Tuesday, 24 May 2005 - 3:50 PM
659

This presentation is part of: Visions in Chemistry II

Calcium Channels as Drug Targets: Why Some ARE and Some Are NOT

David Triggle, State University of New York at Buffalo, Amherst, NY

The therapeutically available calcium channel antagonists are a chemically heterogeneous group of small molecules that are widely employed in a number of cardiovascular diseases, most notably hypertension, and have simultaneously been invaluable molecular tools with which to probe the structure and function of voltage-gated calcium channels. They owe their therapeutic success to a specific interaction with one subclass of channel–the L-type voltage-gated calcium channel.With the realization that the L-type channel is but one member of a widely distributed family that includes the CaV1.1-1.4 (L) types, the CaV2.1-2.3 (P/Q, N and R types) and the CaV3.1-3.3 (T-type) widely distributed in both the peripheral and central nervous systems and elsewhere an intensive search was initiated for molecules that were selectively effective at these channel types and that might offer therapeutic utility in neuronal disorders including pain, epilepsy, stroke, affective disorders etc as well as in cardiovascular disorders, notably arrhythmias. These efforts have not been successful and small molecule equivalents of diltiazem, nifedipine and verapamil with therapeutic utility have not yet been found. The underlying reasons for this are discussed and comments made on the virtues of selective vs non-selective agents and on whether all diseases are susceptible to “magic bullets.”

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