Results 41 to 50 of about 187,893 (285)

Signal Transduction and Pathogenic Modifications at the Melanocortin-4 Receptor: A Structural Perspective [PDF]

, 2019
The melanocortin-4 receptor (MC4R) can be endogenously activated by binding of melanocyte-stimulating hormones (MSH), which mediates anorexigenic effects. In contrast, the agouti-related peptide (AgRP) acts as an endogenous inverse agonist and suppresses
Biebermann, Heike, Cerdá-Reverter, José Miguel, Heyder, Nicolas, Kleinau, Gunnar, Krude, Heiko, Kwiatkowski, Dennis, Kühnen, Peter, Scheerer, Patrick, Soletto, Lucia, Speck, David, Szczepek, Michal   +10 more
core   +1 more source

β-Arrestin-Mediated Signaling Improves the Efficacy of Therapeutics

Journal of Pharmacological Sciences, 2012
β-Arrestins (β-arrestin-1 and β-arrestin-2) were first identified as proteins that have the ability to desensitize G protein-coupled receptors (GPCRs). However, it has recently been found that β-arrestins can activate signaling pathways independent of G ...
Islam A.A.E.-H. Ibrahim, Hitoshi Kurose
doaj   +1 more source

The Gαs‐protein‐mediated pathway may be steadily stimulated by prostanoid EP2 receptors, but not by EP4 receptors

FEBS Open Bio, 2022
EP2 and EP4 prostanoid receptors have long been considered to have similar roles, since they are known to couple with Gαs‐protein and activate cAMP‐mediated signaling pathways.
Keijo Fukushima, Kanaho Senoo, Naoki Kurata, John W. Regan, Hiromichi Fujino   +4 more
doaj   +1 more source

Quinolones modulate ghrelin receptor signaling: potential for a novel small molecule scaffold in the treatment of cachexia [PDF]

, 2018
Cachexia is a metabolic wasting disorder characterized by progressive weight loss, muscle atrophy, fatigue, weakness, and appetite loss. Cachexia is associated with almost all major chronic illnesses including cancer, heart failure, obstructive ...
Cano, Rafael, Juan Rodríguez, Rocío, Kandil, Dalia, McGlacken, Gerard P., Pastor Cavada, Elena, Schellekens, Harriët, Shaban, Hamdy, Shanahan, Rachel, Torres-Fuentes, Cristina   +8 more
core   +3 more sources

Biased agonism: the quest for the analgesic holy grail

PAIN Reports, 2018
. Opioids alleviate pain, but adverse effects severely limit their usefulness. To solve this problem, biased ligands favoring 1 signaling pathway downstream of the μ-opioid receptor over another are being developed.
M. Alexander Stanczyk, Ram Kandasamy
doaj   +1 more source

Physical constraints on accuracy and persistence during breast cancer cell chemotaxis [PDF]

, 2019
Directed cell motion in response to an external chemical gradient occurs in many biological phenomena such as wound healing, angiogenesis, and cancer metastasis.
Han, Bumsoo, Moon, Hye-ran, Mugler, Andrew, Saha, Soutick, Varennes, Julien   +4 more
core   +4 more sources

Fusion of the β2‐adrenergic receptor with either Gαs or βarrestin‐2 produces constitutive signaling by each pathway and induces gain‐of‐function in BEAS‐2B cells

FASEB BioAdvances, 2022
The β2AR is a prototypical G protein‐coupled receptor (GPCR) known to orchestrate different cellular responses by the stimulation of specific signaling pathways.
Emilio Y. Lucero‐Garcia Rojas, Arfaxad Reyes‐Alcaraz, Kehe Ruan, Bradley K. McConnell, Richard A. Bond   +4 more
doaj   +1 more source

BMP2/BMPR1A is linked to tumour progression in dedifferentiated liposarcomas [PDF]

, 2016
Bone Morphogenic Protein 2 (BMP2) is a multipurpose cytokine, important in the development of bone and cartilage, and with a role in tumour initiation and progression.
Cassidy, A.P., Cassidy, J.W., Harris, O.B., O’Neill, H.L.   +3 more
core   +3 more sources

Ligand-Induced Biased Activation of GPCRs: Recent Advances and New Directions from In Silico Approaches

Molecules
G-protein coupled receptors (GPCRs) are the largest family of membrane proteins engaged in transducing signals from the extracellular environment into the cell.
Shaima Hashem, Alexis Dougha, Pierre Tufféry   +2 more
doaj   +1 more source

Collagen VI Is a Gi-Biased Ligand of the Adhesion GPCR GPR126/ADGRG6

Cells, 2023
GPR126/ADGRG6, a member of the adhesion G-protein-coupled receptor family, balances cell differentiation and proliferation through fine-tuning of intracellular cAMP levels, which is achieved through coupling to Gs and Gi proteins.
Caroline Wilde, Paulomi Mehta Chaudhry, Rong Luo, Kay-Uwe Simon, Xianhua Piao, Ines Liebscher   +5 more
doaj   +1 more source