Chemoproteomics-Enabled Identification of 4-Oxo-β-Lactams as Inhibitors of Dipeptidyl Peptidases 8 and 9.
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ABSTRACT:
SUBMITTER: Carvalho LAR
PROVIDER: S-EPMC9828149 | biostudies-literature | 2022 Nov
REPOSITORIES: biostudies-literature
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Chemoproteomics-Enabled Identification of 4-Oxo-β-Lactams as Inhibitors of Dipeptidyl Peptidases 8 and 9.
Carvalho Luís A R LAR Ross Breyan B Fehr Lorenz L Bolgi Oguz O Wöhrle Svenja S Lum Kenneth M KM Podlesainski David D Vieira Andreia C AC Kiefersauer Reiner R Félix Rita R Rodrigues Tiago T Lucas Susana D SD Groß Olaf O Geiss-Friedlander Ruth R Cravatt Benjamin F BF Huber Robert R Kaiser Markus M Moreira Rui R
Angewandte Chemie (International ed. in English) 20221028 47
Dipeptidyl peptidases 8 and 9 (DPP8/9) have gathered interest as drug targets due to their important roles in biological processes like immunity and tumorigenesis. Elucidation of their distinct individual functions remains an ongoing task and could benefit from the availability of novel, chemically diverse and selective chemical tools. Here, we report the activity-based protein profiling (ABPP)-mediated discovery of 4-oxo-β-lactams as potent, non-substrate-like nanomolar DPP8/9 inhibitors. X-ray ...[more]
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