ANTAGONIST

作品数：271被引量：653H指数：12
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相关作者：夏霖韩桂秋杨俊伟刘志红丁惠国更多>>
相关机构：北京大学中国药科大学南京医科大学南京军区福州总医院更多>>
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Shikonin is a novel antagonist of prostaglandin E2 receptor 4 that targets myeloid-derived suppressor cells
《Genes & Diseases》2025年第3期80-83,共4页Yang Wang Naijipu Abuduaini Wenjuan Liu Yuanjun Song Zunping Ke Xilong Wang Wei Jiao Si Chen Xianhua Lin Weiwei Yu Weiqiang Lu Bo Feng Jiacheng He 
supported by the Shanghai Key Medical Specialty Program(China)(No.ZK2019A03 to Y.W.);Natural Science Research Funds of Minhang District,Shanghai,China(No.2021MHZ071 to Y.W.);Scientific Research Project funded by Shanghai Fifth People’s Hospital,Fudan University(No.2020WYZT02 to Y.W.);the National Natural Science Foundation of China(No.82373237 to B.F.,82172644 to W.Q.L);ECNU Multifunctional Platform for Innovation(011);The Instruments Sharing Platform of School of Life Science,East China Normal University.
Myeloid-derived suppressor cells(MDSCs)constitute a crucial component of the immunosuppressive tumor microenvironment.1 Prostaglandin E2 receptor 4(EP4)is involved in regulating immunosuppressive MDSC differentiation ...
关键词：myeloid derived suppressor cells prostaglandin e receptor MDSCS cancer immunotherapy EP prostaglandin e receptor ep g protein SHIKONIN 
A structure-based virtual screening identifies a novel MDM2 antagonist in the activation of the p53 signaling and inhibition of tumor growth
《Acta Pharmacologica Sinica》2025年第3期740-750,共11页Qing-yong Hu Lei Li Yu-huang Li Hai-bo Zhang Tao Deng Yang Liu Feng-tian Li Zhi-xiong Xiao Yang Cao 
supported by the National Natural Science Foundation of China(Grant numbers 81973243,81861148031,81520108020 and 31401130).
p53,a tumor suppressor protein,has a vital role in the regulation of the cell cycle,apoptosis,and DNA damage repair.The degradation of p53 is predominantly controlled by the murine double minute 2(MDM2)protein,a ubiqu...
关键词：MDM2 P53 virtual screening inhibitor 
“Relative symmetry with electronegativity of different key-groups” strategy for MRGPRX2 antagonist design and its effect on antigeninduced pulmonary inflammation
《Acta Pharmaceutica Sinica B》2025年第1期494-507,共14页Jiayu Lu Zhaomin Xia Yongjing Zhang He Wang Wen Yang Siqi Wang Nan Wang Yun Liu Huaizhen He Cheng Wang Langchong He 
supported by the National Natural Science Foundation of China(grant Nos.81930096 and 82373830).
MRGPRX2 antagonists possess the potential for the treatment of allergic rhinitis,atopic dermatitis,and chronic urticaria.Previously,we identified a class of diaryl urea(DPU)MRGPRX2 antagonists with sub-micromolar IC50...
关键词：MRGPRX2 ANTAGONIST Diaryl urea Relative symmetrywith electronegativity Antiallergicactivity Antigen-induced pulmonary inflammation Structure-activity relationships Electrostatic 
Effects of G protein-coupled receptor 55 antagonist CID16020046 on renal fibrosis in mice
《China Medical Abstracts(Internal Medicine)》2024年第4期223-224,共2页ZHANG Yu 
Objective To explore the ffects of G protein-coupled receptor 55(GPR55)antagonist CIDI 6020046 on renal fibrosis in mice,and provide a new method and idea for the treatment of renal fibrosis.Methods(1)GPR55 overexpres...
关键词：ANTAGONIST RENAL RATS 
Molecular Mechanism of Action of GPR91 Agonists and Antagonists:Insights from Molecular Dynamics Simulation
《Chemical Research in Chinese Universities》2024年第6期1201-1211,共11页ZHANG Junjie LV Lunan ZHU Haoran ZHANG Ying XU Xiaodi LONG Lanxin FU Wei 
supported by the National Natural Science Foundation of China(Nos.82073765,82273853).
G protein-coupled receptor 91(GPR91)has garnered widespread attention as a prospective therapeutic target for metabolic diseases.However,no structural data for human GPR91(hGPR91);detailed molecular mechanism of actio...
