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Page 1
Structure-guided design of potent and selective pyrimidylpyrrole inhibitors of extracellular signal-regulated kinase (ERK) using conformational control.
Aronov AM, Tang Q, Martinez-Botella G, Bemis GW, Cao J, Chen G, Ewing NP, Ford PJ, Germann UA, Green J, Hale MR, Jacobs M, Janetka JW, Maltais F, Markland W, Namchuk MN, Nanthakumar S, Poondru S, Straub J, ter Haar E, Xie X. Aronov AM, et al. Among authors: hale mr. J Med Chem. 2009 Oct 22;52(20):6362-8. doi: 10.1021/jm900630q. J Med Chem. 2009. PMID: 19827834
Flipped out: structure-guided design of selective pyrazolylpyrrole ERK inhibitors.
Aronov AM, Baker C, Bemis GW, Cao J, Chen G, Ford PJ, Germann UA, Green J, Hale MR, Jacobs M, Janetka JW, Maltais F, Martinez-Botella G, Namchuk MN, Straub J, Tang Q, Xie X. Aronov AM, et al. Among authors: hale mr. J Med Chem. 2007 Mar 22;50(6):1280-7. doi: 10.1021/jm061381f. Epub 2007 Feb 15. J Med Chem. 2007. PMID: 17300186
Negishi cross-coupling enabled synthesis of novel NAD(+)-dependent DNA ligase inhibitors and SAR development.
Murphy-Benenato KE, Gingipalli L, Boriack-Sjodin PA, Martinez-Botella G, Carcanague D, Eyermann CJ, Gowravaram M, Harang J, Hale MR, Ioannidis G, Jahic H, Johnstone M, Kutschke A, Laganas VA, Loch JT 3rd, Miller MD, Oguto H, Patel SJ. Murphy-Benenato KE, et al. Among authors: hale mr. Bioorg Med Chem Lett. 2015 Nov 15;25(22):5172-7. doi: 10.1016/j.bmcl.2015.09.075. Epub 2015 Oct 14. Bioorg Med Chem Lett. 2015. PMID: 26463129
Ultra-potent P1 modified arylsulfonamide HIV protease inhibitors: the discovery of GW0385.
Miller JF, Andrews CW, Brieger M, Furfine ES, Hale MR, Hanlon MH, Hazen RJ, Kaldor I, McLean EW, Reynolds D, Sammond DM, Spaltenstein A, Tung R, Turner EM, Xu RX, Sherrill RG. Miller JF, et al. Among authors: hale mr. Bioorg Med Chem Lett. 2006 Apr 1;16(7):1788-94. doi: 10.1016/j.bmcl.2006.01.035. Epub 2006 Feb 3. Bioorg Med Chem Lett. 2006. PMID: 16458505
Exploring the UDP pocket of LpxC through amino acid analogs.
Hale MR, Hill P, Lahiri S, Miller MD, Ross P, Alm R, Gao N, Kutschke A, Johnstone M, Prince B, Thresher J, Yang W. Hale MR, et al. Bioorg Med Chem Lett. 2013 Apr 15;23(8):2362-7. doi: 10.1016/j.bmcl.2013.02.055. Epub 2013 Mar 1. Bioorg Med Chem Lett. 2013. PMID: 23499237
Synthesis, Structure, and SAR of Tetrahydropyran-Based LpxC Inhibitors.
Murphy-Benenato KE, Olivier N, Choy A, Ross PL, Miller MD, Thresher J, Gao N, Hale MR. Murphy-Benenato KE, et al. Among authors: hale mr. ACS Med Chem Lett. 2014 Sep 23;5(11):1213-8. doi: 10.1021/ml500210x. eCollection 2014 Nov 13. ACS Med Chem Lett. 2014. PMID: 25408833 Free PMC article.
Translating slow-binding inhibition kinetics into cellular and in vivo effects.
Walkup GK, You Z, Ross PL, Allen EK, Daryaee F, Hale MR, O'Donnell J, Ehmann DE, Schuck VJ, Buurman ET, Choy AL, Hajec L, Murphy-Benenato K, Marone V, Patey SA, Grosser LA, Johnstone M, Walker SG, Tonge PJ, Fisher SL. Walkup GK, et al. Among authors: hale mr. Nat Chem Biol. 2015 Jun;11(6):416-23. doi: 10.1038/nchembio.1796. Epub 2015 Apr 20. Nat Chem Biol. 2015. PMID: 25894085 Free PMC article.
In vitro antiviral activity of the novel, tyrosyl-based human immunodeficiency virus (HIV) type 1 protease inhibitor brecanavir (GW640385) in combination with other antiretrovirals and against a panel of protease inhibitor-resistant HIV.
Hazen R, Harvey R, Ferris R, Craig C, Yates P, Griffin P, Miller J, Kaldor I, Ray J, Samano V, Furfine E, Spaltenstein A, Hale M, Tung R, St Clair M, Hanlon M, Boone L. Hazen R, et al. Antimicrob Agents Chemother. 2007 Sep;51(9):3147-54. doi: 10.1128/AAC.00401-07. Epub 2007 Jul 9. Antimicrob Agents Chemother. 2007. PMID: 17620375 Free PMC article.
Preclinical pharmacology and pharmacokinetics of GW433908, a water-soluble prodrug of the human immunodeficiency virus protease inhibitor amprenavir.
Furfine ES, Baker CT, Hale MR, Reynolds DJ, Salisbury JA, Searle AD, Studenberg SD, Todd D, Tung RD, Spaltenstein A. Furfine ES, et al. Among authors: hale mr. Antimicrob Agents Chemother. 2004 Mar;48(3):791-8. doi: 10.1128/AAC.48.3.791-798.2004. Antimicrob Agents Chemother. 2004. PMID: 14982766 Free PMC article.
12 results