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Plerixafor
Plerixafor (rINN and USAN, also known as MOZOBIL, JM 3100 and AMD3100) is a macrocyclic compound and potential fusion inhibitor. It is an antagonist (or perhaps more accurately a partial agonist) of the alpha-chemokine receptor CXCR4. Additional recommended knowledge
ResearchHIVIt was initially developed for potential use in the treatment of HIV, for its role in the blocking of CXCR4, a chemokine receptor which acts as a co-receptor for certain strains of HIV (along with the virus's main cellular receptor, CD4). However, clinical trials in patients with HIV-AIDS have to date shown relatively little useful anti-viral activity.
Mobilization of hematopoietic stem cellsHowever, the CXCR4 alpha-chemokine receptor and its ligand SDF-1 are also important in hematopoietic stem cell homing to the bone marrow and in hematopoietic stem cell quiescence. Plerixafor has been found to be a strong inducer of "mobilization" of hematopoietic stem cells from the bone marrow to the bloodstream as peripheral blood stem cells.[1] Peripheral blood stem cell mobilization, which has become extremely important as a source of hematopoietic stem cells for transplantation over the past 10 to 15 years, is generally performed using the cytokine drug G-CSF, but is ineffective in around 15 to 20% of patients. AMD3100 offers clinical promise as a drug for peripheral blood stem cell mobilization, and has recently completed Phase 3 clinical trials.[2] It is not yet in routine clinical use. Small molecule cancer therapyAMD3100 was seen to decrease metastasis in mice in several studies.[3] References
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This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Plerixafor". A list of authors is available in Wikipedia. |