Three-dimensional solution structure of EM703 with potent promoting activity of monocyte-to-macrophage differentiation.
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.
School of Pharmaceutical Sciences, Kitasato University, 5-9-1 Shirokane, Minato-ku, Tokyo 108-8641, Japan. godah@pharm.kitasato-u.ac.jp
Hiroaki
H
Gouda
Toshiaki
T
Sunazuka
Kiminari
K
Yoshida
Akihiro
A
Sugawara
Yusuke
Y
Sakoh
Satoshi
S
Omura
Shuichi
S
Hirono
D002454:Cell Differentiation / Q000187:drug effects; D004353:Drug Evaluation, Preclinical; D004917:Erythromycin / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D006860:Hydrogen Bonding; D021621:Imaging, Three-Dimensional / Q000379:methods*; D066298:In Vitro Techniques; D008264:Macrophages / Q000187:drug effects*; D009682:Magnetic Resonance Spectroscopy; D008958:Models, Molecular; D009000:Monocytes / Q000187:drug effects*; D012996:Solutions / Q000737:chemistry; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
C509870:EM703; D012996:Solutions; D004917:Erythromycin