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Structure-activity analysis of peptidic Chlamydia HtrA inhibitors

Abstract:

Chlamydia trachomatis high temperature requirement A (CtHtrA) is a serine protease that performs proteolytic and chaperone functions in pathogenic Chlamydiae; and is seen as a prospective drug target. This study details the strategies employed in optimizing the irreversible CtHtrA inhibitor JO146 [Boc-Val-Pro-ValP(OPh)2] for potency and selectivity. A series of adaptations both at the warhead and specificity residues P1 and P3 yielded 23 analogues, which were tested in human neutrophil elasta...

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Publication status:
Published
Peer review status:
Peer reviewed

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Publisher copy:
10.1016/j.bmc.2019.07.049

Authors


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Name:
Wellcome Trust
Grant:
106064/Z/14/Z
Publisher:
Elsevier
Journal:
Bioorganic and Medicinal Chemistry More from this journal
Volume:
27
Issue:
18
Pages:
4185-4199
Publication date:
2019-07-30
Acceptance date:
2019-07-29
DOI:
EISSN:
1464-3391
ISSN:
0968-0896
Pmid:
31395511
Language:
English
Keywords:
Pubs id:
1046196
Local pid:
pubs:1046196
Deposit date:
2020-06-12

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