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Page 1
Dual Exosite-binding Inhibitors of Insulin-degrading Enzyme Challenge Its Role as the Primary Mediator of Insulin Clearance in Vivo.
Durham TB, Toth JL, Klimkowski VJ, Cao JX, Siesky AM, Alexander-Chacko J, Wu GY, Dixon JT, McGee JE, Wang Y, Guo SY, Cavitt RN, Schindler J, Thibodeaux SJ, Calvert NA, Coghlan MJ, Sindelar DK, Christe M, Kiselyov VV, Michael MD, Sloop KW. Durham TB, et al. Among authors: klimkowski vj. J Biol Chem. 2015 Aug 14;290(33):20044-59. doi: 10.1074/jbc.M115.638205. Epub 2015 Jun 17. J Biol Chem. 2015. PMID: 26085101 Free PMC article.
Identification of potent and selective hydantoin inhibitors of aggrecanase-1 and aggrecanase-2 that are efficacious in both chemical and surgical models of osteoarthritis.
Durham TB, Klimkowski VJ, Rito CJ, Marimuthu J, Toth JL, Liu C, Durbin JD, Stout SL, Adams L, Swearingen C, Lin C, Chambers MG, Thirunavukkarasu K, Wiley MR. Durham TB, et al. Among authors: klimkowski vj. J Med Chem. 2014 Dec 26;57(24):10476-85. doi: 10.1021/jm501522n. Epub 2014 Dec 5. J Med Chem. 2014. PMID: 25415648
Novel lipoglycopeptides as inhibitors of bacterial signal peptidase I.
Kulanthaivel P, Kreuzman AJ, Strege MA, Belvo MD, Smitka TA, Clemens M, Swartling JR, Minton KL, Zheng F, Angleton EL, Mullen D, Jungheim LN, Klimkowski VJ, Nicas TI, Thompson RC, Peng SB. Kulanthaivel P, et al. Among authors: klimkowski vj. J Biol Chem. 2004 Aug 27;279(35):36250-8. doi: 10.1074/jbc.M405884200. Epub 2004 Jun 1. J Biol Chem. 2004. PMID: 15173160 Free article.
1,2-Dibenzamidobenzene inhibitors of human factor Xa.
Herron DK, Goodson T Jr, Wiley MR, Weir LC, Kyle JA, Yee YK, Tebbe AL, Tinsley JM, Mendel D, Masters JJ, Franciskovich JB, Sawyer JS, Beight DW, Ratz AM, Milot G, Hall SE, Klimkowski VJ, Wikel JH, Eastwood BJ, Towner RD, Gifford-Moore DS, Craft TJ, Smith GF. Herron DK, et al. Among authors: klimkowski vj. J Med Chem. 2000 Mar 9;43(5):859-72. doi: 10.1021/jm990326m. J Med Chem. 2000. PMID: 10715153
Structure-based design of potent, amidine-derived inhibitors of factor Xa: evaluation of selectivity, anticoagulant activity, and antithrombotic activity.
Wiley MR, Weir LC, Briggs S, Bryan NA, Buben J, Campbell C, Chirgadze NY, Conrad RC, Craft TJ, Ficorilli JV, Franciskovich JB, Froelich LL, Gifford-Moore DS, Goodson T Jr, Herron DK, Klimkowski VJ, Kurz KD, Kyle JA, Masters JJ, Ratz AM, Milot G, Shuman RT, Smith T, Smith GF, Tebbe AL, Tinsley JM. Wiley MR, et al. Among authors: klimkowski vj. J Med Chem. 2000 Mar 9;43(5):883-99. doi: 10.1021/jm9903287. J Med Chem. 2000. PMID: 10715155
Dibasic benzo[b]thiophene derivatives as a novel class of active site directed thrombin inhibitors: 2. Sidechain optimization and demonstration of in vivo efficacy.
Zhang M, Bailey DL, Bastian JA, Briggs SL, Chirgadze NY, Clawson DK, Denney ML, Gifford-Moore DS, Harper RW, Johnson LM, Klimkowski VJ, Kohn TJ, Lin HS, McCowan JR, Richett ME, Sall DJ, Smith AJ, Smith GF, Snyder DW, Takeuchi K, Utterback BG, Yan SC. Zhang M, et al. Among authors: klimkowski vj. Bioorg Med Chem Lett. 1999 Mar 8;9(5):775-80. doi: 10.1016/s0960-894x(99)00074-8. Bioorg Med Chem Lett. 1999. PMID: 10201846
Investigation of the terminal P4 domain in a series of D-phenylglycinamide-based factor Xa inhibitors.
Franciskovich JB, Masters JJ, Weber WW, Klimkowski VJ, Chouinard M, Sipes PR, Johnson LM, Snyder DW, Chastain MK, Craft TJ, Towner RD, Gifford-Moore DS, Froelich LL, Smallwood JK, Foster RS, Smith GF, Liebeschuetz JW, Murray CW, Young SC. Franciskovich JB, et al. Among authors: klimkowski vj. Bioorg Med Chem Lett. 2007 Dec 15;17(24):6910-3. doi: 10.1016/j.bmcl.2007.09.105. Epub 2007 Oct 24. Bioorg Med Chem Lett. 2007. PMID: 17976987
N(2)-Aroylanthranilamide inhibitors of human factor Xa.
Yee YK, Tebbe AL, Linebarger JH, Beight DW, Craft TJ, Gifford-Moore D, Goodson T Jr, Herron DK, Klimkowski VJ, Kyle JA, Sawyer JS, Smith GF, Tinsley JM, Towner RD, Weir L, Wiley MR. Yee YK, et al. Among authors: klimkowski vj. J Med Chem. 2000 Mar 9;43(5):873-82. doi: 10.1021/jm990327e. J Med Chem. 2000. PMID: 10715154
Dibasic benzo[b]thiophene derivatives as a novel class of active site-directed thrombin inhibitors. 1. Determination of the serine protease selectivity, structure-activity relationships, and binding orientation.
Sall DJ, Bastian JA, Briggs SL, Buben JA, Chirgadze NY, Clawson DK, Denney ML, Giera DD, Gifford-Moore DS, Harper RW, Hauser KL, Klimkowski VJ, Kohn TJ, Lin HS, McCowan JR, Palkowitz AD, Smith GF, Takeuchi K, Thrasher KJ, Tinsley JM, Utterback BG, Yan SC, Zhang M. Sall DJ, et al. Among authors: klimkowski vj. J Med Chem. 1997 Oct 24;40(22):3489-93. doi: 10.1021/jm9704107. J Med Chem. 1997. PMID: 9357512 No abstract available.
D-phenylglycinol-derived non-covalent factor Xa inhibitors: effect of non-peptidic S4 linkage elements on affinity and anticoagulant activity.
Klimkowski VJ, Watson BM, Wiley MR, Liebeschuetz J, Franciskovich JB, Marimuthu J, Bastian JA, Sall DJ, Smallwood JK, Chirgadze NY, Smith GF, Foster RS, Craft T, Sipes P, Chastain M, Sheehan SM. Klimkowski VJ, et al. Bioorg Med Chem Lett. 2007 Nov 1;17(21):5801-5. doi: 10.1016/j.bmcl.2007.08.051. Epub 2007 Aug 28. Bioorg Med Chem Lett. 2007. PMID: 17881231
30 results