Molecular mechanism of diltiazem interaction with L-type Ca2+ channels.

  title={Molecular mechanism of diltiazem interaction with L-type Ca2+ channels.},
  author={Richard L. Kraus and Steffen Hering and M. Grabner and Dominique Ostler and J{\"o}rg Striessnig},
  journal={The Journal of biological chemistry},
  volume={273 42},
Benzothiazepine Ca2+ antagonists (such as (+)-cis-diltiazem) interact with transmembrane segments IIIS6 and IVS6 in the alpha1 subunit of L-type Ca2+ channels. We investigated the contribution of individual IIIS6 amino acid residues for diltiazem sensitivity by employing alanine scanning mutagenesis in a benzothiazepine-sensitive alpha1 subunit chimera (ALDIL) expressed in Xenopus laevis oocytes. The most dramatic decrease of block by 100 microM diltiazem (ALDIL 45 +/- 4.8% inhibition) during… CONTINUE READING

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