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Intermittent oral coadministration of a gamma secretase inhibitor with dexamethasone mitigates intestinal goblet cell hyperplasia in rats.

Aguirre SA, Liu L, Hosea NA, Scott W, May JR, Burns-Naas LA, Randolph S, Denlinger RH, Han B.

Toxicol Pathol. 2014;42(2):422-34. doi: 10.1177/0192623313486315. Epub 2013 May 7.


N-(Pyridin-2-yl) arylsulfonamide inhibitors of 11β-hydroxysteroid dehydrogenase type 1: strategies to eliminate reactive metabolites.

Nair SK, Matthews JJ, Cripps SJ, Cheng H, Hoffman JE, Smith C, Kupchinsky S, Siu M, Taylor WD, Wang Y, Johnson TO, Dress KR, Edwards MP, Zhou S, Hosea NA, Lapaglia A, Kang P, Castro A, Ermolieff J, Fanjul A, Vogel JE, Rejto P, Dalvie D.

Bioorg Med Chem Lett. 2013 Apr 15;23(8):2344-8. doi: 10.1016/j.bmcl.2013.02.066. Epub 2013 Feb 24.


Predicting pharmacokinetic profiles using in silico derived parameters.

Hosea NA, Jones HM.

Mol Pharm. 2013 Apr 1;10(4):1207-15. doi: 10.1021/mp300482w. Epub 2013 Mar 7.


Dose-dependent effects of small-molecule antagonists on the genomic landscape of androgen receptor binding.

Zhu Z, Shi M, Hu W, Estrella H, Engebretsen J, Nichols T, Briere D, Hosea N, Los G, Rejto PA, Fanjul A.

BMC Genomics. 2012 Jul 31;13:355. doi: 10.1186/1471-2164-13-355.


Discovery of 3-aryloxy-lactam analogs as potent androgen receptor full antagonists for treating castration resistant prostate cancer.

Guo C, Kephart S, Ornelas M, Gonzalez J, Linton A, Pairish M, Nagata A, Greasley S, Elleraas J, Hosea N, Engebretsen J, Fanjul AN.

Bioorg Med Chem Lett. 2012 Jan 15;22(2):1230-6. doi: 10.1016/j.bmcl.2011.11.068. Epub 2011 Dec 9.


Discovery of aryloxy tetramethylcyclobutanes as novel androgen receptor antagonists.

Guo C, Linton A, Kephart S, Ornelas M, Pairish M, Gonzalez J, Greasley S, Nagata A, Burke BJ, Edwards M, Hosea N, Kang P, Hu W, Engebretsen J, Briere D, Shi M, Gukasyan H, Richardson P, Dack K, Underwood T, Johnson P, Morell A, Felstead R, Kuruma H, Matsimoto H, Zoubeidi A, Gleave M, Los G, Fanjul AN.

J Med Chem. 2011 Nov 10;54(21):7693-704. doi: 10.1021/jm201059s. Epub 2011 Oct 7.


Simulation of human intravenous and oral pharmacokinetics of 21 diverse compounds using physiologically based pharmacokinetic modelling.

Jones HM, Gardner IB, Collard WT, Stanley PJ, Oxley P, Hosea NA, Plowchalk D, Gernhardt S, Lin J, Dickins M, Rahavendran SR, Jones BC, Watson KJ, Pertinez H, Kumar V, Cole S.

Clin Pharmacokinet. 2011 May;50(5):331-47. doi: 10.2165/11539680-000000000-00000.


Evaluation of selective gamma-secretase inhibitor PF-03084014 for its antitumor efficacy and gastrointestinal safety to guide optimal clinical trial design.

Wei P, Walls M, Qiu M, Ding R, Denlinger RH, Wong A, Tsaparikos K, Jani JP, Hosea N, Sands M, Randolph S, Smeal T.

Mol Cancer Ther. 2010 Jun;9(6):1618-28. doi: 10.1158/1535-7163.MCT-10-0034. Epub 2010 Jun 8.


The development and SAR of pyrrolidine carboxamide 11beta-HSD1 inhibitors.

Cheng H, Hoffman J, Le P, Nair SK, Cripps S, Matthews J, Smith C, Yang M, Kupchinsky S, Dress K, Edwards M, Cole B, Walters E, Loh C, Ermolieff J, Fanjul A, Bhat GB, Herrera J, Pauly T, Hosea N, Paderes G, Rejto P.

