未登录 Optimization of the Potency and Pharmacokinetic Properties of a Macrocyclic Ghrelin Receptor Agonist (Part I): Development of Ulimorelin (TZP-101) from Hit to Clinic Hoveyda, Hamid R.; Marsault, Eric; Gagnon, Rene; Mathieu, Axel P.; Vezina, Martin; Landry, Annick; Wang, Zhigang; Benakli, Kamel; Beaubien, Sylvie; Saint-Louis, Carl; Brassard, Martin; Pinault, Jean-Francois; Ouellet, Luc; Bhat, Shridhar; Ramaseshan, Mahesh; Peng, Xiaowen; Foucher, Laurence; Beauchemin, Sophie; Bherer, Patrick; Veber, Daniel F.; Peterson, Mark L.; Fraser, Graeme L. 分享 收藏
Peptide aldehyde inhibitors of cathepsin K inhibit bone resorption both in vitro and in vivo Votta, BJ; Levy, MA; Badger, A; Bradbeer, J; Dodds, RA; James, IE; Thompson, S; Bossard, MJ; Carr, T; Connor, JR; Tomaszek, TA; Szewczuk, L; Drake, FH; Veber, DF; Gowen, M 分享 收藏
Human osteoclast cathepsin K is processed intracellularly prior to attachment and bone resorption Dodds, RA; James, IE; Rieman, D; Ahern, R; Hwang, SM; Connor, JR; Thompson, SD; Veber, DF; Drake, FH; Holmes, S; Lark, MW; Gowen, M 分享 收藏
Potent and selective inhibition of human cathepsin K leads to inhibition of bone resorption in vivo in a nonhuman primate 人组织蛋白酶K的有效和选择性抑制导致非人灵长类动物体内骨吸收的抑制 Stroup, GB; Lark, MW; Veber, DF; Bhattacharyya, A; Blake, S; Dare, LC; Erhard, KF; Hoffman, SJ; James, IE; Marquis, RW; Ru, Y; Vasko-Moser, JA; Smith, BR; Tomaszek, T; Gowen, M 分享 收藏
Highly potent inhibitors of methionine aminopeptidase-2 based on a 1,2,4-triazole pharmacophore Marino, Joseph P., Jr.; Fisher, Paul W.; Hofmann, Glenn A.; Kirkpatrick, Robert B.; Janson, Cheryl A.; Johnson, Randall K.; Ma, Chun; Mattern, Michael; Meek, Thomas D.; Ryan, M. Dominic; Schulz, Christina; Smith, Ward W.; Tew, David G.; Tomazek, Thaddeus A., Jr.; Veber, Daniel F.; Xiong, Wenfang C.; Yamamoto, Yuuichi; Yamashita, Keizo; Yang, Guang; Thompson, Scott K. 分享 收藏
A highly potent inhibitor of cathepsin K (relacatib) reduces biomarkers of bone resorption both in vitro and in an acute model of elevated bone turnover in vivo in monkeys 组织蛋白酶K的高效抑制剂 (relacatib) 在体外和猴子体内骨转换升高的急性模型中均降低了骨吸收的生物标志物 Kumar, S.; Dare, L.; Vasko-Moser, J. A.; James, I. E.; Blake, S. M.; Rickard, D. J.; Hwang, S. -M.; Tomaszek, T.; Yamashita, D. S.; Marquis, R. W.; Oh, H.; Jeong, J. U.; Veber, D. F.; Gowen, M.; Lark, M. W.; Stroup, G. 分享 收藏
Structure activity relationships of 5-, 6-, and 7-methyl -substituted azepan-3-one cathepsin K inhibitors Yamashita, DS; Marquis, RW; Xie, R; Nidamarthy, SD; Oh, HJ; Jeong, JU; Erhard, KF; Ward, KW; Roethke, TJ; Smith, BR; Cheng, HY; Geng, XL; Lin, F; Offen, PH; Wang, B; Nevins, N; Head, MS; Haltiwanger, RC; Sarjeant, AAN; Liable-Sands, LM; Zhao, BG; Smith, WW; Janson, CA; Gao, E; Tomaszek, T; McQueney, M; Jarnes, IE; Gress, CJ; Zembryki, DL; Lark, MW; Veber, DF 分享 收藏
