A novel small-molecule compound targeting CD147 inhibits the motility and invasion of hepatocellular carcinoma cells.

ABSTRACT: CD147, a type I transmembrane glycoprotein, is highly expressed in various cancer types and plays important roles in tumor progression, especially by promoting the motility and invasion of hepatocellular carcinoma (HCC) cells. These crucial roles make CD147 an attractive target for therapeutic intervention in HCC, but no small-molecule inhibitors of CD147 have been developed to date. To identify a candidate inhibitor, we used a pharmacophore model derived from the structure of CD147 to virtually screen over 300,000 compounds. The 100 highest-ranked compounds were subjected to biological assays, and the most potent one, dubbed AC-73 (ID number: AN-465/42834501), was studied further. We confirmed that AC-73 targeted CD147 and further demonstrated it can specifically disrupt CD147 dimerizatio

SUBMITTER: Fu ZG 

PROVIDER: S-EPMC4891050 | biostudies-literature | 2016 Feb

REPOSITORIES: biostudies-literature