关键词：G protein-coupled receptor 91(GPR91) Mechanism of action(MOA) AGONIST ANTAGONIST Molecular dynamics(MD) 
Discovery of an enantiopure N-[2-hydroxy-3-phenyl piperazine propyl]-aromatic carboxamide derivative as highly selectiveα_(1D/1A)-adrenoceptor antagonist and homology modelling
《Chinese Chemical Letters》2024年第11期435-441,共7页Junjun Huang Ran Chen Yajian Huang Hang Zhang Anran Zheng Qing Xiao Dan Wu Ruxia Duan Zhi Zhou Fei He Wei Yi 
supported by Natural Science Foundation of Guangdong Province(Nos.2021A1515010101,2021A1515011372,2023A1515011895);National Natural Science Foundation of China(Nos.21807017,82273759,32371529);Guangzhou Medical University Scientific Research Capacity Improvement Project(No.02-410-2405104)。
α_(1)-Adrenergic receptor(AR)blockers can be effective for the treatment of benign prostatic hyperplasia/lower urinary tract symptoms(BPH/LUTS),their usage is limited by cardiovascular-related side effects that are c...
关键词：Benign prostatic hyperplasia α_(1)-AR antagonist Phenylpiperazine Homology modelling Subtype selectivity 
LPA_(1) antagonist-derived LNPs deliver A20 mRNA and promote anti-fibrotic activities
《Nano Research》2024年第10期9095-9102,共8页Jingyue Yan Diana D.Kang Chang Wang Xucheng Hou Shi Du Siyu Wang Yonger Xue Zhengwei Liu Haoyuan Li Yichen Zhong Binbin Deng David W.McComb Yizhou Dong 
the Maximizing Investigators’Research Award(No.R35GM119679);the National Institute of General Medical Sciences(No.R35GM144117);the support from the Professor Sylvan G.Frank Graduate Fellowship;the Presidential Fellowship.
Activated fibroblasts are major mediators of pulmonary fibrosis.Fibroblasts are generally found in the connective tissue but upon activation can generate excess extracellular matrix(ECM)in the lung interstitial sectio...
关键词：lysophosphatidic acid receptor 1(LPA_(1))antagonist tumor necrosis factorα-induced protein 3(A20) lung fibrosis lipid nanoparticles MRNA 
A chromatographic method for pursuing potential GPCR ligands with the capacity to characterize their intrinsic activities of regulating downstream signaling pathway
《Chinese Chemical Letters》2024年第10期425-429,共5页Ting Li Xinxin Zheng Lejing Qu Yuanyuan Ou Sai Qiao Xue Zhao Yajun Zhang Xinfeng Zhao Qian Li 
National Natural Science Foundation of China(Nos.22374116,22074118,82174088);Natural Science Basic Research Program of Shaanxi(2024JC-TBZC-21);Shaanxi Administration of Traditional Chinese Medicine(No.2022-SLRH-YQ-007)。
GPCRs are dominant targets for approved drugs and the discovery of lead compound targeting them is still challengeable.Affinity-based screening technique is a promising platform to uncover GPCR ligands.However,the int...
关键词：Intrinsic efficacy GPCR-G protein miniature Circularly permuted HaloTag High-performance receptor chromatography GTP binding Agonist/antagonist 
Neurokinin-2 receptor antagonist SR48968 induced necroptosis of myeloid leukemia cells by calcium overload-driven reactive oxygen species accumulation
《Genes & Diseases》2024年第5期33-35,共3页Zhibin Yan Xiangyu Hong Qihao Lin Leijie Wang Gang Shao Chentao Ge Ruilong Xia Caiyun Fu 
the Zhejiang Provincial Natural Science Foundation of China(No.LD22H310004);the“Pioneer”R&D program of Zhejiang,China(No.2022C03005);the National Natural Science Foundation of China(No.81770176,82204492);the Special Support Plan for Zhejiang Province High-Level Talents(China)(No.2019R52011).
Increasing evidence highlight tachykinin receptors as a prominent player in hematological malignancy.We previously revealed the proto-oncogenic role of neurokinin-1 receptor(NK-1R)in acute myeloid leukemia(AML),1 wher...
关键词：MYELOID ANTAGONIST markedly 
AGTR1 A1166C gene polymorphism is associated with the effectiveness of valsartan monotherapy in Chinese patients with essential hypertension:A retrospective analysis
《Asian Pacific Journal of Tropical Medicine》2024年第9期418-424,共7页Hanzhong Yu Lei Li Shuyao Wei Qianqian Kong Wei Nu Bo Dong Yuewu Zhao Li Wang 
Science and Technology Key Project of Xuzhou Municipal Health Commission,Jiangsu Province,China(XWKYHT20210531);Pengcheng Yingcai-Medical Young Reserve Talent Programme(XWRCHT20220013).
Objective:To investigate whether angiotensinⅡtype 1 receptor(AGTR1 A1166C)gene polymorphism was associated with the effectiveness of valsartan monotherapy in Chinese patients with essential hypertension.Methods:This ...
关键词：Essential hypertension AngiotensinⅡtype 1 receptor antagonist VALSARTAN AGTR1 A1166C Gene polymorphism 
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