Abstract There is increasing concern regarding pollutants disrupting the vertebrate thyroid hormone (TH) system, which is crucial for development. Thus, identification of TH system–disrupting chemicals (THSDCs) is an important requirement in the Organisation for Economic Co‐operation and Development (OECD) testing framework.
Lisa Gölz +9 more
wiley +1 more source
The apelin and Elabela proteins constitute a spatiotemporal double-ligand system that controls apelin receptor (APJ) signal transduction. Phosphorylation of multiple sites within the C-terminus of APJ is essential for the recruitment of β-arrestins.
Jing Chen +9 more
doaj +1 more source
Identification of the first surrogate agonists for the G protein-coupled receptor GPR132 [PDF]
We report the first pharmacological tool agonist for in vitro characterization of the orphan receptor GPR132, preliminary structure–activity relationships based on 32 analogs and a suggested binding mode from docking.M.A.S.
Belcik Christensen, H +6 more
core +3 more sources
The Endothelial CXCR Family in Vascular Health and Disease
ABSTRACT Endothelial cells (ECs) form the dynamic interface between blood and tissue, serving as key regulators of vascular homeostasis, inflammation, and repair. Among the molecular systems governing endothelial behavior, the C‐X‐C motif chemokine receptor (CXCR) family—originally characterized in immunology for its roles in leukocyte trafficking and ...
Zhiming Wu +4 more
wiley +1 more source
ERK5 activation by Gq-coupled muscarinic receptors is independent of receptor internalization and β-arrestin recruitment. [PDF]
G-protein-coupled receptors (GPCRs) are known to activate both G protein- and β-arrestin-dependent signalling cascades. The initiation of mitogen-activated protein kinase (MAPK) pathways is a key downstream event in the control of cellular functions ...
Guzmán Sánchez-Fernández +5 more
doaj +1 more source
Cross-communication between Gi and Gs in a G-protein-coupled receptor heterotetramer guided by a receptor C-terminal domain [PDF]
BACKGROUND: G-protein-coupled receptor (GPCR) heteromeric complexes have distinct properties from homomeric GPCRs, giving rise to new receptor functionalities.
Aguinaga Andrés, David +14 more
core +2 more sources
A compendium of extracellular vesicle biogenesis inhibitors: From bench to bedside
This review explores a decade of research on extracellular vesicles (EVs), detailing their biogenesis and roles in health and disease. It emphasizes EVs' relevance for potential medical applications covering various conditions such as cancer, neurodegeneration, inflammation, and infectious diseases, bridging experimental findings with clinical ...
Stefano Vecchione +2 more
wiley +1 more source
Biphasic activation of β-arrestin 1 upon interaction with a GPCR revealed by methyl-TROSY NMR
β-arrestins commonly bind to two distinct elements in GPCRs: the phosphorylated carboxyl terminal tail (C tail) and the cytoplasmic face of the transmembrane region (TM core).
Yutaro Shiraishi +6 more
doaj +1 more source
β-arrestin/connexin 43 complex anchors ERKs outside the nucleus: a pre-requisite for bisphosphonate anti-apoptotic effect mediated by CX43/ERK in osteocytes [PDF]
Bisphosphonates (BPs) anti-fracture ef cacy may be due in part to inhibition of osteocyte apoptosis. This effect requires opening of con- nexin (Cx) 43 hemichannels and phosphoryla- tion of the extracellular signal regulated kinases (ERKs).
Bellido, Teresita +2 more
core
Cell migration towards CXCL12 in leukemic cells compared to breast cancer cells [PDF]
Chemotaxis or directed cell migration is mediated by signalling events initiated by binding of chemokines to their cognate receptors and the activation of a complex signalling cascade.
Goh, Poh Hui +6 more
core +1 more source

