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Structure Overhaul Affords a Potent Purine PI3Kδ Inhibitor with Improved Tolerability.
Methot JL, Zhou H, Kattar SD, McGowan MA, Wilson K, Garcia Y, Deng Y, Altman M, Fradera X, Lesburg C, Fischmann T, Li C, Alves S, Shah S, Fernandez R, Goldenblatt P, Hill A, Shaffer L, Chen D, Tong V, McLeod RL, Yu H, Bass A, Kemper R, Gatto NT, LaFranco-Scheuch L, Trotter BW, Guzi T, Katz JD. Methot JL, et al. Among authors: bass a. J Med Chem. 2019 May 9;62(9):4370-4382. doi: 10.1021/acs.jmedchem.8b01818. Epub 2019 Apr 22. J Med Chem. 2019. PMID: 30986068
Discovery and optimization of heteroaryl piperazines as potent and selective PI3Kδ inhibitors.
Zhou H, McGowan MA, Lipford K, Christopher M, Fradera X, Witter D, Lesburg CA, Li C, Methot JL, Lampe J, Achab A, Shaffer L, Goldenblatt P, Shah S, Bass A, Schroeder G, Chen D, Zeng H, Augustin MA, Katz JD. Zhou H, et al. Among authors: bass a. Bioorg Med Chem Lett. 2020 Jan 1;30(1):126715. doi: 10.1016/j.bmcl.2019.126715. Epub 2019 Oct 18. Bioorg Med Chem Lett. 2020. PMID: 31757666
Characterizing Pharmacokinetic-Pharmacodynamic Relationships and Efficacy of PI3Kδ Inhibitors in Respiratory Models of TH2 and TH1 Inflammation.
McLeod RL, Gil MA, Chen D, Cabal A, Katz J, Methot J, Woodhouse JD, Dorosh L, Geda P, Mehta K, Cicmil M, Baltus GA, Bass A, Houshyar H, Caniga M, Yu H, Gervais F, Alves S, Shah S. McLeod RL, et al. Among authors: bass a. J Pharmacol Exp Ther. 2019 May;369(2):223-233. doi: 10.1124/jpet.118.252551. Epub 2019 Feb 25. J Pharmacol Exp Ther. 2019. PMID: 30804001
Oxetane Promise Delivered: Discovery of Long-Acting IDO1 Inhibitors Suitable for Q3W Oral or Parenteral Dosing.
Li D, Sloman DL, Achab A, Zhou H, McGowan MA, White C, Gibeau C, Zhang H, Pu Q, Bharathan I, Hopkins B, Liu K, Ferguson H, Fradera X, Lesburg CA, Martinot TA, Qi J, Song ZJ, Yin J, Zhang H, Song L, Wan B, DAddio S, Solban N, Miller JR, Zamlynny B, Bass A, Freeland E, Ykoruk B, Hilliard C, Ferraro J, Zhai J, Knemeyer I, Otte KM, Vincent S, Sciammetta N, Pasternak A, Bennett DJ, Han Y. Li D, et al. Among authors: bass a. J Med Chem. 2022 Apr 28;65(8):6001-6016. doi: 10.1021/acs.jmedchem.1c01670. Epub 2022 Mar 3. J Med Chem. 2022. PMID: 35239336
Overcoming mutagenicity and ion channel activity: optimization of selective spleen tyrosine kinase inhibitors.
Ellis JM, Altman MD, Bass A, Butcher JW, Byford AJ, Donofrio A, Galloway S, Haidle AM, Jewell J, Kelly N, Leccese EK, Lee S, Maddess M, Miller JR, Moy LY, Osimboni E, Otte RD, Reddy MV, Spencer K, Sun B, Vincent SH, Ward GJ, Woo GH, Yang C, Houshyar H, Northrup AB. Ellis JM, et al. Among authors: bass a. J Med Chem. 2015 Feb 26;58(4):1929-39. doi: 10.1021/jm5018169. Epub 2015 Feb 16. J Med Chem. 2015. PMID: 25625541
A Series of Novel, Highly Potent, and Orally Bioavailable Next-Generation Tricyclic Peptide PCSK9 Inhibitors.
Tucker TJ, Embrey MW, Alleyne C, Amin RP, Bass A, Bhatt B, Bianchi E, Branca D, Bueters T, Buist N, Ha SN, Hafey M, He H, Higgins J, Johns DG, Kerekes AD, Koeplinger KA, Kuethe JT, Li N, Murphy B, Orth P, Salowe S, Shahripour A, Tracy R, Wang W, Wu C, Xiong Y, Zokian HJ, Wood HB, Walji A. Tucker TJ, et al. Among authors: bass a. J Med Chem. 2021 Nov 25;64(22):16770-16800. doi: 10.1021/acs.jmedchem.1c01599. Epub 2021 Oct 27. J Med Chem. 2021. PMID: 34704436
Discovery of liver-targeted inhibitors of stearoyl-CoA desaturase (SCD1).
Deng Y, Yang Z, Shipps GW Jr, Lo SM, West R, Hwa J, Zheng S, Farley C, Lachowicz J, van Heek M, Bass AS, Sinha DP, Mahon CR, Cartwright ME. Deng Y, et al. Bioorg Med Chem Lett. 2013 Feb 1;23(3):791-6. doi: 10.1016/j.bmcl.2012.11.075. Epub 2012 Dec 5. Bioorg Med Chem Lett. 2013. PMID: 23265904
Time for a Fully Integrated Nonclinical-Clinical Risk Assessment to Streamline QT Prolongation Liability Determinations: A Pharma Industry Perspective.
Vargas HM, Rolf MG, Wisialowski TA, Achanzar W, Bahinski A, Bass A, Benson CT, Chaudhary KW, Couvreur N, Dota C, Engwall MJ, Michael Foley C, Gallacher D, Greiter-Wilke A, Guillon JM, Guth B, Himmel HM, Hegele-Hartung C, Ito M, Jenkinson S, Chiba K, Lagrutta A, Levesque P, Martel E, Okai Y, Peri R, Pointon A, Qu Y, Teisman A, Traebert M, Yoshinaga T, Gintant GA, Leishman DJ, Valentin JP. Vargas HM, et al. Among authors: bass a. Clin Pharmacol Ther. 2021 Feb;109(2):310-318. doi: 10.1002/cpt.2029. Epub 2020 Sep 24. Clin Pharmacol Ther. 2021. PMID: 32866317 Free PMC article. Review.
Characterization of indoleamine-2,3-dioxygenase 1, tryptophan-2,3-dioxygenase, and Ido1/Tdo2 knockout mice.
Aslamkhan AG, Xu Q, Loughlin A, Vu H, Pacchione S, Bhatt B, Garfinkel I, Styring TG, LaFranco-Scheuch L, Pearson K, Reynolds S, Li N, Zhou H, Miller JR, Solban N, Bass A, Glaab WE. Aslamkhan AG, et al. Among authors: bass a. Toxicol Appl Pharmacol. 2020 Nov 1;406:115216. doi: 10.1016/j.taap.2020.115216. Epub 2020 Aug 29. Toxicol Appl Pharmacol. 2020. PMID: 32871117
1,046 results