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31 results

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Page 1
Discovery and optimization of imidazo[1,2-a]pyridine inhibitors of insulin-like growth factor-1 receptor (IGF-1R).
Emmitte KA, Wilson BJ, Baum EW, Emerson HK, Kuntz KW, Nailor KE, Salovich JM, Smith SC, Cheung M, Gerding RM, Stevens KL, Uehling DE, Mook RA Jr, Moorthy GS, Dickerson SH, Hassell AM, Leesnitzer MA, Shewchuk LM, Groy A, Rowand JL, Anderson K, Atkins CL, Yang J, Sabbatini P, Kumar R. Emmitte KA, et al. Among authors: kuntz kw. Bioorg Med Chem Lett. 2009 Feb 1;19(3):1004-8. doi: 10.1016/j.bmcl.2008.11.058. Epub 2008 Nov 20. Bioorg Med Chem Lett. 2009. PMID: 19101143
Discovery of thiophene inhibitors of polo-like kinase.
Emmitte KA, Andrews CW, Badiang JG, Davis-Ward RG, Dickson HD, Drewry DH, Emerson HK, Epperly AH, Hassler DF, Knick VB, Kuntz KW, Lansing TJ, Linn JA, Mook RA Jr, Nailor KE, Salovich JM, Spehar GM, Cheung M. Emmitte KA, et al. Among authors: kuntz kw. Bioorg Med Chem Lett. 2009 Feb 1;19(3):1018-21. doi: 10.1016/j.bmcl.2008.11.041. Epub 2008 Nov 18. Bioorg Med Chem Lett. 2009. PMID: 19097784
Design of potent thiophene inhibitors of polo-like kinase 1 with improved solubility and reduced protein binding.
Emmitte KA, Adjabeng GM, Andrews CW, Alberti JG, Bambal R, Chamberlain SD, Davis-Ward RG, Dickson HD, Hassler DF, Hornberger KR, Jackson JR, Kuntz KW, Lansing TJ, Mook RA Jr, Nailor KE, Pobanz MA, Smith SC, Sung CM, Cheung M. Emmitte KA, et al. Among authors: kuntz kw. Bioorg Med Chem Lett. 2009 Mar 15;19(6):1694-7. doi: 10.1016/j.bmcl.2009.01.094. Epub 2009 Jan 31. Bioorg Med Chem Lett. 2009. PMID: 19237286
Imidazo[5,1-f][1,2,4]triazin-2-amines as novel inhibitors of polo-like kinase 1.
Cheung M, Kuntz KW, Pobanz M, Salovich JM, Wilson BJ, Andrews CW 3rd, Shewchuk LM, Epperly AH, Hassler DF, Leesnitzer MA, Smith JL, Smith GK, Lansing TJ, Mook RA Jr. Cheung M, et al. Among authors: kuntz kw. Bioorg Med Chem Lett. 2008 Dec 1;18(23):6214-7. doi: 10.1016/j.bmcl.2008.09.100. Epub 2008 Oct 2. Bioorg Med Chem Lett. 2008. PMID: 18929484
Discovery of an inhibitor of insulin-like growth factor 1 receptor activation: implications for cellular potency and selectivity over insulin receptor.
Wood ER, Shewchuk L, Hassel A, Nichols J, Truesdale AT, Smith D, Carter HL, Weaver K, Barrett G, Leesnitzer T, Alvarez E, Bardera AI, Alamillo A, Cantizani J, Martin J, Smith GK, Jensen DE, Xie H, Mook R, Kumar R, Kuntz K. Wood ER, et al. Biochem Pharmacol. 2009 Dec 15;78(12):1438-47. doi: 10.1016/j.bcp.2009.07.022. Epub 2009 Aug 7. Biochem Pharmacol. 2009. PMID: 19665448
EPZ011989, A Potent, Orally-Available EZH2 Inhibitor with Robust in Vivo Activity.
Campbell JE, Kuntz KW, Knutson SK, Warholic NM, Keilhack H, Wigle TJ, Raimondi A, Klaus CR, Rioux N, Yokoi A, Kawano S, Minoshima Y, Choi HW, Porter Scott M, Waters NJ, Smith JJ, Chesworth R, Moyer MP, Copeland RA. Campbell JE, et al. Among authors: kuntz kw. ACS Med Chem Lett. 2015 Mar 4;6(5):491-5. doi: 10.1021/acsmedchemlett.5b00037. eCollection 2015 May 14. ACS Med Chem Lett. 2015. PMID: 26005520 Free PMC article.
Novel Oxindole Sulfonamides and Sulfamides: EPZ031686, the First Orally Bioavailable Small Molecule SMYD3 Inhibitor.
Mitchell LH, Boriack-Sjodin PA, Smith S, Thomenius M, Rioux N, Munchhof M, Mills JE, Klaus C, Totman J, Riera TV, Raimondi A, Jacques SL, West K, Foley M, Waters NJ, Kuntz KW, Wigle TJ, Scott MP, Copeland RA, Smith JJ, Chesworth R. Mitchell LH, et al. Among authors: kuntz kw. ACS Med Chem Lett. 2015 Aug 27;7(2):134-8. doi: 10.1021/acsmedchemlett.5b00272. eCollection 2016 Feb 11. ACS Med Chem Lett. 2015. PMID: 26985287 Free PMC article.
Forced Self-Modification Assays as a Strategy to Screen MonoPARP Enzymes.
Wigle TJ, Church WD, Majer CR, Swinger KK, Aybar D, Schenkel LB, Vasbinder MM, Brendes A, Beck C, Prahm M, Wegener D, Chang P, Kuntz KW. Wigle TJ, et al. Among authors: kuntz kw. SLAS Discov. 2020 Mar;25(3):241-252. doi: 10.1177/2472555219883623. Epub 2019 Dec 19. SLAS Discov. 2020. PMID: 31855104 Free PMC article.
Selective inhibition of EZH2 by EPZ-6438 leads to potent antitumor activity in EZH2-mutant non-Hodgkin lymphoma.
Knutson SK, Kawano S, Minoshima Y, Warholic NM, Huang KC, Xiao Y, Kadowaki T, Uesugi M, Kuznetsov G, Kumar N, Wigle TJ, Klaus CR, Allain CJ, Raimondi A, Waters NJ, Smith JJ, Porter-Scott M, Chesworth R, Moyer MP, Copeland RA, Richon VM, Uenaka T, Pollock RM, Kuntz KW, Yokoi A, Keilhack H. Knutson SK, et al. Among authors: kuntz kw. Mol Cancer Ther. 2014 Apr;13(4):842-54. doi: 10.1158/1535-7163.MCT-13-0773. Epub 2014 Feb 21. Mol Cancer Ther. 2014. PMID: 24563539
31 results