Results 111 to 120 of about 27,334 (199)

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

ATHENA: A Phase 3, Open-Label Study Of The Safety And Effectiveness Of Oliceridine (TRV130), A G-Protein Selective Agonist At The µ-Opioid Receptor, In Patients With Moderate To Severe Acute Pain Requiring Parenteral Opioid Therapy. [PDF]

, 2019
Background:Pain management with conventional opioids can be challenging due to dose-limiting adverse events (AEs), some of which may be related to the simultaneous activation of β-arrestin (a signaling pathway associated with opioid-related AEs) and G ...
Beard, Timothy L, Bergese, Sergio D, Berkowitz, Richard D, Brzezinski, Marek, Cochrane, Kristina, Habib, Ashraf S, Hammer, Gregory B, Mace, Sharon E, Minkowitz, Harold S, Pan, Peter H, Wase, Linda   +10 more
core  

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

Concepts of GPCR-controlled navigation in the immune system

, 2019
G-protein-coupled receptor (GPCR) signaling is essential for the spatiotemporal control of leukocyte dynamics during immune responses. For efficient navigation through mammalian tissues, most leukocyte types express more than one GPCR on their surface ...
Boneschansker L, Brandt SL, Chan EC, Filippo K, Freedman NJ, Hjorto GM, Hons M, Katakai T, Kitayama J, Lemos C, Ley K, Miyabe Y, Moussavi‐Harami SF, Proudfoot AEI, Purvanov V, Rot A, Scheiermann C, Schwarz J, Sokol CL, Sotsios Y, Steury MD, Takeda A, Thiriot A, Tomhave ED, Wang Y, Yanagihara S, Zhang Y   +26 more
core   +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

β-arrestin 1 regulates β2-adrenergic receptor-mediated skeletal muscle hypertrophy and contractility

Skeletal Muscle, 2018
Background β2-adrenergic receptors (β2ARs) are the target of catecholamines and play fundamental roles in cardiovascular, pulmonary, and skeletal muscle physiology.
Jihee Kim, Chad A. Grotegut, James W. Wisler, Tianyu Li, Lan Mao, Minyong Chen, Wei Chen, Paul B. Rosenberg, Howard A. Rockman, Robert J. Lefkowitz   +9 more
doaj   +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

Troglitazone stimulates beta-arrestin-dependent cardiomyocyte contractility via the angiotensin II type 1A receptor. [PDF]

, 2010
Peroxisome proliferator-activated receptor gamma (PPAR gamma) agonists are commonly used to treat cardiovascular diseases, and are reported to have several effects on cardiovascular function that may be due to PPAR gamma-independent signaling events ...
Nguyen, Anny D., Rockman, Howard A., Tilley, Douglas G G.   +2 more
core   +1 more source

Evidence for a Two‐Step Model for Activation of GPR25 by the Chemoattractant CXCL17

Basic &Clinical Pharmacology &Toxicology, Volume 139, Issue 1, July 2026.
ABSTRACT CXCL17 was recently reported to activate GPR25, a receptor expressed by T‐regulatory cells. Although classified as a chemokine, the activity of CXCL17 is ablated by minor C‐terminal truncation, suggesting a novel mode of receptor activation. We set out to test this hypothesis by mutagenesis. GPR25 was expressed in the murine pre‐B cell line L1.
Wuqing Yang, Sean P. Giblin, James E. Pease   +2 more
wiley   +1 more source