What is P2Y2 receptor?
As one of G-protein-coupled receptors, P2Y2 receptor can transactivate EGFR and increase mitogen-activated protein kinase and phosphoinositide 3-kinase activity in many cancer cells (Soltoff, 1998; Muscella et al, 2003). P2Y2 receptor exerts contrasting effects on cell proliferation of different cancers.
What does receptor desensitization mean?
Receptor desensitization refers to the decreased responsiveness that occurs with repeated or chronic exposure to agonist and is a general feature of most signaling membrane receptors.
What are the two mechanisms for receptor desensitization?
While the different mechanisms for desensitization are still being characterized, there are currently four known mechanisms: uncoupling of receptors from associated G proteins, endocytosis, degradation, and downregulation.
How do P2Y receptors work?
P2Y receptors are present in almost all human tissues where they exert various biological functions based on their G-protein coupling. P2Y receptors mediate responses including vasodilation, blood clotting, and immune response.
Where are P2Y2 receptors found?
P2X5 and P2X7 receptors are expressed by epithelial cells of the rat nasal mucosa. P2Y1, P2Y2, P2Y6 and P2Y11 receptors are found to be expressed by respiratory epithelium. While adenosine receptors are known to be expressed by apical epithelial cells, as yet they have only been characterized as A2 receptors.
Is clopidogrel a P2Y12?
P2Y12 receptor blockers are another group of antiplatelet drugs. This group of drugs includes: clopidogrel, ticlopidine, ticagrelor, prasugrel, and cangrelor.
What causes receptor desensitisation?
What is desensitization biochemistry?
Typically, desensitization is a receptor (biochemistry)-based phenomenon in which one receptor type, when bound to its ligand, becomes unable to further influence the signalling pathways by which it regulates cells and, in the case of cell surface membrane receptors, may thereafter be internalized.
Where are P2Y receptors found?
Pharmacology of Purine and Pyrimidine Receptors P2Y receptors are expressed in both neurons and glial cell types in the CNS (Abbracchio et al., 2009; Fischer & Krügel, 2007).
Is clopidogrel an anticoagulant drug?
Some common antiplatelet drugs are aspirin, dipyridamole and clopidogrel. Anticoagulants Anticoagulants also stop your blood from being able to clot as easily. They do this by stopping your blood from producing certain proteins, which platelets need to help them form a clot.
What is the function of P2Y2 receptors?
P2Y 2 receptors can directly couple to PLC β1 via G αq/11 protein to mediate the production of InsP 3 and diacylglycerol, which are second messengers for calcium release from intracellular stores and protein kinase C (PKC) activation, respectively. Expression of P2Y 2 receptor mRNA and protein has been detected in many tissues.
What is a P2Y 2 receptor knockout mouse?
A P2Y 2 receptor knockout mouse has been produced that is defective in nucleotide-stimulated ion secretion in airway epithelial cells. P2Y 2 receptors have been shown to inhibit bone formation by osteoblasts, and N-type calcium currents in neurons.
Is suramin a P2Y 2 antagonist?
For example, suramin has been shown to be an antagonist of the P2Y 2 receptor (see below), but the low affinity of this antagonism together with weak activity at the P2Y 4 and P2Y 6 receptors makes it unsuitable for clear pharmacological distinction among the three receptors.
Where are P2X receptors found in the nose?
P2X3 receptors are expressed by primary olfactory neurones located both in the olfactory epithelium and on subepithelial nerve fibres in the respiratory region. P2X5 and P2X7 receptors are expressed by epithelial cells of the rat nasal mucosa. P2Y 1, P2Y 2, P2Y 6 and P2Y 11 receptors are found to be expressed by respiratory epithelium.