Fujiwara, Daisuke published the artcileChemical Modification of Phage-Displayed Helix-Loop-Helix Peptides to Construct Kinase-Focused Libraries, COA of Formula: C20H19NO4, the publication is ChemBioChem (2021), 22(24), 3406-3409, database is CAplus and MEDLINE.
Conformationally constrained peptides hold promise as mol. tools in chem. biol. and as a new modality in drug discovery. The construction and screening of a target-focused library could be a promising approach for the generation of de novo ligands or inhibitors against target proteins. Here, we have prepared a protein kinase-focused library by chem. modifying helix-loop-helix (HLH) peptides displayed on phage and subsequently tethered to adenosine. The library was screened against aurora kinase A (AurA). The selected HLH peptide Bip-3 retained the ¦Á-helical structure and bound to AurA with a KD value of 13.7 ¦ÌM. Bip-3 and the adenosine-tethered peptide Bip-3-Adc provided IC50 values of 103 ¦ÌM and 7.7 ¦ÌM, resp., suggesting that Bip-3-Adc bivalently inhibited AurA. In addition, the selectivity of Bip-3-Adc to several protein kinases was tested, and was highest against AurA. These results demonstrate that chem. modification can enable the construction of a kinase-focused library of phage-displayed HLH peptides.
ChemBioChem published new progress about 71989-31-6. 71989-31-6 belongs to catalysis-chemistry, auxiliary class Amino acide derivatives,pyrrolidine, name is Fmoc-Pro-OH, and the molecular formula is C20H19NO4, COA of Formula: C20H19NO4.
Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia