Transfer of high sensitivity for benzothiazepines from L-type to class A (BI) calcium channels
S Hering, S Aczél, M Grabner, F Döring… - Journal of Biological …, 1996 - ASBMB
To investigate the molecular basis of the calcium channel block by diltiazem, we transferred
amino acids of the highly sensitive and stereoselective L-type (α 1S or α 1C) to a weakly
sensitive, nonstereoselective class A (α 1A) calcium channel. Transfer of three amino acids
of transmembrane segment IVS6 of L-type α 1 into the α 1A subunit (I1804Y, S1808A, and
M1811I) was sufficient to support a use-dependent block by diltiazem and by the
phenylalkylamine (−)-gallopamil after expression in Xenopus oocytes. An additional …
amino acids of the highly sensitive and stereoselective L-type (α 1S or α 1C) to a weakly
sensitive, nonstereoselective class A (α 1A) calcium channel. Transfer of three amino acids
of transmembrane segment IVS6 of L-type α 1 into the α 1A subunit (I1804Y, S1808A, and
M1811I) was sufficient to support a use-dependent block by diltiazem and by the
phenylalkylamine (−)-gallopamil after expression in Xenopus oocytes. An additional …
