Mass Spectrometry Structural Proteomics Enabled by Limited Proteolysis and Cross‐Linking
ABSTRACT The exploration of protein structure and function stands at the forefront of life science and represents an ever‐expanding focus in the development of proteomics. As mass spectrometry (MS) offers readout of protein conformational changes at both the protein and peptide levels, MS‐based structural proteomics is making significant strides in the
Haiyan Lu +4 more
wiley +1 more source
Functional competence of a partially engaged GPCR–β-arrestin complex
β-arrestins initially contact with the phosphorylated carboxyl-terminus of GPCRs before engaging with the GPCR core. Here, the authors use a chimeric GPCR partially and fully engaged with β-arrestin1 and show that the core interaction is dispensable for ...
Punita Kumari +10 more
doaj +1 more source
P2Y receptors in the mammalian nervous system: pharmacology, ligands and therapeutic potential [PDF]
P2Y receptors for extracellular nucleotides are coupled to activation of a variety of G proteins and stimulate diverse intracellular signaling pathways that regulate functions of cell types that comprise the central nervous system (CNS).
Erb, Laurie +3 more
core +1 more source
Advances in GPCRs Associated With Wnt Signaling Within the Auditory System
ABSTRACT G protein‐coupled receptors (GPCRs) that interact with the Wnt signaling pathway are pivotal for auditory system homeostasis, as they orchestrate inner ear development, hair cell (HC) regeneration, and hearing preservation. Frizzled (FZD) receptors, the core Wnt‐related GPCRs, bind Wnt ligands and co‐receptors (e.g., LRP5/6) to activate both ...
Liang Wang +3 more
wiley +1 more source
Preclinical models for evaluating psychedelics in the treatment of major depressive disorder
Psychedelic drugs have seen a resurgence in interest as a next generation of psychiatric medicines with potential as rapid‐acting antidepressants (RAADs). Despite promising early clinical trials, the mechanisms which underlie the effects of psychedelics are poorly understood.
Laith Alexander +5 more
wiley +1 more source
Fluorescence correlation spectroscopy, combined with bimolecular fluorescence complementation, reveals the effects of β-arrestin complexes and endocytic targeting on the membrane mobility of neuropeptide Y receptors [PDF]
Fluorescence correlation spectroscopy (FCS) and photon counting histogram (PCH) analysis are powerful ways to study mobility and stoichiometry of G protein coupled receptor complexes, within microdomains of single living cells.
Briddon, Stephen J. +2 more
core
Neuropsychopharmacology of hallucinogenic and non‐hallucinogenic 5‐HT2A receptor agonists
Psychedelic drugs such as LSD and psilocin were once relegated to the fringes of medical research because of their association with counterculture movements and a perceived concern about harm through recreational use, and their consequent legal prohibition in the early 1970s.
Trevor Sharp, Aurelija Ippolito
wiley +1 more source
SNX9 family mediates βarrestin-independent GPCR endocytosis
Agonist-stimulated GPCR endocytosis typically occurs via the multi-faceted adaptor proteins known as βarrestins. However, endocytosis of several GPCRs occurs independently of β-arrestins, suggesting an additional mode of GPCR endocytosis, but the ...
Valeria L. Robleto +4 more
doaj +1 more source
The effect of arrestin conformation on the recruitment of c-Raf1, MEK1, and ERK1/2 activation.
Arrestins are multifunctional signaling adaptors originally discovered as proteins that "arrest" G protein activation by G protein-coupled receptors (GPCRs).
Sergio Coffa +6 more
doaj +1 more source
Nuclear β-arrestin1 is a critical cofactor of hypoxia-inducible factor-1α signaling in endothelin-1-induced ovarian tumor progression [PDF]
Hypoxia-inducible factor-1α (HIF-1α) mediates the response to hypoxia or other stimuli, such as growth factors, including endothelin-1 (ET-1), to promote malignant progression in numerous tumors.
Bagnato, Anna +6 more
core +1 more source

