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Wang X, Pai JT, Wiedenfeld EA, Medina JC, Slaughter CA, Goldstein JL, Brown MS. Purification of an interleukin-1 beta converting enzyme-related cysteine protease that cleaves sterol regulatory element-binding proteins between the leucine zipper and transmembrane domains. J Biol Chem. 1995 Jul 28;270(30):18044-50. doi: 10.1074/jbc.270.30.18044. PubMed PMID: 7629113.
Medina JC, Shan B, Beckmann H, Farrell RP, Clark DL, Learned RM, Roche D, Li A, Baichwal V, Case C, Baeuerle PA, Rosen T, Jaen JC. Novel antineoplastic agents with efficacy against multidrug resistant tumor cells. Bioorg Med Chem Lett. 1998 Oct 6;8(19):2653-6. doi: 10.1016/s0960-894x(98)00477-6. PubMed PMID: 9873597.
Shan B, Medina JC, Santha E, Frankmoelle WP, Chou TC, Learned RM, Narbut MR, Stott D, Wu P, Jaen JC, Rosen T, Timmermans PB, Beckmann H. Selective, covalent modification of beta-tubulin residue Cys-239 by T138067, an antitumor agent with in vivo efficacy against multidrug-resistant tumors. Proc Natl Acad Sci U S A. 1999 May 11;96(10):5686-91. doi: 10.1073/pnas.96.10.5686. PubMed PMID: 10318945; PubMed Central PMCID: PMC21921.
Medina JC, Roche D, Shan B, Learned RM, Frankmoelle WP, Clark DL, Rosen T, Jaen JC. Novel halogenated sulfonamides inhibit the growth of multidrug resistant MCF-7/ADR cancer cells. Bioorg Med Chem Lett. 1999 Jul 5;9(13):1843-6. doi: 10.1016/s0960-894x(99)00276-0. PubMed PMID: 10406652.
Frankmoelle WP, Medina JC, Shan B, Narbut MR, Beckmann H. Glutathione S-transferase metabolism of the antineoplastic pentafluorophenylsulfonamide in tissue culture and mice. Drug Metab Dispos. 2000 Aug;28(8):951-8. PubMed PMID: 10901706.
Repa JJ, Turley SD, Lobaccaro JA, Medina J, Li L, Lustig K, Shan B, Heyman RA, Dietschy JM, Mangelsdorf DJ. Regulation of absorption and ABC1-mediated efflux of cholesterol by RXR heterodimers. Science. 2000 Sep 1;289(5484):1524-9. doi: 10.1126/science.289.5484.1524. PubMed PMID: 10968783.
Schultz JR, Tu H, Luk A, Repa JJ, Medina JC, Li L, Schwendner S, Wang S, Thoolen M, Mangelsdorf DJ, Lustig KD, Shan B. Role of LXRs in control of lipogenesis. Genes Dev. 2000 Nov 15;14(22):2831-8. doi: 10.1101/gad.850400. PubMed PMID: 11090131; PubMed Central PMCID: PMC317060.
Li L, Liu J, Zhu L, Cutler S, Hasegawa H, Shan B, Medina JC. Discovery and optimization of a novel series of liver X receptor-alpha agonists. Bioorg Med Chem Lett. 2006 Mar 15;16(6):1638-42. doi: 10.1016/j.bmcl.2005.12.015. Epub 2005 Dec 28. PubMed PMID: 16386417.
Wang X, Xu F, Xu Q, Mahmud H, Houze J, Zhu L, Akerman M, Tonn G, Tang L, McMaster BE, Dairaghi DJ, Schall TJ, Collins TL, Medina JC. Optimization of 2-aminothiazole derivatives as CCR4 antagonists. Bioorg Med Chem Lett. 2006 May 15;16(10):2800-3. doi: 10.1016/j.bmcl.2006.01.126. Epub 2006 Feb 23. PubMed PMID: 16497499.
