标题:PD-1/PD-L1 Inhibitors for Immuno-oncology: From Antibodies to Small Molecules
作者:Geng, Qiaohong; Jiao, Peifu; Jin, Peng; Su, Gaoxing; Dong, Jinlong; Yan, Bing
作者机构:[Geng, Qiaohong; Jiao, Peifu; Jin, Peng] Qilu Normal Univ, Dept Chem, Jinan 250013, Shandong, Peoples R China.; [Yan, Bing] Shandong Univ, Sch Envir 更多
通讯作者:Jiao, PF;Yan, B
通讯作者地址:[Jiao, PF]Qilu Normal Univ, Dept Chem, Jinan 250013, Shandong, Peoples R China;[Yan, B]Shandong Univ, Sch Environm Sci & Engn, Jinan 250100, Shandong, 更多
来源:CURRENT PHARMACEUTICAL DESIGN
出版年:2017
卷:23
期:39
页码:6033-6041
DOI:10.2174/1381612823666171004120152
关键词:Cancer immunotherapy; therapeutic antibody; small molecules; peptides;; structure-activity relationships; tumor cells
摘要:Background: The recent regulatory approvals of immune checkpoint protein inhibitors, such as ipilimumab, pembrolizumab, nivolumab, atezolizumab, durvalumab, and avelumab ushered a new era in cancer therapy. These inhibitors do not attack tumor cells directly but instead mobilize the immune system to re-recognize and eradicate tumors, which endows them with unique advantages including durable clinical responses and substantial clinical benefits. PD-1/PD-L1 inhibitors, a pillar of immune checkpoint protein inhibitors, have demonstrated unprecedented clinical efficacy in more than 20 cancer types. Besides monoclonal antibodies, diverse PD1/PD-L1 inhibiting candidates, such as peptides, small molecules have formed a powerful collection of weapons to fight cancer.; Methods: The goal of this review is to summarize and discuss the current PD-1/PD-L1 inhibitors including candidates under clinical development, their molecular interactions with PD-1 or PD-L1, the disclosed structure-activity relationships of peptides and small molecules as inhibitors.; Results: Current PD-1/PD-L1 inhibitors under clinical development are exclusively dominated by antibodies. The molecular interactions of therapeutic antibodies with PD-1 or PD-L1 have been gradually elucidated for the design of novel inhibitors. Various peptides and traditional small molecules have been investigated in preclinical model to discover novel PD-1/PD-L1 inhibitors.; Conclusion: Peptides and small molecules may play an important role in immuno-oncology because they may bind to multiple immune checkpoint proteins via rational design, opening opportunity for a new generation of novel PD-1/PD-L1 inhibitors.
收录类别:SCOPUS;SCIE
WOS核心被引频次:1
资源类型:期刊论文
原文链接:https://www.scopus.com/inward/record.uri?eid=2-s2.0-85043346698&doi=10.2174%2f1381612823666171004120152&partnerID=40&md5=8a527cc60a92e26f278520a1f352bb13
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