CXCR4

Chemokine (C-X-C motif) receptor 4
CXCR4 in complex with IT1t(PDB 3OE9)
有效结构 PDB 直系同源检索：PDBe, RCSB PDB查询代码列表 2K03, 2K04, 2K05, 3ODU, 3OE0, 3OE6, 3OE8, 3OE9
标识
代号	CXCR4; CD184; D2S201E; FB22; HM89; HSY3RR; LAP3; LCR1; LESTR; NPY3R; NPYR; NPYRL; NPYY3R; WHIM
扩展标识	遗传学：162643 鼠基因：109563 同源基因：20739 IUPHAR:  CXCR4 ChEMBL: 2107 GeneCards: CXCR4 Gene
基因本体论描述 分子功能 · actin binding · G-protein coupled receptor activity · protein binding · coreceptor activity · C-X-C chemokine receptor activity · C-X-C chemokine binding · ubiquitin protein ligase binding · myosin light chain binding · ubiquitin binding 细胞成分 · cytoplasm · plasma membrane · external side of plasma membrane · cell surface · integral to membrane · cytoplasmic membrane-bounded vesicle · growth cone · cell leading edge · cytoplasmic vesicle 生物过程 · activation of MAPK activity · patterning of blood vessels · response to hypoxia · ameboidal cell migration · neuron migration · dendritic cell chemotaxis · apoptotic process · inflammatory response · G-protein coupled receptor signaling pathway · elevation of cytosolic calcium ion concentration · germ cell development · brain development · motor neuron axon guidance · germ cell migration · response to virus · viral reproduction · virus-host interaction · calcium-mediated signaling · viral reproductive process · entry into host cell · regulation of cell migration · T cell proliferation · neutrophil activation · myelin maintenance · positive regulation of oligodendrocyte differentiation · regulation of chemotaxis · neural precursor cell proliferation Sources: Amigo / QuickGO
RNA表达模式
更多表达数据
直系同源体
物种	人类	小鼠
Entrez	7852	12767
Ensembl	ENSG00000121966	ENSMUSG00000045382
UniProt	P61073	P70658
mRNA序列	NM_001008540	NM_009911
蛋白序列	NP_001008540	NP_034041
基因位置	Chr 2: 136.87 – 136.88 Mb	Chr 1: 128.59 – 128.59 Mb
PubMed查询	[1]	[2]

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。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。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.