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Development and validation of a novel assay to identify radiosensitizers that target nucleophosmin 1.

Abstract：

:A series of indole analogs that are synthesized using the scaffold of a potent radiosensitizer, YTR107, were tested for their ability to alter the solubility of phosphorylated nucleophosmin 1 (pNPM1). NPM1 is critical for DNA double strand break (DSB) repair. In response to formation of DNA DSBs, phosphorylated T199 NPM1 binds to ubiquitinated chromatin, in a RNF8/RNF168-dependent manner, forming irradiation-induced foci (IRIF) that promote repair of DNA DSBs. A Western blot assay was developed using lead molecule, YTR107, for the purpose of screening newly synthesized molecules that target pNPM1 in irradiated cells. A colony formation assay was used to demonstrate the radiosensitization properties of the compounds. Compounds that enhanced the extractability of pNPM1 upon radiation treatment possessed radiosensitization properties.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Penthala NR,Crooks PA,Freeman ML,Sekhar KR

doi

10.1016/j.bmc.2015.04.018

subject

Has Abstract

pub_date

2015-07-01 00:00:00

pages

3681-6

issue

13

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(15)00315-6

journal_volume

23

pub_type

杂志文章

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