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Page 1
Pharmacokinetic drivers of toxicity for basic molecules: strategy to lower pKa results in decreased tissue exposure and toxicity for a small molecule Met inhibitor.
Diaz D, Ford KA, Hartley DP, Harstad EB, Cain GR, Achilles-Poon K, Nguyen T, Peng J, Zheng Z, Merchant M, Sutherlin DP, Gaudino JJ, Kaus R, Lewin-Koh SC, Choo EF, Liederer BM, Dambach DM. Diaz D, et al. Among authors: sutherlin dp. Toxicol Appl Pharmacol. 2013 Jan 1;266(1):86-94. doi: 10.1016/j.taap.2012.10.026. Epub 2012 Nov 7. Toxicol Appl Pharmacol. 2013. PMID: 23142475
Structure-based optimization of pyrazolo-pyrimidine and -pyridine inhibitors of PI3-kinase.
Staben ST, Heffron TP, Sutherlin DP, Bhat SR, Castanedo GM, Chuckowree IS, Dotson J, Folkes AJ, Friedman LS, Lee L, Lesnick J, Lewis C, Murray JM, Nonomiya J, Olivero AG, Plise E, Pang J, Prior WW, Salphati L, Rouge L, Sampath D, Tsui V, Wan NC, Wang S, Weismann C, Wu P, Zhu BY. Staben ST, et al. Among authors: sutherlin dp. Bioorg Med Chem Lett. 2010 Oct 15;20(20):6048-51. doi: 10.1016/j.bmcl.2010.08.067. Epub 2010 Aug 19. Bioorg Med Chem Lett. 2010. PMID: 20822905
Second generation 2-pyridyl biphenyl amide inhibitors of the hedgehog pathway.
Castanedo GM, Wang S, Robarge KD, Blackwood E, Burdick D, Chang C, Dijkgraaf GJ, Gould S, Gunzner J, Guichert O, Halladay J, Khojasteh C, Lee L, Marsters JC Jr, Murray L, Peterson D, Plise E, Salphati L, de Sauvage FJ, Wong S, Sutherlin DP. Castanedo GM, et al. Among authors: sutherlin dp. Bioorg Med Chem Lett. 2010 Nov 15;20(22):6748-53. doi: 10.1016/j.bmcl.2010.08.134. Epub 2010 Sep 15. Bioorg Med Chem Lett. 2010. PMID: 20875741
Potent and selective inhibitors of PI3Kδ: obtaining isoform selectivity from the affinity pocket and tryptophan shelf.
Sutherlin DP, Baker S, Bisconte A, Blaney PM, Brown A, Chan BK, Chantry D, Castanedo G, DePledge P, Goldsmith P, Goldstein DM, Hancox T, Kaur J, Knowles D, Kondru R, Lesnick J, Lucas MC, Lewis C, Murray J, Nadin AJ, Nonomiya J, Pang J, Pegg N, Price S, Reif K, Safina BS, Salphati L, Staben S, Seward EM, Shuttleworth S, Sohal S, Sweeney ZK, Ultsch M, Waszkowycz B, Wei B. Sutherlin DP, et al. Bioorg Med Chem Lett. 2012 Jul 1;22(13):4296-302. doi: 10.1016/j.bmcl.2012.05.027. Epub 2012 May 17. Bioorg Med Chem Lett. 2012. PMID: 22672799
Fibroblast Activation Protein Cleaves and Inactivates Fibroblast Growth Factor 21.
Dunshee DR, Bainbridge TW, Kljavin NM, Zavala-Solorio J, Schroeder AC, Chan R, Corpuz R, Wong M, Zhou W, Deshmukh G, Ly J, Sutherlin DP, Ernst JA, Sonoda J. Dunshee DR, et al. Among authors: sutherlin dp. J Biol Chem. 2016 Mar 11;291(11):5986-5996. doi: 10.1074/jbc.M115.710582. Epub 2016 Jan 21. J Biol Chem. 2016. PMID: 26797127 Free PMC article.
Discovery of a potent, selective, and orally available class I phosphatidylinositol 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) kinase inhibitor (GDC-0980) for the treatment of cancer.
Sutherlin DP, Bao L, Berry M, Castanedo G, Chuckowree I, Dotson J, Folks A, Friedman L, Goldsmith R, Gunzner J, Heffron T, Lesnick J, Lewis C, Mathieu S, Murray J, Nonomiya J, Pang J, Pegg N, Prior WW, Rouge L, Salphati L, Sampath D, Tian Q, Tsui V, Wan NC, Wang S, Wei B, Wiesmann C, Wu P, Zhu BY, Olivero A. Sutherlin DP, et al. J Med Chem. 2011 Nov 10;54(21):7579-87. doi: 10.1021/jm2009327. Epub 2011 Oct 7. J Med Chem. 2011. PMID: 21981714
A selective, slow binding inhibitor of factor VIIa binds to a nonstandard active site conformation and attenuates thrombus formation in vivo.
Olivero AG, Eigenbrot C, Goldsmith R, Robarge K, Artis DR, Flygare J, Rawson T, Sutherlin DP, Kadkhodayan S, Beresini M, Elliott LO, DeGuzman GG, Banner DW, Ultsch M, Marzec U, Hanson SR, Refino C, Bunting S, Kirchhofer D. Olivero AG, et al. Among authors: sutherlin dp. J Biol Chem. 2005 Mar 11;280(10):9160-9. doi: 10.1074/jbc.M409068200. Epub 2005 Jan 4. J Biol Chem. 2005. PMID: 15632123 Free article.
Identification of GNE-477, a potent and efficacious dual PI3K/mTOR inhibitor.
Heffron TP, Berry M, Castanedo G, Chang C, Chuckowree I, Dotson J, Folkes A, Gunzner J, Lesnick JD, Lewis C, Mathieu S, Nonomiya J, Olivero A, Pang J, Peterson D, Salphati L, Sampath D, Sideris S, Sutherlin DP, Tsui V, Wan NC, Wang S, Wong S, Zhu BY. Heffron TP, et al. Among authors: sutherlin dp. Bioorg Med Chem Lett. 2010 Apr 15;20(8):2408-11. doi: 10.1016/j.bmcl.2010.03.046. Epub 2010 Mar 12. Bioorg Med Chem Lett. 2010. PMID: 20346656
51 results