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Next-generation Bruton's tyrosine kinase inhibitor BIIB091 selectively and potently inhibits B cell and Fc receptor signaling and downstream functions in B cells and myeloid cells.
Bame E, Tang H, Burns JC, Arefayene M, Michelsen K, Ma B, Marx I, Prince R, Roach AM, Poreci U, Donaldson D, Cullen P, Casey F, Zhu J, Carlile TM, Sangurdekar D, Zhang B, Trapa P, Santoro J, Muragan P, Pellerin A, Rubino S, Gianni D, Bajrami B, Peng X, Coppell A, Riester K, Belachew S, Mehta D, Palte M, Hopkins BT, Scaramozza M, Franchimont N, Mingueneau M. Bame E, et al. Among authors: trapa p. Clin Transl Immunology. 2021 Jun 14;10(6):e1295. doi: 10.1002/cti2.1295. eCollection 2021. Clin Transl Immunology. 2021. PMID: 34141433 Free PMC article.
Optimization of dose and route of administration of the P-glycoprotein inhibitor, valspodar (PSC-833) and the P-glycoprotein and breast cancer resistance protein dual-inhibitor, elacridar (GF120918) as dual infusion in rats.
Rowbottom C, Pietrasiewicz A, Tuczewycz T, Grater R, Qiu D, Kapadnis S, Trapa P. Rowbottom C, et al. Among authors: trapa p. Pharmacol Res Perspect. 2021 Apr;9(2):e00740. doi: 10.1002/prp2.740. Pharmacol Res Perspect. 2021. PMID: 33660938 Free PMC article.
Target occupancy study and whole-body dosimetry with a MAGL PET ligand [11C]PF-06809247 in non-human primates.
Arakawa R, Takano A, Nag S, Jia Z, Amini N, Maresca KP, Zhang L, Keliher EJ, Butler CR, Piro JR, Samad TA, Smith D, Nason D, O'Neil S, Trapa P, Fonseca KR, Litchfield J, McCarthy T, Carson RE, Halldin C. Arakawa R, et al. Among authors: trapa p. EJNMMI Res. 2022 Mar 4;12(1):13. doi: 10.1186/s13550-022-00882-2. EJNMMI Res. 2022. PMID: 35244788 Free PMC article.
Translational pharmacokinetic-pharmacodynamic analysis in the pharmaceutical industry: an IQ Consortium PK-PD Discussion Group perspective.
Wong H, Bohnert T, Damian-Iordache V, Gibson C, Hsu CP, Krishnatry AS, Liederer BM, Lin J, Lu Q, Mettetal JT, Mudra DR, Nijsen MJMA, Schroeder P, Schuck E, Suryawanshi S, Trapa P, Tsai A, Wang H, Wu F. Wong H, et al. Among authors: trapa p. Drug Discov Today. 2017 Oct;22(10):1447-1459. doi: 10.1016/j.drudis.2017.04.015. Epub 2017 May 2. Drug Discov Today. 2017. PMID: 28476536 Review.
Discovery and preclinical characterization of 1-methyl-3-(4-methylpyridin-3-yl)-6-(pyridin-2-ylmethoxy)-1H-pyrazolo-[3,4-b]pyrazine (PF470): a highly potent, selective, and efficacious metabotropic glutamate receptor 5 (mGluR5) negative allosteric modulator.
Zhang L, Balan G, Barreiro G, Boscoe BP, Chenard LK, Cianfrogna J, Claffey MM, Chen L, Coffman KJ, Drozda SE, Dunetz JR, Fonseca KR, Galatsis P, Grimwood S, Lazzaro JT, Mancuso JY, Miller EL, Reese MR, Rogers BN, Sakurada I, Skaddan M, Smith DL, Stepan AF, Trapa P, Tuttle JB, Verhoest PR, Walker DP, Wright AS, Zaleska MM, Zasadny K, Shaffer CL. Zhang L, et al. Among authors: trapa p. J Med Chem. 2014 Feb 13;57(3):861-77. doi: 10.1021/jm401622k. Epub 2014 Jan 22. J Med Chem. 2014. PMID: 24392688
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