SYNTHESIS AND BIOLOGICAL-ACTIVITY OF A DESTRUXIN ANALOG - D-LAC-6 DESTRUXIN-E

Authors
CALMES M CAVELIERFRONTIN F JACQUIER R MERCADIER JL SABIL S VERDUCCI J QUIOT JM VEY A
Citation
M. Calmes et al., SYNTHESIS AND BIOLOGICAL-ACTIVITY OF A DESTRUXIN ANALOG - D-LAC-6 DESTRUXIN-E, International journal of peptide & protein research, 41(6), 1993, pp. 528-535
Citations number
47
Categorie Soggetti
Biology
Journal title
International journal of peptide & protein research → ACNP
ISSN journal
03678377
Volume
41
Issue
6
Year of publication
1993
Pages
528 - 535
Database
ISI
SICI code
0367-8377(1993)41:6<528:SABOAD>2.0.ZU;2-X
Abstract
A general strategy for the synthesis of destruxin analogues is describ ed and applied to a particular example, D-Lac-6 destruxin E. The tetra peptide Boc-Ile-N-MeVal-N-MeAla-beta-Ala-OMe (2) was chosen as the bas ic starting compound, and its preparation was optimized. This fragment was then coupled with the compound (D)Lac-Pro, and the resulting pept ide was cyclized by the DEPC or DPPA/HOBt/DMAP methods at 21 and 30% y ield, respectively. The biological activity of the analogue obtained w as established by injection to an insect host.