Azepanone-based inhibitors of human cathepsin L Marquis, RW; James, I; Zeng, J; Trout, REL; Thompson, S; Rahman, A; Yamashita, DS; Xie, R; Ru, Y; Gress, CJ; Blake, S; Lark, MA; Hwang, SM; Tomaszek, T; Offen, P; Head, MS; Cummings, MD; Veber, DF 分享 收藏
4-Aryl-1,2,3-triazole: A novel template for a reversible methionine aminopeptidase 2 inhibitor, optimized to inhibit angiogenesis in vivo Kallander, LS; Lu, Q; Chen, WF; Tomaszek, T; Yang, G; Tew, D; Meek, TD; Hofmann, GA; Schulz-Pritchard, CK; Smith, WW; Janson, CA; Ryan, MD; Zhang, GF; Johanson, KO; Kirkpatrick, RB; Ho, TF; Fisher, PW; Mattern, MR; Johnson, RK; Hansbury, MJ; Winkler, JD; Ward, KW; Veber, DF; Thompson, SK 分享 收藏
Evaluation of potent and selective small-molecule antagonists for the CXCR2 chemokine receptor Widdowson, KL; Elliott, JD; Veber, DF; Nie, H; Rutledge, MC; McCleland, BW; Xiang, JN; Jurewicz, AJ; Hertzberg, RP; Foley, JJ; Griswold, DE; Martin, L; Lee, JM; White, JR; Sarau, HM 分享 收藏
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2ND-GENERATION BENZODIAZEPINE CCK-B ANTAGONISTS - DEVELOPMENT OF SUBNANOMOLAR ANALOGS WITH SELECTIVITY AND WATER SOLUBILITY BOCK, MG; DIPARDO, RM; MELLIN, EC; NEWTON, RC; VEBER, DF; FREEDMAN, SB; SMITH, AJ; PATEL, S; KEMP, JA; MARSHALL, GR; FLETCHER, AE; CHAPMAN, KL; ANDERSON, PS; FREIDINGER, RM 分享 收藏
ORALLY ACTIVE, NONPEPTIDE OXYTOCIN ANTAGONISTS EVANS, BE; LEIGHTON, JL; RITTLE, KE; GILBERT, KF; LUNDELL, GF; GOULD, NP; HOBBS, DW; DIPARDO, RM; VEBER, DF; PETTIBONE, DJ; CLINESCHMIDT, BV; ANDERSON, PS; FREIDINGER, RM 分享 收藏
A potent small molecule, nonpeptide inhibitor of cathepsin K (SB 331750) prevents bone matrix resorption in the ovariectomized rat Lark, MW; Stroup, GB; James, IE; Dodds, RA; Hwang, SN; Blake, SM; Lechowska, BA; Hoffman, SJ; Smith, BR; Kapadia, R; Liang, X; Erhard, K; Ru, Y; Dong, X; Marquis, RW; Veber, D; Gowen, M 分享 收藏
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Potent and selective cathepsin L inhibitors do not inhibit human osteoclast resorption in vitro James, IE; Marquis, RW; Blake, SM; Hwang, SM; Gress, CJ; Ru, Y; Zembryki, D; Yamashita, DS; McQueney, MS; Tomaszek, TA; Oh, HJ; Gowen, M; Veber, DF; Lark, MW 分享 收藏
Azepanone-based inhibitors of human and rat cathepsin K Marquis, RW; Ru, Y; LoCastro, SM; Zeng, J; Yamashita, DS; Oh, HJ; Erhard, KF; Davis, LD; Tomaszek, TA; Tew, D; Salyers, K; Proksch, J; Ward, K; Smith, B; Levy, M; Cummings, MD; Haltiwanger, RC; Trescher, G; Wang, B; Hemling, ME; Quinn, CJ; Cheng, HY; Lin, F; Smith, WW; Janson, CA; Zhao, BG; McQueney, MS; D'Alessio, K; Lee, CP; Marzulli, A; Dodds, RA; Blake, S; Hwang, SM; James, IE; Gress, CJ; Bradley, BR; Lark, MW; Gowen, M; Veber, DF 分享 收藏
Cyclic ketone inhibitors of the cysteine protease cathepsin K Marquis, RW; Ru, Y; Zeng, J; Trout, REL; LoCastro, SM; Gribble, AD; Witherington, J; Fenwick, AE; Garnier, B; Tomaszek, T; Tew, D; Hemling, ME; Quinn, CJ; Smith, WW; Zhao, BG; McQueney, MS; Janson, CA; D'Alessio, K; Veber, DF 分享 收藏
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