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Items: 7

1.

Identification of (R)-(2-Chloro-3-(trifluoromethyl)phenyl)(1-(5-fluoropyridin-2-yl)-4-methyl-6,7-dihydro-1H-imidazo[4,5-c]pyridin-5(4H)-yl)methanone (JNJ 54166060), a Small Molecule Antagonist of the P2X7 receptor.

Swanson DM, Savall BM, Coe KJ, Schoetens F, Koudriakova T, Skaptason J, Wall J, Rech J, Deng X, De Angelis M, Everson A, Lord B, Wang Q, Ao H, Scott B, Sepassi K, Lovenberg TW, Carruthers NI, Bhattacharya A, Letavic MA.

J Med Chem. 2016 Sep 22;59(18):8535-48. doi: 10.1021/acs.jmedchem.6b00989. Epub 2016 Sep 8.

PMID:
27548392
2.

Prolyl hydroxylase inhibition corrects functional iron deficiency and inflammation-induced anaemia in rats.

Barrett TD, Palomino HL, Brondstetter TI, Kanelakis KC, Wu X, Yan W, Merton KP, Schoetens F, Ma JY, Skaptason J, Gao J, Tran DT, Venkatesan H, Rosen MD, Shankley NP, Rabinowitz MH.

Br J Pharmacol. 2015 Aug;172(16):4078-88. doi: 10.1111/bph.13188. Epub 2015 Jun 26.

3.

Prediction of oral pharmacokinetics of cMet kinase inhibitors in humans: physiologically based pharmacokinetic model versus traditional one-compartment model.

Yamazaki S, Skaptason J, Romero D, Vekich S, Jones HM, Tan W, Wilner KD, Koudriakova T.

Drug Metab Dispos. 2011 Mar;39(3):383-93. doi: 10.1124/dmd.110.035857. Epub 2010 Nov 23.

PMID:
21098644
4.

Dihydroxyphenylisoindoline amides as orally bioavailable inhibitors of the heat shock protein 90 (hsp90) molecular chaperone.

Kung PP, Huang B, Zhang G, Zhou JZ, Wang J, Digits JA, Skaptason J, Yamazaki S, Neul D, Zientek M, Elleraas J, Mehta P, Yin MJ, Hickey MJ, Gajiwala KS, Rodgers C, Davies JF, Gehring MR.

J Med Chem. 2010 Jan 14;53(1):499-503. doi: 10.1021/jm901209q.

PMID:
19908836
5.

Application of stable isotope methodology in the evaluation of the pharmacokinetics of (S,S)-3-[3-(methylsulfonyl)phenyl]-1-propylpiperidine hydrochloride in rats.

Yamazaki S, Toth LN, Kimoto E, Bower J, Skaptason J, Romero D, Heath TG.

Drug Metab Dispos. 2009 May;37(5):937-45. doi: 10.1124/dmd.108.025478. Epub 2009 Feb 23.

PMID:
19237512
6.

Pharmacologic properties of AG-012986, a pan-cyclin-dependent kinase inhibitor with antitumor efficacy.

Zhang C, Lundgren K, Yan Z, Arango ME, Price S, Huber A, Higgins J, Troche G, Skaptason J, Koudriakova T, Nonomiya J, Yang M, O'Connor P, Bender S, Los G, Lewis C, Jessen B.

Mol Cancer Ther. 2008 Apr;7(4):818-28. doi: 10.1158/1535-7163.MCT-07-0440.

7.

Pharmacokinetic-pharmacodynamic modeling of biomarker response and tumor growth inhibition to an orally available cMet kinase inhibitor in human tumor xenograft mouse models.

Yamazaki S, Skaptason J, Romero D, Lee JH, Zou HY, Christensen JG, Koup JR, Smith BJ, Koudriakova T.

Drug Metab Dispos. 2008 Jul;36(7):1267-74. doi: 10.1124/dmd.107.019711. Epub 2008 Apr 1.

PMID:
18381487

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