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 - Review article
C2 - 12448697
AN - SCOPUS:0036888975
SN - 1389-4501
VL - 3
SP - 455
EP - 464
JO - Current drug targets
JF - Current drug targets
IS - 6
ER -