机构：[1]Targeted Tracer Research and Development Laboratory, Institute of Respiratory Health, Frontiers Science Center for Disease-related Molecular Network, Joint Research Institution of Altitude Health, National Clinical Research Center for Geriatrics, West China Hospital, Sichuan University, Chengdu 610041, Sichuan, China.四川大学华西医院[2]College of Life Sciences, Sichuan University, Chengdu 610064, Sichuan, China.[3]State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, Sichuan University, Chengdu 610041, Sichuan, China.四川大学华西医院[4]Department of Pharmaceutical Sciences, College of Pharmacy, University of Tennessee Health Science Center, Memphis, Tennessee 38163, United States.
Toll-like receptors (TLRs) are key components of the innate immune system and serve as a crucial link between innate and acquired immunity. In addition to immune function, TLRs are involved in other important pathological processes, including tumorigenesis. TLRs have dual regulatory effects on tumor immunity by activating nuclear factor κ-B signaling pathways, which induce tumor immune evasion or enhance the antitumor immune response. Therefore, TLRs have become a popular target for cancer prevention and treatment, and TLR agonists and antagonists offer considerable potential for drug development. The TLR7 agonist imiquimod (1) has been approved by the U.S. Food and Drug Administration as a treatment for malignant skin cancer. Herein, the structure, signaling pathways, and function of the TLR family are summarized, and the structure-activity relationships associated with TLR selective and multitarget modulators and their potential application in tumor therapy are systematically discussed.
基金：
This review was supported by the National Natural Science
Foundation of China (82073318 and 81903502), the Sichuan
Science and Technology Program (2019YFS0003), and the
National Major Scientific and Technological Special Project for
Significant New Drugs Development (2018ZX09201018-021).
语种：
外文
PubmedID：
中科院(CAS)分区：
出版当年[2023]版：
大类|1 区医学
小类|1 区药物化学
最新[2023]版：
大类|1 区医学
小类|1 区药物化学
第一作者：
第一作者机构：[1]Targeted Tracer Research and Development Laboratory, Institute of Respiratory Health, Frontiers Science Center for Disease-related Molecular Network, Joint Research Institution of Altitude Health, National Clinical Research Center for Geriatrics, West China Hospital, Sichuan University, Chengdu 610041, Sichuan, China.[2]College of Life Sciences, Sichuan University, Chengdu 610064, Sichuan, China.
共同第一作者：
通讯作者：
通讯机构：[1]Targeted Tracer Research and Development Laboratory, Institute of Respiratory Health, Frontiers Science Center for Disease-related Molecular Network, Joint Research Institution of Altitude Health, National Clinical Research Center for Geriatrics, West China Hospital, Sichuan University, Chengdu 610041, Sichuan, China.[3]State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, Sichuan University, Chengdu 610041, Sichuan, China.
推荐引用方式(GB/T 7714)：
Wang Jiayu,Zhang Jifa,Wang Jiaxing,et al.Small-Molecule Modulators Targeting Toll-like Receptors for Potential Anticancer Therapeutics[J].Journal of medicinal chemistry.2023,66(10):6437-6462.doi:10.1021/acs.jmedchem.2c01655.
APA：
Wang Jiayu,Zhang Jifa,Wang Jiaxing,Hu Xinyue,Ouyang Liang&Wang Yuxi.(2023).Small-Molecule Modulators Targeting Toll-like Receptors for Potential Anticancer Therapeutics.Journal of medicinal chemistry,66,(10)
MLA：
Wang Jiayu,et al."Small-Molecule Modulators Targeting Toll-like Receptors for Potential Anticancer Therapeutics".Journal of medicinal chemistry 66..10(2023):6437-6462
医学