Antagonist binding sites of voltage-dependent calcium channels

✍ Scribed by Gerald W. Zamponi

• Publisher: John Wiley and Sons
• Year: 1997
• Tongue: English
• Weight: 222 KB
• Volume: 42
• Category: Article
• ISSN: 0272-4391
• DOI: 10.1002/(sici)1098-2299(199711/12)42:3/4<131::aid-ddr4>3.0.co;2-r

✦ Synopsis

Voltage-dependent calcium channels are crucial targets for a wide range of clinically active small organic pharmacological agents. These agents fall into several distinct classes of blockers, each associated with a unique site on the calcium channel α 1 subunit. In addition, a number of peptide toxins isolated from invertebrates specifically bind to and block certain subtypes of voltage-dependent calcium channels. Voltage-dependent calcium channels are comprised of multiple subtypes, and not each of those subtypes are equally sensitive to small organic compounds and peptide blockers. Here, I present an overview of the classes of calcium channel blockers and our current understanding of their sites of action on the calcium channel protein.