整合霉肽A和B是两种新型非核糖体线性肽，由真菌发酵产生，含有9个α-甲基氨基酸，是HIV-1整合酶的抑制剂。
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.
作者信息
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
机构信息
Merck Research Laboratories, Rahway, New Jersey 07065, and West Point, Pennsylvania 19486, USA.
出版信息
Org Lett. 2002 May 2;4(9):1431-4. doi: 10.1021/ol025540a.
[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.
[结构：见正文]。整合肽A和B是两种新型的16聚体线性肽，富含α-甲基氨基酸，它们是通过使用重组HIV-1整合酶的生物测定引导分离程序从树舌菌属真菌提取物中分离得到的。通过二维核磁共振、电喷雾电离和快原子轰击质谱（包括串联质谱研究）以及马尔菲方法相结合的方式阐明了其结构和立体化学。整合肽A和B抑制HIV-1整合酶的偶联反应，半数抑制浓度（IC50）值分别为17和10微摩尔。
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