A new pyridoxal-5-phosphate （PLP） derivative FHMDP was developed for the transamination of different pep- tides with three most hindered amino acid residues （Leu, Ile, Val） as their N-terminus. Compared to the pre...A new pyridoxal-5-phosphate （PLP） derivative FHMDP was developed for the transamination of different pep- tides with three most hindered amino acid residues （Leu, Ile, Val） as their N-terminus. Compared to the previously reported reactions of PLP derivatives, the N-terminus transamination could be accomplished efficiently with the new compound.展开更多
We have developed a facile N-terminus helix-nucleating strategy using an unnaturally tethered aspartic acid(TD strategy). Relatively weak nuclear translocation efficiency of TD PERM limits its further biological appli...We have developed a facile N-terminus helix-nucleating strategy using an unnaturally tethered aspartic acid(TD strategy). Relatively weak nuclear translocation efficiency of TD PERM limits its further biological applications. A potent peptide inhibitor of estrogen receptor α(ER-α) with significantly increased cellular uptake and cellular distribution was developed by cell penetrating peptide attachment.The resulted peptide conjugate showed selective toxicity towards estrogen receptor positive cell lines and induced decreased transcription of estrogen receptor a downstream genes.展开更多
基金Project supported by the National Natural Science Foundation of China （Nos. 20932006 and 21002056）.
文摘A new pyridoxal-5-phosphate （PLP） derivative FHMDP was developed for the transamination of different pep- tides with three most hindered amino acid residues （Leu, Ile, Val） as their N-terminus. Compared to the previously reported reactions of PLP derivatives, the N-terminus transamination could be accomplished efficiently with the new compound.
基金financial support from the National Natural Science Foundation of China (Nos. 21778009 and 81701818 MOST2015DFA31590)the Shenzhen Science and Technology Innovation Committee (Nos. JCYJ20170412150719814 and GJHS20170310093122365)
文摘We have developed a facile N-terminus helix-nucleating strategy using an unnaturally tethered aspartic acid(TD strategy). Relatively weak nuclear translocation efficiency of TD PERM limits its further biological applications. A potent peptide inhibitor of estrogen receptor α(ER-α) with significantly increased cellular uptake and cellular distribution was developed by cell penetrating peptide attachment.The resulted peptide conjugate showed selective toxicity towards estrogen receptor positive cell lines and induced decreased transcription of estrogen receptor a downstream genes.
