Literature DB >> 27501251

Inhibition of Sodium Ion Channel Function with Truncated Forms of Batrachotoxin.

Tatsuya Toma1, Matthew M Logan1, Frederic Menard1, A Sloan Devlin1, J Du Bois1.   

Abstract

A novel family of small molecule inhibitors of voltage-gated sodium channels (NaVs) based on the structure of batrachotoxin (BTX), a well-known channel agonist, is described. Protein mutagenesis and electrophysiology experiments reveal the binding site as the inner pore region of the channel, analogous to BTX, alkaloid toxins, and local anesthetics. Homology modeling of the eukaryotic channel based on recent crystallographic analyses of bacterial NaVs suggests a mechanism of action for ion conduction block.

Entities:  

Keywords:  SAR; Site II; batrachotoxin; electrophysiology; protein mutagenesis; sodium channel

Mesh：

Substances：

Year:  2016        PMID： 27501251      PMCID： PMC5555364          DOI： 10.1021/acschemneuro.6b00212

Source DB:  PubMed          Journal:  ACS Chem Neurosci        ISSN： 1948-7193            Impact factor:   4.418


  65 in total

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Journal:  Experientia       Date:  1963-07-15

Review 2.  Voltage-gated sodium channels as therapeutic targets in epilepsy and other neurological disorders.

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Journal:  Lancet Neurol       Date:  2010-04       Impact factor: 44.182

3.  Conformer generation with OMEGA: learning from the data set and the analysis of failures.

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Journal:  J Am Chem Soc       Date:  1965-01-05       Impact factor: 15.419

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Authors:  J Tanguy; J Z Yeh
Journal:  Biophys J       Date:  1988-10       Impact factor: 4.033

7.  Modification of cardiac Na+ channels by batrachotoxin: effects on gating, kinetics, and local anesthetic binding.

Authors:  J A Wasserstrom; K Liberty; J Kelly; P Santucci; M Myers
Journal:  Biophys J       Date:  1993-07       Impact factor: 4.033

8.  Crystal structure of a voltage-gated sodium channel in two potentially inactivated states.

Authors:  Jian Payandeh; Tamer M Gamal El-Din; Todd Scheuer; Ning Zheng; William A Catterall
Journal:  Nature       Date:  2012-05-20       Impact factor: 49.962

9.  Identification of a cluster of residues in transmembrane segment 6 of domain III of the cockroach sodium channel essential for the action of pyrethroid insecticides.

Authors:  Yuzhe Du; Jung-Eun Lee; Yoshiko Nomura; Tianxiang Zhang; Boris S Zhorov; Ke Dong
Journal:  Biochem J       Date:  2009-04-15       Impact factor: 3.857

10.  Modular Synthesis of the Pentacyclic Core of Batrachotoxin and Select Batrachotoxin Analogue Designs.

Authors:  A Sloan Devlin; J Du Bois
Journal:  Chem Sci       Date:  2013-03-01       Impact factor: 9.825
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  4 in total

1.  Natural Products and Their Mimics as Targets of Opportunity for Discovery.

Authors:  Stephen F Martin
Journal:  J Org Chem       Date:  2017-09-15       Impact factor: 4.354

2.  Single rat muscle Na+ channel mutation confers batrachotoxin autoresistance found in poison-dart frog Phyllobates terribilis.

Authors:  Sho-Ya Wang; Ging Kuo Wang
Journal:  Proc Natl Acad Sci U S A       Date:  2017-09-05       Impact factor: 11.205

3.  Differential effects of modified batrachotoxins on voltage-gated sodium channel fast and slow inactivation.

Authors:  Tim M G MacKenzie; Fayal Abderemane-Ali; Catherine E Garrison; Daniel L Minor; J Du Bois
Journal:  Cell Chem Biol       Date:  2021-12-27       Impact factor: 9.039

4.  Batrachotoxin acts as a stent to hold open homotetrameric prokaryotic voltage-gated sodium channels.

Authors:  Rocio K Finol-Urdaneta; Jeffrey R McArthur; Marcel P Goldschen-Ohm; Rachelle Gaudet; Denis B Tikhonov; Boris S Zhorov; Robert J French
Journal:  J Gen Physiol       Date:  2018-12-26       Impact factor: 4.086
  4 in total

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