107 , pp. 1039
- Krishna, M.T.¹ Chauhan, A.² Little, L.³ Sampson, K.⁴ Hawksworth, R.⁵ Mant, T.⁶ Djukanovic, R.⁷ Lee, T.⁸ Holgate, S.⁹

4
- 40749154575
- J.M. Clark, R.E. Van Dyke, and M.C. Kurth Prog. Respir. Res. 31 2001 170
- (2001) Prog. Respir. Res. , vol.31 , pp. 170
- Clark, J.M.¹ Van Dyke, R.E.² Kurth, M.C.³

5
- 1642370953
- S. He, A. Aslam, M.D.A. Gaca, Y. He, M.G. Buckley, M.D. Hollenberg, and A.F. Walls J. Pharmacol. Exp. Ther. 309 2004 119
- (2004) J. Pharmacol. Exp. Ther. , vol.309 , pp. 119
- He, S.¹ Aslam, A.² Gaca, M.D.A.³ He, Y.⁴ Buckley, M.G.⁵ Hollenberg, M.D.⁶ Walls, A.F.⁷

6
- 33846160570
- C.P. Sommerhoff, and N. Schaschke Curr. Pharm. Des. 13 2007 313
- (2007) Curr. Pharm. Des. , vol.13 , pp. 313
- Sommerhoff, C.P.¹ Schaschke, N.²

7
- 52949152455
- G. Huetter, S. Ganepola, E. Thiel, and W.K. Hofmann Biosci. Hypotheses 1 2008 213
- (2008) Biosci. Hypotheses , vol.1 , pp. 213
- Huetter, G.¹ Ganepola, S.² Thiel, E.³ Hofmann, W.K.⁴

8
- 0034867321
- P. Berger, D.-W. Perng, H. Thabrew, S.J. Compton, J.A. Cairns, A.R. McEuen, R. Marthan, J.-M. Tunon De Lara, and A.F. Walls J. Appl. Physiol. 91 2001 1372
- (2001) J. Appl. Physiol. , vol.91 , pp. 1372
- Berger, P.¹ Perng, D.-W.² Thabrew, H.³ Compton, S.J.⁴ Cairns, J.A.⁵ McEuen, A.R.⁶ Marthan, R.⁷ Tunon De Lara, J.-M.⁸ Walls, A.F.⁹

9
- 0037083293
- S.-W. Oh, C.I. Pae, D.-K. Lee, F. Jones, G.K.S. Chiang, H.-O. Kim, S.-H. Moon, B. Cao, C. Ogbu, K.-W. Jeong, G. Kozu, H. Nakanishi, M. Kahn, E.Y. Chi, and W.R. Henderson Jr. J. Immunol. 168 2002 1992
- (2002) J. Immunol. , vol.168 , pp. 1992
- Oh, S.-W.¹ Pae, C.I.² Lee, D.-K.³ Jones, F.⁴ Chiang, G.K.S.⁵ Kim, H.-O.⁶ Moon, S.-H.⁷ Cao, B.⁸ Ogbu, C.⁹ Jeong, K.-W.¹⁰ Kozu, G.¹¹ Nakanishi, H.¹² Kahn, M.¹³ Chi, E.Y.¹⁴ Henderson, Jr.W.R.¹⁵

10
- 0033530812
- S.I. Ono, S. Kuwahara, M. Takeuchi, H. Sakashita, Y. Naito, and T. Kondo Bioorg. Med. Chem. Lett. 9 1999 3285
- (1999) Bioorg. Med. Chem. Lett. , vol.9 , pp. 3285
- Ono, S.I.¹ Kuwahara, S.² Takeuchi, M.³ Sakashita, H.⁴ Naito, Y.⁵ Kondo, T.⁶

11
- 0034675805
- K.D. Rice, A.R. Gangloff, E.Y.L. Kuo, J.M. Dener, V.R. Wang, R. Lum, W.S. Newcomb, C. Havel, D. Putnam, L. Cregar, M. Wong, and R.L. Warne Bioorg. Med. Chem. Lett. 10 2000 2357
- (2000) Bioorg. Med. Chem. Lett. , vol.10 , pp. 2357
- Rice, K.D.¹ Gangloff, A.R.² Kuo, E.Y.L.³ Dener, J.M.⁴ Wang, V.R.⁵ Lum, R.⁶ Newcomb, W.S.⁷ Havel, C.⁸ Putnam, D.⁹ Cregar, L.¹⁰ Wong, M.¹¹ Warne, R.L.¹²

