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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
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
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.
Utilization of Metabolite Identification and Structural Data to Guide Design of Low-Dose IDO1 Inhibitors.
Hopkins B, Zhang H, Bharathan I, Li D, Pu Q, Zhou H, Martinot TA, Fradera X, Lammens A, Lesburg CA, Cohen RD, Ballard J, Knemeyer I, Otte K, Vincent S, Miller JR, Solban N, Cheng M, Geda P, Smotrov N, Song X, Bennett DJ, Han Y. Hopkins B, et al. Among authors: knemeyer i. ACS Med Chem Lett. 2021 Aug 18;12(9):1435-1440. doi: 10.1021/acsmedchemlett.1c00265. eCollection 2021 Sep 9. ACS Med Chem Lett. 2021. PMID: 34531952 Free PMC article.
Rapid Affinity and Microsomal Stability Ranking of Crude Mixture Libraries of Histone Deacetylase Inhibitors.
Tyagarajan S, Andrews CL, Beshore DC, Buevich AV, Curran PJ, Dandliker P, Greshock TJ, Hoar J, Kim A, Karnachi P, Knemeyer I, Kozlowski J, Liu J, Maletic M, Myers R, Rada V, Sha D, Sauvagnat B, Vachal P, Wolkenberg S, Yu W, Yu Y, Krska SW. Tyagarajan S, et al. Among authors: knemeyer i. ACS Med Chem Lett. 2024 Sep 12;15(10):1787-1794. doi: 10.1021/acsmedchemlett.4c00345. eCollection 2024 Oct 10. ACS Med Chem Lett. 2024. PMID: 39411537
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 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
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
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.
26 results