FC-1

FC-1 is a small molecule proteolysis-targeting chimera (PROTAC) designed to induce the selective degradation of focal adhesion kinase (FAK). Developed by researchers at Tsinghua University, FC-1 consists of a FAK-binding moiety linked to a Cereblon (CRBN) E3 ubiquitin ligase ligand. This bifunctional molecule brings FAK into close proximity with the E3 ligase complex, triggering the polyubiquitination and subsequent proteasomal degradation of the FAK protein. FAK is a non-receptor tyrosine kinase that is frequently overexpressed in various cancers, where it plays a critical role in tumor cell signaling, survival, and metastasis through both its kinase activity and its scaffolding functions. By eliminating the entire protein, FC-1 potentially offers a more comprehensive therapeutic approach than traditional kinase inhibitors, which only block enzymatic activity.

Other names

FAK-degrader 1FAK-degrader1FAK-degrader-1