In this review, we highlight the studies of CXCR4-targeted small-molecule and peptide HIV-1 entry inhibitors discovered during the last two decades and provide a reference for further potential HIV-1 exploration in the future.

HIV病毒除了需要通过结合 CD4受体 进入人体细胞，还需要两个辅助受体，分别是CCR5和CXCR4. 这两个辅助受体只要存在一个，人体细胞即可能感染艾滋病毒 [1]。 利用何种辅助受体侵入细胞决定HIV病毒株的嗜性。 单核细胞／巨噬细胞嗜性的病毒株利用CCR5侵入细胞，称为R5嗜性；T细胞嗜性的病毒株利用趋化CXCR4侵入细胞，称为X4嗜性；而既能利用CCR5，又能利用CXCR4侵入细胞的病毒株称为R5/X4嗜性。 此外，HIV病毒与何种辅助受体结合是随着侵入靶 …

通过与细胞膜上的这两个蛋白质的结合，病毒颗粒将自己固定在cd4+t细胞的表面。因这个缘故，ccr5/cxcr4也被称为hiv的“共受体”（coreceptor，相对于cd4来说）。此外，ccr1，ccr2b，ccr3，ccr4，ccr8，ccr9，ccr5与cxcr4等也都可以作为hiv的共受体，但ccr5与cxcr4是主要的。

2024年12月16日 · 鉴于cxcr4在hiv感染中的核心作用，研发针对cxcr4的抑制剂成为了抗艾滋病药物研发的新方向。 这类药物通过阻断HIV与CXCR4的结合，有效阻止了病毒的入侵，为那些对传统抗病毒药物产生耐药性或治疗失败的患者提供了新的治疗选择。

The identification of CXCR4 as an HIV coreceptor triggered a wide range of research activities to investigate the biological roles of the CXCL12/CXCR4 axis. CXCL12 is a highly conserved chemokine that has 99% homology between mouse and human, allowing CXCL12 to act across species barriers.

The chemokine receptors CCR5 and CXCR4 are the two major coreceptors for HIV entry. Numerous efforts have been made to develop a new class of anti-HIV agents that target these coreceptors as an additional or alternative therapy to standard HAART.

1997年3月4日 · The chemokine receptors CXCR4 and CCR5 function as coreceptors for HIV-1 entry into CD4+ cells. During the early stages of HIV infection, viral isolates tend to use CCR5 for viral entry, while late...

2022年12月15日 · The human immunodeficiency virus type 1 (HIV-1) recognizes one of its principal coreceptors, the CXC chemokine receptor 4 (CXCR4) on the host cell via the third variable loop (V3 loop) of HIV-1 envelope glycoprotein gp120 during the viral entry process.

A protein on the surface of certain immune system cells, including CD4 T lymphocytes (CD4 cells). CXCR4 can act as a coreceptor (a second receptor binding site) for HIV when the virus enters a host cell.

The chemokine receptor CXCR4 is required for the entry of human immunodeficiency virus type 1 (HIV-1) into target cells and its expression correlates with more profound pathogenicity, rapid progression to acquired immunodeficiency syndrome (AIDS), and greater AIDS-related mortality.