Deprecated: Implicit conversion from float 211.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534
Deprecated: Implicit conversion from float 211.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534
Deprecated: Implicit conversion from float 211.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534
Deprecated: Implicit conversion from float 211.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534
Deprecated: Implicit conversion from float 211.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534
Deprecated: Implicit conversion from float 211.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534
Deprecated: Implicit conversion from float 245.2 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534
Deprecated: Implicit conversion from float 245.2 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534
Deprecated: Implicit conversion from float 245.2 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534
Deprecated: Implicit conversion from float 245.2 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534
Deprecated: Implicit conversion from float 245.2 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534
Deprecated: Implicit conversion from float 245.2 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534
Deprecated: Implicit conversion from float 278.79999999999995 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534
Deprecated: Implicit conversion from float 278.79999999999995 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534
Warning: imagejpeg(C:\Inetpub\vhosts\kidney.de\httpdocs\phplern\26390015
.jpg): Failed to open stream: No such file or directory in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 117 PLoS+One
2015 ; 10
(9
): e0138780
Nephropedia Template TP
gab.com Text
Twit Text FOAVip
Twit Text #
English Wikipedia
Identification of Small-Molecule Inhibitors of the HuR/RNA Interaction Using a
Fluorescence Polarization Screening Assay Followed by NMR Validation
#MMPMID26390015
Wang Z
; Bhattacharya A
; Ivanov DN
PLoS One
2015[]; 10
(9
): e0138780
PMID26390015
show ga
The human antigen R (HuR) stabilizes many mRNAs of proto-oncogene, transcription
factors, cytokines and growth factors by recognizing AU-rich elements (AREs)
presented in their 3' or 5' untranslated region (UTR). Multiple lines of
experimental evidence suggest that this process plays a key role in cancer
development. Thus, destabilizing HuR/RNA interaction by small molecules presents
an opportunity for cancer treatment/prevention. Here we present an integrated
approach to identify inhibitors of HuR/RNA interaction using a combination of
fluorescence-based and NMR-based high throughput screening (HTS). The HTS assay
with fluorescence polarization readout and Z'-score of 0.8 was used to perform a
screen of the NCI diversity set V library in a 384 well plate format. An
NMR-based assay with saturation transfer difference (STD) detection was used for
hits validation. Protein NMR spectroscopy was used to demonstrate that some hit
compounds disrupt formation of HuR oligomer, whereas others block RNA binding.
Thus, our integrated high throughput approach provides a new avenue for
identification of small molecules targeting HuR/RNA interaction.