Cleavage-resistant fusion proteins of the M2 muscarinic receptor and Gαi1. Homotropic and heterotropic effects in the binding of ligands

W.-S., Amy; Dong, John Y.; Ma, Dengbo; Wells, James W.

doi:10.1016/j.bbagen.2011.03.003

Cited by 2 publications

(2 citation statements)

References 54 publications

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“…After GPCR activation by the ligand(s) the receptor rearranges, which induces signal transduction to the cytoplasmic side (Serebryany et al, 2012). According to the existence or the non existence of bound ligands to it, GPCRs have two states, high and low affinity states, which correspond to G protein-coupled and uncoupled states (Ma et al, 2011). The physical description of ligand-receptor interactions involves intermolecular forces including ionic bonds, hydrogen bonds and van der Waals forces that, all together, induce a spatial conformational change in the tertiary structure of the GPCR (Ma et al, 2002).…”

Section: Signal Transduction and Pathwaysmentioning

confidence: 99%

Targeting G protein coupled receptor-related pathways as emerging molecular therapies

Ghanemi

2015

Saudi Pharmaceutical Journal

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G protein coupled receptors (GPCRs) represent the most important targets in modern pharmacology because of the different functions they mediate, especially within brain and peripheral nervous system, and also because of their functional and stereochemical properties. In this paper, we illustrate, via a variety of examples, novel advances about the GPCR-related molecules that have been shown to play diverse roles in GPCR pathways and in pathophysiological phenomena. We have exemplified how those GPCRs' pathways are, or might constitute, potential targets for different drugs either to stimulate, modify, regulate or inhibit the cellular mechanisms that are hypothesized to govern some pathologic, physiologic, biologic and cellular or molecular aspects both in vivo and in vitro. Therefore, influencing such pathways will, undoubtedly, lead to different therapeutical applications based on the related pharmacological implications. Furthermore, such new properties can be applied in different fields. In addition to offering fruitful directions for future researches, we hope the reviewed data, together with the elements found within the cited references, will inspire clinicians and researchers devoted to the studies on GPCR's properties.

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Section: Signal Transduction and Pathwaysmentioning

confidence: 99%

Targeting G protein coupled receptor-related pathways as emerging molecular therapies

Ghanemi

2015

Saudi Pharmaceutical Journal

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“…Catecholamines act on target cells by binding to and activating G protein-coupled receptors (GPCRs), including α-adrenergic receptors (subdivided into α1 and α2 subtypes), beta-adrenergic receptors (subdivided into β1, β2, and β3 subtypes), and dopamine receptors. The activation of these receptors by catecholamines initiates a signaling cascade that involves the activation of G proteins, second messenger systems, and ultimately leads to changes in gene expression and cellular function [ 8 , 9 , 10 , 11 ].…”

Section: Introductionmentioning

confidence: 99%

Catecholamines Promote Ovarian Cancer Progression through Secretion of CXC-Chemokines

Kim,

Chang,

Lee

et al. 2023

IJMS

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Considerable evidence has accumulated in the last decade supporting the notion that chronic stress is closely related to the growth, metastasis, and angiogenesis of ovarian cancer. In this study, we analyzed the conditioned media in SKOV3 ovarian cancer cell lines treated with catecholamines to identify secreted proteins responding to chronic stress. Here, we observed that epinephrine and norepinephrine enhanced the secretion and mRNA expression of CXC-chemokines (CXCL1, 2, 3, and 8). Neutralizing antibodies to CXCL8 and CXCL8 receptor (CXCR2) inhibitors significantly reduced catecholamine-mediated invasion of SKOV3 cells. Finally, we found that the concentration of CXCL1 and CXCL8 in the plasma of ovarian cancer patients increased with stage progression. Taken together, these findings suggest that stress-related catecholamines may influence ovarian cancer progression through the secretion of CXC-chemokines.

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Cleavage-resistant fusion proteins of the M2 muscarinic receptor and Gαi1. Homotropic and heterotropic effects in the binding of ligands

Cited by 2 publications

References 54 publications

Targeting G protein coupled receptor-related pathways as emerging molecular therapies

Targeting G protein coupled receptor-related pathways as emerging molecular therapies

Catecholamines Promote Ovarian Cancer Progression through Secretion of CXC-Chemokines

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