Walser TC, Rifat S, Ma X, Kundu N, Ward C, Goloubeva O, Johnson MG, Medina JC, Collins TL, Fulton AM. Antagonism of CXCR3 inhibits lung metastasis in a murine model of metastatic breast cancer. Cancer Res. 2006 Aug 1;66(15):7701-7. doi: 10.1158/0008-5472.CAN-06-0709. PubMed PMID: 16885372.
Johnson M, Li AR, Liu J, Fu Z, Zhu L, Miao S, Wang X, Xu Q, Huang A, Marcus A, Xu F, Ebsworth K, Sablan E, Danao J, Kumer J, Dairaghi D, Lawrence C, Sullivan T, Tonn G, Schall T, Collins T, Medina J. Discovery and optimization of a series of quinazolinone-derived antagonists of CXCR3. Bioorg Med Chem Lett. 2007 Jun 15;17(12):3339-43. doi: 10.1016/j.bmcl.2007.03.106. Epub 2007 Apr 6. PubMed PMID: 17448658.
Du X, Chen X, Mihalic JT, Deignan J, Duquette J, Li AR, Lemon B, Ma J, Miao S, Ebsworth K, Sullivan TJ, Tonn G, Collins TL, Medina JC. Design and optimization of imidazole derivatives as potent CXCR3 antagonists. Bioorg Med Chem Lett. 2008 Jan 15;18(2):608-13. doi: 10.1016/j.bmcl.2007.11.072. Epub 2007 Nov 28. PubMed PMID: 18063364.
Li AR, Johnson MG, Liu J, Chen X, Du X, Mihalic JT, Deignan J, Gustin DJ, Duquette J, Fu Z, Zhu L, Marcus AP, Bergeron P, McGee LR, Danao J, Lemon B, Carabeo T, Sullivan T, Ma J, Tang L, Tonn G, Collins TL, Medina JC. Optimization of the heterocyclic core of the quinazolinone-derived CXCR3 antagonists. Bioorg Med Chem Lett. 2008 Jan 15;18(2):688-93. doi: 10.1016/j.bmcl.2007.11.060. Epub 2007 Nov 21. PubMed PMID: 18061451.
Beck HP, Kohn T, Rubenstein S, Hedberg C, Schwandner R, Hasslinger K, Dai K, Li C, Liang L, Wesche H, Frank B, An S, Wickramasinghe D, Jaen J, Medina J, Hungate R, Shen W. Discovery of potent LPA2 (EDG4) antagonists as potential anticancer agents. Bioorg Med Chem Lett. 2008 Feb 1;18(3):1037-41. doi: 10.1016/j.bmcl.2007.12.024. Epub 2008 Jan 4. PubMed PMID: 18178086.
Cameron CM, Cameron MJ, Bermejo-Martin JF, Ran L, Xu L, Turner PV, Ran R, Danesh A, Fang Y, Chan PK, Mytle N, Sullivan TJ, Collins TL, Johnson MG, Medina JC, Rowe T, Kelvin DJ. Gene expression analysis of host innate immune responses during Lethal H5N1 infection in ferrets. J Virol. 2008 Nov;82(22):11308-17. doi: 10.1128/JVI.00691-08. Epub 2008 Aug 6. PubMed PMID: 18684821; PubMed Central PMCID: PMC2573250.
Rosenblum JM, Zhang QW, Siu G, Collins TL, Sullivan T, Dairaghi DJ, Medina JC, Fairchild RL. CXCR3 antagonism impairs the development of donor-reactive, IFN-gamma-producing effectors and prolongs allograft survival. Transplantation. 2009 Feb 15;87(3):360-9. doi: 10.1097/TP.0b013e31819574e9. PubMed PMID: 19202440; PubMed Central PMCID: PMC2738925.
Tonn GR, Wong SG, Wong SC, Johnson MG, Ma J, Cho R, Floren LC, Kersey K, Berry K, Marcus AP, Wang X, Van Lengerich B, Medina JC, Pearson PG, Wong BK. An inhibitory metabolite leads to dose- and time-dependent pharmacokinetics of (R)-N-{1-[3-(4-ethoxy-phenyl)-4-oxo-3,4-dihydro-pyrido[2,3-d]pyrimidin-2-yl]-ethyl}-N-pyridin-3-yl-methyl-2-(4-trifluoromethoxy-phenyl)-acetamide (AMG 487) in human subjects after multiple dosing. Drug Metab Dispos. 2009 Mar;37(3):502-13. doi: 10.1124/dmd.108.021931. Epub 2008 Dec 16. PubMed PMID: 19088267.
