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Development of a small molecule that corrects misfolding and increases secretion of Z α1 -antitrypsin.
Lomas DA, Irving JA, Arico-Muendel C, Belyanskaya S, Brewster A, Brown M, Chung CW, Dave H, Denis A, Dodic N, Dossang A, Eddershaw P, Klimaszewska D, Haq I, Holmes DS, Hutchinson JP, Jagger AM, Jakhria T, Jigorel E, Liddle J, Lind K, Marciniak SJ, Messer J, Neu M, Olszewski A, Ordonez A, Ronzoni R, Rowedder J, Rüdiger M, Skinner S, Smith KJ, Terry R, Trottet L, Uings I, Wilson S, Zhu Z, Pearce AC. Lomas DA, et al. Among authors: jigorel e. EMBO Mol Med. 2021 Mar 5;13(3):e13167. doi: 10.15252/emmm.202013167. Epub 2021 Jan 29. EMBO Mol Med. 2021. PMID: 33512066 Free PMC article.
The development of highly potent and selective small molecule correctors of Z α1-antitrypsin misfolding.
Liddle J, Pearce AC, Arico-Muendel C, Belyanskaya S, Brewster A, Brown M, Chung CW, Denis A, Dodic N, Dossang A, Eddershaw P, Klimaszewska D, Haq I, Holmes DS, Jagger A, Jakhria T, Jigorel E, Lind K, Messer J, Neu M, Olszewski A, Ronzoni R, Rowedder J, Rüdiger M, Skinner S, Smith KJ, Trottet L, Uings I, Zhu Z, Irving JA, Lomas DA. Liddle J, et al. Among authors: jigorel e. Bioorg Med Chem Lett. 2021 Jun 1;41:127973. doi: 10.1016/j.bmcl.2021.127973. Epub 2021 Mar 19. Bioorg Med Chem Lett. 2021. PMID: 33753261
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. Harris PA, et al. Among authors: jigorel e. J Med Chem. 2019 May 23;62(10):5096-5110. doi: 10.1021/acs.jmedchem.9b00318. Epub 2019 May 2. J Med Chem. 2019. PMID: 31013427
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. Buchler I, et al. Among authors: jigorel e. J Med Chem. 2018 Nov 8;61(21):9647-9665. doi: 10.1021/acs.jmedchem.8b01126. Epub 2018 Oct 19. J Med Chem. 2018. PMID: 30272964 Free PMC article.
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. Ernst G, et al. Among authors: jigorel e. ACS Med Chem Lett. 2019 Oct 22;10(11):1573-1578. doi: 10.1021/acsmedchemlett.9b00345. eCollection 2019 Nov 14. ACS Med Chem Lett. 2019. PMID: 32038769 Free PMC article.
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. Jnoff E, et al. Among authors: jigorel e. ChemMedChem. 2014 Apr;9(4):699-705. doi: 10.1002/cmdc.201300525. Epub 2014 Feb 6. ChemMedChem. 2014. PMID: 24504667
11 results