Critical Roles of Hydrophobicity and Orientation of Side Chains for Inactivation of Sarcoplasmic Reticulum Ca(2+)-ATPase with Thapsigargin and Thapsigargin Analogs

Thapsigargin (Tg), a specific inhibitor of sarco/endoplasmic Ca(2+)-ATPases (SERCA), binds with high affinity to the E2 conformation of these ATPases. SERCA inhibition leads to elevated calcium levels in the cytoplasm, which in turn induces apoptosis. We present x-ray crystallographic and intrinsic...

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Detalhes bibliográficos
Main Authors: Winther, Anne-Marie L., Liu, Huizhen, Sonntag, Yonathan, Olesen, Claus, le Maire, Marc, Soehoel, Helmer, Olsen, Carl-Erik, Christensen, S. Brøgger, Nissen, Poul, Møller, Jesper V.
Formato: Artigo
Idioma:Inglês
Publicado em: American Society for Biochemistry and Molecular Biology 2010
Assuntos:
Membrane Biology
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC2937915/
https://ncbi.nlm.nih.gov/pubmed/20551329
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1074/jbc.M110.136242
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