12
- 0034675757
- K.D. Rice, V.R. Wang, A.R. Gangloff, E.Y.L. Kuo, J.M. Dener, W.S. Newcomb, W.B. Young, D. Putnam, L. Cregar, M. Wong, and P.J. Simpson Bioorg. Med. Chem. Lett. 10 2000 2361
- (2000) Bioorg. Med. Chem. Lett. , vol.10 , pp. 2361
- Rice, K.D.¹ Wang, V.R.² Gangloff, A.R.³ Kuo, E.Y.L.⁴ Dener, J.M.⁵ Newcomb, W.S.⁶ Young, W.B.⁷ Putnam, D.⁸ Cregar, L.⁹ Wong, M.¹⁰ Simpson, P.J.¹¹

13
- 18644381739
- W.A. Slusarchyk, S.A. Bolton, K.S. Hartl, M.-H. Huang, G. Jacobs, W. Meng, M.L. Ogletree, Z. Pi, W.A. Schumacher, S.M. Seiler, J.C. Sutton, U. Treuner, R. Zahler, G. Zhao, and G.S. Bisacchi Bioorg. Med. Chem. Lett. 12 2002 3235
- (2002) Bioorg. Med. Chem. Lett. , vol.12 , pp. 3235
- Slusarchyk, W.A.¹ Bolton, S.A.² Hartl, K.S.³ Huang, M.-H.⁴ Jacobs, G.⁵ Meng, W.⁶ Ogletree, M.L.⁷ Pi, Z.⁸ Schumacher, W.A.⁹ Seiler, S.M.¹⁰ Sutton, J.C.¹¹ Treuner, U.¹² Zahler, R.¹³ Zhao, G.¹⁴ Bisacchi, G.S.¹⁵

14
- 0347990534
- G. Zhao, S.A. Bolton, C. Kwon, K.S. Hartl, S.M. Seiler, W.A. Slusarchyk, J.C. Sutton, and G.S. Bisacchi Bioorg. Med. Chem. Lett. 14 2004 309
- (2004) Bioorg. Med. Chem. Lett. , vol.14 , pp. 309
- Zhao, G.¹ Bolton, S.A.² Kwon, C.³ Hartl, K.S.⁴ Seiler, S.M.⁵ Slusarchyk, W.A.⁶ Sutton, J.C.⁷ Bisacchi, G.S.⁸

15
- 20144374671
- J. Levell, P. Astles, P. Eastwood, J. Cairns, O. Houille, S. Aldous, G. Merriman, B. Whiteley, J. Pribish, M. Czekaj, G. Liang, S. Maignan, J.-P. Guilloteau, A. Dupuy, J. Davidson, T. Harrison, A. Morley, S. Watson, G. Fenton, C. McCarthy, J. Romano, R. Mathew, D. Engers, M. Gardyan, K. Sides, J. Kwong, J. Tsay, S. Rebello, L. Shen, J. Wang, Y. Luo, O. Giardino, H.-K. Lim, K. Smith, and H. Pauls Bioorg. Med. Chem. 13 2005 2859
- (2005) Bioorg. Med. Chem. , vol.13 , pp. 2859
- Levell, J.¹ Astles, P.² Eastwood, P.³ Cairns, J.⁴ Houille, O.⁵ Aldous, S.⁶ Merriman, G.⁷ Whiteley, B.⁸ Pribish, J.⁹ Czekaj, M.¹⁰ Liang, G.¹¹ Maignan, S.¹² Guilloteau, J.-P.¹³ Dupuy, A.¹⁴ Davidson, J.¹⁵ Harrison, T.¹⁶ Morley, A.¹⁷ Watson, S.¹⁸ Fenton, G.¹⁹ McCarthy, C.²⁰ more..

