Additional Programs
ChemoCentryx is currently evaluating a series of compounds that target the C5a chemo-attractant receptor, which is believed to play a role in age-related macular degeneration (AMD), rheumatoid arthritis and systemic lupus erythematosus (SLE) and other inflammatory disorders. We are also conducting preclinical evaluation of a series of anticancer compounds that target the CXCR7 chemokine receptor. ChemoCentryx's compounds are designed to selectively target this receptor, which is associated with tumor growth, with the aim of stopping cancer progression without affecting healthy cells. In addition, we have other compounds targeting novel chemokine receptors such as CCR5, CCR10, CCR12, CXCR2 and CXCR4 that we are evaluating for preclinical development.
Inflammatory disorders
A set of proteins known collectively as the complement system serves to regulate certain types of inflammatory responses. Fragments of complement proteins such as C5a can serve as chemo-attractants in that they recruit other immune system cells such as macrophages and neutrophils to the site of inflammation. C5a interacts specifically with the C5a receptor (C5aR) which belongs to the super class of G-protein coupled receptors. This class represents an attractive type of target for small molecule therapeutics. Given architectural similarities between the C5a and chemokine receptors, as well as the fact that the C5a receptor mediates migration of immune cells in a similar fashion to chemokine receptors, we used several of our proprietary EnabaLink drug discovery technologies to screen a small molecule library against the C5a receptor. We are currently optimizing the pharmacokinetics properties of the resulting lead series
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CXCR7 program in Cancer
ChemoCentryx is developing orally-administered cancer therapies targeting CXCR7, a novel chemokine receptor that combines an anti-angiogenic approach to stopping the blood supply to cancerous cells with anti-tumor activity via direct attack of tumor cells.
We have demonstrated that CXCR7 expression can directly control tumor growth in vivo. Our data show that CXCR7 regulates several important biological processes including cell survival and tumor development in in vivo models. We also established that CXCR7 promotes growth of tumors formed from breast and lung cancer cells. Tissue staining in primary human breast and lung tumor cells revealed that this receptor is highly expressed on a majority of tumor-associated blood vessels and malignant cells but not on the normal vasculature of cells surrounding those two types of tumors.
We have developed highly potent small molecule compounds for CXCR7 whose pharmacokinetic properties are being optimized further to enable their efficacy evaluation in animal models of cancer. In contrast to standard chemotherapies, which can be highly toxic, our compounds are designed to selectively target CXCR7 in an effort to halt cancer progression while minimizing detrimental effects, such as generalized immunosuppression or cytotoxicity.
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