Cambien B, Karimdjee BF, Richard-Fiardo P, Bziouech H, Barthel R, Millet MA, Martini V, Birnbaum D, Scoazec JY, Abello J, Al Saati T, Johnson MG, Sullivan TJ, Medina JC, Collins TL, Schmid-Alliana A, Schmid-Antomarchi H. Organ-specific inhibition of metastatic colon carcinoma by CXCR3 antagonism. Br J Cancer. 2009 Jun 2;100(11):1755-64. doi: 10.1038/sj.bjc.6605078. Epub 2009 May 12. PubMed PMID: 19436305; PubMed Central PMCID: PMC2695685.
Liu J, Fu Z, Li AR, Johnson M, Zhu L, Marcus A, Danao J, Sullivan T, Tonn G, Collins T, Medina J. Optimization of a series of quinazolinone-derived antagonists of CXCR3. Bioorg Med Chem Lett. 2009 Sep 1;19(17):5114-8. doi: 10.1016/j.bmcl.2009.07.032. Epub 2009 Jul 10. PubMed PMID: 19632842.
Du X, Gustin DJ, Chen X, Duquette J, McGee LR, Wang Z, Ebsworth K, Henne K, Lemon B, Ma J, Miao S, Sabalan E, Sullivan TJ, Tonn G, Collins TL, Medina JC. Imidazo-pyrazine derivatives as potent CXCR3 antagonists. Bioorg Med Chem Lett. 2009 Sep 1;19(17):5200-4. doi: 10.1016/j.bmcl.2009.07.021. Epub 2009 Jul 9. PubMed PMID: 19631529.
Liu J, Fu Z, Wang Y, Schmitt M, Huang A, Marshall D, Tonn G, Seitz L, Sullivan T, Lucy Tang H, Collins T, Medina J. Discovery and optimization of CRTH2 and DP dual antagonists. Bioorg Med Chem Lett. 2009 Nov 15;19(22):6419-23. doi: 10.1016/j.bmcl.2009.09.052. Epub 2009 Sep 17. PubMed PMID: 19804971.
Pradelli E, Karimdjee-Soilihi B, Michiels JF, Ricci JE, Millet MA, Vandenbos F, Sullivan TJ, Collins TL, Johnson MG, Medina JC, Kleinerman ES, Schmid-Alliana A, Schmid-Antomarchi H. Antagonism of chemokine receptor CXCR3 inhibits osteosarcoma metastasis to lungs. Int J Cancer. 2009 Dec 1;125(11):2586-94. doi: 10.1002/ijc.24665. PubMed PMID: 19544560; PubMed Central PMCID: PMC2772145.
Liu J, Wang Y, Sun Y, Marshall D, Miao S, Tonn G, Anders P, Tocker J, Tang HL, Medina J. Tetrahydroquinoline derivatives as CRTH2 antagonists. Bioorg Med Chem Lett. 2009 Dec 15;19(24):6840-4. doi: 10.1016/j.bmcl.2009.10.094. Epub 2009 Oct 25. PubMed PMID: 19896843.
Yu M, Lizarzaburu M, Beckmann H, Connors R, Dai K, Haller K, Li C, Liang L, Lindstrom M, Ma J, Motani A, Wanska M, Zhang A, Li L, Medina JC. Identification of piperazine-bisamide GHSR antagonists for the treatment of obesity. Bioorg Med Chem Lett. 2010 Mar 1;20(5):1758-62. doi: 10.1016/j.bmcl.2010.01.043. Epub 2010 Jan 20. PubMed PMID: 20137933.
