Results 61 to 70 of about 18,849 (159)

In silico prediction of novel effective combinational treatment of chronic pain in individual patients: A joint white paper of the H2020 QSPainRelief consortium

British Journal of Pharmacology, EarlyView.
Abstract Opioids are prescribed widely for chronic pain despite well‐recognised risks and variable long‐term benefit, reflecting the lack of effective alternatives for many patients. Combination therapies offer a promising strategy to enhance efficacy whilst reducing side effects.
André Mouraux, Solenn Gousset, Beltrán Alvarez, Monica Baiula, Wouter Bakker, Andrea Bedini, Monir Bertayli, Divakar Budda, Robert Carr, Elisabetta Cuna, Óscar Díaz, Nina Donner, Jesús Giraldo, Geert‐Jan Groeneveld, Berfin Gülave, David Guydan, Hemme Hijma, Rafael Maldonado, Pedro Renault, Carlos Rinaudo, Jeroen Elaissaiss‐Schaap, Athan Spiros, Sara Stoeber, Petri Takkala, Daan van Valkengoed, Coen van Hasselt, Elizabeth (Liesbeth) CM de Lange   +26 more
wiley   +1 more source

Decoding functional specialization in G protein‐coupled receptors (GPCRs) through evolution‐guided residue profiling

British Journal of Pharmacology, EarlyView.
Background and Purpose G protein‐coupled receptors (GPCRs) are integral membrane proteins that mediate physiological processes by enabling cells to detect and respond to diverse stimuli. Although many subfamily‐specific functional hotspots have been described, the family‐wide determinants of common and subfamily‐specific functions remain incomplete ...
Berkay Selçuk, Gunnar Schulte, Igor B. Zhulin, Ogün Adebali   +3 more
wiley   +1 more source

Peripheral κ opioid receptor in pain and inflammation: From molecular signalling and gene expression to drug discovery

British Journal of Pharmacology, EarlyView.
The κ opioid receptor (κ receptor, KOR) is a G protein‐coupled receptor with well established roles in analgesia and immune modulation. Although historically studied primarily in the central nervous system (CNS), growing evidence indicates that κ signalling in peripheral tissues plays an important role in regulating pain, inflammation and immune ...
Rumsha Khan, Elena C. A. Becker, Boglarka B. Bata, Christian W. Gruber   +3 more
wiley   +1 more source

β-Arrestin Based Receptor Signaling Paradigms: Potential Therapeutic Targets for Complex Age-Related Disorders

Frontiers in Pharmacology, 2018
G protein coupled receptors (GPCRs) were first characterized as signal transducers that elicit downstream effects through modulation of guanine (G) nucleotide-binding proteins. The pharmacotherapeutic exploitation of this signaling paradigm has created a
Jaana van Gastel, Jaana van Gastel, Jhana O. Hendrickx, Jhana O. Hendrickx, Hanne Leysen, Hanne Leysen, Paula Santos-Otte, Louis M. Luttrell, Bronwen Martin, Stuart Maudsley, Stuart Maudsley   +10 more
doaj   +1 more source

Peripheral targets for neuropathic pain

British Journal of Pharmacology, EarlyView.
Neuropathic pain represents a significant clinical challenge, with still limited pharmacological approaches to symptomatic relief. This review focuses on molecular targets implicated in neuropathic pain, particularly those involved in peripheral mechanisms. Using the IUPHAR/BPS database of biological targets, their occurrence together with ‘neuropathic
Amirhossein Afsharipour, Cosmin I. Ciotu, Felix J. Resch, Michael J. M. Fischer   +3 more
wiley   +1 more source

The chemokine receptor‐like fourth extracellular loop of the apelin receptor differentially regulates apelin and elabela binding and signalling

British Journal of Pharmacology, EarlyView.
Abstract Background and Purpose Apelin and Elabela are endogenous ligands of the apelin receptor (apelin receptor/APJ), a GPCR involved in cardiovascular regulation and body fluid homeostasis. The human receptor contains a conserved disulfide bridge linking the N‐terminal domain to extracellular loop 3 (ECL3) via Cys19 and Cys281, forming a structural ...
Chloé Bonef, Hela Bouhsine, Carine Huynh, Marion Chaigneau, Steven Dubois, Mikel Garcia‐Marcos, Catherine Llorens‐Cortes, Denis Servent, Philippe Robin, Hervé Nozach, Isabel Alves, Xavier Iturrioz   +11 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

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