TY - JOUR
T1 - Three-dimensional solution structure of EM703 with potent promoting activity of monocyte-to-macrophage differentiation
AU - Gouda, Hiroaki
AU - Sunazuka, Toshiaki
AU - Yoshida, Kiminari
AU - Sugawara, Akihiro
AU - Sakoh, Yusuke
AU - Omura, Satoshi
AU - Hirono, Shuichi
N1 - Funding Information:
This work was supported by a grant from the 21st Century COE Program, Ministry of Education, Culture, Sports, Science and Technology (MEXT) of Japan, by The Japan Science and Technology Corporation (JST), by a Grant-in-Aid for Scientific Research from the Ministry of Education, Science, Sports and Culture, Japan, by The Japan Keirin Association and by a Kitasato University Research Grant for Young Researchers (H.G.).
PY - 2006/5/1
Y1 - 2006/5/1
N2 - 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.
AB - 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.
KW - Alignment
KW - Erythromycin A
KW - Erythromycin derivative
KW - Immunomodulatory activity
KW - Molecular dynamics
KW - NMR
KW - QSAR
KW - Three-dimensional solution structure
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U2 - 10.1016/j.bmcl.2006.01.079
DO - 10.1016/j.bmcl.2006.01.079
M3 - Article
C2 - 16480872
AN - SCOPUS:33644974199
SN - 0960-894X
VL - 16
SP - 2496
EP - 2499
JO - Bioorganic and Medicinal Chemistry Letters
JF - Bioorganic and Medicinal Chemistry Letters
IS - 9
ER -