학술논문
Thiocarbazate building blocks enable the construction of azapeptides for rapid development of therapeutic candidates
Document Type
article
Author
Ahmad Altiti; Mingzhu He; Sonya VanPatten; Kai Fan Cheng; Umair Ahmed; Pui Yan Chiu; Ibrahim T. Mughrabi; Bayan Al Jabari; Ronald M. Burch; Kirk R. Manogue; Kevin J. Tracey; Betty Diamond; Christine N. Metz; Huan Yang; LaQueta K. Hudson; Stavros Zanos; Myoungsun Son; Barbara Sherry; Thomas R. Coleman; Yousef Al-Abed
Source
Nature Communications, Vol 13, Iss 1, Pp 1-13 (2022)
Subject
Language
English
ISSN
2041-1723
Abstract
The rapid protease degradation of peptides is currently limiting their therapeutic utility. Here, the authors report functionalised thiocarbazate scaffolds as precursors of aza-amino acids that can be integrated in peptide sequences, extending their bioavailability, and demonstrate this on FSSE/P5779 and bradykinin.