Zhong Shangwei, Jeong Ji-Hak, Chen Zhikang, Chen Zihua, Luo Jun-Li
The Hunan Provincial Key Lab of Precision Diagnosis and Treatment for Gastrointestinal Tumor, Xiangya Hospital, Central South University, Hunan, 410008, China; Department of Molecular Medicine, The Scripps Research Institute, Jupiter, FL 33458, USA.
Department of Molecular Medicine, The Scripps Research Institute, Jupiter, FL 33458, USA.
Transl Oncol. 2020 Jan;13(1):57-69. doi: 10.1016/j.tranon.2019.10.001. Epub 2019 Nov 27.
The tumor microenvironment (TME) is a hypoxic, acidic, and immune/inflammatory cell-enriched milieu that plays crucial roles in tumor development, growth, progression, and therapy resistance. Targeting TME is an attractive strategy for the treatment of solid tumors. Conventional cancer chemotherapies are mostly designed to directly kill cancer cells, and the effectiveness is always compromised by their penetration and accessibility to cancer cells. Small-molecule inhibitors, which exhibit good penetration and accessibility, are widely studied, and many of them have been successfully applied in clinics for cancer treatment. As TME is more penetrable and accessible than tumor cells, a lot of efforts have recently been made to generate small-molecule inhibitors that specifically target TME or the components of TME or develop special drug-delivery systems that release the cytotoxic drugs specifically in TME. In this review, we briefly summarize the recent advances of small-molecule inhibitors that target TME for the tumor treatment.
肿瘤微环境（TME）是一种富含缺氧、酸性以及免疫/炎症细胞的环境，在肿瘤的发生、生长、进展及治疗抵抗中发挥着关键作用。靶向肿瘤微环境是治疗实体瘤的一种有吸引力的策略。传统的癌症化疗大多旨在直接杀死癌细胞，但其有效性总是受到对癌细胞的渗透和可达性的影响。具有良好渗透和可达性的小分子抑制剂得到了广泛研究，其中许多已成功应用于癌症治疗的临床实践。由于肿瘤微环境比肿瘤细胞更易渗透和可达，最近人们做出了很多努力来开发特异性靶向肿瘤微环境或其组成成分的小分子抑制剂，或开发能在肿瘤微环境中特异性释放细胞毒性药物的特殊给药系统。在本综述中，我们简要总结了靶向肿瘤微环境用于肿瘤治疗的小分子抑制剂的最新进展。
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