CXCR4, or C-X-C receptor type 4, is the receptor for the chemokine CXCL12 (also known as stromal derived factor-1, or SDF-1). The CXCR4/CXCL12 pathway has been shown to play an essential role in the normal trafficking of key immune cells to direct immune surveillance throughout the body. Aberrant ligand-receptor signaling causes immune suppression, blocking normal immune function.
- In cancer, CXCL12 is over-produced in the tumor microenvironment which promotes multiple mechanisms of tumor growth, progression and poor immune surveillance.
- In certain rare diseases of the immune system, genetic mutations in the CXCR4 gene result in over-active signaling, resulting in immunodeficiency.
The X4 team has combined its drug development expertise, as well as its insights into CXCR4 biology, to establish a proprietary platform for the discovery and advancement of best-in-class CXCR4 inhibitors. Our platform includes:
- Intellectual property that includes a portfolio of issued patents and pending applications related to a family of small molecules that antagonize CXCR4
- Fundamental knowledge of CXCR4 structure and function to identify molecules that demonstrate an allosteric mechanism of inhibition that may result in a prolonged biological effect
- Deep understanding of the clinical applications of CXCR4 inhibition within multi-drug cancer treatment regimens