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Items: 9


Synthesis and Evaluation of Bicyclic Hydroxypyridones as Inhibitors of Catechol O-Methyltransferase.

Ernst G, Akuma D, Au V, Buchler IP, Byers S, Carr GV, Defays S, de León P, Demaude T, DePasquale M, Durieu V, Huang Y, Jigorel E, Kimos M, Kolobova A, Montel F, Moureau F, Poslusney M, Swinnen D, Vandergeten MC, Van Houtvin N, Wei H, White N, Wood M, Barrow JC.

ACS Med Chem Lett. 2019 Oct 22;10(11):1573-1578. doi: 10.1021/acsmedchemlett.9b00345. eCollection 2019 Nov 14.


Discovery and Lead-Optimization of 4,5-Dihydropyrazoles as Mono-Kinase Selective, Orally Bioavailable and Efficacious Inhibitors of Receptor Interacting Protein 1 (RIP1) Kinase.

Harris PA, Faucher N, George N, Eidam PM, King BW, White GV, Anderson NA, Bandyopadhyay D, Beal AM, Beneton V, Berger SB, Campobasso N, Campos S, Capriotti CA, Cox JA, Daugan A, Donche F, Fouchet MH, Finger JN, Geddes B, Gough PJ, Grondin P, Hoffman BL, Hoffman SJ, Hutchinson SE, Jeong JU, Jigorel E, Lamoureux P, Leister LK, Lich JD, Mahajan MK, Meslamani J, Mosley JE, Nagilla R, Nassau PM, Ng SL, Ouellette MT, Pasikanti KK, Potvain F, Reilly MA, Rivera EJ, Sautet S, Schaeffer MC, Sehon CA, Sun H, Thorpe JH, Totoritis RD, Ward P, Wellaway N, Wisnoski DD, Woolven JM, Bertin J, Marquis RW.

J Med Chem. 2019 May 23;62(10):5096-5110. doi: 10.1021/acs.jmedchem.9b00318. Epub 2019 May 2.


Optimization of 8-Hydroxyquinolines as Inhibitors of Catechol O-Methyltransferase.

Buchler I, Akuma D, Au V, Carr G, de León P, DePasquale M, Ernst G, Huang Y, Kimos M, Kolobova A, Poslusney M, Wei H, Swinnen D, Montel F, Moureau F, Jigorel E, Schulze MED, Wood M, Barrow JC.

J Med Chem. 2018 Nov 8;61(21):9647-9665. doi: 10.1021/acs.jmedchem.8b01126. Epub 2018 Oct 19.


Binding mode and structure-activity relationships around direct inhibitors of the Nrf2-Keap1 complex.

Jnoff E, Albrecht C, Barker JJ, Barker O, Beaumont E, Bromidge S, Brookfield F, Brooks M, Bubert C, Ceska T, Corden V, Dawson G, Duclos S, Fryatt T, Genicot C, Jigorel E, Kwong J, Maghames R, Mushi I, Pike R, Sands ZA, Smith MA, Stimson CC, Courade JP.

ChemMedChem. 2014 Apr;9(4):699-705. doi: 10.1002/cmdc.201300525. Epub 2014 Feb 6.


Utility of drug depletion-time profiles in isolated hepatocytes for accessing hepatic uptake clearance: identifying rate-limiting steps and role of passive processes.

Jigorel E, Houston JB.

Drug Metab Dispos. 2012 Aug;40(8):1596-602. doi: 10.1124/dmd.112.045732. Epub 2012 May 16.


Differential regulation of sinusoidal and canalicular hepatic drug transporter expression by xenobiotics activating drug-sensing receptors in primary human hepatocytes.

Jigorel E, Le Vee M, Boursier-Neyret C, Parmentier Y, Fardel O.

Drug Metab Dispos. 2006 Oct;34(10):1756-63. Epub 2006 Jul 12.


Functional expression of sinusoidal and canalicular hepatic drug transporters in the differentiated human hepatoma HepaRG cell line.

Le Vee M, Jigorel E, Glaise D, Gripon P, Guguen-Guillouzo C, Fardel O.

Eur J Pharm Sci. 2006 May;28(1-2):109-17. Epub 2006 Feb 20.


Functional expression of sinusoidal drug transporters in primary human and rat hepatocytes.

Jigorel E, Le Vee M, Boursier-Neyret C, Bertrand M, Fardel O.

Drug Metab Dispos. 2005 Oct;33(10):1418-22. Epub 2005 Jul 13.


Physiological, pharmacological and clinical features of the multidrug resistance protein 2.

Fardel O, Jigorel E, Le Vee M, Payen L.

Biomed Pharmacother. 2005 Apr;59(3):104-14. Review.


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