16
- 4444286148
- C. Hopkins, K. Neuenschwander, A. Scotese, S. Jackson, T. Nieduzak, H. Pauls, G. Liang, K. Sides, D. Cramer, J. Cairns, S. Maignan, and M. Mathieu Bioorg. Med. Chem. Lett. 14 2004 4819
- (2004) Bioorg. Med. Chem. Lett. , vol.14 , pp. 4819
- Hopkins, C.¹ Neuenschwander, K.² Scotese, A.³ Jackson, S.⁴ Nieduzak, T.⁵ Pauls, H.⁶ Liang, G.⁷ Sides, K.⁸ Cramer, D.⁹ Cairns, J.¹⁰ Maignan, S.¹¹ Mathieu, M.¹²

17
- 21144450350
- C.R. Hopkins, M. Czekaj, S.S. Kaye, Z. Gao, J. Pribish, H. Pauls, G. Liang, K. Sides, D. Cramer, J. Cairns, Y. Luo, H.-K. Lim, R. Vaz, S. Rebello, S. Maignan, A. Dupuy, M. Mathieu, and J. Levell Bioorg. Med. Chem. Lett. 15 2005 2734
- (2005) Bioorg. Med. Chem. Lett. , vol.15 , pp. 2734
- Hopkins, C.R.¹ Czekaj, M.² Kaye, S.S.³ Gao, Z.⁴ Pribish, J.⁵ Pauls, H.⁶ Liang, G.⁷ Sides, K.⁸ Cramer, D.⁹ Cairns, J.¹⁰ Luo, Y.¹¹ Lim, H.-K.¹² Vaz, R.¹³ Rebello, S.¹⁴ Maignan, S.¹⁵ Dupuy, A.¹⁶ Mathieu, M.¹⁷ Levell, J.¹⁸

18
- 33646059854
- Y. Miyazaki, Y. Kato, T. Manabe, H. Shimada, M. Mizuno, T. Egusa, M. Ohkouchi, I. Shiromizu, T. Matsusue, and I. Yamamoto Bioorg. Med. Chem. Lett. 16 2006 2986
- (2006) Bioorg. Med. Chem. Lett. , vol.16 , pp. 2986
- Miyazaki, Y.¹ Kato, Y.² Manabe, T.³ Shimada, H.⁴ Mizuno, M.⁵ Egusa, T.⁶ Ohkouchi, M.⁷ Shiromizu, I.⁸ Matsusue, T.⁹ Yamamoto, I.¹⁰

19
- 77958032471
- G. Liang, Y.M. Choi-Sledeski, G. Poli, X. Chen, P. Shum, A. Minnich, Q. Wang, J. Tsay, K. Sides, J. Cairns, G. Stoklosa, T. Nieduzak, Z. Zhao, J. Wang, and R.J. Vaz Bioorg. Med. Chem. Lett. 20 2010 6721
- (2010) Bioorg. Med. Chem. Lett. , vol.20 , pp. 6721
- Liang, G.¹ Choi-Sledeski, Y.M.² Poli, G.³ Chen, X.⁴ Shum, P.⁵ Minnich, A.⁶ Wang, Q.⁷ Tsay, J.⁸ Sides, K.⁹ Cairns, J.¹⁰ Stoklosa, G.¹¹ Nieduzak, T.¹² Zhao, Z.¹³ Wang, J.¹⁴ Vaz, R.J.¹⁵

20
- 33745137909
- D. Sperandio, V.W.F. Tai, J. Lohman, B. Hirschbein, R. Mendonca, C.-S. Lee, J.R. Spencer, J. Janc, M. Nguyen, J. Beltman, P. Sprengeler, H. Scheerens, T. Lin, L. Liu, A. Gadre, A. Kellogg, M.J. Green, and M.E. McGrath Bioorg. Med. Chem. Lett. 16 2006 4085
- (2006) Bioorg. Med. Chem. Lett. , vol.16 , pp. 4085
- Sperandio, D.¹ Tai, V.W.F.² Lohman, J.³ Hirschbein, B.⁴ Mendonca, R.⁵ Lee, C.-S.⁶ Spencer, J.R.⁷ Janc, J.⁸ Nguyen, M.⁹ Beltman, J.¹⁰ Sprengeler, P.¹¹ Scheerens, H.¹² Lin, T.¹³ Liu, L.¹⁴ Gadre, A.¹⁵ Kellogg, A.¹⁶ Green, M.J.¹⁷ McGrath, M.E.¹⁸

21
- 2642600031
- P.J.B. Pereira, A. Bergner, S. Macedo-Ribeiro, R. Huber, G. Matschiner, H. Fritz, C.P. Sommerhoff, and W. Bode Nature (London) 392 1998 306
- (1998) Nature (London) , vol.392 , pp. 306
- Pereira, P.J.B.¹ Bergner, A.² MacEdo-Ribeiro, S.³ Huber, R.⁴ Matschiner, G.⁵ Fritz, H.⁶ Sommerhoff, C.P.⁷ Bode, W.⁸

