A New Way Forward in Cancer Drug Discovery: Inhibiting the SWI/SNF Chromatin Remodelling Complex.

Zinzalla G

Chembiochem 17 (8) 677-682 [2016-04-15; online 2016-01-28]

Mutations in subunits of the SWI/SNF chromatin remodelling complex are found in 20‚ÄČ% of human cancers. At face value, this would appear to indicate that this multiprotein complex is a potent tumour suppressor. However, it has recently emerged that some mutations in the SWI/SNF complex can have a gain-of-function effect and that in other tumours, such as pancreatic cancer, leukaemia, and breast cancer, the wild-type complex is used to drive cancer. Thus, paradoxically, this "tumour suppressor" has become an attractive target for developing anticancer agents. The SWI/SNF complex makes several protein-protein interactions both within the complex and with a wide range of transcription factors, and targeting these protein-protein interactions is emerging as the best approach to modulating the activity of the complex selectively.

Affiliated researcher

PubMed 26684344

DOI 10.1002/cbic.201500565

Crossref 10.1002/cbic.201500565