CXCL1 (Gro-α, MGSA) is a chemokine functionally similar to CXCL8/IL-8, as both activate the same receptor, CXCR2. CXCL1 levels are frequently elevated in tumors compared to healthy tissue, where they play a key role in promoting cancer cell migration, angiogenesis, and neutrophil recruitment. While the involvement of CXCL1 in tumor progression is well established, its relevance to cancer therapy remains underexplored. This review examines the therapeutic potential of targeting CXCL1 and its receptor, CXCR2, in cancer treatment. It discusses anti-CXCL1 antibodies and CXCR2 antagonists, including AZD5069, SB225002, SCH-479833, navarixin/SCH-527123, ladarixin/DF2156A, and reparixin, as well as strategies to enhance CXCR2 expression in lymphocytes during adoptive cell therapy to improve immunotherapy outcomes. Particular attention is given to the role of CXCL1 in treatment resistance, including resistance to chemotherapy, radiotherapy, and anti-angiogenic therapy. Cancer therapies often upregulate CXCL1 expression, which in turn drives treatment resistance. Additionally, this review explores the contribution of CXCL1 to therapy-induced side effects, such as chemotherapy-induced metastasis, neuropathy, nephrotoxicity, diarrhea, and cardiotoxicity. CXCR2 inhibitors are well tolerated by patients in clinical trials. However, the limited number of studies evaluating these agents in combination with standard chemotherapy precludes any definitive conclusions.
CXCL1（Gro-α，MGSA）是一种功能与CXCL8/IL-8相似的趋化因子，两者均通过激活同一受体CXCR2发挥作用。相较于健康组织，肿瘤组织中CXCL1水平常显著升高，其在促进癌细胞迁移、血管生成及中性粒细胞募集过程中发挥关键作用。尽管CXCL1在肿瘤进展中的作用已较为明确，但其与癌症治疗的相关性仍待深入探索。本综述系统探讨了靶向CXCL1及其受体CXCR2在癌症治疗中的潜在价值，重点评述了抗CXCL1抗体及CXCR2拮抗剂（包括AZD5069、SB225002、SCH-479833、navarixin/SCH-527123、ladarixin/DF2156A和reparixin）的研究进展，并分析了在过继性细胞治疗中通过提升淋巴细胞CXCR2表达以增强免疫治疗效果的策略。特别关注CXCL1在治疗抵抗中的作用机制，包括对化疗、放疗及抗血管生成治疗的耐药性。值得注意的是，癌症治疗本身常会上调CXCL1表达，进而驱动治疗抵抗。此外，本文还探讨了CXCL1在治疗相关副作用（如化疗诱导的转移、神经病变、肾毒性、腹泻及心脏毒性）中的潜在作用。临床研究显示CXCR2抑制剂患者耐受性良好，但现有评估该类药物联合标准化疗的研究数量有限，尚无法得出明确结论。
肿瘤(癌症)患者之家