Results 101 to 110 of about 142,523 (351)

Targeting Gi/o protein–coupled receptor signaling blocks HER2-induced breast cancer development and enhances HER2-targeted therapy

JCI Insight, 2021
GPCRs are highly desirable drug targets for human disease. Although GPCR dysfunction drives development and progression of many tumors, including breast cancer (BC), targeting individual GPCRs has limited efficacy as a cancer therapy because numerous ...
Cancan Lyu, Yuanchao Ye, Maddison M. Lensing, Kay-Uwe Wagner, Ronald J. Weigel, Songhai Chen   +5 more
doaj   +1 more source

The role of ECL2 in CGRP receptor activation: a combined modelling and experimental approach [PDF]

, 2013
The calcitonin gene-related peptide (CGRP) receptor is a complex of a calcitonin receptor-like receptor (CLR), which is a family B G-protein-coupled receptor (GPCR) and receptor activity modifying protein 1.
Alex C. Conner, Barwell J, Bruck Taddese, Christopher A. Reynolds, Conner AC, David R. Poyner, Debbie L. Hay, Harriet A. Watkins, James Barwell, Kevin J. Smith, Michael. J. Woolley, Urano D, Watkins HA, Z. Gamze Karakullukcu   +13 more
core   +2 more sources

Dual role of mitochondria in producing melatonin and driving GPCR signaling to block cytochrome c release

Proceedings of the National Academy of Sciences of the United States of America, 2017
Significance This paper describes the finding that mitochondria synthesize and release melatonin and have their selective G protein-coupled receptor (GPCR) in the outer membrane.
Y. Suofu, Wei Li, F. Jean-Alphonse, J. Jia, Nicolas K. Khattar, Jiatong Li, S. Baranov, Daniela Leronni, A. C. Mihalik, Yanqing He, E. Cecon, Vanessa L. Wehbi, Jinho Kim, Brianna E. Heath, Oxana V. Baranova, Xiaomin Wang, Matthew J. Gable, E. Kretz, Giulietta Di Benedetto, T. Lezon, Lisa M. Ferrando, Timothy M. Larkin, M. Sullivan, S. Yablonska, Jingjing Wang, M. B. Minnigh, G. Guillaumet, F. Suzenet, R. M. Richardson, S. Poloyac, D. Stolz, R. Jockers, P. Witt‐Enderby, D. Carlisle, J. Vilardaga, R. Friedlander   +35 more
semanticscholar   +1 more source

Gut Microbial Genetic Variation Prolongs Host Healthy Longevity and Remodels Metabolome and Proteome in Drosophila Melanogaster

Advanced Science, EarlyView.
This study reveals that specific genetic variations in gut‐residing Saccharomyces cerevisiae significantly extend healthspan and lifespan in Drosophila melanogaster. These mutants rejuvenate aged intestinal metabolism, upregulate mitochondrial proteins, and enhance energy pathways.
Liying Wang, Ziling Yang, Yulu Pang, Xinyue Wu, Xinrong Zhang, Tao Zhu, Xiaoyue Ding, Wei Liu, Yuan Zhou, Pengcheng Zhang, Ying Li, Zuobin Zhu   +11 more
wiley   +1 more source

Combinatorial targeting of G‐protein‐coupled bile acid receptor 1 and cysteinyl leukotriene receptor 1 reveals a mechanistic role for bile acids and leukotrienes in drug‐induced liver injury

Hepatology, EarlyView., 2022
CHIN117 is a dual cysteinyl leukotriene receptor 1 (CYSLTR1) antagonist and G‐protein‐coupled bile acid receptor 1 (GPBAR1) agonist. In the liver, GPBAR1 and CYSLTR1 are coexpressed by liver sinusoidal endothelial cells (LSECs), HSCs, circulating monocytes/macrophages, and liver resident macrophages (Kupffer cells).
Michele Biagioli, Silvia Marchianò, Cristina di Giorgio, Rosalinda Roselli, Martina Bordoni, Rachele Bellini, Bianca Fiorillo, Valentina Sepe, Bruno Catalanotti, Chiara Cassiano, Maria Chiara Monti, Eleonora Distrutti, Angela Zampella, Stefano Fiorucci   +13 more
wiley   +1 more source

Crystal structure of rhodopsin bound to arrestin by femtosecond X-ray laser. [PDF]

