Results 171 to 180 of about 95,273 (247)

Discovery of a Reversible Sub‐Picomolar Thrombin Inhibitor Using DCC

open access: yesAngewandte Chemie, EarlyView.
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

Water, Alcohols, Amines, and Amides as Formal Hydrogen‐Atom‐Transfer Reagents Through Activation With Redox‐Active Lewis Acids

open access: yesAngewandte Chemie, EarlyView.
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

Isosteric Engineering of Enzymes: Overcoming Activity–Stability Trade‐Offs by Site‐Selective CH → N Substitutions

open access: yesAngewandte Chemie, EarlyView.
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

A Comprehensive 19F NMR Framework for Fragment‐Based Drug Discovery: The Validated Screening Library OpenFL600 and Efficient Affinity Ranking by CSAR

open access: yesAngewandte Chemie, EarlyView.
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

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