Constitutive Activity at the α 1 ‐Adrenoceptors: Past and Future Implications

2005 ◽  
pp. 159-176 ◽  
Author(s):  
Susanna Cotecchia ◽  
Francesca Fanelli ◽  
Alexander Scheer ◽  
Tommaso Costa
Keyword(s):  
Constitutive Activity

Involvement of the constitutive activity of the GHS-R1a (ghrelin G-protein coupled receptor) in the tumorigenesis of somatotroph adenomas

2013 ◽  
Author(s):  
Yves Louis Mear ◽  
Xavier Come Donato ◽  
Marie Pierre Blanchard ◽  
Celine Defilles ◽  
Christophe Lisbonis ◽  
...  
Keyword(s):  
G Protein ◽  
Constitutive Activity ◽  
G Protein Coupled Receptor ◽  
G Protein Coupled

scholarly journals Constitutive Activity of Serotonin Receptor 6 Regulates Human Cerebral Organoids Formation and Depression-like Behaviors

2020 ◽  
Author(s):  
Qinying Wang ◽  
Xiaoxu Dong ◽  
Tingting Hu ◽  
Chao Qu ◽  
Jing Lu ◽  
...  
Keyword(s):  
Serotonin Receptor ◽  
Constitutive Activity

scholarly journals Constitutive activity of the A2A adenosine receptor and compartmentalised cyclic AMP signalling fine-tune noradrenaline release

2012 ◽  
Vol 8 (4) ◽  
pp. 677-692 ◽  
Author(s):  
Edin Ibrisimovic ◽  
Helmut Drobny ◽  
Qiong Yang ◽  
Thomas Höfer ◽  
Stefan Boehm ◽  
...  
Keyword(s):  
Cyclic Amp ◽  
Noradrenaline Release ◽  
Adenosine Receptor ◽  
Constitutive Activity ◽  
A2a Adenosine Receptor ◽  
Fine Tune

Protein kinase CK2: a newcomer in the ‘druggable kinome’

2006 ◽  
Vol 34 (6) ◽  
pp. 1303-1306 ◽  
Author(s):  
M.A. Pagano ◽  
L. Cesaro ◽  
F. Meggio ◽  
L.A. Pinna
Keyword(s):  
Protein Kinase ◽  
Consensus Sequence ◽  
Side Chain ◽  
Constitutive Activity ◽  
Eukaryotic Protein Kinase ◽  
Pathological Conditions ◽  
Cardiovascular Pathologies ◽  
Special Circumstances ◽  
Kinase Ck2 ◽  
Different Sources

The acronym CK2 (derived from the misnomer ‘casein kinase’ 2) denotes one of the most pleiotropic members of the eukaryotic protein kinase superfamily, characterized by an acidic consensus sequence in which a carboxylic acid (or pre-phosphorylated) side chain at position n+3 relative to the target serine/threonine residue plays a crucial role. The latest repertoire of CK2 substrates includes approx. 300 proteins, but the analysis of available phosphopeptide databases from different sources suggests that CK2 alone may be responsible for the generation of a much larger proportion (10–20%) of the eukaryotic phosphoproteome. Although for the time being CK2 is not included among protein kinases whose inhibitors are in clinical practice or in advanced clinical trials, evidence is accumulating that elevated CK2 constitutive activity co-operates to induce a number of pathological conditions, including cancer, infectious diseases, neurodegeneration and cardiovascular pathologies. The development and usage of cell-permeant, selective inhibitors discloses a scenario whereby CK2 plays a global anti-apoptotic role, which under special circumstances may lead to untimely and pathogenic cell survival.

scholarly journals The 5-Hydroxytryptamine(4a) Receptor Is Palmitoylated at Two Different Sites, and Acylation Is Critically Involved in Regulation of Receptor Constitutive Activity