Liu J, Li AR, Wang Y, Johnson MG, Su Y, Shen W, Wang X, Lively S, Brown M, Lai S, Gonzalez Lopez De Turiso F, Xu Q, Van Lengerich B, Schmitt M, Fu Z, Sun Y, Lawlis S, Seitz L, Danao J, Wait J, Ye Q, Tang HL, Grillo M, Collins TL, Sullivan TJ, Medina JC. Discovery of AMG 853, a CRTH2 and DP Dual Antagonist. ACS Med Chem Lett. 2011 May 12;2(5):326-30. doi: 10.1021/ml1002234. eCollection 2011 May 12. PubMed PMID: 24900313; PubMed Central PMCID: PMC4018074.
Du X, Lizarzaburu M, Turcotte S, Lee T, Greenberg J, Shan B, Fan P, Ling Y, Medina JC, Houze J. Optimization of triazoles as novel and potent nonphlorizin SGLT2 inhibitors. Bioorg Med Chem Lett. 2011 Jun 15;21(12):3774-9. doi: 10.1016/j.bmcl.2011.04.053. Epub 2011 Apr 20. PubMed PMID: 21565497.
Liu JJ, Cheng AC, Tang HL, Medina JC. Benzodiazepinone Derivatives as CRTH2 Antagonists. ACS Med Chem Lett. 2011 Jul 14;2(7):515-8. doi: 10.1021/ml200019y. eCollection 2011 Jul 14. PubMed PMID: 24900341; PubMed Central PMCID: PMC4018144.
Chen X, Mihalic J, Deignan J, Gustin DJ, Duquette J, Du X, Chan J, Fu Z, Johnson M, Li AR, Henne K, Sullivan T, Lemon B, Ma J, Miao S, Tonn G, Collins T, Medina JC. Discovery of potent and specific CXCR3 antagonists. Bioorg Med Chem Lett. 2012 Jan 1;22(1):357-62. doi: 10.1016/j.bmcl.2011.10.120. Epub 2011 Nov 9. PubMed PMID: 22130135.
Wang Y, Fu Z, Schmitt M, Wang X, Shen W, Rickel E, Martin T, Budelsky A, Marshall D, Collins T, Tang HL, Medina JC, Liu JJ. Optimization of phenylacetic acid derivatives for CRTH2 and DP selective antagonism. Bioorg Med Chem Lett. 2012 Jan 1;22(1):367-70. doi: 10.1016/j.bmcl.2011.10.123. Epub 2011 Nov 9. PubMed PMID: 22119474.
Houze JB, Zhu L, Sun Y, Akerman M, Qiu W, Zhang AJ, Sharma R, Schmitt M, Wang Y, Liu J, Liu J, Medina JC, Reagan JD, Luo J, Tonn G, Zhang J, Lu JY, Chen M, Lopez E, Nguyen K, Yang L, Tang L, Tian H, Shuttleworth SJ, Lin DC. AMG 837: a potent, orally bioavailable GPR40 agonist. Bioorg Med Chem Lett. 2012 Jan 15;22(2):1267-70. doi: 10.1016/j.bmcl.2011.10.118. Epub 2011 Nov 6. PubMed PMID: 22217876.
Liu JJ, Wang Y, Johnson MG, Li AR, Shen W, Wang X, Su Y, Brown M, Van Lengerich B, Rickel E, Martin T, Budelsky A, Seitz L, Danao J, Tang HL, Collins T, Medina JC. Optimization of phenylacetic acid derivatives for balanced CRTH2 and DP dual antagonists. Bioorg Med Chem Lett. 2012 Feb 15;22(4):1686-9. doi: 10.1016/j.bmcl.2011.12.107. Epub 2011 Dec 30. PubMed PMID: 22264478.
