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Article

A Single Amino Acid Determines the Selectivity and Efficacy of Selective Negative Allosteric Modulators of CaV1.3 L-Type Calcium Channels.

ACS chemical biology - 18 Sept 2020

Cooper Garry, Kang Soosung, Perez-Rosello Tamara, Guzman Jaime N, Galtieri Daniel, Xie Zhong, Kondapalli Jyothisri, Mordell Jack, Silverman Richard B, Surmeier D James

Abstract excerpt

Ca2+ channels with a CaV1.3 pore-forming α1 subunit have been implicated in both neurodegenerative and neuropsychiatric disorders, motivating the development of selective and potent inhibitors of CaV1.3 versus CaV1.2 channels, the calcium channels implicated in hypertensive disorders. We have previously identified pyrimidine-2,4,6-triones (PYTs) that preferentially inhibit CaV1.3 channels, but the structural...

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Identifiers

PMID: 32881483
DOI: 10.1021/acschembio.0c00577
PMCID: PMC7502546

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