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Page 1
Development and Application of a Transcriptomic Signature of Bioactivation in an Advanced In Vitro Liver Model to Reduce Drug-induced Liver Injury Risk Early in the Pharmaceutical Pipeline.
Kang W, Podtelezhnikov AA, Tanis KQ, Pacchione S, Su M, Bleicher KB, Wang Z, Laws GM, Griffiths TG, Kuhls MC, Chen Q, Knemeyer I, Marsh DJ, Mitra K, Lebron J, Sistare FD. Kang W, et al. Among authors: knemeyer i. Toxicol Sci. 2020 Sep 1;177(1):121-139. doi: 10.1093/toxsci/kfaa094. Toxicol Sci. 2020. PMID: 32559289
Definitive Metabolite Identification Coupled with Automated Ligand Identification System (ALIS) Technology: A Novel Approach to Uncover Structure-Activity Relationships and Guide Drug Design in a Factor IXa Inhibitor Program.
Zhang T, Liu Y, Yang X, Martin GE, Yao H, Shang J, Bugianesi RM, Ellsworth KP, Sonatore LM, Nizner P, Sherer EC, Hill SE, Knemeyer IW, Geissler WM, Dandliker PJ, Helmy R, Wood HB. Zhang T, et al. J Med Chem. 2016 Mar 10;59(5):1818-29. doi: 10.1021/acs.jmedchem.5b01293. Epub 2016 Feb 22. J Med Chem. 2016. PMID: 26871940
Discovery of Spirocyclic Aldosterone Synthase Inhibitors as Potential Treatments for Resistant Hypertension.
Petrilli WL, Hoyt SB, London C, McMasters D, Verras A, Struthers M, Cully D, Wisniewski T, Ren N, Bopp C, Sok A, Chen Q, Li Y, Tung E, Tang W, Salituro G, Knemeyer I, Karanam B, Clemas J, Zhou G, Gibson J, Shipley CA, MacNeil DJ, Duffy R, Tata JR, Ujjainwalla F, Ali A, Xiong Y. Petrilli WL, et al. Among authors: knemeyer i. ACS Med Chem Lett. 2016 Nov 22;8(1):128-132. doi: 10.1021/acsmedchemlett.6b00455. eCollection 2017 Jan 12. ACS Med Chem Lett. 2016. PMID: 28105288 Free PMC article.
siRNA-mediated knockdown of P450 oxidoreductase in rats: a tool to reduce metabolism by CYPs and increase exposure of high clearance compounds.
Burke RS, Somasuntharam I, Rearden P, Brown D, Deshmukh SV, DiPietro MA, DiMuzio J, Eisenhandler R, Fauty SE, Gibson C, Gindy ME, Hamilton KA, Knemeyer I, Koeplinger KA, Kwon HW, Lifsted TQ, Menzel K, Patel M, Pudvah N, Rudd DJ, Seitzer J, Strapps WR, Prueksaritanont T, Thompson CD, Hochman JH, Carr BA. Burke RS, et al. Among authors: knemeyer i. Pharm Res. 2014 Dec;31(12):3445-60. doi: 10.1007/s11095-014-1433-0. Epub 2014 Jul 1. Pharm Res. 2014. PMID: 24980206
SAR towards indoline and 3-azaindoline classes of IDO1 inhibitors.
Yu W, Deng Y, Hopkins B, Huang X, Sloman D, Zhang H, Li D, McGowan MA, White C, Pu Q, Liu K, Fradera X, Lesburg CA, Martinot T, Doty A, Ferguson H, Nickbarg EB, Cheng M, Geda P, Song X, Smotrov N, Abeywickrema P, Andrews C, Chamberlin C, Mabrouk O, Curran P, Richards M, Saradjian P, Miller JR, Knemeyer I, Otte K, Vincent S, Sciammetta N, Bennett DJ, Han Y. Yu W, et al. Among authors: knemeyer i. Bioorg Med Chem Lett. 2021 Sep 1;47:128214. doi: 10.1016/j.bmcl.2021.128214. Epub 2021 Jun 21. Bioorg Med Chem Lett. 2021. PMID: 34166782
An orally available non-nucleotide STING agonist with antitumor activity.
