Please use this identifier to cite or link to this item:
Title: Identification of a polyoxometalate inhibitor of the DNA binding activity of sox2
Authors: Narasimhan, K.
Pillay, S.
Bin Ahmad, N.R.
Bikadi, Z.
Hazai, E.
Yan, L.
Kolatkar, P.R. 
Pervushin, K.
Jauch, R.
Issue Date: 17-Jun-2011
Source: Narasimhan, K., Pillay, S., Bin Ahmad, N.R., Bikadi, Z., Hazai, E., Yan, L., Kolatkar, P.R., Pervushin, K., Jauch, R. (2011-06-17). Identification of a polyoxometalate inhibitor of the DNA binding activity of sox2. ACS Chemical Biology 6 (6) : 573-581. ScholarBank@NUS Repository.
Abstract: Aberrant expression of transcription factors is a frequent cause of disease, yet drugs that modulate transcription factor protein-DNA interactions are presently unavailable. To this end, the chemical tractability of the DNA binding domain of the stem cell inducer and oncogene Sox2 was explored in a high-throughput fluorescence anisotropy screen. The screening revealed a Dawson polyoxometalate (K 6[P 2Mo 18O 62]) as a direct and nanomolar inhibitor of the DNA binding activity of Sox2. The Dawson polyoxometalate (Dawson-POM) was found to be selective for Sox2 and related Sox-HMG family members when compared to unrelated paired and zinc finger DNA binding domains. [ 15N, 1H]-Transverse relaxation optimized spectroscopy (TROSY) experiments coupled with docking studies suggest an interaction site of the POM on the Sox2 surface that enabled the rationalization of its inhibitory activity. The unconventional molecular scaffold of the Dawson-POM and its inhibitory mode provides strategies for the development of drugs that modulate transcription factors. © 2011 American Chemical Society.
Source Title: ACS Chemical Biology
ISSN: 15548929
DOI: 10.1021/cb100432x
Appears in Collections:Staff Publications

Show full item record
Files in This Item:
There are no files associated with this item.


checked on Mar 6, 2018


checked on Mar 6, 2018

Page view(s)

checked on Feb 25, 2018

Google ScholarTM



Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.