Cyclopamine modulates smoothened receptor activity in a binding position dependent manner.

Autor: Kim, Kihong¹ (AUTHOR), Bansal, Prateek D.¹ (AUTHOR), Shukla, Diwakar^1,2,3,4,5 (AUTHOR) diwakar@illinois.edu

Publikováno v: Communications Biology. 9/28/2024, Vol. 7 Issue 1, p1-14. 14p.

Structure based design of novel 6,5 heterobicyclic mitogen-activated protein kinase kinase (MEK) inhibitors leading to the discovery of imidazo[1,5-a] pyrazine G-479.

Autor: Robarge KD; Discovery Chemistry, Genentech Inc., 1 DNA Way, South San Francisco, CA, USA. Electronic address: kir@gene.com., Lee W; Discovery Chemistry, Genentech Inc., 1 DNA Way, South San Francisco, CA, USA., Eigenbrot C; Structural Biology, Genentech Inc., 1 DNA Way, South San Francisco, CA, USA., Ultsch M; Structural Biology, Genentech Inc., 1 DNA Way, South San Francisco, CA, USA., Wiesmann C; Structural Biology, Genentech Inc., 1 DNA Way, South San Francisco, CA, USA., Heald R; Argenta, Discovery Services Charles River, 8-9 Spire Greene Centre, Harlow, Essex CM19 5TR, United Kingdom., Price S; Argenta, Discovery Services Charles River, 8-9 Spire Greene Centre, Harlow, Essex CM19 5TR, United Kingdom., Hewitt J; Argenta, Discovery Services Charles River, 8-9 Spire Greene Centre, Harlow, Essex CM19 5TR, United Kingdom., Jackson P; Argenta, Discovery Services Charles River, 8-9 Spire Greene Centre, Harlow, Essex CM19 5TR, United Kingdom., Savy P; Argenta, Discovery Services Charles River, 8-9 Spire Greene Centre, Harlow, Essex CM19 5TR, United Kingdom., Burton B; Argenta, Discovery Services Charles River, 8-9 Spire Greene Centre, Harlow, Essex CM19 5TR, United Kingdom., Choo EF; Drug Metabolism and Pharmacokinetics, Genentech Inc., 1 DNA Way, South San Francisco, CA, USA., Pang J; Drug Metabolism and Pharmacokinetics, Genentech Inc., 1 DNA Way, South San Francisco, CA, USA., Boggs J; Drug Metabolism and Pharmacokinetics, Genentech Inc., 1 DNA Way, South San Francisco, CA, USA., Yang A; Drug Metabolism and Pharmacokinetics, Genentech Inc., 1 DNA Way, South San Francisco, CA, USA., Yang X; Drug Metabolism and Pharmacokinetics, Genentech Inc., 1 DNA Way, South San Francisco, CA, USA., Baumgardner M; Drug Metabolism and Pharmacokinetics, Genentech Inc., 1 DNA Way, South San Francisco, CA, USA.

Publikováno v: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2014 Oct 01; Vol. 24 (19), pp. 4714-4723. Date of Electronic Publication: 2014 Aug 15.

Potent, selective, and orally bioavailable inhibitors of mammalian target of rapamycin (mTOR) kinase based on a quaternary substituted dihydrofuropyrimidine.

Autor: Cohen F; Department of Discovery Chemistry, Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States. fcohen@gene.com, Bergeron P, Blackwood E, Bowman KK, Chen H, Dipasquale AG, Epler JA, Koehler MF, Lau K, Lewis C, Liu L, Ly CQ, Malek S, Nonomiya J, Ortwine DF, Pei Z, Robarge KD, Sideris S, Trinh L, Truong T, Wu J, Zhao X, Lyssikatos JP

Publikováno v: Journal of medicinal chemistry [J Med Chem] 2011 May 12; Vol. 54 (9), pp. 3426-35. Date of Electronic Publication: 2011 Apr 15.

GDC-0449-a potent inhibitor of the hedgehog pathway.

Autor: Robarge KD; Genentech, Small Molecule Drug Discovery 1 DNA Way, South San Francisco, CA 94080, United States. kir@gene.com, Brunton SA, Castanedo GM, Cui Y, Dina MS, Goldsmith R, Gould SE, Guichert O, Gunzner JL, Halladay J, Jia W, Khojasteh C, Koehler MF, Kotkow K, La H, Lalonde RL, Lau K, Lee L, Marshall D, Marsters JC Jr, Murray LJ, Qian C, Rubin LL, Salphati L, Stanley MS, Stibbard JH, Sutherlin DP, Ubhayaker S, Wang S, Wong S, Xie M

Publikováno v: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2009 Oct 01; Vol. 19 (19), pp. 5576-81. Date of Electronic Publication: 2009 Aug 15.

Stability of alkoxycarbonylamidine prodrugs.

Autor: Shahrokh Z; Department of Pharmaceutical R&D, Genentech Inc., South San Francisco, California 94080, USA. zahra@gene.com, Lee E, Olivero AG, Matamoros RA, Robarge KD, Lee A, Weise KJ, Blackburn BK, Powell MF

Publikováno v: Pharmaceutical research [Pharm Res] 1998 Mar; Vol. 15 (3), pp. 434-41.