Large inter-individual variation in platelet response to endogenous agonists and pharmacological agents, including resistance to antiplatelet therapy, prompts a search for novel platelet inhibitors and development new antithrombotic strategies.
Nina Wolska+7 more
doaj +1 more source
Molecular determinants involved in the allosteric control of agonist affinity in the GABAB receptor by the GABAB2 subunit [PDF]
The gamma-aminobutyric acid type B (GABAB) receptor is an allosteric complex made of two subunits, GABAB1 (GB1) and GABAB2 (GB2). Both subunits are composed of an extracellular Venus flytrap domain (VFT) and a heptahelical domain (HD). GB1 binds GABA, and GB2 plays a major role in G-protein activation as well as in the high agonist affinity state of ...
arxiv +1 more source
P2X3 Receptor Ligands: Structural Features and Potential Therapeutic Applications
The ionotropic P2X3 receptor (P2X3R) subtype is one of the seven mammalian P2X1-7 receptor belonging to the P2 purinergic receptor family together with the metabotropic P2Y1-2, 4-6,11-14 ones (Fredholm et al., 2011).
A. Spinaci+5 more
semanticscholar +1 more source
The role of purinergic receptors in stem cell differentiation
A major challenge modern society has to face is the increasing need for tissue regeneration due to degenerative diseases or tumors, but also accidents or warlike conflicts.
Constanze Kaebisch+3 more
doaj +1 more source
The relationship between P2X4 and P2X7: a physiologically important interaction? [PDF]
Purinergic signaling within the kidney is becoming an important focus in the study of renal health and disease. The effectors of ATP signaling, the P2Y and P2X receptors, are expressed to varying extents in and along the nephron.
Birch, Rebecca E+3 more
core +3 more sources
Neuroreceptor Activation by Vibration-Assisted Tunneling [PDF]
G protein-coupled receptors (GPCRs) constitute a large family of receptor proteins that sense molecular signals on the exterior of a cell and activate signal transduction pathways within the cell. Modeling how an agonist activates such a receptor is fundamental for an understanding of a wide variety of physiological processes and it is of tremendous ...
arxiv +1 more source
Coexpression of rat P2X2 and P2X6 subunits in Xenopus oocytes. [PDF]
Transcripts for P2X(2) and P2X(6) subunits are present in rat CNS and frequently colocalize in the same brainstem nuclei. When rat P2X(2) (rP2X(2)) and rat P2X(6) (rP2X(6)) receptors were expressed individually in Xenopus oocytes and studied under ...
Burnstock, G+5 more
core +1 more source
Extracellular ATP released by osteoblasts is a key local inhibitor of bone mineralisation [PDF]
Previous studies have shown that exogenous ATP (>1µM) prevents bone formation in vitro by blocking mineralisation of the collagenous matrix. This effect is thought to be mediated via both P2 receptor-dependent pathways and a receptor-independent ...
A Brandao-Burch+49 more
core +9 more sources
Pharmacological characterization of P2X1 and P2X3 purinergic receptors in bovine chondrocytes [PDF]
SummaryObjectiveThe aim of the present study is that of characterizing, for the first time in a quantitative way, from a biochemical, physico chemical and functional point of view P2X1 and P2X3 purinergic receptors in bovine chondrocytes.
Borea, P.A.+9 more
core +1 more source
Synthesis and Structure-Activity Relationships of Pyridoxal-6-arylazo-5'-phosphate and Phosphonate Derivatives as P2 Receptor Antagonists. [PDF]
Novel analogs of the P2 receptor antagonist pyridoxal-5'-phosphate-6-phenylazo-2',4'-disulfonate (PPADS) were synthesized. Modifications were made through functional group substitution on the sulfophenyl ring and at the phosphate moiety through the ...
Boyer, José L.+13 more
core +3 more sources