An optimized strategy for the ribosomal synthesis of thioisoindole‐bridged bicyclic (TiB) peptides is incorporated into the RaPID platform, enabling high‐throughput discovery from topologically defined TiB libraries. Proof‐of‐concept selection against TNIK identifies nanomolar‐affinity ligands with inhibitory activity, while x‐ray crystallography ...
Yue Zhang +5 more
wiley +1 more source
Exploiting Multicomponent Reactions to Drive the Development of Novel Antitubercular Agents: An Overview. [PDF]
Nunes D, Moreira R, Perry MJ, Lopes F.
europepmc +1 more source
Unnatural α-amino acid synthesis enabled by nickel-catalysed enantioselective hydrocarbamoylation of enamides via C‒H functionalisation. [PDF]
Chen X, Kramer S.
europepmc +1 more source
Discovery of Ligands for the TNFR1 Extracellular Domain Using Fragment-Based Drug Discovery. [PDF]
Chédotal H +6 more
europepmc +1 more source
Platinum Meets Pyridine: Affinity Studies of Pyridinecarboxylic Acids and Nicotinamide for Platinum-Based Drugs. [PDF]
Szefler B, Szupryczyński K, Czeleń P.
europepmc +1 more source
A multi-tiered workflow for examining organic acid profiles delineates tissue-specific changes in fatty acyl partitioning during aging. [PDF]
Zhou Z +8 more
europepmc +1 more source
X-ray Crystallography-Guided Design and Synthesis of Cyclopentyl Heteroaryl Carboxylic Acid-Based Inhibitors of the SARS-CoV-2 Nsp3 Macrodomain (Mac1). [PDF]
Wang X +16 more
europepmc +1 more source
Enzyme-catalysed synthesis of pyridines from biomass-derived feedstocks.
Sodré V +3 more
europepmc +1 more source

