Okuma, Rika published the artcileA macrocyclic peptide library with a structurally constrained cyclopropane-containing building block leads to thiol-independent inhibitors of phosphoglycerate mutase, COA of Formula: C4H11NOS, the main research area is peptide cyclopropane macrocycle library thioether synthesis mRNA encoded; cyclopropane amino acid synthesis peptide cyclization anthelmintic agent filarial; anthelmintic drug target phosphoglycerate mutase enzyme inhibiting structure activity; DNA library sequence mutagenesis genetic code reprogramming SPR; cyclopropane; genetic code reprogramming; mRNA display; macrocyclic peptide.
Here we report the construction of an mRNA-encoded library of thioether-closed macrocyclic peptides by using an N-chloroacetyl-cyclopropane-containing exotic initiator whose structure is more constrained than the ordinary N-chloroacetyl-α-amino acid initiators. The use of such an initiator has led to a macrocycle library with significantly suppressed population of lariat-shaped species compared with the conventional libraries. We previously used a conventional library and identified a small lariat thioether-macrocycle with a tail peptide with a C-terminal free Cys whose side-chain plays an essential role in potent inhibitory activity against a parasitic model enzyme, phosphoglycerate mutase. On the other hand, the cyclopropane-containing macrocycle library has yielded a larger thioether-macrocycle lacking a free Cys residue, which exhibits potent inhibitory activity to the same enzyme with a different mode of action. This result indicates that such a cyclopropane-containing macrocycle library would allow us to access mechanistically distinct macrocycles.
Chemistry – An Asian Journal published new progress about Aminoacylation. 343338-28-3 belongs to class amides-buliding-blocks, name is (S)-2-Methylpropane-2-sulfinamide, and the molecular formula is C4H11NOS, COA of Formula: C4H11NOS.
Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics