AGONISM

作品数：16被引量：11H指数：2
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相关领域：医药卫生生物学更多>>
相关作者：和友金文桥更多>>
相关机构：中国科学院上海生命科学研究院更多>>
相关期刊：《World Journal of Respirology》《Acta Pharmacologica Sinica》《Pharmacology & Pharmacy》《Journal of Clinical & Translational Research》更多>>
相关基金：国家自然科学基金国家重点基础研究发展计划更多>>
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Structural basis of tethered agonism and G protein coupling of protease-activated receptors
《Cell Research》2024年第10期725-734,共10页Jia Guo Yun-Li Zhou Yixin Yang Shimeng Guo Erli You Xin Xie Yi Jiang Chunyou Mao H.Eric Xu Yan Zhan 
the National Natural Science Foundation of China(32371249/32100959/82322070 to C.M.,92353303/32141004 to Y.Z.,32171187 to Y.J.82121005 to YJ.and H.E.X.,32130022 to H.E.X.);the Ministry of Science and Technology(2019YFA050880 to Y.Z.);the"Pioneer"and"Leading Goose"R&D Program of Zhejiang(2024C03147 to Y.Z.);the Key R&D Projects of Zhejiang Province(2021C03039 to Y.Z.);the Leading Innovative and Entrepreneur Team Introduction Program of Zhejiang(2020R01006 to Y.Z.);the Zhejiang Province Natural Science Fund for Excellent Young Scholars(LR22C050002 to C.M.);the Ministry of Science and Technology(2023YFC2306800 to C.M.);the Lingang Laboratory(LG-GG-202204-01 to YJ.and H.E.X.);CAS Strategic Priority Research Program(XDB37030103 to H.E.X.);Shanghai Municipal Science and Technology Major Project(2019SHZDZX02 to H.E.X.);Shanghai Municipal Science and Technology Major Project(H.E.X.);the Fundamental Research Funds for the Central Universities(226-2022-00205 to Y.Z.).
Protease-activated receptors(PARs)are a unique group within the G protein-coupled receptor superfamily,orchestrating cellular responses to extracellular proteases via enzymatic cleavage,which triggers intracellular si...
关键词：ACTIVATION COUPLING ROTATION 
Predicting Chemical Immunotoxicity through Data-Driven QSAR Modeling of Aryl Hydrocarbon Receptor Agonism and Related Toxicity Mechanisms
《Environment & Health》2024年第7期474-485,共12页Nada J.Daood Daniel P.Russo Elena Chung Xuebin Qin Hao Zhu 
National Institute of General Medical Sciences(Grant R01GM148743);National Institute of Child Health and Human Development(Grant UHD113039);National Science Foundation(Grant 2402311);National Institute of Environmental Health Sciences(Grants R01ES031080 and R35ES031709).
Computational modeling has emerged as a time-saving and cost-effective alternative to traditional animal testing for assessing chemicals for their potential hazards.However,few computational modeling studies for immun...
关键词：IMMUNOTOXICITY QSAR Machine learning Aryl hydrocarbon receptor Data mining 
Small molecule conjugates with selective estrogen receptor β agonism promote anti-aging benefits in metabolism and skin recovery被引量：2
《Acta Pharmaceutica Sinica B》2024年第5期2137-2152,共16页Tarik Zahr Vijay K.Boda Jian Ge Lexiang Yu Zhongzhi Wu Jianwen Que Wei Li Li Qiang 
This work was supported by the Columbia University startup packages(Li Qiang and Jianwen Que)and the University of Tennessee College of Pharmacy Drug Discovery Center(Wei Li).
Estrogen is imperative to mammalian reproductivity,metabolism,and aging.However,the hormone activating estrogen receptor(ERs)αcan cause major safety concerns due to the enrichment of ERαin female tissues and certain...
关键词：Estrogen receptorβ Aging METABOLISM Skin injury Muscle metabolism Small molecule conjugates Regeneration ADIPOSITY 
Design and discovery of a highly potent ultralong-acting GLP-1 and glucagon co-agonist for attenuating renal fibrosis
《Acta Pharmaceutica Sinica B》2024年第3期1283-1301,共19页Qian Zhao Jiale Dong Han Liu Hui Chen Huan Yu Shuyin Ye Shuangjin Yu Yu Li Longhui Qiu Nazi Song Hongjiao Xu Qi Liu Zhiteng Luo Yuyi Li Rui Wang Guodong Chen Xianxing Jiang 
financial support from the National Natural Science Foundation of China(No.82273761 and No.81871257);the Medical Innovation and Development Project of Lanzhou University(lzuyxcx-2022-156,China);the Undergraduate Teaching Quality Engineering Project of Sun Yat-sen University[2021]93;the Guangdong Provincial Key Laboratory of Construction Foundation(2023B1212060022,China)。
The role of co-agonists of glucagon-like peptide-1 receptor(GLP-1R)and glucagon receptor(GCGR)in chronic kidney disease(CKD)remains unclear.Herein we found that GLP-1R and GCGR expression levels were lower in the kidn...
关键词：GLP-1 receptor Glucagon receptor Chronic kidney disease Diabetic nephropathy Kidney fibrosis Dual-agonism 
Pramipexole in Treatment Resistant Depression: A Case Review
《Pharmacology & Pharmacy》2023年第7期223-227,共5页Nada Abdallah Jeffrey Kahn 
Pramipexole is a dopamine agonist used in the treatment of Parkinson’s disease and Restless legs syndrome. Although off-label, the use of Pramipexole as an adjunct therapy in treatment resistant depression has recent...
