Prospects for rational development of pharmacological gap junction channel blockers

David C. Spray, Renato Rozental, Miduturu Srinivas

Research output: Contribution to journalArticle

67 Citations (Scopus)

Abstract

Connexin-null mice and human genetic gap junction diseases illustrate the important roles that gap junction channels play under normal conditions, and the neuro- and cardioprotective effects of gap junction blocking agents demonstrate that closure of these channels may be beneficial in certain pathological situations. This overview summarizes studies in which gap junction modifying reagents have been characterized, highlighting examples of agents for which selectivity for gap junction subtypes has been demonstrated. In addition, strategies for targeting connexin domains through peptide inhibitors are outlined, which may ultimately provide agents that are not only connexin-selective in their actions, but also affect only a subset of a gap junction channel's gating responses.

Original languageEnglish (US)
Pages (from-to)455-464
Number of pages10
JournalCurrent Drug Targets
Volume3
Issue number6
DOIs
StatePublished - Dec 2002

Fingerprint

Connexins
Gap Junctions
Pharmacology
Peptides
Medical Genetics
Neuroprotective Agents

ASJC Scopus subject areas

  • Molecular Medicine
  • Pharmaceutical Science

Cite this

Prospects for rational development of pharmacological gap junction channel blockers. / Spray, David C.; Rozental, Renato; Srinivas, Miduturu.

In: Current Drug Targets, Vol. 3, No. 6, 12.2002, p. 455-464.

Research output: Contribution to journalArticle

Spray, David C. ; Rozental, Renato ; Srinivas, Miduturu. / Prospects for rational development of pharmacological gap junction channel blockers. In: Current Drug Targets. 2002 ; Vol. 3, No. 6. pp. 455-464.
@article{1f8ccf71e2b649b5ace3ef63f8114a21,
title = "Prospects for rational development of pharmacological gap junction channel blockers",
abstract = "Connexin-null mice and human genetic gap junction diseases illustrate the important roles that gap junction channels play under normal conditions, and the neuro- and cardioprotective effects of gap junction blocking agents demonstrate that closure of these channels may be beneficial in certain pathological situations. This overview summarizes studies in which gap junction modifying reagents have been characterized, highlighting examples of agents for which selectivity for gap junction subtypes has been demonstrated. In addition, strategies for targeting connexin domains through peptide inhibitors are outlined, which may ultimately provide agents that are not only connexin-selective in their actions, but also affect only a subset of a gap junction channel's gating responses.",
author = "Spray, {David C.} and Renato Rozental and Miduturu Srinivas",
year = "2002",
month = "12",
doi = "10.2174/1389450023347353",
language = "English (US)",
volume = "3",
pages = "455--464",
journal = "Current Drug Targets",
issn = "1389-4501",
publisher = "Bentham Science Publishers B.V.",
number = "6",

}

TY - JOUR

T1 - Prospects for rational development of pharmacological gap junction channel blockers

AU - Spray, David C.

AU - Rozental, Renato

AU - Srinivas, Miduturu

PY - 2002/12

Y1 - 2002/12

N2 - Connexin-null mice and human genetic gap junction diseases illustrate the important roles that gap junction channels play under normal conditions, and the neuro- and cardioprotective effects of gap junction blocking agents demonstrate that closure of these channels may be beneficial in certain pathological situations. This overview summarizes studies in which gap junction modifying reagents have been characterized, highlighting examples of agents for which selectivity for gap junction subtypes has been demonstrated. In addition, strategies for targeting connexin domains through peptide inhibitors are outlined, which may ultimately provide agents that are not only connexin-selective in their actions, but also affect only a subset of a gap junction channel's gating responses.

AB - Connexin-null mice and human genetic gap junction diseases illustrate the important roles that gap junction channels play under normal conditions, and the neuro- and cardioprotective effects of gap junction blocking agents demonstrate that closure of these channels may be beneficial in certain pathological situations. This overview summarizes studies in which gap junction modifying reagents have been characterized, highlighting examples of agents for which selectivity for gap junction subtypes has been demonstrated. In addition, strategies for targeting connexin domains through peptide inhibitors are outlined, which may ultimately provide agents that are not only connexin-selective in their actions, but also affect only a subset of a gap junction channel's gating responses.

UR - http://www.scopus.com/inward/record.url?scp=0036888975&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=0036888975&partnerID=8YFLogxK

U2 - 10.2174/1389450023347353

DO - 10.2174/1389450023347353

M3 - Article

C2 - 12448697

AN - SCOPUS:0036888975

VL - 3

SP - 455

EP - 464

JO - Current Drug Targets

JF - Current Drug Targets

SN - 1389-4501

IS - 6

ER -