TY - JOUR
T1 - Unprecedented NES non-antagonistic inhibitor for nuclear export of Rev from Sida cordifolia
AU - Tamura, Satoru
AU - Kaneko, Masafumi
AU - Shiomi, Atsushi
AU - Yang, Guang Ming
AU - Yamaura, Toshiaki
AU - Murakami, Nobutoshi
N1 - Funding Information:
This work was supported in part by Grants-in-Aid for Scientific Research (Grant No. 19590100 ) from the Ministry of Education, Science, Culture and Sports . The authors are grateful to the Shorai Foundation for Science and Technology for financial support.
PY - 2010/3/15
Y1 - 2010/3/15
N2 - Bioassay-guided separation from the MeOH extract of the South American medicinal plant Sida cordifolia resulted in isolation of (10E,12Z)-9-hydroxyoctadeca-10,12-dienoic acid (1) as an unprecedented NES non-antagonistic inhibitor for nuclear export of Rev. This mechanism of action was established by competitive experiment by the biotinylated probe derived from leptomycin B, the known NES antagonistic inhibitor. Additionally, structure-activity relationship analysis by use of the synthesized analogs clarified cooperation of several functionalities in the Rev-export inhibitory activity of 1.
AB - Bioassay-guided separation from the MeOH extract of the South American medicinal plant Sida cordifolia resulted in isolation of (10E,12Z)-9-hydroxyoctadeca-10,12-dienoic acid (1) as an unprecedented NES non-antagonistic inhibitor for nuclear export of Rev. This mechanism of action was established by competitive experiment by the biotinylated probe derived from leptomycin B, the known NES antagonistic inhibitor. Additionally, structure-activity relationship analysis by use of the synthesized analogs clarified cooperation of several functionalities in the Rev-export inhibitory activity of 1.
KW - (10E,12Z)-9-hydroxyoctadeca-10,12-dienoic acid
KW - Anti-HIV
KW - NES non-antagonistic inhibitor
KW - Rev-export inhibitor
KW - Sida cordifolia
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U2 - 10.1016/j.bmcl.2010.01.165
DO - 10.1016/j.bmcl.2010.01.165
M3 - Article
C2 - 20176483
AN - SCOPUS:77549085127
VL - 20
SP - 1837
EP - 1839
JO - Bioorganic and Medicinal Chemistry Letters
JF - Bioorganic and Medicinal Chemistry Letters
SN - 0960-894X
IS - 6
ER -