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The CXCL12/CXCR4 Axis as a Therapeutic Target in Cancer and HIV-1 Infection

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The seven-spanning transmembrane G-protein coupled receptor CXCR4, which specifically binds to the chemokine CXCL12, is expressed on many cell types, including various types of tumour cells. CXCR4 plays a crucial role in organ-specific metastasis, directing migration of malignant cells expressing this receptor toward microenvironments where the cognate ligand is secreted. CXCL12 has a direct growth and survival-promoting effect for various cancer cells and enhances moreover tumour angiogenesis by recruiting endothelial progenitor cells to tumours. Drugs which modulate the CXCL12/CXCR4 axis are therefore promising candidates in anti-cancer therapies. CXCR4 is also a coreceptor for human immunodeficiency virus type 1 (HIV-1) X4 virus and, as such, plays an important role in virus entry into target cells. Hence, antiviral agents that bind to CXCR4 are expected to inhibit HIV-1 entry. Here we review the structure, mechanism of action and biological activity of the main CXCR4 antagonists (peptide inhibitors, non-peptide antagonists, neutralizing antibodies, modified analogues of CXCL12) and agonists (CXCL12 peptide analogues) and discuss the CXCL12/CXCR4 axis as an important target in development of anti-tumoral and anti-HIV-1 therapies.

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Keywords: 4F-benzoyl-TN14003; AMD3100; AMD3100-Based Non-Cyclam Compounds; CXCL12; CXCR4; Dipicolylamine zinc(II)-Based Compounds; Epstein-Barr virus-encoded; G-protein coupled receptor (GPCR); HIV-1; HSEFFR-CPC-RFFESH; Limulus polyphemus; Linear T140-Based Oligopeptides; T-140-Based Cyclic Pentapeptides; TC14012; TN14003; TZ14004; Tachypleus tridentatus; aberrant hematopoiesi; agonist; analogue; angiogenesis; antagonist; bone marrow; brain; cancer; chemokine receptors; cognate ligand; hematopoietic progenitor mobilization; homodimerization; human immunodeficiency virus type 1; liver; lung; lymph nodes; p-fluorobenzoylated tripeptide mimetics; peptide; peptide inhibitors; tripeptide mimetics

Document Type: Research Article

Publication date: 2011-02-01

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