Affiliation:
1. Division of Chemistry and Structural Biology, Institute for Molecular Bioscience, the University of Queensland, Brisbane Qld 4072, Australia
Abstract
Low Voltage-Activated (LVA) T-type calcium channels are characterized by transient
current and Low Threshold Spikes (LTS) that trigger neuronal firing and oscillatory behavior.
Combined with their preferential localization in dendrites and their specific “window
current”, T-type calcium channels are considered to be key players in signal amplification and
synaptic integration. Assisted by the emerging pharmacological tools, the structural determinants
of channel gating and kinetics, as well as novel physiological and pathological functions
of T-type calcium channels, are being uncovered. In this review, we provide an overview of
structural determinants in T-type calcium channels, their involvement in disorders and diseases,
the development of novel channel modulators, as well as Structure-Activity Relationship
(SAR) studies that lead to rational drug design.
Publisher
Bentham Science Publishers Ltd.
Subject
Pharmacology,Molecular Medicine,Drug Discovery,Biochemistry,Organic Chemistry
Cited by
7 articles.
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