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Citations Publications citing this paper. Activation of apical P2U purine receptors permits inhibition of adrenaline-evoked cyclic AMP accumulation in cultured equine sweat gland epithelial cells. Stuart M. The role of P2Y2 nucleotide receptors in vascular inflammation Niefang Yu. A pulsed DC electric field affects P2-purinergic receptor functions by altering the ATP levels in in vitro and in vivo systems.

Untersuchungen zur Charakterisierung eines Purinozeptors und zur Expression von Komplementfaktoren des klassischen Aktivierungsweges in humanen Praeadipozyten Christian Kramheller. Human Fallopian tubal epithelial cells in vitro: establishment of polarity and potential role of intracellular calcium and extracellular ATP in fluid secretion.

Molecular Recognition at Purine and Pyrimidine Nucleotide (P2) Receptors

References Publications referenced by this paper. Activation of phospholipase C and protein kinase C has little involvement in ADP-induced primary aggregation of human platelets: effects of diacylglycerols, the diacylglycerols, the diacylglycerol kinase inhibitor R, staurosporine and okadaic acid.

  • Purine and Pyrimidine (P2) Receptors as Drug Targets | Journal of Medicinal Chemistry;
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Marian A. Packham , Avinoam Livne , Douglas H. Ruben , Margaret L. Louise C. Morris , Donald H. Under physiological conditions, P2Y14 appears to be neither essential for normal embryonic development nor for the maintenance of tissue homeostasis in the adult organism.

P2 receptors: new frontiers

However, the embryo is exceptionally sensitive to radiation-induced damage, and under the stress conditions of total body irradiation TBI , P2Y14 KO embryos were more prone to undergoing IR-induced senescence than WT embryos. In the adult, hematopoietic cells are among the most sensitive cells to radiation injury.

P2Y14 KO mice were more sensitive to radiation, showing a more severe reduction in the number of BM cells than that observed in WT mice.

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  3. PET imaging of P2 purinoceptors.
  4. Together, radiation stress, aging, sequential exposure to chemotherapy, and serial bone marrow transplantation increased senescence in animals lacking P2Y There is growing interest in abnormal expression and dysfunction of P2 receptors in tumor cells. Different P2 receptor subtypes are involved in the growth inhibitory response observed in the different malignant cell types challenged with ATP or other nucleotides However, it is likely that the final effect is caused by the combination of contributions from multiple P2 receptor subtypes than a single subtype.

    To date, five P2 receptor subtypes have primarily been implicated in the growth inhibition of tumor cells, namely P2X5, P2X7, P2Y1, P2Y2 and P2Y11 42 , however, the significance of these receptors differ among cell lines. Among P2 receptors, the P2X7 subtype is most widely accepted as the purinergic receptor mediator of apoptotic or necrotic cell death as initially suggested by early experiments in mouse tumor cell lines where ATP was shown to trigger cell death via a necrosis or apoptosis.

    Purinergic receptor - Wikipedia

    However, analysis of the effect of the P2X7 receptor on tumor growth made it more complex by the observation that tonic, as opposed to pharmacological, stimulation may have a trophic, growth-promoting, rather than cytotoxic effect in leukemia cells 43 , such as chronic lymphocytic leukemia CLL 44 , 45 , chronic myeloid leukemia CML , acute lymphocytic leukemia ALL and acute myeloid leukemia AML. In pediatric AML patients, Chong et al. A significant decrease in the expression of P2X4, P2X5 and P2X7 receptors was observed after complete remission after chemotherapy Salvestrini et al.

    The abnormal expression of purinergic receptors in leukemia cells suggested a wide dysregulation and a possible pathogenic role of purinergic signaling in hematologic malignancies. Besides over-expression of P2X7 in leukemia and tumor cells, evidence from in vitro and in vivo studies indicated that the addition of exogenous ATP to leukemia and colon cancer cells inhibited cell growth Hence, the pro-apoptotic effects of P2X7 receptor was firstly proposed in early studies.

    The binding of ATP induced within milliseconds the opening of a channel selective for small cations, and then within seconds a larger pore non-selectively permeable to molecules with a mass of up to Da, resulting in cell apoptosis Then, Salvestrini et al.

    Expression and function of P2 receptors in hematopoietic stem and progenitor cells

    This changes on expression of cell-cycle related genes resulted in a cell-cycle arrest in the G0 phase, and a decrease of G1- and S-phase cells, and finally inhibition of AML proliferation and CFU-Ls formation Moreover, a series of P2X7 polymorphisms have been discovered, and their impacts on P2X7 functions, mechanisms, and relationship with diseases were studied in a number of variants Among several loss-of-function polymorphisms 50 - 52 , a hyposensitive mutant is also found in leukemia cells 53 , whose DNA sequencing analysis revealed a substitution of A with G, causing an ND substitution.

    This mutation is hyposensitive to its ligand, and leukemia cells bearing this P2X7 mutant have a greater growth potential in vitro experiment and in a nude mouse model. Furthermore, elevated angiogenesis and CDpositive macrophage infiltration could be detected in tumor tissues formed by K cells bearing this mutant P2Y2 and P2Y4 receptors appeared to be the primary subtypes involved in this process. In addition to abnormal expression and dysfunction of P2 receptors in tumors, cells within tumor microenvironment also have altered expression of P2 receptors and exhibited the surprising function.

    Recently, there are some new reports about the amusing role of P2X7 in tumorgenesis. Adinolfi et al.

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    They showed that host P2X7 expression was critical to support an antitumor immune response, and to restrict tumor growth and metastatic diffusion Hofman et al. Finally, P2X7 blockade altered immune cell infiltration and promoted Treg accumulation within lesions of the digestive system. Hence, based on the apparently contradictory evidence, the precise role of P2X7 in vivo in the context of inflammation-associated carcinogenesis needs to be carefully addressed, and the use of P2X7 inhibitors to treat IBD give the possibility of increasing risks CAC as a result.

    Similar to the above-mentioned, not only abnormal expression and dysfunction of P2 receptors were found in leukemia cells, cells within leukemia microenvironment also have altered expression of P2 receptors.


    In Notch1-induced leukemia model, during the development of leukemia, the expression levels of multiple subtypes of P2X in macrophages from bone marrow, spleen and peritoneal cavity were changed. In particular, P2X7 expression in macrophages from these microenvironments significantly increased. Abnormal expression and function of P2X7 could be associated with apoptosis of macrophages in late stage of leukemia P2Y family has 8 receptors that can be divided into two sub-families depending upon the structural similarity.

    P2X receptors are activated with ATP while P2Y receptors are activated by diphosphates, triphosphates, purines, pyrimidines, etc. From Wikipedia, the free encyclopedia. P2 receptor may refer to: Nucleotides if get released into the extracellular environment can lead to cell death or some other harmful cellular consequences. Purinergic Signalling. Seminars in Thrombosis and Hemostasis. Categories : G protein-coupled receptors Biochemistry stubs.