Pan BS, Perera SA, Piesvaux JA, Presland JP, Schroeder GK, Cumming JN, Trotter BW, Altman MD, Buevich AV, Cash B, Cemerski S, Chang W, Chen Y, Dandliker PJ, Feng G, Haidle A, Henderson T, Jewell J, Kariv I, Knemeyer I, Kopinja J, Lacey BM, Laskey J, Lesburg CA, Liang R, Long BJ, Lu M, Ma Y, Minnihan EC, O'Donnell G, Otte R, Price L, Rakhilina L, Sauvagnat B, Sharma S, Tyagarajan S, Woo H, Wyss DF, Xu S, Bennett DJ, Addona GH. Pan BS, et al. Among authors: knemeyer i. Science. 2020 Aug 21;369(6506):eaba6098. doi: 10.1126/science.aba6098. Science. 2020. PMID: 32820094
Discovery of 8-Amino-imidazo[1,5-a]pyrazines as Reversible BTK Inhibitors for the Treatment of Rheumatoid Arthritis.
Liu J, Guiadeen D, Krikorian A, Gao X, Wang J, Boga SB, Alhassan AB, Yu Y, Vaccaro H, Liu S, Yang C, Wu H, Cooper A, de Man J, Kaptein A, Maloney K, Hornak V, Gao YD, Fischmann TO, Raaijmakers H, Vu-Pham D, Presland J, Mansueto M, Xu Z, Leccese E, Zhang-Hoover J, Knemeyer I, Garlisi CG, Bays N, Stivers P, Brandish PE, Hicks A, Kim R, Kozlowski JA. Liu J, et al. Among authors: knemeyer i. ACS Med Chem Lett. 2015 Dec 19;7(2):198-203. doi: 10.1021/acsmedchemlett.5b00463. eCollection 2016 Feb 11. ACS Med Chem Lett. 2015. PMID: 26985298 Free PMC article.
Discovery of Amino-cyclobutarene-derived Indoleamine-2,3-dioxygenase 1 (IDO1) Inhibitors for Cancer Immunotherapy.
Zhang H, Liu K, Pu Q, Achab A, Ardolino MJ, Cheng M, Deng Y, Doty AC, Ferguson H, Fradera X, Knemeyer I, Kurukulasuriya R, Lam YH, Lesburg CA, Martinot TA, McGowan MA, Miller JR, Otte K, Biju PJ, Sciammetta N, Solban N, Yu W, Zhou H, Wang X, Bennett DJ, Han Y. Zhang H, et al. Among authors: knemeyer i. ACS Med Chem Lett. 2019 Sep 18;10(11):1530-1536. doi: 10.1021/acsmedchemlett.9b00344. eCollection 2019 Nov 14. ACS Med Chem Lett. 2019. PMID: 31749906 Free PMC article.
Discovery of MK-1454: A Potent Cyclic Dinucleotide Stimulator of Interferon Genes Agonist for the Treatment of Cancer.
Chang W, Altman MD, Lesburg CA, Perera SA, Piesvaux JA, Schroeder GK, Wyss DF, Cemerski S, Chen Y, DiNunzio E, Haidle AM, Ho T, Kariv I, Knemeyer I, Kopinja JE, Lacey BM, Laskey J, Lim J, Long BJ, Ma Y, Maddess ML, Pan BS, Presland JP, Spooner E, Steinhuebel D, Truong Q, Zhang Z, Fu J, Addona GH, Northrup AB, Parmee E, Tata JR, Bennett DJ, Cumming JN, Siu T, Trotter BW. Chang W, et al. Among authors: knemeyer i. J Med Chem. 2022 Apr 14;65(7):5675-5689. doi: 10.1021/acs.jmedchem.1c02197. Epub 2022 Mar 25. J Med Chem. 2022. PMID: 35332774
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