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Two Small Molecules Restore Stability to a Subpopulation of the Cystic Fibrosis Transmembrane Conductance Regulator with the Predominant Disease-causing Mutation.

Meng X, Wang Y, Wang X, Wrennall JA, Rimington TL, Li H, Cai Z, Ford RC, Sheppard DN. Meng X, et al. J Biol Chem. 2017 Mar 3;292(9):3706-3719. doi: 10.1074/jbc.M116.751537. Epub 2017 Jan 13. J Biol Chem. 2017. PMID: 28087700 Free PMC article.

Differential thermostability and response to cystic fibrosis transmembrane conductance regulator potentiators of human and mouse F508del-CFTR.

Bose SJ, Bijvelds MJC, Wang Y, Liu J, Cai Z, Bot AGM, de Jonge HR, Sheppard DN. Bose SJ, et al. Am J Physiol Lung Cell Mol Physiol. 2019 Jul 1;317(1):L71-L86. doi: 10.1152/ajplung.00034.2019. Epub 2019 Apr 10. Am J Physiol Lung Cell Mol Physiol. 2019. PMID: 30969810 Free PMC article.

ORKAMBI-Mediated Rescue of Mucociliary Clearance in Cystic Fibrosis Primary Respiratory Cultures Is Enhanced by Arginine Uptake, Arginase Inhibition, and Promotion of Nitric Oxide Signaling to the Cystic Fibrosis Transmembrane Conductance Regulator Channel.

Wu YS, Jiang J, Ahmadi S, Lew A, Laselva O, Xia S, Bartlett C, Ip W, Wellhauser L, Ouyang H, Gonska T, Moraes TJ, Bear CE. Wu YS, et al. Mol Pharmacol. 2019 Oct;96(4):515-525. doi: 10.1124/mol.119.117143. Epub 2019 Aug 19. Mol Pharmacol. 2019. PMID: 31427400

Potentiation of the cystic fibrosis transmembrane conductance regulator Cl^- channel by ivacaftor is temperature independent.

Wang Y, Cai Z, Gosling M, Sheppard DN. Wang Y, et al. Am J Physiol Lung Cell Mol Physiol. 2018 Nov 1;315(5):L846-L857. doi: 10.1152/ajplung.00235.2018. Epub 2018 Aug 23. Am J Physiol Lung Cell Mol Physiol. 2018. PMID: 30136610 Free article.

Lumacaftor alone and combined with ivacaftor: preclinical and clinical trial experience of F508del CFTR correction.

Brewington JJ, McPhail GL, Clancy JP. Brewington JJ, et al. Expert Rev Respir Med. 2016;10(1):5-17. doi: 10.1586/17476348.2016.1122527. Epub 2015 Dec 9. Expert Rev Respir Med. 2016. PMID: 26581802

Correctors (specific therapies for class II CFTR mutations) for cystic fibrosis.

Southern KW, Patel S, Sinha IP, Nevitt SJ. Southern KW, et al. Cochrane Database Syst Rev. 2018 Aug 2;8(8):CD010966. doi: 10.1002/14651858.CD010966.pub2. Cochrane Database Syst Rev. 2018. PMID: 30070364 Free PMC article. Updated. Review.

Lipophilicity of the Cystic Fibrosis Drug, Ivacaftor (VX-770), and Its Destabilizing Effect on the Major CF-causing Mutation: F508del.

Chin S, Hung M, Won A, Wu YS, Ahmadi S, Yang D, Elmallah S, Toutah K, Hamilton CM, Young RN, Viirre RD, Yip CM, Bear CE. Chin S, et al. Mol Pharmacol. 2018 Aug;94(2):917-925. doi: 10.1124/mol.118.112177. Epub 2018 Jun 14. Mol Pharmacol. 2018. PMID: 29903751

Corrector therapies (with or without potentiators) for people with cystic fibrosis with class II CFTR gene variants (most commonly F508del).

Southern KW, Murphy J, Sinha IP, Nevitt SJ. Southern KW, et al. Cochrane Database Syst Rev. 2020 Dec 17;12(12):CD010966. doi: 10.1002/14651858.CD010966.pub3. Cochrane Database Syst Rev. 2020. PMID: 33331662 Free PMC article. Updated.

F508del-cystic fibrosis transmembrane regulator correctors for treatment of cystic fibrosis: a patent review.

Yang H, Ma T. Yang H, et al. Expert Opin Ther Pat. 2015;25(9):991-1002. doi: 10.1517/13543776.2015.1045878. Epub 2015 May 15. Expert Opin Ther Pat. 2015. PMID: 25971311 Review.

CFTR potentiators partially restore channel function to A561E-CFTR, a cystic fibrosis mutant with a similar mechanism of dysfunction as F508del-CFTR.

Wang Y, Liu J, Loizidou A, Bugeja LA, Warner R, Hawley BR, Cai Z, Toye AM, Sheppard DN, Li H. Wang Y, et al. Br J Pharmacol. 2014 Oct;171(19):4490-503. doi: 10.1111/bph.12791. Epub 2014 Sep 5. Br J Pharmacol. 2014. PMID: 24902474 Free PMC article.

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