Assays for Modulators of Ryanodine Receptor (RyR)/Ca2+ Release Channel Activity for Drug Discovery for Skeletal Muscle and Heart Diseases.

This article describes assays to evaluate RyR channel activity, including an ER Ca2+ measurement assay that is compatible with high-throughput screening and a [3 H]-ryanodine binding assay that provides a quantitative measure of RyR channel activity as a second screen for compound hits. © 2019 by John Wiley & Sons, Inc. Basic Protocol 1: [Ca2+ ]ER assay for ryanodine receptor (RyR) channel activity Support Protocol 1: Determination of dose dependence and isoform selectivity of RyR inhibitors using [Ca2+ ]ER assay Basic Protocol 2: [3 H]-Ryanodine binding assay for RyR channel activity Support Protocol 2: Isolation of microsomes from RyR-expressing HEK293 cells. PMID: 31834676 [PubMed - in process]
Source: Current Protocols in Pharmacology - Category: Drugs & Pharmacology Tags: Curr Protoc Pharmacol Source Type: research