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Selective mechanism-based inactivation of CYP3A4 by CYP3cide (PF-04981517) and its utility as an in vitro tool for delineating the relative roles of CYP3A4 versus CYP3A5 in the metabolism of drugs.
Walsky RL, Obach RS, Hyland R, Kang P, Zhou S, West M, Geoghegan KF, Helal CJ, Walker GS, Goosen TC, Zientek MA. Walsky RL, et al. Among authors: geoghegan kf. Drug Metab Dispos. 2012 Sep;40(9):1686-97. doi: 10.1124/dmd.112.045302. Epub 2012 May 29. Drug Metab Dispos. 2012. PMID: 22645092
Phosphodiesterase 9A regulates central cGMP and modulates responses to cholinergic and monoaminergic perturbation in vivo.
Kleiman RJ, Chapin DS, Christoffersen C, Freeman J, Fonseca KR, Geoghegan KF, Grimwood S, Guanowsky V, Hajós M, Harms JF, Helal CJ, Hoffmann WE, Kocan GP, Majchrzak MJ, McGinnis D, McLean S, Menniti FS, Nelson F, Roof R, Schmidt AW, Seymour PA, Stephenson DT, Tingley FD, Vanase-Frawley M, Verhoest PR, Schmidt CJ. Kleiman RJ, et al. Among authors: geoghegan kf. J Pharmacol Exp Ther. 2012 May;341(2):396-409. doi: 10.1124/jpet.111.191353. Epub 2012 Feb 10. J Pharmacol Exp Ther. 2012. PMID: 22328573
Pharmacodynamics and pharmacokinetics of the gamma-secretase inhibitor PF-3084014.
Lanz TA, Wood KM, Richter KE, Nolan CE, Becker SL, Pozdnyakov N, Martin BA, Du P, Oborski CE, Wood DE, Brown TM, Finley JE, Sokolowski SA, Hicks CD, Coffman KJ, Geoghegan KF, Brodney MA, Liston D, Tate B. Lanz TA, et al. Among authors: geoghegan kf. J Pharmacol Exp Ther. 2010 Jul;334(1):269-77. doi: 10.1124/jpet.110.167379. Epub 2010 Apr 2. J Pharmacol Exp Ther. 2010. PMID: 20363853
Discovery of a Selective Covalent Inhibitor of Lysophospholipase-like 1 (LYPLAL1) as a Tool to Evaluate the Role of this Serine Hydrolase in Metabolism.
Ahn K, Boehm M, Brown MF, Calloway J, Che Y, Chen J, Fennell KF, Geoghegan KF, Gilbert AM, Gutierrez JA, Kalgutkar AS, Lanba A, Limberakis C, Magee TV, O'Doherty I, Oliver R, Pabst B, Pandit J, Parris K, Pfefferkorn JA, Rolph TP, Patel R, Schuff B, Shanmugasundaram V, Starr JT, Varghese AH, Vera NB, Vernochet C, Yan J. Ahn K, et al. Among authors: geoghegan kf. ACS Chem Biol. 2016 Sep 16;11(9):2529-40. doi: 10.1021/acschembio.6b00266. Epub 2016 Jul 19. ACS Chem Biol. 2016. PMID: 27391855
Glutathione s-transferase omega 1-1 is a target of cytokine release inhibitory drugs and may be responsible for their effect on interleukin-1beta posttranslational processing.
Laliberte RE, Perregaux DG, Hoth LR, Rosner PJ, Jordan CK, Peese KM, Eggler JF, Dombroski MA, Geoghegan KF, Gabel CA. Laliberte RE, et al. Among authors: geoghegan kf. J Biol Chem. 2003 May 9;278(19):16567-78. doi: 10.1074/jbc.M211596200. Epub 2003 Mar 6. J Biol Chem. 2003. PMID: 12624100 Free article.
Activation of Liver AMPK with PF-06409577 Corrects NAFLD and Lowers Cholesterol in Rodent and Primate Preclinical Models.
Esquejo RM, Salatto CT, Delmore J, Albuquerque B, Reyes A, Shi Y, Moccia R, Cokorinos E, Peloquin M, Monetti M, Barricklow J, Bollinger E, Smith BK, Day EA, Nguyen C, Geoghegan KF, Kreeger JM, Opsahl A, Ward J, Kalgutkar AS, Tess D, Butler L, Shirai N, Osborne TF, Steinberg GR, Birnbaum MJ, Cameron KO, Miller RA. Esquejo RM, et al. Among authors: geoghegan kf. EBioMedicine. 2018 May;31:122-132. doi: 10.1016/j.ebiom.2018.04.009. Epub 2018 Apr 8. EBioMedicine. 2018. PMID: 29673898 Free PMC article.
Concentration-dependent modulation of amyloid-beta in vivo and in vitro using the gamma-secretase inhibitor, LY-450139.
Lanz TA, Karmilowicz MJ, Wood KM, Pozdnyakov N, Du P, Piotrowski MA, Brown TM, Nolan CE, Richter KE, Finley JE, Fei Q, Ebbinghaus CF, Chen YL, Spracklin DK, Tate B, Geoghegan KF, Lau LF, Auperin DD, Schachter JB. Lanz TA, et al. Among authors: geoghegan kf. J Pharmacol Exp Ther. 2006 Nov;319(2):924-33. doi: 10.1124/jpet.106.110700. Epub 2006 Aug 18. J Pharmacol Exp Ther. 2006. PMID: 16920992
88 results