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Journal article

Ligand induced activation of human TRPM2 requires the terminal ribose of ADPR and involves Arg 1433 and Tyr 1349

Abstract:

TRPM2 is a Ca2+-permeable non-selective cation channel activated by binding of adenosine 5ʹ-diphosphoribose (ADPR) to its cytoplasmic NUDT9H domain. Activation of TRPM2 by ADPR downstream of oxidative stress has been implicated in the pathogenesis of a number of human diseases rendering TRPM2 an attractive novel target for pharmacological intervention. However, the structural basis underlying this activation is largely unknown. Since ADP alone did not activate or antagonize the channel, we us...

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Publication status:
Published
Peer review status:
Peer reviewed

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Publisher copy:
10.1042/BCJ20170091

Authors


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Institution:
University of Oxford
Division:
MSD
Department:
Pharmacology
Role:
Author
More from this funder
Funding agency for:
Potter, B
Grant:
082837
082837 to BVLP
Publisher:
Portland Press
Journal:
Biochemical Journal More from this journal
Volume:
474
Issue:
13
Pages:
2159-2175
Publication date:
2017-05-17
Acceptance date:
2017-05-15
DOI:
EISSN:
1470-8728
ISSN:
0264-6021
Keywords:
Pubs id:
pubs:695951
UUID:
uuid:5eed8820-4189-436c-812b-c806a5ffefb2
Local pid:
pubs:695951
Source identifiers:
695951
Deposit date:
2017-05-19

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