Discovery of a Reversible Sub‐Picomolar Thrombin Inhibitor Using DCC
An ultrapotent yet fully reversible trivalent thrombin inhibitor discovered through screening a large dynamic combinatorial library (DCL) of 125 000 members of self‐assembled fragments. The innovative approach leverages size‐exclusion‐based affinity selection, coupled with MALDI‐TOF mass spectrometry readout, enabling the full workflow to be completed ...
Millicent Dockerill +2 more
wiley +2 more sources
Neutrophil-derived serine proteases induce FOXA2-mediated autophagy dysfunction and exacerbate colitis-associated carcinogenesis via protease activated receptor 2. [PDF]
Yuan J +11 more
europepmc +1 more source
Protic molecules containing strong O─H or N─H bonds typically resist hydrogen‐atom abstraction because of the high reactivity of the resulting heteroatom‐centered radicals. However, association of the protic molecules with redox‐active Lewis acids can provide powerful hydrogen‐atom donors or proton‐coupled‐electron‐transfer reagents.
Petra Vojáčková, Armido Studer
wiley +2 more sources
New advances in understanding inhibition of myeloperoxidase and neutrophil serine proteases by two families of staphylococcal innate immune evasion proteins. [PDF]
Herdendorf TJ +5 more
europepmc +1 more source
Structural Catalytic Core in Subtilisin-like Proteins and Its Comparison to Trypsin-like Serine Proteases and Alpha/Beta-Hydrolases. [PDF]
Denesyuk AI +3 more
europepmc +1 more source
Coupling biosynthetic noncanonical amino acid production with genetic code expansion enables site‐specific incorporation of azatryptophans into PET‐degrading enzymes (PETases). By isosteric single‐atom editing of a conserved tryptophan, AzaPETases break the activity–stability trade‐off, delivering higher catalytic efficiency at elevated temperature and
Elwy H. Abdelkader +3 more
wiley +2 more sources
Proteomics of Bacterial and Mouse Extracellular Vesicles Released in the Gastrointestinal Tracts of Nutrient-Stressed Animals Reveals an Interplay Between Microbial Serine Proteases and Mammalian Serine Protease Inhibitors. [PDF]
Stentz R +8 more
europepmc +1 more source
NMR screening is a powerful method for hit detection in drug‐discovery. We designed and validated the OpenFL600 19F$^{19}{\rm F}$ NMR library to probe diverse targets, including RNA, GPCRs, kinases, and proteases. This library yields target‐specific ligands without generating promiscuous binders.
Simon H. Rüdisser +16 more
wiley +2 more sources
Homology-based identification and structural analysis of Pangasius hypophthalmus Annexins and Serine proteases to search molecules for wound healing applications. [PDF]
Avila Rodríguez MI +4 more
europepmc +1 more source

