Results 71 to 80 of about 92,511 (354)
An Alternative Mode of GPCR Transactivation: Activation of GPCRs by Adhesion GPCRs
International Journal of Molecular SciencesG protein-coupled receptors (GPCRs), critical for cellular communication and signaling, represent the largest cell surface protein family and play important roles in numerous pathophysiological processes. Consequently, GPCRs have become a primary focus in drug discovery efforts. Beyond their traditional G protein-dependent signaling pathways, GPCRs are
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Neuropeptide GPCRs in Neuroendocrinology [PDF]
Frontiers in Endocrinology, 2014 The human genome encompasses ~ 860 G protein-coupled receptors (GPCRs) including 374 non-chemosensory GPCRs. Half of these latter GPCRs recognize (neuro)peptides as natural ligands. GPCRs thus play a pivotal role in neuroendocrine communication. In particular, GPCRs are involved in the neuroendocrine control of feeding behavior, reproduction, growth ...
Vaudry, Hubert, Seong, Jae Young
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Advanced Science, EarlyView.Psychological stress activates the sympathetic–adrenal axis, elevating norepinephrine (NE) and suppressing reproductive hormones, thereby impairing male reproduction. Excess NE overactivates and desensitizes β‐adrenergic receptors (β‐ARs), triggering Sertoli cell ferroptosis and disrupting spermatogenesis.
Lingyu Zhang +12 more
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Structure of an Endosomal Signaling GPCR–G Protein–β-arrestin Mega-Complex
Nature Structural & Molecular Biology, 2019 Classically, G-protein-coupled receptors (GPCRs) are thought to activate G protein from the plasma membrane and are subsequently desensitized by β-arrestin (β-arr).
Anthony H. Nguyen +23 more
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Cardiac GPCRs: GPCR signaling in healthy and failing hearts
Biochimica et Biophysica Acta (BBA) - Biomembranes, 2007 G protein-coupled receptors (GPCRs) are widely implicated in human heart disease, making them an important target for cardiac drug therapy. The most commonly studied and clinically targeted cardiac GPCRs include the adrenergic, angiotensin, endothelin, and adenosine receptors.
Salazar, Natasha C. +2 more
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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 +16 more
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Dampening of neurotransmitter action: molecular similarity within the melatonin structure
Endocrine Regulations, 2018 Objectives. Melatonin initiates physiologic and therapeutic responses in various tissues through binding to poorly defined MT receptors regulated by G-proteins and purine nucleotides.
Williams Wynford R.
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Advanced Science, EarlyView.A proposed mechanism to explain the role of CYP4X1/sEH‐14,15‐EET‐EA system in colon cancer immune escape. 14,15‐EET‐EA, 14,15‐epoxyeicosatrienoic acid‐ethanolamide; sEH, soluble epoxide hydrolase; CYP4X1, cytochrome P450 4X1; GPR119, G‐protein coupled receptor 119; EGFR, epidermal growth factor receptor; Gs, Gαs subunit; cAMP, cyclic adenosine ...
Min Mo +10 more
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Deep hierarchical embedding for simultaneous modeling of GPCR proteins in a unified metric space
Scientific Reports, 2021 GPCR proteins belong to diverse families of proteins that are defined at multiple hierarchical levels. Inspecting relationships between GPCR proteins on the hierarchical structure is important, since characteristics of the protein can be inferred from ...
Taeheon Lee +3 more
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