Regulation of Membrane Targeting of the G Protein-coupled Receptor Kinase 2 by Protein Kinase A and Its Anchoring Protein AKAP79 [PDF]
, 2001 The beta 2 adrenergic receptor (beta 2AR) undergoes desensitization by a process involving its phosphorylation by both protein kinase A (PKA) and G protein-coupled receptor kinases (GRKs). The protein kinase A-anchoring protein AKAP79 influences beta 2AR
Chen, Wei +8 more
core
FEM1B enhances TRAIL‐induced apoptosis in T lymphocytes and monocytes
FEBS Open Bio, EarlyView.FEM1B facilitates TRAIL‐induced apoptosis through distinct mechanisms in T lymphocytes and monocytes. In T lymphocytes, FEM1B engages with TRAF2, leading to a reduction in TRAF2 expression, which subsequently lessens TRAF2's inhibitory influence on caspase‐8.
Chenbo Yang +5 more
wiley +1 more source
Molecular dynamics simulations reveal the role of ceramicine B as novel PPARγ partial agonist against type 2 diabetes [PDF]
arXiv, 2018 Peroxisome proliferator-activated receptors gamma (PPAR{\gamma}) are ligand-activated controllers of various metabolic actions and insulin sensitivity. PPAR{\gamma} is thus considered as an important target to treat type 2 diabetes. Available PPAR{\gamma} drugs (full agonists) have robust insulin-sensitizing properties but are accompanied by severe ...
arxiv
Modeling Suggests Combined-Drug Treatments for Disorders Impairing Synaptic Plasticity via Shared Signaling Pathways [PDF]
arXiv, 2020 Genetic disorders such as Rubinstein-Taybi syndrome (RTS) and Coffin-Lowry syndrome (CLS) cause lifelong cognitive disability, including deficits in learning and memory. Can pharmacological therapies be suggested to improve learning and memory in these disorders?
arxiv
Cannabinoid receptor interacting protein suppresses agonist-driven CB1 receptor internalization and regulates receptor replenishment in an agonist-biased manner [PDF]
, 2016 Cannabinoid receptor interacting protein 1a (CRIP1a) is a CB1 receptor (CB1R) distal C-terminus-associated protein that modulates CB1R signaling via G proteins, and CB1R down-regulation but not desensitization (Blume et al.
Bass, Caroline E. +8 more
core +2 more sources
Cortical Excitability Before and After Long‐Term Perampanel Treatment for Epilepsy
Annals of Clinical and Translational Neurology, EarlyView.ABSTRACT Objective Antiseizure medications (ASMs), which may influence cortical excitability, are the mainstay of epilepsy treatment. Transcranial magnetic stimulation (TMS) helps evaluate cortical excitability. We assessed changes in TMS responses using serial TMS measurements in people treated with an adjunctive noncompetitive AMPA‐receptor ...
Robert M. Helling +6 more
wiley +1 more source
Long-Range Coupling in an Allosteric Receptor Revealed by Mutant Cycle Analysis [PDF]
, 2009 The functional coupling of residues that are far apart in space is the quintessential property of allosteric proteins. For example, in Cys-loop receptors, the gating of an intrinsic ion channel is allosterically regulated by the binding of small molecule
Dougherty, Dennis A. +4 more
core +2 more sources
Advanced Functional Materials, EarlyView.Ultrathin, flexible neural probes are developed with an innovative, biomimetic design incorporating brain tissue‐compatible materials. The material system employs biomolecule‐based encapsulation agents to mitigate inflammatory responses, as demonstrated through comprehensive in vitro and in vivo studies.
Jeonghwa Jeong +7 more
wiley +1 more source
Effects of kappa-opioid agonist U-50488 and p38 MAPK inhibitor SB203580 on the spike activity of pyramidal neurons in the basolateral amygdala [PDF]
Research Results in Pharmacology 10(1): 1-6 (2024)Introduction: Kappa-opioid receptor (KOR) signaling in the basolateral amygdala (BLA) underlies KOR agonist-induced aversion. In this study, we aimed to understand the individual and combined effects of KOR agonist U-50488 and p38 MAPK inhibitor SB203580 on the spiking activity of pyramidal neurons in the BLA to shed light on the complex interplay ...
arxiv +1 more source
Molecules, 2019 The modulators of farnesoid X receptor (FXR), a bile acid receptor, regulate various biological processes including bile acid metabolism, and are associated with the control of fatty liver and osteoporosis.
Ko Fujimori +4 more
doaj +1 more source