Preclinical validation of the small molecule drug quininib as a novel therapeutic for colorectal cancer.

ABSTRACT: Colorectal cancer (CRC) is a leading cause of cancer deaths. Molecularly targeted therapies (e.g. bevacizumab) have improved survival rates but drug resistance ultimately develops and newer therapies are required. We identified quininib as a small molecule drug with anti-angiogenic activity using in vitro, ex vivo and in vivo screening models. Quininib (2-[(E)-2-(Quinolin-2-yl) vinyl] phenol), is a small molecule drug (molecular weight 283.75?g/mol), which significantly inhibited blood vessel development in zebrafish embryos (p?v?₃ integrin fluorescence probe in tumours 10 days after treatment initiation, indicative of angiogenic inhibition. Furthermore, quininib reduced the expression of angiogenic genes in xenografted tumours. Collectively, these findings support further development of quininib as a novel therapeutic agent for CRC.

SUBMITTER: Murphy AG 

PROVIDER: S-EPMC5064353 | biostudies-literature | 2016 Oct

REPOSITORIES: biostudies-literature