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Items: 13

1.

A small-molecule inhibitor of sarcomere contractility suppresses hypertrophic cardiomyopathy in mice.

Green EM, Wakimoto H, Anderson RL, Evanchik MJ, Gorham JM, Harrison BC, Henze M, Kawas R, Oslob JD, Rodriguez HM, Song Y, Wan W, Leinwand LA, Spudich JA, McDowell RS, Seidman JG, Seidman CE.

Science. 2016 Feb 5;351(6273):617-21. doi: 10.1126/science.aad3456.

2.

Imidazopyridine-Based Fatty Acid Synthase Inhibitors That Show Anti-HCV Activity and in Vivo Target Modulation.

Oslob JD, Johnson RJ, Cai H, Feng SQ, Hu L, Kosaka Y, Lai J, Sivaraja M, Tep S, Yang H, Zaharia CA, Evanchik MJ, McDowell RS.

ACS Med Chem Lett. 2012 Dec 2;4(1):113-7. doi: 10.1021/ml300335r. eCollection 2013 Jan 10.

3.

Discovery and Development of Potent LFA-1/ICAM-1 Antagonist SAR 1118 as an Ophthalmic Solution for Treating Dry Eye.

Zhong M, Gadek TR, Bui M, Shen W, Burnier J, Barr KJ, Hanan EJ, Oslob JD, Yu CH, Zhu J, Arkin MR, Evanchik MJ, Flanagan WM, Hoch U, Hyde J, Prabhu S, Silverman JA, Wright J.

ACS Med Chem Lett. 2012 Jan 31;3(3):203-6. doi: 10.1021/ml2002482. eCollection 2012 Mar 8.

4.

Structure-activity relationship (SAR) of the α-amino acid residue of potent tetrahydroisoquinoline (THIQ)-derived LFA-1/ICAM-1 antagonists.

Zhong M, Hanan EJ, Shen W, Bui M, Arkin MR, Barr KJ, Evanchik MJ, Hoch U, Hyde J, Martell JR, Oslob JD, Paulvannan K, Prabhu S, Silverman JA, Wright J, Yu CH, Zhu J, Flanagan WM.

Bioorg Med Chem Lett. 2011 Jan 1;21(1):307-10. doi: 10.1016/j.bmcl.2010.11.014. Epub 2010 Nov 5.

PMID:
21109434
5.

Discovery of tetrahydroisoquinoline (THIQ) derivatives as potent and orally bioavailable LFA-1/ICAM-1 antagonists.

Zhong M, Shen W, Barr KJ, Arbitrario JP, Arkin MR, Bui M, Chen T, Cunningham BC, Evanchik MJ, Hanan EJ, Hoch U, Huen K, Hyde J, Kumer JL, Lac T, Lawrence CE, Martell JR, Oslob JD, Paulvannan K, Prabhu S, Silverman JA, Wright J, Yu CH, Zhu J, Flanagan WM.

Bioorg Med Chem Lett. 2010 Sep 1;20(17):5269-73. doi: 10.1016/j.bmcl.2010.06.145. Epub 2010 Jul 23.

PMID:
20655213
6.

2-Aminobenzimidazoles as potent Aurora kinase inhibitors.

Zhong M, Bui M, Shen W, Baskaran S, Allen DA, Elling RA, Flanagan WM, Fung AD, Hanan EJ, Harris SO, Heumann SA, Hoch U, Ivy SN, Jacobs JW, Lam S, Lee H, McDowell RS, Oslob JD, Purkey HE, Romanowski MJ, Silverman JA, Tangonan BT, Taverna P, Yang W, Yoburn JC, Yu CH, Zimmerman KM, O'Brien T, Lew W.

Bioorg Med Chem Lett. 2009 Sep 1;19(17):5158-61. doi: 10.1016/j.bmcl.2009.07.016. Epub 2009 Jul 9.

PMID:
19646866
7.

Water-soluble prodrugs of an Aurora kinase inhibitor.

Oslob JD, Heumann SA, Yu CH, Allen DA, Baskaran S, Bui M, Delarosa E, Fung AD, Hashash A, Hau J, Ivy S, Jacobs JW, Lew W, Maung J, McDowell RS, Ritchie S, Romanowski MJ, Silverman JA, Yang W, Zhong M, Fuchs-Knotts T.

Bioorg Med Chem Lett. 2009 Mar 1;19(5):1409-12. doi: 10.1016/j.bmcl.2009.01.043. Epub 2009 Jan 19.

PMID:
19186057
8.

Discovery of a potent and selective aurora kinase inhibitor.

Oslob JD, Romanowski MJ, Allen DA, Baskaran S, Bui M, Elling RA, Flanagan WM, Fung AD, Hanan EJ, Harris S, Heumann SA, Hoch U, Jacobs JW, Lam J, Lawrence CE, McDowell RS, Nannini MA, Shen W, Silverman JA, Sopko MM, Tangonan BT, Teague J, Yoburn JC, Yu CH, Zhong M, Zimmerman KM, O'Brien T, Lew W.

Bioorg Med Chem Lett. 2008 Sep 1;18(17):4880-4. doi: 10.1016/j.bmcl.2008.07.073. Epub 2008 Jul 24.

PMID:
18678489
9.

Small-molecule inhibition of TNF-alpha.

He MM, Smith AS, Oslob JD, Flanagan WM, Braisted AC, Whitty A, Cancilla MT, Wang J, Lugovskoy AA, Yoburn JC, Fung AD, Farrington G, Eldredge JK, Day ES, Cruz LA, Cachero TG, Miller SK, Friedman JE, Choong IC, Cunningham BC.

Science. 2005 Nov 11;310(5750):1022-5.

10.

Identification of nonpeptidic small-molecule inhibitors of interleukin-2.

Waal ND, Yang W, Oslob JD, Arkin MR, Hyde J, Lu W, McDowell RS, Yu CH, Raimundo BC.

Bioorg Med Chem Lett. 2005 Feb 15;15(4):983-7.

PMID:
15686897
11.

Integrating fragment assembly and biophysical methods in the chemical advancement of small-molecule antagonists of IL-2: an approach for inhibiting protein-protein interactions.

Raimundo BC, Oslob JD, Braisted AC, Hyde J, McDowell RS, Randal M, Waal ND, Wilkinson J, Yu CH, Arkin MR.

J Med Chem. 2004 Jun 3;47(12):3111-30.

PMID:
15163192
12.

Discovery of a potent small molecule IL-2 inhibitor through fragment assembly.

Braisted AC, Oslob JD, Delano WL, Hyde J, McDowell RS, Waal N, Yu C, Arkin MR, Raimundo BC.

J Am Chem Soc. 2003 Apr 2;125(13):3714-5.

PMID:
12656598
13.

Binding of small molecules to an adaptive protein-protein interface.

Arkin MR, Randal M, DeLano WL, Hyde J, Luong TN, Oslob JD, Raphael DR, Taylor L, Wang J, McDowell RS, Wells JA, Braisted AC.

Proc Natl Acad Sci U S A. 2003 Feb 18;100(4):1603-8. Epub 2003 Feb 11.

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