Three-dimensional solution structure of EM703 with potent promoting activity of monocyte-to-macrophage differentiation

被引：7

作者：

Gouda, H

Sunazuka, T

Yoshida, K

Sugawara, A

Sakoh, Y

Omura, S

Hirono, S

机构：

[1] Kitasato Univ, Sch Pharmaceut Sci, Minato Ku, Tokyo 1088642, Japan

[2] Kitasato Inst Life Sci, Minato Ku, Tokyo 1088641, Japan

[3] Grad Sch Infect Control Sci, Minato Ku, Tokyo 1088641, Japan

[4] Kitasato Inst, Minato Ku, Tokyo 1088642, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 09期

关键词：

erythromycin A; erythromycin derivative; immunomodulatory activity; NMR; molecular dynamics; three-dimensional solution structure; alignment; QSAR;

D O I：

10.1016/j.bmcl.2006.01.079

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

EM703, which is an erythromycin derivative synthesized by Our group, has a potent promoting activity of monocyte-to-macrophage differentiation in vitro. Its activity is approximately 300 times higher than that of erythromycin A (EM-A). In this study, we determined three-dimensional (3D) solution structures of EM703 and EM-A, and compared them using a superposition method, in order to investigate the 3D structure-activity relationship. We found a distinct difference between the 3D structures of these molecules, which might be an important factor in their divergent activities. (C) 2006 Elsevier Ltd. All rights reserved.

引用

页码：2496 / 2499

页数：4

共 13 条

[1] CROSS RELAXATION WITHOUT TOCSY - TRANSVERSE ROTATING-FRAME OVERHAUSER EFFECT SPECTROSCOPY [J].