Abstract：
Chemokine receptor 4 (CXCR4) is a subtype receptor protein of the GPCR family with a seven-transmembrane structure widely distributed in human tissues. CXCR4 is involved in diseases (e.g., HIV-1 infection), cancer proliferation and metastasis, inflammation signaling pathways, and leukemia, making it a promising drug target. Clinical trials on CXCR4 antagonists mainly focused on peptides and antibodies, with a few small molecule compounds, such as AMD11070 (2) and MSX-122 (3), showing promise in cancer treatment. This perspective discusses the structure-activity relationship (SAR) of CXCR4 and its role in diseases, mainly focusing on the SAR of CXCR4 antagonists. It also explores the standard structural features and target interactions of CXCR4 binding in different disease categories. Furthermore, it investigates various modification strategies to propose potential improvements in the effectiveness of CXCR4 drugs.
摘要：
趋化因子受体4（CXCR4）是GPCR家族的一种亚型受体蛋白，具有七跨膜结构，广泛分布于人体组织中。CXCR4与疾病有关(例如，HIV-1感染），癌症增殖和转移，炎症信号通路，和白血病，使其成为有希望的药物靶标。关于CXCR4拮抗剂的临床试验主要集中在肽和抗体，有一些小分子化合物，如AMD11070(2)和MSX-122(3)，在癌症治疗中显示出希望。本文讨论了CXCR4的构效关系(SAR)及其在疾病中的作用,主要关注CXCR4拮抗剂的SAR。它还探讨了不同疾病类别中CXCR4结合的标准结构特征和靶标相互作用。此外，它研究了各种修饰策略,以提出CXCR4药物有效性的潜在改善.