, 2015
G-protein-coupled receptors (GPCRs) signal primarily through G proteins or arrestins. Arrestin binding to GPCRs blocks G protein interaction and redirects signalling to numerous G-protein-independent pathways.
Barty, Anton, Basu, Shibom, Boutet, Sébastien, Caffrey, Martin, Caro, Lydia N, Carragher, Bridget, Chapman, Henry N, Cherezov, Vadim, Coe, Jesse, Conrad, Chelsie E, de Waal, Parker W, Diederichs, Kay, Dong, Yuhui, Ernst, Oliver P, Fromme, Petra, Fromme, Raimund, Gao, Xiang, Gati, Cornelius, Griffin, Patrick R, Grotjohann, Ingo, Gu, Xin, Gurevich, Vsevolod V, Han, Gye Won, He, Yuanzheng, Howe, Nicole, Hubbell, Wayne L, Ishchenko, Andrii, James, Daniel, Jiang, Hualiang, Jiang, Yi, Kang, Yanyong, Katritch, Vsevolod, Ke, Jiyuan, Kupitz, Christopher, Lee, Regina J, Li, Dianfan, Li, Jun, Lisova, Stella, Liu, Haiguang, Liu, Wei, Ma, Jinming, Melcher, Karsten, Messerschmidt, Marc, Moeller, Arne, Pal, Kuntal, Pascal, Bruce D, Potter, Clinton S, Roy-Chowdhury, Shatabdi, Spence, John CH, Standfuss, Jörg, Stevens, Raymond C, Suino-Powell, Kelly M, Tan, MH Eileen, Tan, Minjia, Van Eps, Ned, Vishnivetskiy, Sergey A, Wang, Dingjie, Wang, Meitian, Weierstall, Uwe, West, Graham M, White, Thomas A, Williams, Garth J, Xu, H Eric, Xu, Qingping, Yang, Huaiyu, Yefanov, Oleksandr, Zatsepin, Nadia A, Zhang, Chenghai, Zhao, Yingming, Zheng, Zhong, Zhi, Xiaoyong, Zhou, X Edward   +71 more
core   +1 more source

TSHR‐Targeting Nucleic Acid Aptamer Treats Graves' Ophthalmopathy via Novel Allosteric Inhibition

Advanced Science, EarlyView.
This study presents YC3, a novel inhibitory TSHR‐targeting aptamer, as a promising therapeutic for Graves' ophthalmopathy (GO). YC3 suppresses pathological phenotypes in human orbital fibroblasts and improves outcomes in GO mice by binding to a previously unidentified allosteric site on TSHR, demonstrating the potential of aptamers in advancing ...
Yanchen Zhang, Ende Wu, Weibin Liu, Ling Zeng, Neng Ling, Hongmei Wang, Zhixing Li, Shuang Yao, Tonghe Pan, Xuanwen Li, Yate Huang, Xiaojing Li, Yunhai Tu, Wentao Yan, Jianzhang Wu, Mao Ye, Wencan Wu   +16 more
wiley   +1 more source

Lactate Activates the HCAR1/β‐Arrestin2/PP2A Signaling Axis to Mediate STAT1/2 Dephosphorylation and Drive Osteosarcoma Progression

Advanced Science, EarlyView.
In the present study, it is found that in osteosarcoma, lactate‐activated HCAR1 promotes β‐arrestin 2 translocation from cytoplasm to nucleus. In the nucleus, β‐arrestin 2 recruits PP2A to the activated STAT1/2 dimers, mediating STAT1/2 dephosphorylation and inhibiting the transcription of downstream anti‐oncogenes to promote OS progression.
Zhitao Han, Qi Jia, Guangjian Bai, Zhao Li, Jin Zeng, Zhenhua Wang, Jing Zhang, Jiashi Cao, Baoquan Xin, Yonggang Liu, Jingyu Shen, Lining Wang, Xing Huang, Chunlei Zhang, Kai Tong, Fenglei Dai, Yajie Zhang, Weina Zhu, Songyi Cheng, Yuanming Chen, Xinghai Yang, Guanghui Chen, Zhenhua Zhou, Yong Ma, Weibo Liu, Ting Wang, Tielong Liu   +26 more
wiley   +1 more source

G protein-coupled receptor kinase-2 (GRK-2) regulates serotonin metabolism through the monoamine oxidase AMX-2 in Caenorhabditis elegans. [PDF]

, 2017
G protein-coupled receptors (GPCRs) regulate many animal behaviors. GPCR signaling is mediated by agonist-promoted interactions of GPCRs with heterotrimeric G proteins, GPCR kinases (GRKs), and arrestins.
Aryal, Dipendra K., Benovic, Jeffrey L., Luo, Jiansong, Nass, Richard, Wang, Jianjun, Wetsel, William C.   +5 more
core   +2 more sources

AI‐Driven De Novo Design of Ultra Long‐Acting GLP‐1 Receptor Agonists

Advanced Science, EarlyView.
De novo GLP‐1RAs can be computationally designed to exhibit extended half‐life and superior efficacy compared to Semaglutide. Abstract Peptide drugs have revolutionized modern therapeutics, offering novel treatment avenues for various diseases. Nevertheless, low design efficacy, time consumption, and high cost still hinder peptide drug design and ...
Ting Wei, Jiating Ma, Xiaochen Cui, Jiahui Lin, Zhuoqi Zheng, Liu Cheng, Taiying Cui, Xiaoqian Lin, Junjie Zhu, Xuyang Ran, Xiaokun Hong, Luke Johnston, Zhangsheng Yu, Haifeng Chen   +13 more
wiley   +1 more source