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Page 1
Points to consider regarding the use and implementation of virtual controls in nonclinical general toxicology studies.
Palazzi X, Anger LT, Boulineau T, Grevot A, Guffroy M, Henson K, Hoepp N, Jacobsen M, Kale VP, Kreeger J, Lane JH, Li D, Muster W, Paisley B, Ramaiah L, Robertson N, Shultz V, Steger Hartmann T, Westhouse R. Palazzi X, et al. Among authors: westhouse r. Regul Toxicol Pharmacol. 2024 Apr 27;150:105632. doi: 10.1016/j.yrtph.2024.105632. Online ahead of print. Regul Toxicol Pharmacol. 2024. PMID: 38679316
Cytochrome P450 11A1 bioactivation of a kinase inhibitor in rats: use of radioprofiling, modulation of metabolism, and adrenocortical cell lines to evaluate adrenal toxicity.
Zhang D, Flint O, Wang L, Gupta A, Westhouse RA, Zhao W, Raghavan N, Caceres-Cortes J, Marathe P, Shen G, Zhang Y, Allentoff A, Josephs J, Gan J, Borzilleri R, Humphreys WG. Zhang D, et al. Among authors: westhouse ra. Chem Res Toxicol. 2012 Mar 19;25(3):556-71. doi: 10.1021/tx200524d. Epub 2012 Mar 2. Chem Res Toxicol. 2012. PMID: 22295996
Discovery and Preclinical Pharmacology of an Oral Bromodomain and Extra-Terminal (BET) Inhibitor Using Scaffold-Hopping and Structure-Guided Drug Design.
Gavai AV, Norris D, Delucca G, Tortolani D, Tokarski JS, Dodd D, O'Malley D, Zhao Y, Quesnelle C, Gill P, Vaccaro W, Huynh T, Ahuja V, Han WC, Mussari C, Harikrishnan L, Kamau M, Poss M, Sheriff S, Yan C, Marsilio F, Menard K, Wen ML, Rampulla R, Wu DR, Li J, Zhang H, Li P, Sun D, Yip H, Traeger SC, Zhang Y, Mathur A, Zhang H, Huang C, Yang Z, Ranasinghe A, Everlof G, Raghavan N, Tye CK, Wee S, Hunt JT, Vite G, Westhouse R, Lee FY. Gavai AV, et al. Among authors: westhouse r. J Med Chem. 2021 Oct 14;64(19):14247-14265. doi: 10.1021/acs.jmedchem.1c00625. Epub 2021 Sep 20. J Med Chem. 2021. PMID: 34543572
Discovery of Branebrutinib (BMS-986195): A Strategy for Identifying a Highly Potent and Selective Covalent Inhibitor Providing Rapid in Vivo Inactivation of Bruton's Tyrosine Kinase (BTK).
Watterson SH, Liu Q, Beaudoin Bertrand M, Batt DG, Li L, Pattoli MA, Skala S, Cheng L, Obermeier MT, Moore R, Yang Z, Vickery R, Elzinga PA, Discenza L, D'Arienzo C, Gillooly KM, Taylor TL, Pulicicchio C, Zhang Y, Heimrich E, McIntyre KW, Ruan Q, Westhouse RA, Catlett IM, Zheng N, Chaudhry C, Dai J, Galella MA, Tebben AJ, Pokross M, Li J, Zhao R, Smith D, Rampulla R, Allentoff A, Wallace MA, Mathur A, Salter-Cid L, Macor JE, Carter PH, Fura A, Burke JR, Tino JA. Watterson SH, et al. Among authors: westhouse ra. J Med Chem. 2019 Apr 11;62(7):3228-3250. doi: 10.1021/acs.jmedchem.9b00167. Epub 2019 Mar 29. J Med Chem. 2019. PMID: 30893553
Development of BET Inhibitors as Potential Treatments for Cancer: Optimization of Pharmacokinetic Properties.
Hill MD, Fang H, Norris D, Delucca GV, Huang H, DeBenedetto M, Quesnelle C, Schmitz WD, Tokarski JS, Sheriff S, Yan C, Fanslau C, Haarhoff Z, Huang C, Kramer M, Madari S, Menard K, Monereau L, Morrison J, Raghavan N, Shields EE, Simmermacher-Mayer J, Sinz M, Tye CK, Westhouse R, Xie C, Zhang H, Zhang L, Zvyaga T, Lee F, Gavai AV, Degnan AP. Hill MD, et al. Among authors: westhouse r. ACS Med Chem Lett. 2022 Jul 5;13(7):1165-1171. doi: 10.1021/acsmedchemlett.2c00219. eCollection 2022 Jul 14. ACS Med Chem Lett. 2022. PMID: 35859878 Free PMC article.
Development of BET inhibitors as potential treatments for cancer: A search for structural diversity.
Hill MD, Fang H, Tokarski J, Fanslau C, Haarhoff Z, Huang C, Kramer M, Menard K, Monereau L, Morrison J, Ranasinghe A, Shields EE, Tye CK, Westhouse R, Everlof G, Sheriff S, Yan C, Marsilio F, Zhang L, Zvyaga T, Lee F, Gavai AV, Degnan AP. Hill MD, et al. Among authors: westhouse r. Bioorg Med Chem Lett. 2021 Jul 15;44:128108. doi: 10.1016/j.bmcl.2021.128108. Epub 2021 May 13. Bioorg Med Chem Lett. 2021. PMID: 33991625
Development of BET inhibitors as potential treatments for cancer: A new carboline chemotype.
Hill MD, Quesnelle C, Tokarski J, Fang H, Fanslau C, Haarhoff Z, Kramer M, Madari S, Wiebesiek A, Morrison J, Simmermacher-Mayer J, Sinz M, Westhouse R, Xie C, Zhao J, Huang L, Sheriff S, Yan C, Marsilio F, Everlof G, Zvyaga T, Lee F, Gavai AV, Degnan AP. Hill MD, et al. Among authors: westhouse r. Bioorg Med Chem Lett. 2021 Nov 1;51:128376. doi: 10.1016/j.bmcl.2021.128376. Epub 2021 Sep 21. Bioorg Med Chem Lett. 2021. PMID: 34560263
Tumor development by transgenic expression of a constitutively active insulin-like growth factor I receptor.
Carboni JM, Lee AV, Hadsell DL, Rowley BR, Lee FY, Bol DK, Camuso AE, Gottardis M, Greer AF, Ho CP, Hurlburt W, Li A, Saulnier M, Velaparthi U, Wang C, Wen ML, Westhouse RA, Wittman M, Zimmermann K, Rupnow BA, Wong TW. Carboni JM, et al. Among authors: westhouse ra. Cancer Res. 2005 May 1;65(9):3781-7. doi: 10.1158/0008-5472.CAN-04-4602. Cancer Res. 2005. PMID: 15867374
17 results