Immune Checkpoint PD-1/PD-L1: Is There Life Beyond Antibodies?

被引：115

作者：

Konstantinidou, Markella ^{[1
]}

Zarganes-Tzitzikas, Tryfon ^{[1
]}

Magiera-Mularz, Katarzyna ^{[2
]}

Holak, Tad A. ^{[2
,3
]}

Domling, Alexander ^{[1
]}

机构：

[1] Univ Groningen, Dept Drug Design, A Deusinglaan 1, NL-9713 AV Groningen, Netherlands

[2] Jagiellonian Univ, Fac Chem, Ingardena 3, PL-30060 Krakow, Poland

[3] Max Planck Inst Biochem, Klopferspitz 18a, D-82152 Martinsried, Germany

来源：

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION | 2018年 / 57卷 / 18期

基金：

新加坡国家研究基金会;

关键词：

antitumor agents; protein-protein interactions; PD-1; PD-L1; protein structures; PROGRAMMED DEATH-1; STRUCTURAL BASIS; CANCER-IMMUNOTHERAPY; CRYSTAL-STRUCTURE; HUMAN PD-1; CELL; INHIBITORS; BLOCKADE; LIGANDS; COMPLEX;

D O I：

10.1002/anie.201710407

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

The PD-1/PD-L1 interaction has emerged as a significant target in cancer immunotherapy. Current medications include monoclonal antibodies, which have shown impressive clinical results in the treatment of several types of tumors. The cocrystal structure of human PD-1 and PD-L1 is expected to be a valuable starting point for the design of novel inhibitors, along with the recent crystal structures with monoclonal antibodies, small molecules, and macrocycles.

引用

页码：4840 / 4848

页数：9

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