22
- 0034615569
- C.P. Sommerhoff, W. Bode, G. Matschiner, A. Bergner, and H. Fritz Biochim. biophys. Acta 1477 2000 75
- (2000) Biochim. Biophys. Acta , vol.1477 , pp. 75
- Sommerhoff, C.P.¹ Bode, W.² Matschiner, G.³ Bergner, A.⁴ Fritz, H.⁵

23
- 70349786321
- H. Matter, M. Nazare, S. Guessregen, D.W. Will, H. Schreuder, A. Bauer, M. Urmann, K. Ritter, M. Wagner, and V. Wehner Angew. Chem., Int. Ed. 48 2009 2911
- (2009) Angew. Chem., Int. Ed. , vol.48 , pp. 2911
- Matter, H.¹ Nazare, M.² Guessregen, S.³ Will, D.W.⁴ Schreuder, H.⁵ Bauer, A.⁶ Urmann, M.⁷ Ritter, K.⁸ Wagner, M.⁹ Wehner, V.¹⁰

24
- 84990701901
- L. Turi, and N. Naray-Szabo Int. J. Quantum Chem. 42 1992 1537
- (1992) Int. J. Quantum Chem. , vol.42 , pp. 1537
- Turi, L.¹ Naray-Szabo, N.²

25
- 0031423107
- D. Xie, S. Gulnik, L. Collins, E. Gustchina, L. Suvorov, and J.W. Erickson Biochemistry 36 1997 16166
- (1997) Biochemistry , vol.36 , pp. 16166
- Xie, D.¹ Gulnik, S.² Collins, L.³ Gustchina, E.⁴ Suvorov, L.⁵ Erickson, J.W.⁶

26
- 0035850539
- S. Piana, D. Sebastiani, P. Carloni, and M. Parrinello J. Am. Chem. Soc. 123 2001 8730
- (2001) J. Am. Chem. Soc. , vol.123 , pp. 8730
- Piana, S.¹ Sebastiani, D.² Carloni, P.³ Parrinello, M.⁴

27
- 0347694970
- H. Park, and S. Lee J. Am. Chem. Soc. 125 2003 16416
- (2003) J. Am. Chem. Soc. , vol.125 , pp. 16416
- Park, H.¹ Lee, S.²

28
- 77956013896
- J.L. Dominguez, T. Christopeit, M.C. Villaverde, T. Gossas, J.M. Otero, S. Nystrom, V. Baraznenok, E. Lindstrom, U.H. Danielson, and F. Sussman Biochemistry 49 2010 7255
- (2010) Biochemistry , vol.49 , pp. 7255
- Dominguez, J.L.¹ Christopeit, T.² Villaverde, M.C.³ Gossas, T.⁴ Otero, J.M.⁵ Nystrom, S.⁶ Baraznenok, V.⁷ Lindstrom, E.⁸ Danielson, U.H.⁹ Sussman, F.¹⁰

29
- 0029757151
- Y.-X. Wang, D.I. Freedberg, T. Yamazaki, P.T. Wingfield, S.J. Stahl, J.D. Kaufman, Y. Kiso, and D.A. Torchia Biochemistry 35 1996 9945
- (1996) Biochemistry , vol.35 , pp. 9945
- 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

30
- 0028114966
- T. Yamazaki, L.K. Nicholson, P. Wingfield, S.J. Stahl, J.D. Kaufman, C.J. Eyermann, C.N. Hodge, P.Y.S. Lam, and D.A. Torchia J. Am. Chem. Soc. 116 1994 10791
- (1994) J. Am. Chem. Soc. , vol.116 , pp. 10791
- Yamazaki, T.¹ Nicholson, L.K.² Wingfield, P.³ Stahl, S.J.⁴ Kaufman, J.D.⁵ Eyermann, C.J.⁶ Hodge, C.N.⁷ Lam, P.Y.S.⁸ Torchia, D.A.⁹

31
- 0027181741
- W.E. Harte Jr., and D.L. Beveridge J. Am. Chem. Soc. 115 1993 3883
- (1993) J. Am. Chem. Soc. , vol.115 , pp. 3883
- Harte, Jr.W.E.¹ Beveridge, D.L.²

* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.