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Items: 12


Inhibition of IL-23 mediated inflammation with a novel small molecule inverse agonist of RORgt.

Gauld S, Jacquet S, Gauvin D, Wallace C, Wang Y, McCarthy R, Goess C, Leys L, Huang S, Su Z, Edelmayer R, Wetter J, Salte K, McGaraughty S, Argiriadi M, Honore P, Luccarini JM, Bressac D, Desino K, Breinlinger E, Cusack K, Potin D, Kort M, Masson P.

J Pharmacol Exp Ther. 2019 Aug 2. pii: jpet.119.258046. doi: 10.1124/jpet.119.258046. [Epub ahead of print]


Discovery of 4-[(2R,4R)-4-({[1-(2,2-Difluoro-1,3-benzodioxol-5-yl)cyclopropyl]carbonyl}amino)-7-(difluoromethoxy)-3,4-dihydro-2H-chromen-2-yl]benzoic Acid (ABBV/GLPG-2222), a Potent Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) Corrector for the Treatment of Cystic Fibrosis.

Wang X, Liu B, Searle X, Yeung C, Bogdan A, Greszler S, Singh A, Fan Y, Swensen AM, Vortherms T, Balut C, Jia Y, Desino K, Gao W, Yong H, Tse C, Kym P.

J Med Chem. 2018 Feb 22;61(4):1436-1449. doi: 10.1021/acs.jmedchem.7b01339. Epub 2018 Jan 5.


In Silico Absorption, Distribution, Metabolism, Excretion, and Pharmacokinetics (ADME-PK): Utility and Best Practices. An Industry Perspective from the International Consortium for Innovation through Quality in Pharmaceutical Development.

Lombardo F, Desai PV, Arimoto R, Desino KE, Fischer H, Keefer CE, Petersson C, Winiwarter S, Broccatelli F.

J Med Chem. 2017 Nov 22;60(22):9097-9113. doi: 10.1021/acs.jmedchem.7b00487. Epub 2017 Jun 27. Review.


Placental ABC Transporters: Biological Impact and Pharmaceutical Significance.

Joshi AA, Vaidya SS, St-Pierre MV, Mikheev AM, Desino KE, Nyandege AN, Audus KL, Unadkat JD, Gerk PM.

Pharm Res. 2016 Dec;33(12):2847-2878. Epub 2016 Sep 19. Review.


Hit-to-lead evaluation of a novel class of sphingosine 1-phosphate lyase inhibitors.

Dinges J, Harris CM, Wallace GA, Argiriadi MA, Queeney KL, Perron DC, Dominguez E, Kebede T, Desino KE, Patel H, Vasudevan A.

Bioorg Med Chem Lett. 2016 May 1;26(9):2297-302. doi: 10.1016/j.bmcl.2016.03.043. Epub 2016 Mar 14.


In silico, in vitro and in situ models to assess interplay between CYP3A and P-gp.

Mudra DR, Desino KE, Desai PV.

Curr Drug Metab. 2011 Oct;12(8):750-73. Review.


(3R,5S,7as)-(3,5-Bis(4-fluorophenyl)tetrahydro-1H-oxazolo[3,4-c]oxazol-7a-yl)methanol, a novel neuroprotective agent.

Desino KE, Ansar S, Georg GI, Himes RH, Michaelis ML, Powell DR, Reiff EA, Telikepalli H, Audus KL.

J Med Chem. 2009 Dec 10;52(23):7537-43. doi: 10.1021/jm900254k.


TCP-FA4: a derivative of tranylcypromine showing improved blood-brain permeability.

Desino KE, Pignatello R, Guccione S, Basile L, Ansar S, Michaelis ML, Ramsay RR, Audus KL.

Biochem Pharmacol. 2009 Dec 1;78(11):1412-7. doi: 10.1016/j.bcp.2009.07.027. Epub 2009 Aug 11.


Paclitaxel succinate analogs: Anionic and amide introduction as a strategy to impart blood-brain barrier permeability.

Turunen BJ, Ge H, Oyetunji J, Desino KE, Vasandani V, G├╝the S, Himes RH, Audus KL, Seelig A, Georg GI.

Bioorg Med Chem Lett. 2008 Nov 15;18(22):5971-4. doi: 10.1016/j.bmcl.2008.09.103. Epub 2008 Oct 2.


Preclinical absorption, distribution, metabolism and excretion (ADME) characterization of ICAM1988, an LFA-1/ICAM antagonist, and its prodrug.

Khojasteh SC, Leipold DD, Lai F, La H, Baumgardner MJ, Desino KE, Gudmundsson OS, Bloedow DC, Bodary SC, Reynolds ME, Gadek TR, Kenkare-Mitra S.

Xenobiotica. 2008 Mar;38(3):340-52. doi: 10.1080/00498250701813248 .


A non-toxic Hsp90 inhibitor protects neurons from Abeta-induced toxicity.

Ansar S, Burlison JA, Hadden MK, Yu XM, Desino KE, Bean J, Neckers L, Audus KL, Michaelis ML, Blagg BS.

Bioorg Med Chem Lett. 2007 Apr 1;17(7):1984-90. Epub 2007 Jan 17.


Single-site chemical modification at C10 of the baccatin III core of paclitaxel and Taxol C reduces P-glycoprotein interactions in bovine brain microvessel endothelial cells.

Spletstoser JT, Turunen BJ, Desino K, Rice A, Datta A, Dutta D, Huff JK, Himes RH, Audus KL, Seelig A, Georg GI.

Bioorg Med Chem Lett. 2006 Feb;16(3):495-8. Epub 2005 Nov 10.


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