Literature DB >> 15808474

Discovery of 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid diamides that increase CFTR mediated chloride transport.

Bradford H Hirth1, Shuang Qiao, Lisa M Cuff, Brian M Cochran, Marko J Pregel, Jill S Gregory, Scott F Sneddon, John L Kane.   

Abstract

A series of 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid diamides that increase chloride transport in cells expressing mutant cystic fibrosis transmembrane conductance regulator (CFTR) protein has been identified from our compound library. Analoging efforts and the resulting structure-activity relationships uncovered are detailed. Compound potency was improved over 30-fold from the original lead, yielding several analogs with EC(50) values below 10nM in our cellular chloride transport assay.

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Year:  2005        PMID： 15808474     DOI： 10.1016/j.bmcl.2005.02.041

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  4 in total

1.  Small molecule correctors of F508del-CFTR discovered by structure-based virtual screening.

Authors:  Ori Kalid; Martin Mense; Sharon Fischman; Alina Shitrit; Hermann Bihler; Efrat Ben-Zeev; Nili Schutz; Nicoletta Pedemonte; Philip J Thomas; Robert J Bridges; Diana R Wetmore; Yael Marantz; Hanoch Senderowitz
Journal:  J Comput Aided Mol Des       Date:  2010-10-26       Impact factor: 3.686

Review 2.  One Size Does Not Fit All: The Past, Present and Future of Cystic Fibrosis Causal Therapies.

Authors:  Marjolein M Ensinck; Marianne S Carlon
Journal:  Cells       Date:  2022-06-08       Impact factor: 7.666

3.  Residual function of cystic fibrosis mutants predicts response to small molecule CFTR modulators.

Authors:  Sangwoo T Han; Andras Rab; Matthew J Pellicore; Emily F Davis; Allison F McCague; Taylor A Evans; Anya T Joynt; Zhongzhou Lu; Zhiwei Cai; Karen S Raraigh; Jeong S Hong; David N Sheppard; Eric J Sorscher; Garry R Cutting
Journal:  JCI Insight       Date:  2018-07-26

4.  Stimulation of Wild-Type, F508del- and G551D-CFTR Chloride Channels by Non-Toxic Modified pyrrolo[2,3-b]pyrazine Derivatives.

Authors:  Luc Dannhoffer; Arnaud Billet; Mathilde Jollivet; Patricia Melin-Heschel; Christelle Faveau; Frédéric Becq
Journal:  Front Pharmacol       Date:  2011-08-23       Impact factor: 5.810
  4 in total

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