Rew Y, Sun D, Gonzalez-Lopez De Turiso F, Bartberger MD, Beck HP, Canon J, Chen A, Chow D, Deignan J, Fox BM, Gustin D, Huang X, Jiang M, Jiao X, Jin L, Kayser F, Kopecky DJ, Li Y, Lo MC, Long AM, Michelsen K, Oliner JD, Osgood T, Ragains M, Saiki AY, Schneider S, Toteva M, Yakowec P, Yan X, Ye Q, Yu D, Zhao X, Zhou J, Medina JC, Olson SH. Structure-based design of novel inhibitors of the MDM2-p53 interaction. J Med Chem. 2012 Jun 14;55(11):4936-54. doi: 10.1021/jm300354j. Epub 2012 May 9. PubMed PMID: 22524527.
Lucas BS, Fisher B, McGee LR, Olson SH, Medina JC, Cheung E. An expeditious synthesis of the MDM2-p53 inhibitor AM-8553. J Am Chem Soc. 2012 Aug 1;134(30):12855-60. doi: 10.1021/ja305123v. Epub 2012 Jul 16. PubMed PMID: 22734631.
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. Discovery of AM-1638: A Potent and Orally Bioavailable GPR40/FFA1 Full Agonist. ACS Med Chem Lett. 2012 Sep 13;3(9):726-30. doi: 10.1021/ml300133f. eCollection 2012 Sep 13. PubMed PMID: 24900539; PubMed Central PMCID: PMC4025659.
Gonzalez-Lopez de Turiso F, Shin Y, Brown M, Cardozo M, Chen Y, Fong D, Hao X, He X, Henne K, Hu YL, Johnson MG, Kohn T, Lohman J, McBride HJ, McGee LR, Medina JC, Metz D, Miner K, Mohn D, Pattaropong V, Seganish J, Simard JL, Wannberg S, Whittington DA, Yu G, Cushing TD. Discovery and in vivo evaluation of dual PI3Kβ/δ inhibitors. J Med Chem. 2012 Sep 13;55(17):7667-85. doi: 10.1021/jm300679u. Epub 2012 Aug 29. PubMed PMID: 22876881.
Lizarzaburu M, Turcotte S, Du X, Duquette J, Fu A, Houze J, Li L, Liu J, Murakoshi M, Oda K, Okuyama R, Nara F, Reagan J, Yu M, Medina JC. Discovery and optimization of a novel series of GPR142 agonists for the treatment of type 2 diabetes mellitus. Bioorg Med Chem Lett. 2012 Sep 15;22(18):5942-7. doi: 10.1016/j.bmcl.2012.07.063. Epub 2012 Jul 23. PubMed PMID: 22884988.
Du X, Kim YJ, Lai S, Chen X, Lizarzaburu M, Turcotte S, Fu Z, Liu Q, Zhang Y, Motani A, Oda K, Okuyama R, Nara F, Murakoshi M, Fu A, Reagan JD, Fan P, Xiong Y, Shen W, Li L, Houze J, Medina JC. Phenylalanine derivatives as GPR142 agonists for the treatment of type II diabetes. Bioorg Med Chem Lett. 2012 Oct 1;22(19):6218-23. doi: 10.1016/j.bmcl.2012.08.015. Epub 2012 Aug 10. PubMed PMID: 22926069.
Gonzalez-Lopez de Turiso F, Sun D, Rew Y, Bartberger MD, Beck HP, Canon J, Chen A, Chow D, Correll TL, Huang X, Julian LD, Kayser F, Lo MC, Long AM, McMinn D, Oliner JD, Osgood T, Powers JP, Saiki AY, Schneider S, Shaffer P, Xiao SH, Yakowec P, Yan X, Ye Q, Yu D, Zhao X, Zhou J, Medina JC, Olson SH. Rational design and binding mode duality of MDM2-p53 inhibitors. J Med Chem. 2013 May 23;56(10):4053-70. doi: 10.1021/jm400293z. Epub 2013 May 6. PubMed PMID: 23597064.
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. Discovery and Optimization of Potent GPR40 Full Agonists Containing Tricyclic Spirocycles. ACS Med Chem Lett. 2013 Jun 13;4(6):551-5. doi: 10.1021/ml300427u. eCollection 2013 Jun 13. PubMed PMID: 24900707; PubMed Central PMCID: PMC4027505.
