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Competitor Analysis: CXCR and CXCL Agonists and Antagonists
La Merie, Nov 2009, Pages: 30


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The present Competitive Intelligence Report about CXCR agonists and CXCR/CXCL antagonists provides a competitor evaluation in the field of chemokine receptor CXCR or its ligands CXCL targeting molecules for tissue regeneration or treatment of cancer and inflammatory diseases of lung, skin or colon as of November 2009. Purchase of the downloadable pdf report includes a 6-month online access to the data of the report and any updates since the publication date. Credentials to access the database will be sent by e-mail and allow online work with the project data to print or export an individual report.

Chemokines, or chemotactic cytokines, and their receptors have been discovered as essential and selective mediators in leukocyte migration to inflammatory sites and to secondary lymphoid organs. Besides their functions in the immune system, they also play a critical role in tumor initiation, promotion and progression. There are four subgroups of chemokines. The CXC or alpha subgroup is one of the four and can be further subdivided in the ELR(+) and ELR(-) chemokines. Members that contain the ELR motif bind to CXC chemokine receptor 2 (CXCR2) and are angiogenic. In contrast, most of the CXC chemokines without ELR motif bind to CXCR3 and are angiostatic. An exception is the angiogenic ELR(-)CXC chemokine stromal cell-derived factor-1 (CXCL12/SDF-1), which binds to CXCR4 and CXCR7 and is implicated in tumor metastasis.

The CXC receptors and their ligands are promising targets for drug development. The first approved and marketed drug is plerixafor (AMD3100), a small molecule inhibitor of the CXCR-4/SDF-1 axis, used for stem cell mobilization. CXCR1 and CXC chemokine receptor 2 (CXCR2) are believed to be crucially involved in the direct migration and activation of leukocytes. Their ligands are supposed to play a key role in several inflammatory diseases and this makes them and their receptors attractive therapeutic targets for inflammatory diseases such as COPD, asthma, psoriasis, ulcerative colitis and rheumatoid arthritis.

The report includes a compilation of current active projects in research and development of molecules targeting chemokine receptor CXCR or its ligands CXCL. In addition, the report lists company-specific R&D pipelines of CXCR and CXCL targeting small molecules, antibodies, proteins, peptides, RNA and cells. Competitor projects are listed in a tabular format providing information on:

- Drug Codes,
- Target / Mechanism of Action,
- Class of Compound,
- Company,
- Product Category,
- Indication,
- R&D Stage and
- additional comments with a hyperlink leading to the source of information.



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