Referenced in: none

Automatically associated channels: Kv10.1 , Kv11.1 , Kv12.1

Title: Mapping the receptor site for ergtoxin, a specific blocker of ERG channels.

Authors: Liliana Pardo-López, Jesús García-Valdes, Georgina B Gurrola, Gail A Robertson, Lourival D Possani

Journal, date & volume: FEBS Lett., 2002 Jan 2 , 510, 45-9

PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/11755529

Abstract
We show here that ergtoxin (ErgTx) is a bona fide, specific blocker of the human ether-a-go-go-related gene (HERG) channels. It does not affect the function of either M-eag or M-elk channels. A chimeric construction containing a segment of the P-region of M-eag channel inserted into the HERG channel drastically diminished or completely abolished the inhibitory effect of ErgTx, whereas chimeras of the P-region of HERG channel into M-eag channels recovered the inhibitory effect. From the P-region point mutants of HERG channel assays, only the mutant N598Q shows about 25% decrement of the ErgTx inhibitory effect. ErgTx recognizes the P-region of HERG channels, blocking the channel function with a K(d) in the order of 12 nM.