Session 1F: Characterization of Beta Arrestin Induced CXCR4 Internalization after Treatment with Novel Small Molecule Ligands

Chemokines are traditionally known for their roles in the inflammatory response although we now understand that they are also important in a wide variety of physiological and developmental processes A particular chemokine named stromal derived factor 1 (SDF-1) or CXCL12 and its cognate receptor CXCR4 plays a role in a number of biological processes such as embryonic development, stem cell migration, inflammation, and is associated with several diseases. CXCR4 is important in cancer metastasis and acts as a co-receptor for HIV-1 entry into cells. The CXCR4 receptor is a potential therapeutic target for a variety of diseases. Potential approaches to this aim could include the synthesis of novel small molecule and synthetic peptide ligands. There are a wide variety of small molecule and peptide antagonists for CXCR4 because inhibition of CXCR4 could be helpful for preventing HIV-1 infectivity. The discovery of effective small molecule agonists could be useful in helping to mobilize stem cell populations for transplant purposes, have useful effects in cancer biology and a host of other interesting possibilities. In order to understand the pharmacological properties of these small molecule agonists, a variety of assays such as cell internalization imaging is used characterize their molecular potential