Zhang JK, Li AR, Yu M, Wang Y, Zhu J, Kayser F, Medina JC, Siegler K, Conn M, Shan B, Grillo MP, Eksterowicz J, Coward P, Liu JJ. Discovery and optimization of arylsulfonyl 3-(pyridin-2-yloxy)anilines as novel GPR119 agonists. Bioorg Med Chem Lett. 2013 Jun 15;23(12):3609-13. doi: 10.1016/j.bmcl.2013.04.014. Epub 2013 Apr 15. PubMed PMID: 23648181.
Toda N, Hao X, Ogawa Y, Oda K, Yu M, Fu Z, Chen Y, Kim Y, Lizarzaburu M, Lively S, Lawlis S, Murakoshi M, Nara F, Watanabe N, Reagan JD, Tian H, Fu A, Motani A, Liu Q, Lin YJ, Zhuang R, Xiong Y, Fan P, Medina J, Li L, Izumi M, Okuyama R, Shibuya S. Potent and Orally Bioavailable GPR142 Agonists as Novel Insulin Secretagogues for the Treatment of Type 2 Diabetes. ACS Med Chem Lett. 2013 Aug 8;4(8):790-4. doi: 10.1021/ml400186z. eCollection 2013 Aug 8. PubMed PMID: 24900747; PubMed Central PMCID: PMC4027368.
Yu M, Lizarzaburu M, Motani A, Fu Z, Du X, Liu JJ, Jiao X, Lai S, Fan P, Fu A, Liu Q, Murakoshi M, Nara F, Oda K, Okuyama R, Reagan JD, Watanabe N, Yamazaki M, Xiong Y, Zhang Y, Zhuang R, Lin DC, Houze JB, Medina JC, Li L. Aminopyrazole-Phenylalanine Based GPR142 Agonists: Discovery of Tool Compound and in Vivo Efficacy Studies. ACS Med Chem Lett. 2013 Sep 12;4(9):829-34. doi: 10.1021/ml4000854. eCollection 2013 Sep 12. PubMed PMID: 24900757; PubMed Central PMCID: PMC4027463.
Yu M, Ken Zhang J, Wang Y, Zhu J, Kayser F, Medina JC, Siegler K, Conn M, Shan B, Grillo MP, Coward P, Jim Liu J. Discovery and optimization of N-(3-(1,3-dioxo-2,3-dihydro-1H-pyrrolo[3,4-c]pyridin-4-yloxy)phenyl)benzenesulfonamides as novel GPR119 agonists. Bioorg Med Chem Lett. 2014 Jan 1;24(1):156-60. doi: 10.1016/j.bmcl.2013.11.053. Epub 2013 Dec 1. PubMed PMID: 24332491.
Wang Y, Yu M, Zhu J, Zhang JK, Kayser F, Medina JC, Siegler K, Conn M, Shan B, Grillo MP, Liu JJ, Coward P. Discovery and optimization of 5-(2-((1-(phenylsulfonyl)-1,2,3,4-tetrahydroquinolin-7-yl)oxy)pyridin-4-yl)-1,2,4-oxadiazoles as novel gpr119 agonists. Bioorg Med Chem Lett. 2014 Feb 15;24(4):1133-7. doi: 10.1016/j.bmcl.2013.12.127. Epub 2014 Jan 8. PubMed PMID: 24440299.
Sun D, Li Z, Rew Y, Gribble M, Bartberger MD, Beck HP, Canon J, Chen A, Chen X, Chow D, Deignan J, Duquette J, Eksterowicz J, Fisher B, Fox BM, Fu J, Gonzalez AZ, Gonzalez-Lopez De Turiso F, Houze JB, Huang X, Jiang M, Jin L, Kayser F, Liu JJ, Lo MC, Long AM, Lucas B, McGee LR, McIntosh J, Mihalic J, Oliner JD, Osgood T, Peterson ML, Roveto P, Saiki AY, Shaffer P, Toteva M, Wang Y, Wang YC, Wortman S, Yakowec P, Yan X, Ye Q, Yu D, Yu M, Zhao X, Zhou J, Zhu J, Olson SH, Medina JC. Discovery of AMG 232, a potent, selective, and orally bioavailable MDM2-p53 inhibitor in clinical development. J Med Chem. 2014 Feb 27;57(4):1454-72. doi: 10.1021/jm401753e. Epub 2014 Feb 5. PubMed PMID: 24456472.
