Results 61 to 70 of about 18,493 (159)

Modelling G protein-biased agonism using GLP-1 receptor C-terminal mutations

Molecular Metabolism
Background and aim: The glucagon-like peptide-1 receptor (GLP-1R) is a major therapeutic target for type 2 diabetes and obesity. Agonists showing bias in favour of G protein signalling over β-arrestin recruitment and GLP-1R internalisation, e.g ...
Hanh Duyen Tran, Yiming Zuo, Carissa Wong, Alice Pollard, Steve Bloom, Ben Jones   +5 more
doaj   +1 more source

The effect of arrestin conformation on the recruitment of c-Raf1, MEK1, and ERK1/2 activation.

PLoS ONE, 2011
Arrestins are multifunctional signaling adaptors originally discovered as proteins that "arrest" G protein activation by G protein-coupled receptors (GPCRs).
Sergio Coffa, Maya Breitman, Susan M Hanson, Kari Callaway, Seunghyi Kook, Kevin N Dalby, Vsevolod V Gurevich   +6 more
doaj   +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

Pancreatic cancer cachexia promotes cardiac dysfunction through altered adrenergic signalling in the heart

The Journal of Physiology, EarlyView.
Abstract figure legend The β1‐adrenergic receptor is the predominant adrenergic subtype expressed on cardiac myocytes. Upon stimulation it activates downstream signalling pathways that increase the heart rate and cardiac output to meet metabolic demands.
Parham Diba, Peter R. Levasseur, Samuel D. Newton, Khia Min Sabrina Koh, Paige C. Arneson‐Wissink, Xinxia Zhu, Peter Pham, Heike Mendez, Luke Whitcomb, Ariana Sattler, William R Woodward, Beth A. Habecker, Daniel L. Marks, Aaron J. Grossberg   +13 more
wiley   +1 more source

The Serotonin 2B (5‐HT2B) Receptor: A Narrative Review of Preclinical and Clinical Evidence on the Safety Considerations and Therapeutic Potential for the Treatment of Depression

Clinical Pharmacology &Therapeutics, Volume 120, Issue 2, Page 345-356, August 2026.
Major depressive disorder (MDD) and treatment‐resistant depression (TRD) remain leading causes of disability, providing the impetus for receptor‐level treatment strategies beyond monoamine reuptake. The serotonin 5‐HT2B receptor (5‐HT2BR) is uniquely positioned at the interface of central‐antidepressant mechanisms and peripheral cardiac risks.
Gia Han Le, Sabrina Wong, Danica E. Johnson, Diana K. Orsini, Yang Jing Zheng, Kayla M. Teopiz, Christine E. Dri, Joshua D. Rosenblat, Roger S. McIntyre   +8 more
wiley   +1 more source

Extracellular Vesicles in Acute Myeloid Leukemia: Opportunities and Obstacles for Therapeutic Advancement

Journal of Biochemical and Molecular Toxicology, Volume 40, Issue 8, August 2026.
Acute myeloid leukemia (AML) is a disease characterized by uncontrolled proliferation and blocked maturation of hematopoietic stem and progenitor cells. Despite progress in its clinical management, many patients continue to relapse or show limited response to standard therapies, emphasizing the need for novel, safe, and more effective targeted ...
Rongrong Hu, Zaker Ataullev, Luping Lou
wiley   +1 more source

Glucose Transporter 1 in Health and Disease

MedComm, Volume 7, Issue 8, August 2026.
As the quintessential facilitator of basal glucose uptake, glucose transporter 1 (GLUT1) is indispensable for maintaining systemic energy homeostasis. This graphical abstract delineates the multidimensional landscape of GLUT1 in normal physiology. It highlights its tissue‐specific metabolic roles—from fueling erythrocytes and fetal development to ...
Yi Tai, Zhihao Chen, Yuping Zhu, Weidong Han   +3 more
wiley   +1 more source

Ang-(1-7) is an endogenous β-arrestin-biased agonist of the AT1 receptor with protective action in cardiac hypertrophy

Scientific Reports, 2017
The renin-angiotensin system (RAS) plays a key role in the control of vasoconstriction as well as sodium and fluid retention mediated mainly by angiotensin (Ang) II acting at the AT1 receptor (AT1R).
Larissa B. Teixeira, Lucas T. Parreiras-e-Silva, Thiago Bruder-Nascimento, Diego A. Duarte, Sarah C. Simões, Rafael M. Costa, Deisy Y. Rodríguez, Pedro A. B. Ferreira, Carlos A. A. Silva, Emiliana P. Abrao, Eduardo B. Oliveira, Michel Bouvier, Rita C. Tostes, Claudio M. Costa-Neto   +13 more
doaj   +1 more source