T-type calcium channel regulators.

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Presentation transcript:

T-type calcium channel regulators. T-type calcium channel regulators. Examples of classes of blockers known to inhibit T-type calcium channels, including small organic molecules and the peptide toxin kurtoxin. The inhibitors either physically block the pore, or bind to the gating machinery (pathway 1). T-type calcium channels can also be regulated by activation of GPCRs, either directly by G protein βγ subunits (pathway 2a), or indirectly via protein kinases such as Rho kinase, protein kinase C, or CaMKII (pathway 2b). T-type calcium channel expression in the plasma membrane is regulated by ubiquitination and deubiquitinating. The deubiquitinase USP5 removes ubiquitin groups, thus increasing channel stability in the plasma membrane. Interfering with USP5 binding to the channel (pathway 3) leads to channel internalization and degradation. The kurtoxin image is reproduced from the Orientations of Proteins in Membranes database (Lomize et al., 2006; http://opm.phar.umich.edu/protein.php?pdbid=1t1t). Gerald W. Zamponi et al. Pharmacol Rev 2015;67:821-870 Copyright © 2015 by The American Society for Pharmacology and Experimental Therapeutics