Gonzalez AZ, Eksterowicz J, Bartberger MD, Beck HP, Canon J, Chen A, Chow D, Duquette J, Fox BM, Fu J, Huang X, Houze JB, Jin L, Li Y, Li Z, Ling Y, Lo MC, Long AM, McGee LR, McIntosh J, McMinn DL, Oliner JD, Osgood T, Rew Y, Saiki AY, Shaffer P, Wortman S, Yakowec P, Yan X, Ye Q, Yu D, Zhao X, Zhou J, Olson SH, Medina JC, Sun D. Selective and potent morpholinone inhibitors of the MDM2-p53 protein-protein interaction. J Med Chem. 2014 Mar 27;57(6):2472-88. doi: 10.1021/jm401767k. Epub 2014 Mar 4. PubMed PMID: 24548297.
Keegan K, Li C, Li Z, Ma J, Ragains M, Coberly S, Hollenback D, Eksterowicz J, Liang L, Weidner M, Huard J, Wang X, Alba G, Orf J, Lo MC, Zhao S, Ngo R, Chen A, Liu L, Carlson T, Quéva C, McGee LR, Medina J, Kamb A, Wickramasinghe D, Dai K. Preclinical evaluation of AMG 925, a FLT3/CDK4 dual kinase inhibitor for treating acute myeloid leukemia. Mol Cancer Ther. 2014 Apr;13(4):880-9. doi: 10.1158/1535-7163.MCT-13-0858. Epub 2014 Feb 13. PubMed PMID: 24526162.
Gonzalez AZ, Li Z, Beck HP, Canon J, Chen A, Chow D, Duquette J, Eksterowicz J, Fox BM, Fu J, Huang X, Houze J, Jin L, Li Y, Ling Y, Lo MC, Long AM, McGee LR, McIntosh J, Oliner JD, Osgood T, Rew Y, Saiki AY, Shaffer P, Wortman S, Yakowec P, Yan X, Ye Q, Yu D, Zhao X, Zhou J, Olson SH, Sun D, Medina JC. Novel inhibitors of the MDM2-p53 interaction featuring hydrogen bond acceptors as carboxylic acid isosteres. J Med Chem. 2014 Apr 10;57(7):2963-88. doi: 10.1021/jm401911v. Epub 2014 Mar 27. PubMed PMID: 24601644.
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. Improving the Pharmacokinetics of GPR40/FFA1 Full Agonists. ACS Med Chem Lett. 2014 Apr 10;5(4):384-9. doi: 10.1021/ml4005123. eCollection 2014 Apr 10. PubMed PMID: 24900845; PubMed Central PMCID: PMC4027632.
Li Z, Wang X, Eksterowicz J, Gribble MW Jr, Alba GQ, Ayres M, Carlson TJ, Chen A, Chen X, Cho R, Connors RV, DeGraffenreid M, Deignan JT, Duquette J, Fan P, Fisher B, Fu J, Huard JN, Kaizerman J, Keegan KS, Li C, Li K, Li Y, Liang L, Liu W, Lively SE, Lo MC, Ma J, McMinn DL, Mihalic JT, Modi K, Ngo R, Pattabiraman K, Piper DE, Queva C, Ragains ML, Suchomel J, Thibault S, Walker N, Wang X, Wang Z, Wanska M, Wehn PM, Weidner MF, Zhang AJ, Zhao X, Kamb A, Wickramasinghe D, Dai K, McGee LR, Medina JC. Discovery of AMG 925, a FLT3 and CDK4 dual kinase inhibitor with preferential affinity for the activated state of FLT3. J Med Chem. 2014 Apr 24;57(8):3430-49. doi: 10.1021/jm500118j. Epub 2014 Apr 2. PubMed PMID: 24641103.
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