Yongling Xu

China Pharmaceutical University

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Fengze Cai

Wannan Medical College

Xuebin Shen

Wannan Medical College

Le Zhou

Zunyi Normal College

Bingsong Xu

Nanjing University of Chinese Medicine

Hui Wang

Wannan Medical College

Yan Wei

Wannan Medical College

Di Li

Chinese Academy of Sciences

Hui Wang

Qingdao University of Science and Technology

Bingsong Xu

Lei Hu

Wannan Medical College

Cooperative Institutions

Wannan Medical College

China Pharmaceutical University

Chinese Academy of Sciences

Anhui Normal University

University of Science and Technology of China

University of Chinese Academy of Sciences

Shanghai Jiao Tong University

State Key Laboratory of Natural Medicine

Yangzhou University

Nanjing University of Chinese Medicine

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Discovery of Highly Potent Small-Molecule PD-1/PD-L1 Inhibitors with a Novel Scaffold for Cancer Immunotherapy

Journal of Medicinal Chemistry (2024)

Yongling Xu Huijie Du Weibo Guo Beibei Liu Wenxin Yan

Inhibition of the PD-1/PD-L1 interaction through small-molecule inhibitors is a promising therapeutic approach in cancer immunotherapy. Herein, we utilized BMS-202 as the lead compound to develop a series of novel PD-1/PD-L1 small-molecule inhibitors with a naphthyridin scaffold. Among these compounds, X14 displayed the most potent inhibitory activity for the PD-1/PD-L1 interaction (IC50 = 15.73 nM). Furthermore, X14 exhibited good binding affinity to both human PD-L1 (KD = 14.62 nM) and mouse PD-L1 (KD = 392 nM). In particular, X14 showed favorable pharmacokinetic properties (oral bioavailability, F = 58.0%). In the 4T1 (mouse breast cancer cells) syngeneic mouse model, intragastric administration of X14 at 10 mg/kg displayed significant antitumor efficacy (TGI = 66%). Mechanistic investigations revealed that X14 effectively enhanced T-cell infiltration within the tumor microenvironment. Our study demonstrates that compound X14 exhibits potential as a candidate compound for the development of orally effective small-molecule inhibitors targeting PD-1/PD-L1.

IC50

Cancer Immunotherapy

10.1021/acs.jmedchem.3c02362

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Citations (4)

Synthesis and Properties of Red-Emitting Fluorescence Probe for Viscosity Detection

Chinese Journal of Applied Chemistry (2020)

Fengze Cai Yongling Xu Zhou Le Bingsong Xu Hao Chen

10.11944/j.issn.1000-0518.2020.04.190284

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CCDC 1943582: Experimental Crystal Structure Determination

The Cambridge Structural Database (2020)

Hui Wang Yongling Xu Bingsong Xu Haohong Chen Fengze Cai

10.5517/ccdc.csd.cc237g61

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A fluorescent probe based on Ir(III) solvent complex for specific recognition of histidine in aqueous solution and the application in cell imaging

Inorganica Chimica Acta (2020)

Hui Wang Bingsong Xu Hao Chen Di Li Xuebin Shen

Live cell imaging

10.1016/j.ica.2020.119799

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Small-molecule fluorescent dyes based on benzothiazole derivatives for targeting endoplasmic reticulum and tissue imaging

Tetrahedron Letters (2020)

Hui Wang Yongling Xu Bingsong Xu Hao Chen Fengze Cai

Benzothiazole

Biocompatibility

Fluorescence-lifetime imaging microscopy

10.1016/j.tetlet.2020.151703

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Citations (12)

Novel water-soluble fluorescent probe for rapidly detecting SO2 derivatives

Chemical Papers (2019)

Hui Wang Le Zhou Fengze Cai Yongling Xu Di Li

Benzothiazole

10.1007/s11696-019-00825-7

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Citations (1)

CCDC 1943583: Experimental Crystal Structure Determination

The Cambridge Structural Database (2020)

Hui Wang Yongling Xu Bingsong Xu Hao Chen Fengze Cai

10.5517/ccdc.csd.cc237g72

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Investigation on the Ecological Climate Condition for Artificial Cultivation of Kiwifruit in Guizhou

Yongling Xu

The paper reports the investigation result of the ecological climate condition for kiwifruit growth and analyzes the change situation of growth period of kiwifruit planted in different areas,the relationships between growth of spring branch,flowering,fruit development and maturity and meteorological condition.

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