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Small molecule CD38 inhibitors: synthesis of 8-amino-N1-inosine 5'-monophosphate, analogues and early structure-activity relationship

Abstract:

Although a monoclonal antibody targeting the multifunctional ectoenzyme CD38 is an FDA approved drug, few small molecule inhibitors exist for this enzyme that catalyzes inter alia the formation and metabolism of the N1-ribosylated, Ca2+ -mobilizing, second messenger cyclic adenosine 5'-diphosphoribose (cADPR). N1- Inosine 5′-monophosphate (N1-IMP) is a fragment directly related to cADPR. 8-Substituted-N1-IMP derivatives, prepared by degradation of cyclic parent compounds, inhibit CD38-mediate...

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Publication status:
Published
Peer review status:
Peer reviewed

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Publisher copy:
10.3390/molecules26237165

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Institution:
University of Oxford
Division:
MSD
Sub department:
Pharmacology
Oxford college:
University College
Role:
Author
ORCID:
0000-0003-3255-9135
Publisher:
MDPI Publisher's website
Journal:
Molecules Journal website
Volume:
26
Issue:
23
Article number:
7165
Publication date:
2021-11-26
Acceptance date:
2021-11-24
DOI:
EISSN:
1420-3049
Language:
English
Keywords:
Pubs id:
1212020
Local pid:
pubs:1212020
Deposit date:
2021-11-24

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