关键词：PRAMIPEXOLE Treatment Resistant Depression Augmentation Dopamine Agonism Geriatric Psychiatry 
SIRT1 activation synergizes with FXR agonism in hepatoprotection via governing nucleocytoplasmic shuttling and degradation of FXR被引量：4
《Acta Pharmaceutica Sinica B》2023年第2期559-576,共18页Shuang Cui Huijian Hu An Chen Ming Cui Xiaojie Pan Pengfei Zhang Guangji Wang Hong Wang Haiping Hao 
supported by the National Natural Science Foundation of China(grants 81720108032 and 81930109 to Haiping Hao,82073926 to Hong Wang,and 82073928 to Guangji Wang);the National Key Research and Development Programme of China(2021YFA1301300 to Haiping Hao);Leading Technology Foundation Research Project of Jiangsu Province(grant BK20192005 to Guangji Wang,China);the Project Program of State Key Laboratory of Natural Medicines(China Pharmaceutical University,SKLNMZZ202202 to Haiping Hao);Sanming Project of Medicine in Shenzhen(SZSM201801060 to Guangji Wang,China)。
Farnesoid X receptor(FXR)is widely accepted as a promising target for various liver diseases;however,panels of ligands in drug development show limited clinical benefits,without a clear mechanism.Here,we reveal that a...
关键词：FXR Nuclear receptor ACETYLATION PHOSPHORYLATION Nucleocytoplasmic shuttling DEGRADATION Nonalcoholic steatohepatitis Combinatorial drugs 
Orexin receptor type 2 agonism inhibits thermogenesis in brown adipose tissue by attenuating afferent innervation
《The Journal of Biomedical Research》2022年第3期195-207,I0005,I0006,共15页Mo-qiu Jia Yong-jin Wang Kang Fu Han Jiao Jia Sun Yuanqing Gao 
supported by grants from the National Natural Science Foundation of China (Grants No. 31800971 and 81873654)
Orexin signaling has been associated with energy expenditure and brown adipose tissue(BAT)function.However,conflicting data exist in the field about how orexin signaling regulates BAT thermogenesis.In this study,we sh...
关键词：orexin receptor type 2 brown adipose tissue THERMOGENESIS 
Molecular dynamics simulations on RORγt:insights into its functional agonism and inverse agonism被引量：1
《Acta Pharmacologica Sinica》2019年第11期1480-1489,共10页Cong-min Yuan Hai-hong Chen Nan-nan Sun Xiao-jun Ma Jun Xu Wei Fu 
grants from the National Natural Science Foundation of China(Nos.81473136 and 81773635);We thank Dr.Xiao-qin Huang from Rice University(Houston,TX 77005,USA)for great help and discussion about the overall research design and final writing of this work.
The retinoic acid receptor-related orphan receptor(ROR)γt receptor is a member of nuclear receptors,which is indispensable for the expression of pro-in?ammatory cytokine IL-17.RORγt has been established as a drug ta...
关键词：RORΓT molecular dynamics simulation AGONISM inverse AGONISM PROTEIN-BINDING SITE orthosteric-binding pocket allosteric-binding SITE 
Discovery of β-arrestin-biased β2-adrenoceptor agonists from 2-amino-2-phenylethanol derivatives被引量：2
《Acta Pharmacologica Sinica》2019年第8期1095-1105,共11页Yiu-Ho Woo Xin-yue Ge Li Pan Gang Xing Yong-mei Mo Rui-juan Xing Xiao-ran Li Yu-yang Zhang Irving W. Wainer Mao-sheng Cheng Rui-ping Xiao 
We thank Dr. Joseph Kozocas from SRI international, California, USA for providing (R,/T)-FEN and (&R1-MNF for the analysis and Dr. Wei Liang and his team from WuXi AppTec, Shanghai, China for technical assistance in the cAMP assay. This work was supported by the Ministry of Science and Technology of the People's Republic of China under the National Key Research and Development Program of China [grant number 2018YFA0507603 (to R-PX)];the National Science and Technology Major Project [grant numbers 2013ZX09507001-001002 (to AY-HW), 2013ZX09301305-001 (to LP), 2013ZX09508104 (to R-PX), 2018ZX09739009 (to M-SC)];the National Basic Research Program [grant number 2012CB518000 (to R-PX)];the National Natural Science Foundation of China [grant numbers 81673355 (to AY-HW), 81872752 (to MSC), 31521062, 81630008, 81790621 (to R-PX)];Beijing Municipal Science & Technology Commission [grant number Z171100000417006 (to R-PX)], and the intramural research program of the NIH, USA (to IWW).
β-Arrestins are a small family of proteins important for signal transduction at G protein-coupled receptors (GPCRs).β-Arrestins are involved in the desensitization of GPCRs. Recently, biased ligands possessing diffe...
关键词：β2-adrenoceptor AGONISTS cAMP Β-ARRESTIN biased AGONISM FENOTEROL SALMETEROL heart failure asthma 
CB1 agonism prolongs time window for estrogen replacement therapy
《中国药理学与毒理学杂志》2018年第9期683-684,共2页ZHANG Kun LI Yan-jiao YANG Qi LI Yu-jiao YANG Le WANG Xin-shang DANG Rui-li GUAN Shao-yu GUO Yan-yan GE Xiang-wei SUN Ting WU Yu-mei LIU Shui-bing ZHAO Ming-gao 
OBJECTIVE To detect the underlying mechanism of time window for estrogen(E2)replacement treating cognitive decline.METHODS E2 begun 1 week after the ovariectomy(OVXST)or 3 months after the ovariectomy(OVXLT).Learning ...
关键词：CANNABINOID receptor1 ESTROGEN time WINDOW miRNA EPIGENETIC 
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