CXCR4

趋化因子受体CXCR4是趋化因子基质细胞衍生因子-1（CXCL12）的特异受体Deng H, et al., Identification of a major co-receptor for primary isolates of HIV-1. Nature. 1996 Jun 20;381(6584):661-6.Oberlin E, et al., The CXC chemokine SDF-1 is the ligand for LESTR/fusin and prevents infection by T-cell-line-adapted HIV-1. Nature. 1996 Aug 29;382(6594):833，化学式为：C1844H2845O494N453S15。CXCL12对淋巴细胞有强烈的趋化作用。该受体是用来提取纯化艾滋病毒的几个趋化因子受体之一。现在还不清楚是否出现使用CXCR4的人类免疫缺乏病毒是免疫缺乏的原因还是后果。

另外，CXCR4还可能人类胚胎发育中的着床过程中起作用。

作为趋化因子受体与配体，CXCR4和CXCL12比较特殊，他们是一配一的受体配体关系。绝大数趋化因子受体有多个配体，一个趋化因子可以结合到两个或多个受体。

CXCR4的配体CXCL12在造血干细胞移居骨髓在起重要作用Zou YR, Kottmann AH, Kuroda M, Taniuchi I, Littman DR. Function of the chemokine receptor CXCR4 in haematopoiesis and in cerebellar development. Nature. 1998 Jun 11;393(6685):595-9.。影响或阻断CXCR4受体配体结合，可以调节造血干细胞的迁徙，这对骨髓造血干细胞移植可能十分有用。目前的试验药物有：粒细胞集落刺激因子（Granulocyte colony-stimulating factor）和Plerixafor（AMD3100）。但这些药物尚未临床使用。

CXCR4在体内大部分组织和器官上都有表达，它是由352个氨基酸组成的GPCR(G蛋白偶联受体)，具有七次穿膜结构。
CXCR4参与体内多种生理机制，包括参与HIV-1病毒侵染【1】，造血功能【2】，胚胎发育【3-7】，及肿瘤迁移等【8】。

 参考文献 

Dragic, T., An overview of the determinants of CCR5 and CXCR4 co-receptor function. J Gen Virol, 2001. 82(Pt 8): p. 1807-14.
Maekawa, T. and T. Ishii, Chemokine/receptor dynamics in the regulation of hematopoiesis. Intern Med, 2000. 39(2): p. 90-100.
Nagasawa, T., et al., Defects of B-cell lymphopoiesis and bone-marrow myelopoiesis in mice lacking the CXC chemokine PBSF/SDF-1. Nature, 1996. 382(6592): p. 635-8.
Tachibana, K., et al., The chemokine receptor CXCR4 is essential for vascularization of the gastrointestinal tract. Nature, 1998. 393(6685): p. 591-4.
Zou, Y.R., et al., Function of the chemokine receptor CXCR4 in haematopoiesis and in cerebellar development. Nature, 1998. 393(6685): p. 595-9.
McGrath, K.E., et al., Embryonic expression and function of the chemokine SDF-1 and its receptor, CXCR4. Dev Biol, 1999. 213(2): p. 442-56.
Lu, M., E.A. Grove, and R.J. Miller, Abnormal development of the hippocampal dentate gyrus in mice lacking the CXCR4 chemokine receptor. Proc Natl Acad Sci U S A, 2002. 99(10): p. 7090-5.
Burger, J.A. and T.J. Kipps, CXCR4: a key receptor in the crosstalk between tumor cells and their microenvironment. Blood, 2006. 107(5): p. 1761-7.

Category:细胞因子受体