Evaluation of Peptide Ligation Strategies for the Synthesis of the Bivalent Acid-Sensing Ion Channel Inhibitor Hi1a

Org Lett. 2023 Jun 23;25(24):4439-4444. doi: 10.1021/acs.orglett.3c01346. Epub 2023 Jun 12.

Abstract

Hi1a is a naturally occurring bivalent spider-venom peptide that is being investigated as a promising molecule for limiting ischemic damage in strokes, myocardial infarction, and organ transplantation. However, the challenges associated with the synthesis and production of the peptide in large quantities have slowed the progress in this area; hence, access to synthetic Hi1a is an essential milestone for the development of Hi1a as a pharmacological tool and potential therapeutic.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, N.I.H., Intramural

MeSH terms

  • Acid Sensing Ion Channels*
  • Ischemic Stroke / physiopathology
  • Ligation
  • Myocardial Infarction / physiopathology
  • Peptides* / chemistry
  • Spider Venoms / metabolism
  • Spider Venoms / pharmacology

Substances

  • Acid Sensing Ion Channels
  • Peptides
  • Spider Venoms