Results 231 to 240 of about 4,972,291 (253)
Angewandte Chemie, EarlyView.Combining HDX‐MS and NMR enables the mapping of epitopes and paratopes in full‐length antibody complexes, revealing transient interactions and potential artifacts. ABSTRACT Recombinant biomacromolecules have significantly transformed pharmaceuticals, in particular monoclonal antibodies (mAbs) that target key areas in oncology, immunology, inflammation,
Francesca Sacco +13 more
wiley +1 more source
Angewandte Chemie, EarlyView.Modular carbohydrate‐directed labeling probes (CDLPs) convert weak carbohydrate–protein interactions into durable covalent tags in live cells without the need for multivalency or UV irradiation. Ligand binding triggers proximity‐enabled, glycan‐releasing acyl transfer to install a click handle for protein tagging and chemoproteomic profiling.
Matthew C. Russolillo +7 more
wiley +1 more source
Aromatic Pummerer‐Promoted Stereospecific Cross‐Coupling of Thiazoles With Boronic Esters
Angewandte Chemie, EarlyView.A lithiation–borylation–aromatic Pummerer (LiBAP) strategy enables stereospecific, C5‐selective C(sp2)–C(sp3) cross‐coupling of thiazoles with boronic esters. By using exocyclic sulfoxide activation to overcome the low nucleophilicity that frustrates SEAr‐type coupling, the method delivers enantioenriched alkylated thiazoles bearing a versatile C2 ...
Mark John P. Mandigma +4 more
wiley +1 more source
Angewandte Chemie, EarlyView.Strategic incorporation of unnatural amino acids transforms macrocyclic peptides into drug‐like molecules capable of engaging challenging targets. These building blocks enhance stability, permeability, and bioavailability, accelerating the development of next‐generation peptide therapeutics.
Krishna K. Sharma +5 more
wiley +1 more source
Angewandte Chemie, EarlyView.Lenacapavir, the first‐in‐class drug targeting HIV‐1 capsid, is a breakthrough drug in HIV‐1 treatment and prophylaxis. However, a single M66I mutation confers complete viral resistance to lenacapavir. We report herein the design and synthesis of innovative R2 analogs demonstrating low nM potency against HIV‐1 M66I and excellent pharmacokinetics in ...
Nicolas Jamey +13 more
wiley +1 more source