Discovery of a small-molecule binder of the oncoprotein gankyrin that modulates gankyrin activity in the cell.

ABSTRACT: Gankyrin is an ankyrin-repeat oncoprotein whose overexpression has been implicated in the development of many cancer types. Elevated gankyrin levels are linked to aberrant cellular events including enhanced degradation of tumour suppressor protein p53, and inhibition of gankyrin activity has therefore been identified as an attractive anticancer strategy. Gankyrin interacts with several partner proteins, and a number of these protein-protein interactions (PPIs) are of relevance to cancer. Thus, molecules that bind the PPI interface of gankyrin and interrupt these interactions are of considerable interest. Herein, we report the discovery of a small molecule termed cjoc42 that is capable of binding to gankyrin. Cell-based experiments demonstrate that cjoc42 can inhibit gankyrin activity in a

SUBMITTER: Chattopadhyay A 

PROVIDER: S-EPMC4820706 | biostudies-literature | 2016 Apr

REPOSITORIES: biostudies-literature