Interaction of diltiazem with an intracellularly accessible binding site on CaV1.2
| Autor: | Eugen Timin, Waheed Shabbir, Annette Hohaus, Steffen Hering, Denise Schellmann, GH Hockerman, Thomas Erker, Stanislav Beyl |
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| Rok vydání: | 2011 |
| Předmět: |
Protein subunit
Mutant Cav1.2 Cell membrane 03 medical and health sciences 0302 clinical medicine medicine heterocyclic compounds Diltiazem Patch clamp Binding site 030304 developmental biology Pharmacology 0303 health sciences biology Voltage-dependent calcium channel Chemistry musculoskeletal system 3. Good health medicine.anatomical_structure Biochemistry cardiovascular system biology.protein 030217 neurology & neurosurgery circulatory and respiratory physiology medicine.drug |
| Zdroj: | British Journal of Pharmacology. 162:1074-1082 |
| ISSN: | 0007-1188 |
| DOI: | 10.1111/j.1476-5381.2010.01091.x |
| Popis: | BACKGROUND AND PURPOSE Diltiazem inhibits CaV1.2 channels and is widely used in clinical practice to treat cardiovascular diseases. Binding determinants for diltiazem are located on segments IIIS6, IVS6 and the selectivity filter of the pore forming α1 subunit of CaV1.2. The aim of the present study was to clarify the location of the diltiazem binding site making use of its membrane-impermeable quaternary derivative d-cis-diltiazem (qDil) and mutant α1 subunits. |
| Databáze: | OpenAIRE |
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