7TZC
A drug and ATP binding site in type 1 ryanodine receptor
This is a non-PDB format compatible entry.
Summary for 7TZC
| Entry DOI | 10.2210/pdb7tzc/pdb |
| EMDB information | 26205 |
| Descriptor | Calmodulin-1, Peptidyl-prolyl cis-trans isomerase FKBP1A, Ryanodine receptor 1, ... (9 entities in total) |
| Functional Keywords | ryanodine receptor, calcium, ion channel, membrane protein-isomerase complex, membrane protein |
| Biological source | Homo sapiens (human) More |
| Total number of polymer chains | 12 |
| Total formula weight | 2392463.39 |
| Authors | Melville, Z.,Dridi, H.,Yuan, Q.,Reiken, S.,Anetta, W.,Liu, Y.,Clarke, O.B.,Marks, A.R. (deposition date: 2022-02-15, release date: 2022-05-18, Last modification date: 2024-11-13) |
| Primary citation | Melville, Z.,Dridi, H.,Yuan, Q.,Reiken, S.,Wronska, A.,Liu, Y.,Clarke, O.B.,Marks, A.R. A drug and ATP binding site in type 1 ryanodine receptor. Structure, 30:1025-, 2022 Cited by PubMed Abstract: The ryanodine receptor (RyR)/calcium release channel on the sarcoplasmic reticulum (SR) is required for excitation-contraction coupling in skeletal and cardiac muscle. Inherited mutations and stress-induced post-translational modifications result in an SR Ca leak that causes skeletal myopathies, heart failure, and exercise-induced sudden death. A class of therapeutics known as Rycals prevent the RyR-mediated leak, are effective in preventing disease progression and restoring function in animal models, and are in clinical trials for patients with muscle and heart disorders. Using cryogenic-electron microscopy, we present a model of RyR1 with a 2.45-Å resolution before local refinement, revealing a binding site in the RY1&2 domain (3.10 Å local resolution), where the Rycal ARM210 binds cooperatively with ATP and stabilizes the closed state of RyR1. PubMed: 35580609DOI: 10.1016/j.str.2022.04.010 PDB entries with the same primary citation |
| Experimental method | ELECTRON MICROSCOPY (2.45 Å) |
Structure validation
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