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Page 1
AMG 176, a Selective MCL1 Inhibitor, Is Effective in Hematologic Cancer Models Alone and in Combination with Established Therapies.
Caenepeel S, Brown SP, Belmontes B, Moody G, Keegan KS, Chui D, Whittington DA, Huang X, Poppe L, Cheng AC, Cardozo M, Houze J, Li Y, Lucas B, Paras NA, Wang X, Taygerly JP, Vimolratana M, Zancanella M, Zhu L, Cajulis E, Osgood T, Sun J, Damon L, Egan RK, Greninger P, McClanaghan JD, Gong J, Moujalled D, Pomilio G, Beltran P, Benes CH, Roberts AW, Huang DC, Wei A, Canon J, Coxon A, Hughes PE. Caenepeel S, et al. Among authors: brown sp. Cancer Discov. 2018 Dec;8(12):1582-1597. doi: 10.1158/2159-8290.CD-18-0387. Epub 2018 Sep 25. Cancer Discov. 2018. PMID: 30254093
Exploiting MCL1 Dependency with Combination MEK + MCL1 Inhibitors Leads to Induction of Apoptosis and Tumor Regression in KRAS-Mutant Non-Small Cell Lung Cancer.
Nangia V, Siddiqui FM, Caenepeel S, Timonina D, Bilton SJ, Phan N, Gomez-Caraballo M, Archibald HL, Li C, Fraser C, Rigas D, Vajda K, Ferris LA, Lanuti M, Wright CD, Raskin KA, Cahill DP, Shin JH, Keyes C, Sequist LV, Piotrowska Z, Farago AF, Azzoli CG, Gainor JF, Sarosiek KA, Brown SP, Coxon A, Benes CH, Hughes PE, Hata AN. Nangia V, et al. Among authors: brown sp. Cancer Discov. 2018 Dec;8(12):1598-1613. doi: 10.1158/2159-8290.CD-18-0277. Epub 2018 Sep 25. Cancer Discov. 2018. PMID: 30254092 Free PMC article.
Discovery of AM-1638: A Potent and Orally Bioavailable GPR40/FFA1 Full Agonist.
Brown SP, Dransfield PJ, Vimolratana M, Jiao X, Zhu L, Pattaropong V, Sun Y, Liu J, Luo J, Zhang J, Wong S, Zhuang R, Guo Q, Li F, Medina JC, Swaminath G, Lin DC, Houze JB. Brown SP, et al. ACS Med Chem Lett. 2012 Aug 15;3(9):726-30. doi: 10.1021/ml300133f. eCollection 2012 Sep 13. ACS Med Chem Lett. 2012. PMID: 24900539 Free PMC article.
Discovery and in Vivo Evaluation of Macrocyclic Mcl-1 Inhibitors Featuring an α-Hydroxy Phenylacetic Acid Pharmacophore or Bioisostere.
Rescourio G, Gonzalez AZ, Jabri S, Belmontes B, Moody G, Whittington D, Huang X, Caenepeel S, Cardozo M, Cheng AC, Chow D, Dou H, Jones A, Kelly RC, Li Y, Lizarzaburu M, Lo MC, Mallari R, Meleza C, Rew Y, Simonovich S, Sun D, Turcotte S, Yan X, Wong SG, Yanez E, Zancanella M, Houze J, Medina JC, Hughes PE, Brown SP. Rescourio G, et al. Among authors: brown sp. J Med Chem. 2019 Nov 27;62(22):10258-10271. doi: 10.1021/acs.jmedchem.9b01310. Epub 2019 Nov 18. J Med Chem. 2019. PMID: 31736296
Discovery and Optimization of Potent GPR40 Full Agonists Containing Tricyclic Spirocycles.
Wang Y, Liu JJ, Dransfield PJ, Zhu L, Wang Z, Du X, Jiao X, Su Y, Li AR, Brown SP, Kasparian A, Vimolratana M, Yu M, Pattaropong V, Houze JB, Swaminath G, Tran T, Nguyen K, Guo Q, Zhang J, Zhuang R, Li F, Miao L, Bartberger MD, Correll TL, Chow D, Wong S, Luo J, Lin DC, Medina JC. Wang Y, et al. Among authors: brown sp. ACS Med Chem Lett. 2013 May 7;4(6):551-5. doi: 10.1021/ml300427u. eCollection 2013 Jun 13. ACS Med Chem Lett. 2013. PMID: 24900707 Free PMC article.
Improving the Pharmacokinetics of GPR40/FFA1 Full Agonists.
Du X, Dransfield PJ, Lin DC, Wong S, Wang Y, Wang Z, Kohn T, Yu M, Brown SP, Vimolratana M, Zhu L, Li AR, Su Y, Jiao X, Liu JJ, Swaminath G, Tran T, Luo J, Zhuang R, Zhang J, Guo Q, Li F, Connors R, Medina JC, Houze JB. Du X, et al. Among authors: brown sp. ACS Med Chem Lett. 2014 Feb 3;5(4):384-9. doi: 10.1021/ml4005123. eCollection 2014 Apr 10. ACS Med Chem Lett. 2014. PMID: 24900845 Free PMC article.
Optimization of GPR40 Agonists for Type 2 Diabetes.
Liu JJ, Wang Y, Ma Z, Schmitt M, Zhu L, Brown SP, Dransfield PJ, Sun Y, Sharma R, Guo Q, Zhuang R, Zhang J, Luo J, Tonn GR, Wong S, Swaminath G, Medina JC, Lin DC, Houze JB. Liu JJ, et al. Among authors: brown sp. ACS Med Chem Lett. 2014 Feb 6;5(5):517-21. doi: 10.1021/ml400501x. eCollection 2014 May 8. ACS Med Chem Lett. 2014. PMID: 24900872 Free PMC article.
418 results