2001 ◽  
Vol 277 (4) ◽  
pp. 2534-2546 ◽  
Author(s):  
Evgeni G. Ponimaskin ◽  
Martin Heine ◽  
Lara Joubert ◽  
Michèle Sebben ◽  
Ulf Bickmeyer ◽  
...  
Keyword(s):  
Constitutive Activity

scholarly journals Common Structural Basis for Constitutive Activity of the Ghrelin Receptor Family

2004 ◽  
Vol 279 (51) ◽  
pp. 53806-53817 ◽  
Author(s):  
Birgitte Holst ◽  
Nicholas D. Holliday ◽  
Anders Bach ◽  
Christian E. Elling ◽  
Helen M. Cox ◽  
...  
Keyword(s):  
Structural Basis ◽  
Constitutive Activity ◽  
Ghrelin Receptor ◽  
Receptor Family

scholarly journals Constitutive Activity among Orphan Class-A G Protein Coupled Receptors

PLoS ONE ◽  
2015 ◽  
Vol 10 (9) ◽  
pp. e0138463 ◽  
Author(s):  
Adam L. Martin ◽  
Michael A. Steurer ◽  
Robert S. Aronstam
Keyword(s):  
G Protein ◽  
G Protein Coupled Receptors ◽  
Constitutive Activity ◽  
Class A ◽  
G Protein Coupled

scholarly journals Ghrelin Receptor (GHS-R1a) and Its Constitutive Activity in Somatotroph Adenomas: A New Co-targeting Therapy Using GHS-R1a Inverse Agonists and Somatostatin Analogs

2014 ◽  
Vol 99 (12) ◽  
pp. E2463-E2471 ◽  
Author(s):  
Yves Mear ◽  
Marie-Pierre Blanchard ◽  
Céline Defilles ◽  
Thierry Brue ◽  
Dominique Figarella-Branger ◽  
...  
Keyword(s):  
Somatostatin Receptor ◽  
Somatostatin Analogs ◽  
Inverse Agonist ◽  
Receptor Subtype ◽  
Dependent Manner ◽  
Constitutive Activity ◽  
Targeting Therapy ◽  
Ghrelin Receptor ◽  
Gh Secretion

Context: The ghrelin receptor GHS-R1a is highly expressed in human somatotroph adenomas and exhibits unusually high basal signaling activity. In humans, the suppression of this constitutive activity by mutation induces a short stature. Objective: Using a GHS-R1a inverse agonist, modified substance P (MSP), we explored the role of GHS-R1a constitutive activity in GH hypersecretion from somatotroph adenomas and as a putative therapeutic target. Design: The effects of MSP were assessed on GH secretion from 19 human somatotroph tumors in vitro. Moreover, these effects were compared with those of octreotide (somatostatin receptor subtype 2 [sst2] agonist) and with the combination of both drugs. Expression and localization of GHS-R1a and sst2 were studied. Results: For all tumors, MSP inhibited GH secretion in a dose-dependent manner from 13 to 64%. Moreover, MSP enhanced octreotide-induced GH inhibition. For five tumors, the effects of combined MSP plus octreotide treatment were significantly higher than the sum of effects of each drug alone. MSP increased the membrane localization of GHS-R1a and of microdomains colocalizing sst2-GHS-R1a, highlighting the cooperation between the two drugs. Conclusions: The GHS-R1a inverse agonist could open new therapeutic options for acromegalic patients, particularly patients partially sensitive to octreotide whose GH secretion is not completely controlled by the sst2 agonist.

scholarly journals Constitutive activity of the Arabidopsis MAP Kinase 3 confers resistance to Pseudomonas syringae and drives robust immune responses

2017 ◽  
Vol 12 (8) ◽  
pp. e1356533 ◽  
Author(s):  
Julien Lang ◽  
Baptiste Genot ◽  
Heribert Hirt ◽  
Jean Colcombet
Keyword(s):  
Immune Responses ◽  
Map Kinase ◽  
Pseudomonas Syringae ◽  
Constitutive Activity
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