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Characterisation of utrophin modulator SMT C1100 as a non-competitive inhibitor of firefly luciferase

Abstract:

Firefly luciferase (FLuc) is a powerful tool for molecular and cellular biology, and popular in high-throughput screening and drug discovery. However, FLuc assays have been plagued with positive and negative artefacts due to stabilisation and inhibition by small molecules from a range of chemical classes. Here we disclose Phase II clinical compound SMT C1100 for the treatment of Duchenne muscular dystrophy as an FLuc inhibitor (KD of 0.40 ± 0.15 µM). Enzyme kinetic studies using SMT C1100 and...

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Publication status:
Published
Peer review status:
Peer reviewed

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Publisher copy:
10.1016/j.bioorg.2019.103395

Authors


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Role:
Author
ORCID:
0000-0002-6987-3235
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Institution:
University of Oxford
Division:
MPLS Division
Department:
Chemistry
Sub department:
Organic Chemistry
Role:
Author
Publisher:
Elsevier Publisher's website
Journal:
Bioorganic Chemistry Journal website
Volume:
94
Article number:
103395
Publication date:
2019-10-28
Acceptance date:
2019-10-22
DOI:
EISSN:
1090-2120
ISSN:
0045-2068
Pmid:
31733898
Language:
English
Keywords:
Pubs id:
pubs:1074776
UUID:
uuid:d75fc108-26dc-4ec9-bf90-c8560e1be698
Local pid:
pubs:1074776
Source identifiers:
1074776
Deposit date:
2020-01-18

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