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Publication Details
AFRICAN RESEARCH NEXUS
SHINING A SPOTLIGHT ON AFRICAN RESEARCH
biochemistry, genetics and molecular biology
Optimized Fmoc solid-phase synthesis of the cysteine-rich peptide linaclotide.
Biopolymers, Volume 96, No. 1, Year 2011
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Description
Linaclotide, a small 14-mer peptide highly rich in cysteines, is currently in phase III clinical trials for the treatment of gastrointestinal disorders. The challenge in the assembly of linaclotide consists of achieving the correct and clean folding of its three disulfide bridges. For this purpose, a number of regioselective, semiregioselective, and random strategies have been studied. In addition to selecting distinct protecting groups for the thiol function, their position in the sequence, the influence of the neighboring protecting groups, as well as the order in which the disulfides fold were studied. Here we describe an optimized solid-phase synthesis of linaclotide that should allow the production of this peptide in multigram amounts. Copyright © 2010 Wiley Periodicals, Inc.
Authors & Co-Authors
Góngora-Benítez, Miriam
Spain, Barcelona
Irb Barcelona - Institute for Research in Biomedicine
Tulla-Puche, Judit
Unknown Affiliation
Paradís-Bas, Marta
Unknown Affiliation
Giraud, Matthieu
Unknown Affiliation
Alberício, Fernando
Unknown Affiliation
Statistics
Citations: 47
Authors: 5
Affiliations: 1
Identifiers
Doi:
10.1002/bip.21480
ISSN:
00063525