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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
What would you like to do?