Department of Medicinal Chemistry, National Institute of pharmaceutical Education and Research (NIPER) - Hyderabad, Balanagar, 500037, India.
G. Pulla Reddy College of pharmacy, Hyderabad, 500028, India.
Mini Rev Med Chem. 2019;19(16):1369-1378. doi: 10.2174/1389557519666190304120821.
Galectin 1(Gal-1), a β-galactoside binding mammalian lectin of 14KDa, is implicated in many signalling pathways, immune responses associated with cancer progression and immune disorders. Inhibition of human Gal-1 has been regarded as one of the potential therapeutic approaches for the treatment of cancer, as it plays a major role in tumour development and metastasis by modulating various biological functions viz. apoptosis, angiogenesis, migration, cell immune escape. Gal-1 is considered as a biomarker in diagnosis, prognosis and treatment condition. The overexpression of Gal-1 is well established and seen in many types of cancer progression like osteosarcoma, breast, lung, prostate, melanoma, etc. Gal-1 greatly accelerates the binding kinetics of HIV-1 to susceptible cells, leading to faster viral entry and a more robust viral replication by specific binding of CD4 cells. Hence, the Gal-1 is considered a promising molecular target for the development of new therapeutic drugs for cancer and HIV. The present review laid emphasis on structural insights and functional role of Gal-1 in the disease, current Gal-1 inhibitors and future prospects in the design of specific Gal-1 inhibitors.
半乳糖凝集素 1（Gal-1）是一种 14kDa 的β-半乳糖苷结合哺乳动物凝集素，参与多种信号通路、与癌症进展和免疫紊乱相关的免疫反应。抑制人 Gal-1 已被视为治疗癌症的潜在治疗方法之一，因为它通过调节各种生物学功能（如细胞凋亡、血管生成、迁移、细胞免疫逃逸）在肿瘤发展和转移中发挥重要作用。Gal-1 被认为是诊断、预后和治疗状况的生物标志物。Gal-1 的过表达在许多类型的癌症进展中得到了很好的证实，如骨肉瘤、乳腺癌、肺癌、前列腺癌、黑色素瘤等。Gal-1 极大地加速了 HIV-1 与易感细胞的结合动力学，通过 CD4 细胞的特异性结合导致更快的病毒进入和更强的病毒复制。因此，Gal-1 被认为是开发用于治疗癌症和 HIV 的新型治疗药物的有前途的分子靶标。本综述重点介绍了 Gal-1 在疾病中的结构见解和功能作用、当前的 Gal-1 抑制剂以及设计特异性 Gal-1 抑制剂的未来前景。
