Results 61 to 70 of about 27,334 (199)

Serotonin 5‐HT7 receptor signaling in neuropsychiatric disorders

Bulletin of the Korean Chemical Society, EarlyView.
5‐HT7R recruits Gs, G12, and β‐arrestin signaling to regulate neuronal plasticity, circuit function, and kinase‐linked intracellular responses. This review summarizes how these pathway‐selective modules contribute to autism spectrum disorder, depression, and schizophrenia, highlighting 5‐HT7R as a pathway‐informed therapeutic target. Abstract Serotonin
Eunseo Park, Hyunah Choo
wiley   +1 more source

Molecular mechanisms of fentanyl mediated β-arrestin biased signaling.

PLoS Computational Biology, 2020
The development of novel analgesics with improved safety profiles to combat the opioid epidemic represents a central question to G protein coupled receptor structural biology and pharmacology: What chemical features dictate G protein or β-arrestin ...
Parker W de Waal, Jingjing Shi, Erli You, Xiaoxi Wang, Karsten Melcher, Yi Jiang, H Eric Xu, Bradley M Dickson   +7 more
doaj   +1 more source

β-Arrestin1 and 2 differentially regulate PACAP-induced PAC1 receptor signaling and trafficking. [PDF]

PLoS ONE, 2018
A pituitary adenylate cyclase-activating polypeptide (PACAP)-specific receptor, PAC1R, is coupled with multiple signal transduction pathways including stimulation of adenylate cyclase, phospholipase C and extracellular-signal regulated kinase (ERK)1/2 ...
Yusuke Shintani, Atsuko Hayata-Takano, Keita Moriguchi, Takanobu Nakazawa, Yukio Ago, Atsushi Kasai, Kaoru Seiriki, Norihito Shintani, Hitoshi Hashimoto   +8 more
doaj   +1 more source

The Serotonin 2B (5‐HT2B) Receptor: A Narrative Review of Preclinical and Clinical Evidence on the Safety Considerations and Therapeutic Potential for the Treatment of Depression

Clinical Pharmacology &Therapeutics, EarlyView.
Major depressive disorder (MDD) and treatment‐resistant depression (TRD) remain leading causes of disability, providing the impetus for receptor‐level treatment strategies beyond monoamine reuptake. The serotonin 5‐HT2B receptor (5‐HT2BR) is uniquely positioned at the interface of central‐antidepressant mechanisms and peripheral cardiac risks.
Gia Han Le, Sabrina Wong, Danica E. Johnson, Diana K. Orsini, Yang Jing Zheng, Kayla M. Teopiz, Christine E. Dri, Joshua D. Rosenblat, Roger S. McIntyre   +8 more
wiley   +1 more source

Lipids modulate the dynamics of GPCR:β-arrestin interaction

Nature Communications
β-arrestins are key molecular partners of G Protein-Coupled Receptors (GPCRs), triggering not only their desensitization but also intracellular signaling.
Antoniel A. S. Gomes, Michela Di Michele, Rita Ann Roessner, Marjorie Damian, Paulo M. Bisch, Nathalie Sibille, Maxime Louet, Jean-Louis Banères, Nicolas Floquet   +8 more
doaj   +1 more source

Imaging Ligand-Dependent Activation of CXCR7

Neoplasia: An International Journal for Oncology Research, 2009
Chemokine CXCL12 is proposed to promote multiple steps in growth of primary tumors and progression to metastatic disease in more than 20 different cancers.
Kathryn E. Luker, Mudit Gupta, Jessica M. Steele, Bradley R. Foerster, Gary D. Luker   +4 more
doaj   +1 more source

The CXCL12/CXCR4/ACKR3 Signaling Axis Regulates PKM2 and Glycolysis

Cells, 2022
In response to CXCL12, CXCR4 and ACKR3 both recruit β-arrestin 2, regulating the assembly of interacting proteins that drive signaling and contribute to the functions of both receptors in cancer and multiple other diseases.
Kathryn E. Luker, Gary D. Luker
doaj   +1 more source

Phosphorylation-induced conformation of beta(2)-adrenoceptor related to arrestin recruitment revealed by NMR [PDF]

, 2018
The C-terminal region of G-protein-coupled receptors (GPCRs), stimulated by agonist binding, is phosphorylated by GPCR kinases, and the phosphorylated GPCRs bind to arrestin, leading to the cellular responses.
Imai, Shunsuke, Iwai, Hideo, Kofuku, Yutaka, Mizukoshi, Toshimi, Nakata, Kunio, Natsume, Mei, Shimada, Ichio, Shiraishi, Yutaro, Ueda, Takumi   +8 more
core   +2 more sources

Assessment of Abuse Potential‐Related Effects of Oral Dried Kratom Leaf Powder in Healthy Normal Participants Following Single and Multiple Daily Doses

Drug Testing and Analysis, EarlyView.
In a randomized, double‐blind, placebo‐controlled study of oral dried kratom leaf powder in healthy kratom‐naive adults, no participants met the clinically meaningful opioid withdrawal threshold; abuse‐related treatment‐emergent adverse events occurred more frequently at higher doses but were generally mild and resolved without sequelae; and no serious
Marion Coe, Marilyn Huestis, Daniel Wang, Thomas Hudzik, John Bothmer, Jack Henningfield   +5 more
wiley   +1 more source

ACKR3 Regulation of Neuronal Migration Requires ACKR3 Phosphorylation, but Not β-Arrestin

Cell Reports, 2019
Summary: Phosphorylation of heptahelical receptors is thought to regulate G protein signaling, receptor endocytosis, and non-canonical signaling via recruitment of β-arrestins.
Friederike Saaber, Dagmar Schütz, Elke Miess, Philipp Abe, Srinidhi Desikan, Praveen Ashok Kumar, Sara Balk, Ke Huang, Jean Martin Beaulieu, Stefan Schulz, Ralf Stumm   +10 more
doaj   +1 more source