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Page 1
Structure-activity relationships and discovery of a G protein biased μ opioid receptor ligand, [(3-methoxythiophen-2-yl)methyl]({2-[(9R)-9-(pyridin-2-yl)-6-oxaspiro-[4.5]decan-9-yl]ethyl})amine (TRV130), for the treatment of acute severe pain.
Chen XT, Pitis P, Liu G, Yuan C, Gotchev D, Cowan CL, Rominger DH, Koblish M, Dewire SM, Crombie AL, Violin JD, Yamashita DS. Chen XT, et al. Among authors: pitis p. J Med Chem. 2013 Oct 24;56(20):8019-31. doi: 10.1021/jm4010829. Epub 2013 Oct 14. J Med Chem. 2013. PMID: 24063433
A G protein-biased ligand at the μ-opioid receptor is potently analgesic with reduced gastrointestinal and respiratory dysfunction compared with morphine.
DeWire SM, Yamashita DS, Rominger DH, Liu G, Cowan CL, Graczyk TM, Chen XT, Pitis PM, Gotchev D, Yuan C, Koblish M, Lark MW, Violin JD. DeWire SM, et al. Among authors: pitis pm. J Pharmacol Exp Ther. 2013 Mar;344(3):708-17. doi: 10.1124/jpet.112.201616. Epub 2013 Jan 8. J Pharmacol Exp Ther. 2013. PMID: 23300227
2-Ethynylbenzenealkanamines. A new class of calcium entry blockers.
Carson JR, Almond HR, Brannan MD, Carmosin RJ, Flaim SF, Gill A, Gleason MM, Keely SL, Ludovici DW, Pitis PM, et al. Carson JR, et al. Among authors: pitis pm. J Med Chem. 1988 Mar;31(3):630-6. doi: 10.1021/jm00398a023. J Med Chem. 1988. PMID: 3346879
Aroyl(aminoacyl)pyrroles, a new class of anticonvulsant agents.
Carson JR, Carmosin RJ, Pitis PM, Vaught JL, Almond HR, Stables JP, Wolf HH, Swinyard EA, White HS. Carson JR, et al. Among authors: pitis pm. J Med Chem. 1997 May 23;40(11):1578-84. doi: 10.1021/jm9606655. J Med Chem. 1997. PMID: 9171868
Dysregulation of PRMT5 in chronic lymphocytic leukemia promotes progression with high risk of Richter's transformation.
Hing ZA, Walker JS, Whipp EC, Brinton L, Cannon M, Zhang P, Sher S, Cempre CB, Brown F, Smith PL, Agostinelli C, Pileri SA, Skinner JN, Williams K, Phillips H, Shaffer J, Beaver LP, Pan A, Shin K, Gregory CT, Ozer GH, Yilmaz SA, Harrington BK, Lehman AM, Yu L, Coppola V, Yan P, Scherle P, Wang M, Pitis P, Xu C, Vaddi K, Chen-Kiang S, Woyach J, Blachly JS, Alinari L, Yang Y, Byrd JC, Baiocchi RA, Blaser BW, Lapalombella R. Hing ZA, et al. Among authors: pitis p. Nat Commun. 2023 Jan 6;14(1):97. doi: 10.1038/s41467-022-35778-1. Nat Commun. 2023. PMID: 36609611 Free PMC article.