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Receptor

About: Receptor is a research topic. Over the lifetime, 159318 publications have been published within this topic receiving 8299881 citations.


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Journal ArticleDOI
02 Jun 1994-Nature
TL;DR: Evidence is presented that ERK activation is mediated by βγ subunits of heterotrimeric G proteins acting on a ras-dependent pathway.
Abstract: MITOGEN-ACTIVATED protein kinases, MAP kinases or ERKs (extracellular signal-regulated kinases) are rapidly stimulated by growth-promoting factors acting on a variety of cell-surface receptors1,2. In turn, ERKs phosphorylate and regulate key intra-cellular enzymes and transcription factors involved in the control of cellular proliferation3,4. The tyrosine-kinase class of growth-factor receptors transmits signals to ERKs in a multistep process that involves Ras and a limited number of defined molecules5. In contrast, ERK activation by G-protein-coupled receptors is poorly understood3,6, as is the role of ras in this signalling pathway7,8. We have explored in COS-7 cells the mechanism of ERKs activation by ml and m2 muscarinic receptors, typical examples of receptors coupled through Gq proteins to induce phosphatidylinositol hydrolysis and to Gi proteins to inhibit adenylyl cyclase, respectively9. Here we present evidence that ERK activation is mediated by βγ subunits of heterotrimeric G proteins acting on a ras-dependent pathway.

777 citations

Journal ArticleDOI
TL;DR: The melatonin-mediated responses elicited by activation of MT1 and MT2 native melatonin receptors are dependent on circadian time, duration and mode of exposure to endogenous or exogenous melatonin, and functional receptor sensitivity.
Abstract: Melatonin, dubbed the hormone of darkness, is known to regulate a wide variety of physiological processes in mammals. This review describes well-defined functional responses mediated through activation of high-affinity MT1 and MT2 proteinteoupled receptors viewed as potential targets for drug discovery. MT1 melatonin receptors modulate neuronal firing, arterial vasoconstriction, cell proliferation in cancer cells, and reproductive and metabolic functions. Ativation of MT2 melatonin receptors phase shift circadian rhythms of neuronal firing in the suprachiasmatic nucleus, inhibit dopamine release in retina, induce vasodilation and inhibition of leukocyte rolling in arterial beds, and enhance immune responses. The melatonin-mediated responses elicited by activation of MT1 and MT2 native melatonin receptors are dependent on circadian time, duration and mode of exposure to endogenous or exogenous melatonin, and functional receptor sensitivity. Together, these studies underscore the importance of carefully linking each melatonin receptor type to specific functional responses in target tissues to facilitate the design and development of novel therapeutic agent.

776 citations

Journal ArticleDOI
TL;DR: It is concluded that overexpression of beta1-adrenergic receptors in the heart may lead to a short-lived improvement of cardiac function, but that increasedbeta1- adrenergic receptor signalling is ultimately detrimental.
Abstract: Stimulation of cardiac β1-adrenergic receptors is the main mechanism that increases heart rate and contractility. Consequently, several pharmacological and gene transfer strategies for the prevention of heart failure aim at improving the function of the cardiac β-adrenergic receptor system, whereas current clinical treatment favors a reduction of cardiac stimulation. To address this controversy, we have generated mice with heart-specific overexpression of β1-adrenergic receptors. Their cardiac function was investigated in organ bath experiments as well as in vivo by cardiac catheterization and by time-resolved NMR imaging. The transgenic mice had increased cardiac contractility at a young age but also developed marked myocyte hypertrophy (3.5-fold increase in myocyte area). This increase was followed by progressive heart failure with functional and histological deficits typical for humans with heart failure. Contractility was reduced by ≈50% in 35-week-old mice, and ejection fraction was reduced down to a minimum of ≈20%. We conclude that overexpression of β1-adrenergic receptors in the heart may lead to a short-lived improvement of cardiac function, but that increased β1-adrenergic receptor signalling is ultimately detrimental.

775 citations

Journal Article
TL;DR: Vasoactive intestinal peptide and pituitary adenylate cyclase-activating polypeptide are members of a superfamily of structurally related peptide hormones that includes glucagon, glucagon-like peptide, secretin, and growth hormone-releasing factor (GRF).
Abstract: Vasoactive intestinal peptide (VIPb) and pituitary adenylate cyclase-activating polypeptide (PACAP) are members of a superfamily of structurally related peptide hormones that includes glucagon, glucagon-like peptide, secretin, and growth hormone-releasing factor (GRF). At least three receptors for

774 citations

Journal ArticleDOI
TL;DR: The discovery that leptin has direct effects on renal pathophysiological characteristics is discovered, which suggests that the kidney is not only a site of leptin metabolism, but also a target organ for leptin action in pathophysiology states.

773 citations


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Performance
Metrics
No. of papers in the topic in previous years
YearPapers
20241
20234,222
20226,323
20213,048
20203,388
20193,290