Display Settings:

Format

Send to:

Choose Destination
See comment in PubMed Commons below
Curr Opin Drug Discov Devel. 2006 Nov;9(6):765-75.

Emerging methods in amide- and peptide-bond formation.

Author information

  • Department of Chemistry and Biochemistry, University of California, Santa Barbara, CA 93106-9510, USA. bode@chem.ucsb.edu

Abstract

Amide bonds are the key chemical connections in proteins and peptides and have a long-established presence in small-molecule therapeutics. Despite their recognized importance, amide bond synthesis relies almost solely on variants of a single reaction: the dehydrative coupling of carboxylic acids and amines. While phenomenally successful in many applications, this process requires superstoichiometric quantities of expensive reagents and precludes chemoselective ligation reactions. This review summarizes emerging chemical alternatives to amide-bond formation with particular emphasis on the development of ligation reactions that permit the coupling of unprotected peptide fragments.

PMID:
17117685
[PubMed - indexed for MEDLINE]
PubMed Commons home

PubMed Commons

0 comments
How to join PubMed Commons

    Supplemental Content

    Loading ...
    Write to the Help Desk