Butelase-Mediated Macrocyclization of d-Amino-Acid-Containing Peptides
Butelase-Mediated Macrocyclization of d-Amino-Acid-Containing Peptides
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DOI：
10.1002/anie.201607188
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发表时间：
2016-10-04
影响因子：
16.6
通讯作者：
Tam, James P.
中科院分区：
文献类型：
--
作者：
Nguyen, Giang K. T.;Hemu, Xinya;Tam, James P.
Macrocyclic compounds have received increasing attention in recent years. With their large surface area, they hold promise for inhibiting protein-protein interactions, a chemical space that was thought to be undruggable. Although many chemical methods have been developed for peptide macrocyclization, enzymatic methods have emerged as a promising new economical approach. Thus far, most enzymes have been shown to act on l-peptides; their ability to cyclize d-amino-acid-containing peptides has rarely been documented. Herein we show that macrocycles consisting of d-amino acids, except for the Asn residue at the ligating site, were efficiently synthesized by butelase1, an Asn/Asp-specific ligase. Furthermore, by using a peptide-library approach, we show that butelase1 tolerates most of the d-amino acid residues at the P1 and P2 positions.
