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Page 1
Discovery of renin inhibitors containing a simple aspartate binding moiety that imparts reduced P450 inhibition.
Lawhorn BG, Tran T, Hong VS, Morgan LA, Le BT, Harpel MR, Jolivette L, Diaz E, Schwartz B, Gross JW, Tomaszek T, Semus S, Concha N, Smallwood A, Holt DA, Kallander LS. Lawhorn BG, et al. Among authors: harpel mr. Bioorg Med Chem Lett. 2017 Nov 1;27(21):4838-4843. doi: 10.1016/j.bmcl.2017.09.046. Epub 2017 Sep 23. Bioorg Med Chem Lett. 2017. PMID: 28985999
Discovery of 1-(1,3,5-triazin-2-yl)piperidine-4-carboxamides as inhibitors of soluble epoxide hydrolase.
Thalji RK, McAtee JJ, Belyanskaya S, Brandt M, Brown GD, Costell MH, Ding Y, Dodson JW, Eisennagel SH, Fries RE, Gross JW, Harpel MR, Holt DA, Israel DI, Jolivette LJ, Krosky D, Li H, Lu Q, Mandichak T, Roethke T, Schnackenberg CG, Schwartz B, Shewchuk LM, Xie W, Behm DJ, Douglas SA, Shaw AL, Marino JP Jr. Thalji RK, et al. Among authors: harpel mr. Bioorg Med Chem Lett. 2013 Jun 15;23(12):3584-8. doi: 10.1016/j.bmcl.2013.04.019. Epub 2013 Apr 16. Bioorg Med Chem Lett. 2013. PMID: 23664879
Discovery of potent, selective sulfonylfuran urea endothelial lipase inhibitors.
Goodman KB, Bury MJ, Cheung M, Cichy-Knight MA, Dowdell SE, Dunn AK, Lee D, Lieby JA, Moore ML, Scherzer DA, Sha D, Suarez DP, Murphy DJ, Harpel MR, Manas ES, McNulty DE, Annan RS, Matico RE, Schwartz BK, Trill JJ, Sweitzer TD, Wang DY, Keller PM, Krawiec JA, Jaye MC. Goodman KB, et al. Among authors: harpel mr. Bioorg Med Chem Lett. 2009 Jan 1;19(1):27-30. doi: 10.1016/j.bmcl.2008.11.033. Epub 2008 Nov 14. Bioorg Med Chem Lett. 2009. PMID: 19058966
In Vivo Half-Life Extension of BMP1/TLL Metalloproteinase Inhibitors Using Small-Molecule Human Serum Albumin Binders.
Vantourout JC, Mason AM, Yuen J, Simpson GL, Evindar G, Kuai L, Hobbs M, Edgar E, Needle S, Bai X, Wilson S, Scott-Stevens P, Traylen W, Lambert K, Young N, Bunally S, Summerfield SG, Snell R, Lad R, Shi E, Skinner S, Shewchuk L, Watson AJB, Chung CW, Pal S, Holt DA, Kallander LS, Prendergast J, Rivera K, Washburn DG, Harpel MR, Arico-Muendel C, Isidro-Llobet A. Vantourout JC, et al. Among authors: harpel mr. Bioconjug Chem. 2021 Feb 17;32(2):279-289. doi: 10.1021/acs.bioconjchem.0c00662. Epub 2021 Feb 1. Bioconjug Chem. 2021. PMID: 33523652
Targeting enzyme inhibitors in drug discovery.
Copeland RA, Harpel MR, Tummino PJ. Copeland RA, et al. Among authors: harpel mr. Expert Opin Ther Targets. 2007 Jul;11(7):967-78. doi: 10.1517/14728222.11.7.967. Expert Opin Ther Targets. 2007. PMID: 17614764
Nonbenzamidine acylsulfonamide tissue factor-factor VIIa inhibitors.
Glunz PW, Zhang X, Zou Y, Delucca I, Nirschl AH, Cheng X, Weigelt CA, Cheney DL, Wei A, Anumula R, Luettgen JM, Rendina AR, Harpel M, Luo G, Knabb R, Wong PC, Wexler RR, Priestley ES. Glunz PW, et al. Bioorg Med Chem Lett. 2013 Sep 15;23(18):5244-8. doi: 10.1016/j.bmcl.2013.06.027. Epub 2013 Jun 21. Bioorg Med Chem Lett. 2013. PMID: 23845220
A high-throughput screen for endothelial lipase using HDL as substrate.
Keller PM, Rust T, Murphy DJ, Matico R, Trill JJ, Krawiec JA, Jurewicz A, Jaye M, Harpel M, Thrall S, Schwartz B. Keller PM, et al. J Biomol Screen. 2008 Jul;13(6):468-75. doi: 10.1177/1087057108319738. Epub 2008 Jun 19. J Biomol Screen. 2008. PMID: 18566479
Glutamyl-gamma-boronate inhibitors of bacterial Glu-tRNA(Gln) amidotransferase.
Decicco CP, Nelson DJ, Luo Y, Shen L, Horiuchi KY, Amsler KM, Foster LA, Spitz SM, Merrill JJ, Sizemore CF, Rogers KC, Copeland RA, Harpel MR. Decicco CP, et al. Among authors: harpel mr. Bioorg Med Chem Lett. 2001 Sep 17;11(18):2561-4. doi: 10.1016/s0960-894x(01)00499-1. Bioorg Med Chem Lett. 2001. PMID: 11549469
Tetrahydroquinoline derivatives as potent and selective factor XIa inhibitors.
Quan ML, Wong PC, Wang C, Woerner F, Smallheer JM, Barbera FA, Bozarth JM, Brown RL, Harpel MR, Luettgen JM, Morin PE, Peterson T, Ramamurthy V, Rendina AR, Rossi KA, Watson CA, Wei A, Zhang G, Seiffert D, Wexler RR. Quan ML, et al. Among authors: harpel mr. J Med Chem. 2014 Feb 13;57(3):955-69. doi: 10.1021/jm401670x. Epub 2014 Jan 17. J Med Chem. 2014. PMID: 24405333
40 results