Results 101 to 110 of about 12,251 (147)

Discovery of functionally selective C5aR2 ligands: novel modulators of C5a signalling. [PDF]

, 2016
The complement cascade is comprised of a highly sophisticated network of innate immune proteins that are activated in response to invading pathogens or tissue injury. The complement activation peptide, C5a, binds two seven transmembrane receptors, namely
Blaskovich, M.A., Clark, R.J., Cooper, M.A., Croker, D.E., Floudas, C.A., Halai, R., Kaeslin, G., Monk, P.N., Morikis, D., Schofield, Z., Woodruff, T.M., Wu, M.C.   +11 more
core   +1 more source

Drugs that act on both G protein‐coupled receptors (GPCRs) and kinases: potentiation of effects, side effects and general aspects of drug pleiotropy

British Journal of Pharmacology, EarlyView.
Abstract Background A drug designed for a specific target often interacts with multiple targets, either unintentionally or as part of its intended mechanism of action. This has been called pharmacological pleiotropy or polypharmacology. There are key endogenous ligands such as ATP, GABA and glutamate that act on various proteins in humans. Furthermore,
Hampus Ljunggren, Aleksandr Sokolov, Flavio Ballante, Robert Fredriksson, Francisco Lagunas‐Rangel, Alexander S. Hauser, Stefan Knapp, Jörgen Jonsson, Helgi B. Schiöth   +8 more
wiley   +1 more source

T‐2 Toxin‐Mediated β‐Arrestin‐1 O‐GlcNAcylation Exacerbates Glomerular Podocyte Injury via Regulating Histone Acetylation

Advanced Science
T‐2 toxin causes renal dysfunction with proteinuria and glomerular podocyte damage. This work explores the role of metabolic disorder/reprogramming‐mediated epigenetic modification in the progression of T‐2 toxin‐stimulated podocyte injury.
Tushuai Li, Wenxue Sun, Shenglong Zhu, Chengsheng He, Tong Chang, Jie Zhang, Yongquan Chen   +6 more
doaj   +1 more source

Phosducin regulates the expression of transducin betagamma subunits in rod photoreceptors and does not contribute to phototransduction adaptation. [PDF]

, 2007
For over a decade, phosducin's interaction with the betagamma subunits of the G protein, transducin, has been thought to contribute to light adaptation by dynamically controlling the amount of transducin heterotrimer available for activation by ...
Arshavsky, Vadim Y, Burns, Marie E, Chen, Yen-Ming, Herrmann, Rolf, Krispel, Claudia M, Sokolov, Maxim, Song, Hongman   +6 more
core  

GIP in Cardiovascular and Kidney Disease: From Physiology to Pharmacology

Diabetes, Obesity and Metabolism, EarlyView.
ABSTRACT Aims To provide a comprehensive overview of the cardiovascular and renal effects of glucose‐dependent insulinotropic polypeptide (GIP) by integrating its physiological role with recent human trial data on tirzepatide, the first dual GIP and glucagon‐like peptide‐1 (GLP‐1) receptor agonist.
Michelantonio De Fano, Line L. Haurum, Christine R. Schwarz, Francesca Porcellati, Andreas Andersen   +4 more
wiley   +1 more source

Dose–Response Effect of Glucagon on Glucose, Beta‐Cell Secretion and Metabolism in Healthy Individuals

Diabetes, Obesity and Metabolism, EarlyView.
ABSTRACT Aim Glucagon is a key regulator of glucose and energy metabolism, yet the dose–response effects of glucagon on markers of metabolism in humans are not fully characterised. We investigated the dose‐dependent effects of glucagon on glucose metabolism, β‐cell secretion and markers of hepatic metabolism in healthy adults.
Sophie Betty Brock, Nina Lerberg Hansen, Elvar Már Sturlaugsson Jóhönnuson, Sasha Alexandra Sampson Kjeldsen, Nicolai J. Wewer Albrechtsen   +4 more
wiley   +1 more source

Lock, relax, load, and shoot: a molecular perspective on Nedd4 regulation

The FEBS Journal, Volume 293, Issue 11, Page 3097-3110, June 2026.
Structural basis of inactive and active states of the Nedd4 HECT E3 ligase subfamily, following a ‘lock, relax, load, and shoot’ mechanism. In the locked, autoinhibited state, intramolecular domain interactions restrain the HECT domain. Relaxation releases these restraints, allowing loading of ubiquitin onto the catalytic cysteine, followed by the ...
Masa Janosev, Tomas Obsil, Veronika Obsilova   +2 more
wiley   +1 more source

Spatiotemporal dynamics of β‐arrestin‐mediated Src activation in 5‐HT7 receptor signaling pathway

The FEBS Journal, EarlyView.
GPCRs induce distinct cellular responses via G protein‐ or β‐arrestin‐mediated signaling pathways. This study revealed that β‐arrestin‐biased 5‐HT7R ligand induces slow, sustained Src activation, contrasting with transient G protein‐mediated activation.
Hyunbin Kim, Yong Woo Lee, Huimin Lee, Eunseo Park, Jieon Lee, Hae Nim Lee, Kyeong‐Man Kim, Hyunah Choo, Jihye Seong   +8 more
wiley   +1 more source

Innovations in Obesity Treatment: Beyond Adipose Tissue Dysfunction

Obesity Reviews, EarlyView.
Obesity drives chronic inflammation, insulin resistance, type 2 diabetes, and cancer development through adipocyte dysfunction. Addressing this multisystemic disorder requires integrated strategies beyond diet and exercise, such as thermogenesis activation via menthol or capsinoids and appetite control through GLP‐1/GIP agonists and neuromodulation to ...
Jesica Martínez‐Godfrey, Irene Pomares‐Bri, Paula de Juan‐Maciá, Mariló Olivares‐Vicente, Enrique Barrajón‐Catalán, Vicente Micol, Enrique Roche, María Herranz‐López   +7 more
wiley   +1 more source

Integrative Phosphoproteomic Profiling Reveals Stage‐Specific Signalling and Metabolism in Equine Melanocytic Neoplasm

Veterinary and Comparative Oncology, EarlyView.
ABSTRACT Equine melanocytic neoplasms (EMN) are aggressive tumours characterised by high metastatic potential and limited therapeutic options available. However, the molecular mechanisms underlying their progression remain poorly understood. This study therefore presents the integrative phosphoproteomic analysis of EMN tissue, with the aim of ...
Paitoon Srimontri, Amornthep Kingkaw, Nawarus Prapaiwan, Rangsima Sujittosakul, Nichapat Iamkaewprasert, Jiraschaya Piputwat, Puetta Isama‐al, Thanutchanok Munkongdee, Thanapon Chotikaprakal, Petchpailin Yanyongsirikarn, Narumon Phaonakrop, Sittiruk Roytrakul, Wanwipa Vongsangnak, Parichart Tesena   +13 more
wiley   +1 more source