[AVX Seminar] Discovery of Dipeptidyl Peptidases 8 and 9 covalent inhibitors using activity-based protein profiling and structure-based drug design
Rui Moreira, iMED - Universidade de Lisboa
| When |
07 May, 2020
from
11:00 am to 12:00 pm |
|---|---|
| Where | Zoom Webinar |
| Add event to your calendar |
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Title: Discovery of Dipeptidyl Peptidases 8 and 9 covalent inhibitors using activity-based protein profiling and structure-based drug design
Speaker: Rui Moreira
Affiliation: iMED - Universidade de Lisboa
Abstract: Dipeptidyl peptidases 8 (DPP8) and 9 (DPP9) are intracellular serine hydrolases that may have an important role as checkpoints in the modulation of the immune system. Using a comprehensive chemical proteomics profiling, we were able to deconvolute the hidden pharmacology of 4-oxo-β-lactams, showing that these covalent inhibitors potently and distinctively engage DPP8/9. Importantly, by collecting high-resolution X-ray crystal data we characterized to the atomic level a hitherto unknown mode of inhibition. Our findings enable, for the first time, the development of specific DPP8 or DPP9 effectors, which may become suitable for forthcoming medicinal chemistry and translational applications.
Zoom webinar - ITQB NOVA Virtual auditorium AVX Seminars
