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Page 1
Crystal structure of a soluble form of human monoglyceride lipase in complex with an inhibitor at 1.35 Å resolution.
Schalk-Hihi C, Schubert C, Alexander R, Bayoumy S, Clemente JC, Deckman I, DesJarlais RL, Dzordzorme KC, Flores CM, Grasberger B, Kranz JK, Lewandowski F, Liu L, Ma H, Maguire D, Macielag MJ, McDonnell ME, Mezzasalma Haarlander T, Miller R, Milligan C, Reynolds C, Kuo LC. Schalk-Hihi C, et al. Among authors: kuo lc. Protein Sci. 2011 Apr;20(4):670-83. doi: 10.1002/pro.596. Epub 2011 Mar 1. Protein Sci. 2011. PMID: 21308848 Free PMC article.
Discovery of a highly selective chemical inhibitor of matrix metalloproteinase-9 (MMP-9) that allosterically inhibits zymogen activation.
Scannevin RH, Alexander R, Haarlander TM, Burke SL, Singer M, Huo C, Zhang YM, Maguire D, Spurlino J, Deckman I, Carroll KI, Lewandowski F, Devine E, Dzordzorme K, Tounge B, Milligan C, Bayoumy S, Williams R, Schalk-Hihi C, Leonard K, Jackson P, Todd M, Kuo LC, Rhodes KJ. Scannevin RH, et al. Among authors: kuo lc. J Biol Chem. 2017 Oct 27;292(43):17963-17974. doi: 10.1074/jbc.M117.806075. Epub 2017 Aug 31. J Biol Chem. 2017. PMID: 28860188 Free PMC article.
Kinesin spindle protein (KSP) inhibitors. Part 3: synthesis and evaluation of phenolic 2,4-diaryl-2,5-dihydropyrroles with reduced hERG binding and employment of a phosphate prodrug strategy for aqueous solubility.
Garbaccio RM, Fraley ME, Tasber ES, Olson CM, Hoffman WF, Arrington KL, Torrent M, Buser CA, Walsh ES, Hamilton K, Schaber MD, Fernandes C, Lobell RB, Tao W, South VJ, Yan Y, Kuo LC, Prueksaritanont T, Slaughter DE, Shu C, Heimbrook DC, Kohl NE, Huber HE, Hartman GD. Garbaccio RM, et al. Among authors: kuo lc. Bioorg Med Chem Lett. 2006 Apr 1;16(7):1780-3. doi: 10.1016/j.bmcl.2005.12.094. Epub 2006 Jan 24. Bioorg Med Chem Lett. 2006. PMID: 16439122
Synthesis and evaluation of substituted benzoisoquinolinones as potent inhibitors of Chk1 kinase.
Garbaccio RM, Huang S, Tasber ES, Fraley ME, Yan Y, Munshi S, Ikuta M, Kuo L, Kreatsoulas C, Stirdivant S, Drakas B, Rickert K, Walsh ES, Hamilton KA, Buser CA, Hardwick J, Mao X, Beck SC, Abrams MT, Tao W, Lobell R, Sepp-Lorenzino L, Hartman GD. Garbaccio RM, et al. Bioorg Med Chem Lett. 2007 Nov 15;17(22):6280-5. doi: 10.1016/j.bmcl.2007.09.007. Epub 2007 Sep 7. Bioorg Med Chem Lett. 2007. PMID: 17900896
SAR of tertiary carbinamine derived BACE1 inhibitors: role of aspartate ligand amine pKa in enzyme inhibition.
Rajapakse HA, Nantermet PG, Selnick HG, Barrow JC, McGaughey GB, Munshi S, Lindsley SR, Young MB, Ngo PL, Holloway MK, Lai MT, Espeseth AS, Shi XP, Colussi D, Pietrak B, Crouthamel MC, Tugusheva K, Huang Q, Xu M, Simon AJ, Kuo L, Hazuda DJ, Graham S, Vacca JP. Rajapakse HA, et al. Bioorg Med Chem Lett. 2010 Mar 15;20(6):1885-9. doi: 10.1016/j.bmcl.2010.01.137. Epub 2010 Feb 4. Bioorg Med Chem Lett. 2010. PMID: 20176482
369 results