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Journal article

Synthetic partial agonists reveal key steps in IP3 receptor activation

Abstract:

Inositol 1,4,5-trisphosphate receptors (IP3Rs) are ubiquitous intracellular Ca2+ channels. IP3 binding to the IP 3-binding core (IBC) near the N terminus initiates conformational changes that lead to opening of a pore. The mechanisms underlying this process are unresolved. We synthesized 2-O-modified IP3 analogs that are partial agonists of IP3R. These are similar to IP3 in their interactions with the IBC, but they are less effective than IP3 in rearranging the relationship between the IBC an...

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Publication status:
Published
Peer review status:
Peer reviewed

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Publisher copy:
10.1038/nchembio.195

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Institution:
University of Oxford
Division:
MSD
Department:
Pharmacology
Role:
Author
Wellcome Trust More from this funder
Biotechnology and Biological Sciences Research Council More from this funder
Publisher:
Nature Publishing Group Publisher's website
Journal:
Nature Chemical Biology Journal website
Volume:
5
Pages:
631–639
Publication date:
2009-09-01
Acceptance date:
2009-05-28
DOI:
ISSN:
1552-4469 and 1552-4450
Pmid:
19668195
Language:
English
Keywords:
Pubs id:
pubs:640322
UUID:
uuid:1c66249e-d9a0-4845-a7c8-8023c68fc516
Local pid:
pubs:640322
Source identifiers:
640322
Deposit date:
2016-08-24

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