Bioorg Med Chem Lett. 2010 May 1;20(9):2897-902. doi: 10.1016/j.bmcl.2010.03.032. Epub 2010 Mar 10.


Potent and cellularly active 4-aminoimidazole inhibitors of cyclin-dependent kinase 5/p25 for the treatment of Alzheimer's disease.

Helal CJ, Kang Z, Lucas JC, Gant T, Ahlijanian MK, Schachter JB, Richter KE, Cook JM, Menniti FS, Kelly K, Mente S, Pandit J, Hosea N.

Bioorg Med Chem Lett. 2009 Oct 1;19(19):5703-7. doi: 10.1016/j.bmcl.2009.08.019. Epub 2009 Aug 8.


N-(Pyridin-2-yl) arylsulfonamide inhibitors of 11beta-hydroxysteroid dehydrogenase type 1: Discovery of PF-915275.

Siu M, Johnson TO, Wang Y, Nair SK, Taylor WD, Cripps SJ, Matthews JJ, Edwards MP, Pauly TA, Ermolieff J, Castro A, Hosea NA, LaPaglia A, Fanjul AN, Vogel JE.

Bioorg Med Chem Lett. 2009 Jul 1;19(13):3493-7. doi: 10.1016/j.bmcl.2009.05.011. Epub 2009 May 7.


Prediction of human pharmacokinetics from preclinical information: comparative accuracy of quantitative prediction approaches.

Hosea NA, Collard WT, Cole S, Maurer TS, Fang RX, Jones H, Kakar SM, Nakai Y, Smith BJ, Webster R, Beaumont K.

J Clin Pharmacol. 2009 May;49(5):513-33. doi: 10.1177/0091270009333209. Epub 2009 Mar 19.


Evaluation of cerebrospinal fluid concentration and plasma free concentration as a surrogate measurement for brain free concentration.

Liu X, Smith BJ, Chen C, Callegari E, Becker SL, Chen X, Cianfrogna J, Doran AC, Doran SD, Gibbs JP, Hosea N, Liu J, Nelson FR, Szewc MA, Van Deusen J.

Drug Metab Dispos. 2006 Sep;34(9):1443-7. Epub 2006 Jun 7.


Use of a physiologically based pharmacokinetic model to study the time to reach brain equilibrium: an experimental analysis of the role of blood-brain barrier permeability, plasma protein binding, and brain tissue binding.

Liu X, Smith BJ, Chen C, Callegari E, Becker SL, Chen X, Cianfrogna J, Doran AC, Doran SD, Gibbs JP, Hosea N, Liu J, Nelson FR, Szewc MA, Van Deusen J.

J Pharmacol Exp Ther. 2005 Jun;313(3):1254-62. Epub 2005 Mar 2.


The impact of P-glycoprotein on the disposition of drugs targeted for indications of the central nervous system: evaluation using the MDR1A/1B knockout mouse model.

Doran A, Obach RS, Smith BJ, Hosea NA, Becker S, Callegari E, Chen C, Chen X, Choo E, Cianfrogna J, Cox LM, Gibbs JP, Gibbs MA, Hatch H, Hop CE, Kasman IN, Laperle J, Liu J, Liu X, Logman M, Maclin D, Nedza FM, Nelson F, Olson E, Rahematpura S, Raunig D, Rogers S, Schmidt K, Spracklin DK, Szewc M, Troutman M, Tseng E, Tu M, Van Deusen JW, Venkatakrishnan K, Walens G, Wang EQ, Wong D, Yasgar AS, Zhang C.

Drug Metab Dispos. 2005 Jan;33(1):165-74. Epub 2004 Oct 22.


Purification of cytochromes P450: products of bacterial recombinant expression systems.

Guengerich FP, Hosea NA, Martin MV.

Methods Mol Biol. 1998;107:77-83. No abstract available.


Factors affecting the clinical development of cytochrome p450 3A substrates.

Gibbs MA, Hosea NA.

Clin Pharmacokinet. 2003;42(11):969-84. Review.


Purification of cytochrome P-450 enzymes.

Bell-Parikh LC, Hosea NA, Martin MV, Guengerich FP.

Curr Protoc Toxicol. 2002;Chapter 4:Unit4.2. doi: 10.1002/0471140856.tx0402s12.

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