Integramides A and B, two novel non-ribosomal linear peptides containing nine C(alpha)-methyl amino acids produced by fungal fermentations that are inhibitors of HIV-1 integrase |
| |
Authors: | Singh Sheo B Herath Kithsiri Guan Ziqiang Zink Deborah L Dombrowski Anne W Polishook Jon D Silverman Keith C Lingham Russell B Felock Peter J Hazuda Daria J |
| |
Affiliation: | Merck Research Laboratories, Rahway, New Jersey 07065, and West Point, Pennsylvania 19486, USA. sheo_singh@merck.com |
| |
Abstract: | [structure: see text]. Integramides A and B are two novel 16-mer linear peptides rich in C(alpha)-methyl amino acids that were isolated from fungal extracts of Dendrodochium sp. by employing a bioassay-guided isolation procedure using recombinant HIV-1 integrase. The structure and stereochemistry were elucidated by a combination of 2D NMR and ESI- and FAB-MS including MS/MS studies and by Marfey's method. Integramides A and B inhibited the coupled reaction of HIV-1 integrase with IC50 values of 17 and 10 microM, respectively. |
| |
Keywords: | |
本文献已被 PubMed 等数据库收录! |
|