G Protein–Coupled Receptor Deorphanizations [PDF]
G protein–coupled receptors (GPCRs) are major regulators of intercellular interactions. They initiate these actions by being activated by a wide variety of natural ligands. Historically, ligands were discovered first, but the advent of molecular biology reversed this trend.
Zhiwei Wang+5 more
openaire +3 more sources
Calcium-independent inhibitory G-protein signaling induces persistent presynaptic muting of hippocampal synapses [PDF]
Adaptive forms of synaptic plasticity that reduce excitatory synaptic transmission in response to prolonged increases in neuronal activity may prevent runaway positive feedback in neuronal circuits.
Chang, Chun Yun+3 more
core +2 more sources
G Protein-Coupled Receptors in Macrophages
ABSTRACTAs the largest receptor gene family in the human genome, with >800 members, the signal-transducing G protein-coupled receptors (GPCRs) play critical roles in nearly all conceivable physiological processes, ranging from the sensing of photons and odorants to metabolic homeostasis and migration of leukocytes.
Hsi-Hsien Lin, Martin Stacey
openaire +3 more sources
The yeast Saccharomyces cerevisiae is powerful for studying human G protein-coupled receptors as they can be coupled to its mating pathway. Here the authors engineer baker’s yeast to produce human sterols and show that vertebrate G protein coupled ...
Björn D. M. Bean+12 more
doaj +1 more source
Lysophosphatidic Acid Signaling in Cancer Cells: What Makes LPA So Special?
Lysophosphatidic acid (LPA) refers to a family of simple phospholipids that act as ligands for G protein-coupled receptors. While LPA exerts effects throughout the body in normal physiological circumstances, its pathological role in cancer is of great ...
Pravita Balijepalli+2 more
doaj +1 more source
GPCRs in Intracellular Compartments: New Targets for Drug Discovery
The architecture of eukaryotic cells is defined by extensive membrane-delimited compartments, which entails separate metabolic processes that would otherwise interfere with each other, leading to functional differences between cells.
Irene Fasciani+7 more
doaj +1 more source
Mas-related G-protein–coupled receptors inhibit pathological pain in mice [PDF]
An important objective of pain research is to identify novel drug targets for the treatment of pathological persistent pain states, such as inflammatory and neuropathic pain.
Altier+49 more
core +2 more sources
Powdered G-Protein-Coupled Receptors [PDF]
Preparation and storage of functional membrane proteins such as G-protein-coupled receptors (GPCRs) are crucial to the processes of drug delivery and discovery. Here, we describe a method of preparing powdered GPCRs using rhodopsin as the prototype. We purified rhodopsin in CHAPS detergent with low detergent to protein ratio so the bulk of the sample ...
Suchithranga M. D. C. Perera+2 more
openaire +3 more sources
Thrombin Protease-activated Receptor-1 Signals through Gq- and G13-initiated MAPK Cascades Regulating c-Jun Expression to Induce Cell Transformation [PDF]
Although the ability of G protein-coupled receptors to stimulate normal and aberrant cell growth has been intensely investigated, the precise nature of the molecular mechanisms underlying their transforming potential are still not fully understood.
Gutkind, J. Silvio+4 more
core +1 more source
G Protein-Coupled Inwardly Rectifying K+ Channels (GIRKs) Mediate Postsynaptic but Not Presynaptic Transmitter Actions in Hippocampal Neurons [PDF]
To study the role of G protein-coupled, inwardly rectifying K+ (GIRK) channels in mediating neurotransmitter actions in hippocampal neurons, we have examined slices from transgenic mice lacking the GIRK2 gene.
Jan, Lily Y+4 more
core +1 more source