Nature Communications (Nov 2022)

Thiocarbazate building blocks enable the construction of azapeptides for rapid development of therapeutic candidates

  • 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

DOI
https://doi.org/10.1038/s41467-022-34712-9
Journal volume & issue
Vol. 13, no. 1
pp. 1 – 13

Abstract

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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.