Identification, Structure-Activity Relationship, and Biological Characterization of 2,3,4,5-Tetrahydro-1
Journal
Journal of medicinal chemistry
ISSN: 1520-4804
Titre abrégé: J Med Chem
Pays: United States
ID NLM: 9716531
Informations de publication
Date de publication:
08 10 2020
08 10 2020
Historique:
pubmed:
19
9
2020
medline:
8
1
2021
entrez:
18
9
2020
Statut:
ppublish
Résumé
Cystic fibrosis (CF) is a life-threatening autosomal recessive disease, caused by mutations in the CF transmembrane conductance regulator (CFTR) chloride channel. CFTR modulators have been reported to address the basic defects associated with CF-causing mutations, partially restoring the CFTR function in terms of protein processing and/or channel gating. Small-molecule compounds, called potentiators, are known to ameliorate the gating defect. In this study, we describe the identification of the 2,3,4,5-tetrahydro-1
Identifiants
pubmed: 32946228
doi: 10.1021/acs.jmedchem.0c01050
pmc: PMC8011931
doi:
Substances chimiques
CFTR protein, human
0
Indoles
0
Cystic Fibrosis Transmembrane Conductance Regulator
126880-72-6
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
11169-11194Références
Cochrane Database Syst Rev. 2019 Jan 07;1:CD009841
pubmed: 30616300
Am J Physiol Lung Cell Mol Physiol. 2003 Jul;285(1):L180-8
pubmed: 12651632
J Med Chem. 2002 Jan 3;45(1):137-42
pubmed: 11754585
Nature. 1992 Aug 27;358(6389):761-4
pubmed: 1380673
Eur J Med Chem. 2014 Nov 24;87:63-70
pubmed: 25240096
Front Pharmacol. 2019 Feb 27;10:121
pubmed: 30873022
J Med Chem. 2003 Aug 28;46(18):3930-7
pubmed: 12930153
J Med Chem. 2015 Mar 12;58(5):2091-113
pubmed: 25634295
Front Pharmacol. 2018 Sep 27;9:1100
pubmed: 30319426
Cold Spring Harb Perspect Med. 2012 Jun;2(6):a009563
pubmed: 22675668
Chem Rev. 2006 Jul;106(7):2875-911
pubmed: 16836303
Med Chem. 2005 Sep;1(5):519-27
pubmed: 16787336
Bioorg Med Chem Lett. 2009 Jun 15;19(12):3183-7
pubmed: 19443217
Hum Mutat. 2002 Jun;19(6):575-606
pubmed: 12007216
Bioorg Med Chem. 2003 Mar 6;11(5):717-22
pubmed: 12538001
Proc Natl Acad Sci U S A. 2009 Nov 3;106(44):18825-30
pubmed: 19846789
J Med Chem. 1980 Jun;23(6):635-43
pubmed: 6104732
Cell. 1990 Nov 16;63(4):827-34
pubmed: 1699669
J Med Chem. 1993 May 14;36(10):1488-95
pubmed: 8496917
J Biol Chem. 2008 Feb 29;283(9):5364-9
pubmed: 18167357
J Biol Chem. 2003 Sep 12;278(37):35079-85
pubmed: 12832418
Mol Biol Cell. 2016 Feb 1;27(3):424-33
pubmed: 26823392
Cell Mol Life Sci. 2017 Jan;74(1):129-140
pubmed: 27709245
Eksp Klin Farmakol. 2010 Nov;73(11):25-9
pubmed: 21254595
Mol Pharmacol. 2005 Dec;68(6):1736-46
pubmed: 16150931
J Med Chem. 2018 Feb 22;61(4):1425-1435
pubmed: 29148763
J Med Chem. 1993 Feb 5;36(3):343-52
pubmed: 8426363
Toxicol Sci. 2007 Jun;97(2):539-47
pubmed: 17361016
Sci Transl Med. 2014 Jul 23;6(246):246ra96
pubmed: 25101886
Am J Physiol Cell Physiol. 2011 Oct;301(4):C872-85
pubmed: 21753184
Front Pharmacol. 2018 Oct 26;9:1221
pubmed: 30416447
J Pharmacol Exp Ther. 2017 Aug;362(2):359-367
pubmed: 28611092
Eur J Med Chem. 2018 Sep 5;157:447-461
pubmed: 30103193
N Engl J Med. 2015 Jan 22;372(4):351-62
pubmed: 25607428
J Biol Chem. 1993 Oct 15;268(29):21592-8
pubmed: 7691813
Mol Pharmacol. 2007 Jul;72(1):197-207
pubmed: 17452495
Front Pharmacol. 2018 Dec 13;9:1464
pubmed: 30618756
Sci Adv. 2020 Feb 21;6(8):eaay9669
pubmed: 32128418
Sci Transl Med. 2014 Jul 23;6(246):246ra97
pubmed: 25101887
Lancet Respir Med. 2016 Aug;4(8):662-674
pubmed: 27053340
Nature. 1991 Dec 19-26;354(6354):526-8
pubmed: 1722027
Cell Mol Life Sci. 2017 Jan;74(1):93-115
pubmed: 27714410
Proc Natl Acad Sci U S A. 2011 Nov 15;108(46):18843-8
pubmed: 21976485
Curr Drug Discov Technol. 2004 Oct;1(3):211-20
pubmed: 16472248
Curr Med Chem. 2018;25(39):5315-5326
pubmed: 27494393
J Cyst Fibros. 2018 Mar;17(2S):S14-S21
pubmed: 28916430
Expert Rev Respir Med. 2018 Sep;12(9):725-732
pubmed: 30073878
J Biol Chem. 2002 Oct 4;277(40):37235-41
pubmed: 12161441
J Physiol. 2012 Dec 1;590(23):6141-55
pubmed: 22988141