Results 1 to 10 of about 18,849 (159)

Signaling bias of the protease-activated receptor-1 is dictated by distinct GRK5 and β-arrestin-2 determinants [PDF]

Cell Reports
Summary: G protein-coupled receptors (GPCRs) exhibit signaling bias or preferential activation of heterotrimeric G proteins versus GPCR kinase (GRK)-mediated β-arrestin signaling.
Monica L. Gonzalez Ramirez, Lennis B. Orduña-Castillo, Carolyne Bardeleben, Huaping Qin, Ying Lin, Cierra A. Birch, Irina Kufareva, JoAnn Trejo   +7 more
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Rational design of a Kappa opioid receptor peptide agonist with attenuated β-arrestin signaling [PDF]

Nature Communications
Difelikefalin is an FDA-approved κ-opioid receptor (KOR) peptide agonist used to treat chronic pruritus. However, as a balanced agonist that activates both G protein and β-arrestin pathways, difelikefalin remains associated with undesirable side effects ...
Huanhuan Zhang, Ruolan Wang, Pan Shi, Gaoming Wang, Qingjun Zhu, Xinheng He, Youwei Xu, Qingning Yuan, Wen Hu, Kai Wu, Yong Zheng, Li Zhou, Jun Liang, Pei Lv, Ziyan Xu, Fan Yang, Yingbin Liu, Youwen Zhuang, H. Eric Xu, Yue Wang, Changlin Tian   +20 more
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β-arrestin-1 and β-arrestin-2 Restrain MRGPRX2-Triggered Degranulation and ERK1/2 Activation in Human Skin Mast Cells

Frontiers in Allergy, 2022
As a novel receptor that efficiently elicits degranulation upon binding to one of its numerous ligands, MRGPRX2 has moved to the center of attention in mast cell (MC) research.
Zhao Wang, Zhao Wang, Zhao Wang, Zhuoran Li, Zhuoran Li, Gürkan Bal, Gürkan Bal, Kristin Franke, Kristin Franke, Torsten Zuberbier, Torsten Zuberbier, Magda Babina, Magda Babina   +12 more
doaj   +1 more source

ClickArr: a novel, high-throughput assay for evaluating β-arrestin isoform recruitment

Frontiers in Pharmacology, 2023
Background: Modern methods for quantifying signaling bias at G protein–coupled receptors (GPCRs) rely on using a single β-arrestin isoform. However, it is increasingly appreciated that the two β-arrestin isoforms have unique roles, requiring the ability ...
Alexander R. French, Alexander R. French, Yazan J. Meqbil, Yazan J. Meqbil, Richard M. van Rijn, Richard M. van Rijn, Richard M. van Rijn   +6 more
doaj   +1 more source

Exploration of beta-arrestin isoform signaling pathways in delta opioid receptor agonist-induced convulsions

Frontiers in Pharmacology, 2022
The δ-opioid receptor (δOR) has been considered as a therapeutic target in multiple neurological and neuropsychiatric disorders particularly as δOR agonists are deemed safer alternatives relative to the more abuse-liable µ-opioid receptor drugs. Clinical
Arryn T. Blaine, Arryn T. Blaine, Yiming Miao, Jinling Yuan, Sophia Palant, Rebecca J. Liu, Zhong-Yin Zhang, Zhong-Yin Zhang, Zhong-Yin Zhang, Richard. M. van Rijn, Richard. M. van Rijn, Richard. M. van Rijn, Richard. M. van Rijn   +12 more
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CXCR7 controls competition for recruitment of β-arrestin 2 in cells expressing both CXCR4 and CXCR7. [PDF]

PLoS ONE, 2014
Chemokine CXCL12 promotes growth and metastasis of more than 20 different human cancers, as well as pathogenesis of other common diseases. CXCL12 binds two different receptors, CXCR4 and CXCR7, both of which recruit and signal through the cytosolic ...
Nathaniel L Coggins, Danielle Trakimas, S Laura Chang, Anna Ehrlich, Paramita Ray, Kathryn E Luker, Jennifer J Linderman, Gary D Luker   +7 more
doaj   +1 more source

G Protein-Coupled Receptor Kinase 2 Selectively Enhances β-Arrestin Recruitment to the D₂ Dopamine Receptor through Mechanisms That Are Independent of Receptor Phosphorylation

Biomolecules, 2023
The D2 dopamine receptor (D2R) signals through both G proteins and β-arrestins to regulate important physiological processes, such as movement, reward circuitry, emotion, and cognition.
Marta Sánchez-Soto, Noelia M. Boldizsar, Kayla A. Schardien, Nora S. Madaras, Blair K. A. Willette, Laura R. Inbody, Christopher Dasaro, Amy E. Moritz, Julia Drube, Raphael S. Haider, R. Benjamin Free, Carsten Hoffman, David R. Sibley   +12 more
doaj   +1 more source

Targeted disruption of β-arrestin 2-mediated signaling pathways by aptamer chimeras leads to inhibition of leukemic cell growth. [PDF]

PLoS ONE, 2014
β-arrestins, ubiquitous cellular scaffolding proteins that act as signaling mediators of numerous critical cellular pathways, are attractive therapeutic targets because they promote tumorigenesis in several tumor models.
Jonathan W Kotula, Jinpeng Sun, Margie Li, Elizabeth D Pratico, Mark P Fereshteh, Douglas P Ahrens, Bruce A Sullenger, Jeffrey J Kovacs   +7 more
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Prognostic value of β-Arrestins in combination with glucocorticoid receptor in epithelial ovarian cancer

Frontiers in Oncology, 2023
Hormones may be key factors driving cancer development, and epidemiological findings suggest that steroid hormones play a crucial role in ovarian tumorigenesis.
Ji-Won Ryu, Ha-Yeon Shin, Hyo-Sun Kim, Gwan Hee Han, Jeong Won Kim, Hae-Nam Lee, Hanbyoul Cho, Hanbyoul Cho, Hanbyoul Cho, Joon-Yong Chung, Jae-Hoon Kim, Jae-Hoon Kim, Jae-Hoon Kim   +12 more
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High Glucose Attenuates Cardioprotective Effects of Glucagon-Like Peptide-1 Through Induction of Mitochondria Dysfunction via Inhibition of β-Arrestin-Signaling

Frontiers in Physiology, 2021
An increased vulnerability has been detected after ischemia/reperfusion injury in cardiomyocytes in diabetic patients. Glucagon-like peptide-1 (GLP-1) has been proven to have a notable cardioprotective effect in cardiomyocytes.
Xietian Pan, Chengxiang Li, Haokao Gao
doaj   +1 more source