TY - JOUR
T1 - Fluorescent indicator displacement assay of ligands targeting 10 microRNA precursors
AU - Murata, Asako
AU - Harada, Yasue
AU - Fukuzumi, Takeo
AU - Nakatani, Kazuhiko
N1 - Funding Information:
This work was supported by the Program for Promotion of Fundamental Studies in Health Sciences of the National Institute of Biomedical Innovation (NIBIO, 10-22) and Grant-in-Aid for Scientific Research (A) (23241073) for KN, and Grant-in-Aid for Young Scientists (B) (23710270 and 25750393) for AM. We also thank for Open Innovation Center for Drug Discovery of University of Tokyo for supplying chemical library and support for our screening.
PY - 2013/11/15
Y1 - 2013/11/15
N2 - Fluorescent indicator displacement (FID) assay is a rapid and convenient assay for identifying new ligands that bind to the target molecules. In our previous studies, we have shown that a series of 2,7-diaminoalkoxy xanthone and thioxanthone derivatives can be used as fluorescent indicators for detecting the interaction between RNA and a ligand. The xanthone and thioxanthone fluorochromes showed efficient fluorescence quenching upon binding to target RNA. Subsequent displacement of the bound-fluorochrome with a ligand that binds more strongly to the target RNA led to the recovery of the fluorescence by releasing the fluorochrome from RNA. Here we report a pilot screening of a chemical library that contains 9600 structurally diverse compounds for molecules that bind to a specific miRNA precursor using the FID assay.
AB - Fluorescent indicator displacement (FID) assay is a rapid and convenient assay for identifying new ligands that bind to the target molecules. In our previous studies, we have shown that a series of 2,7-diaminoalkoxy xanthone and thioxanthone derivatives can be used as fluorescent indicators for detecting the interaction between RNA and a ligand. The xanthone and thioxanthone fluorochromes showed efficient fluorescence quenching upon binding to target RNA. Subsequent displacement of the bound-fluorochrome with a ligand that binds more strongly to the target RNA led to the recovery of the fluorescence by releasing the fluorochrome from RNA. Here we report a pilot screening of a chemical library that contains 9600 structurally diverse compounds for molecules that bind to a specific miRNA precursor using the FID assay.
UR - http://www.scopus.com/inward/record.url?scp=84885840896&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=84885840896&partnerID=8YFLogxK
U2 - 10.1016/j.bmc.2013.09.007
DO - 10.1016/j.bmc.2013.09.007
M3 - Article
C2 - 24084297
AN - SCOPUS:84885840896
SN - 0968-0896
VL - 21
SP - 7101
EP - 7106
JO - Bioorganic and Medicinal Chemistry
JF - Bioorganic and Medicinal Chemistry
IS - 22
ER -