WebMacrocyclic peptides are an interesting molecular format for drug discovery,1combining the advantages of small-molecule and biological therapeutics: synthetic accessibility, low … WebOct 1, 2024 · Macrocycles, formally defined as compounds that contain a ring with 12 or more atoms, continue to attract great interest due to their important applications in physical, pharmacological, and environmental sciences.
Diversity-Oriented Synthesis of ERα Modulators via Mitsunobu ...
WebJan 1, 2014 · Here we describe a general synthetic platform for side-chain macrocyclization of an unprotected peptide library based on the SNAr reaction between cysteine thiolates and a new generation of highly reactive perfluoroaromatic small molecule linkers. WebMar 21, 2024 · Predicted mechanism of the macrocyclization reaction catalysed by plant asparaginyl endopeptidases (AEPs) using Sunflower Trypsin Inhibitor 1 (SFTI-1) and kalata B1 as examples. (a) Acyclic precursor peptides before cyclization are shown following processing from a preproprotein. (b) The predicted mechanism of macrocyclization … ca\u0027 9j
Affinity selection and sequencing Nature Chemical Biology
WebApr 10, 2024 · Macrocyclization, Metabolism, Potential energy Abstract Polyketide synthases (PKSs) share a subset of biosynthetic steps in construction of a polyketide, and the offload from the PKS main module of specific product release is most often catalyzed by a thioesterase (TE). WebHere we describe a general synthetic platform for side-chain macrocyclization of an unprotected peptide library based on the S N Ar reaction between cysteine thiolates and a new generation of highly reactive perfluoroaromatic small molecule linkers. WebJun 5, 2024 · Enzymes that can catalyze the macrocyclization of linear peptide substrates have long been sought for the production of libraries of structurally diverse scaffolds via … ca\u0027 8p