scholarly journals Mapping the binding sites of UDP and prostaglandin E2 glyceryl ester in the nucleotide receptor P2Y6

ChemMedChem ◽  
2022 ◽  
Author(s):  
Anne Zimmermann ◽  
Oanh Vu ◽  
Antje Brüser ◽  
Gregory Sliwoski ◽  
Lawrence J. Marnett ◽  
...  
Keyword(s):  
Prostaglandin E2 ◽  
Binding Sites ◽  
Nucleotide Receptor

Prostaglandin E2-binding sites and cAMP production in porcine fundic mucosa

1981 ◽  
Vol 241 (4) ◽  
pp. G313-G320
Author(s):  
B. L. Tepperman ◽  
B. D. Soper
Keyword(s):  
Adenylate Cyclase ◽  
Prostaglandin E2 ◽  
Binding Site ◽  
Binding Sites ◽  
Biologically Active ◽  
Cyclase Activity ◽  
Adenylate Cyclase Activity ◽  
Scatchard Analysis ◽  
Fundic Mucosa ◽  
Stimulation Of

Biologically active [3H]prostaglandin E2 (PGE2) bound rapidly and specifically to membrane fractions from hog fundic mucosa. Optimal binding occurred in the 30,000-g membrane preparation at 37 degrees C (pH 5.0). Scatchard analysis of specific PgE2 binding revealed the presence of a heterogeneous population of binding sites with Kd values and binding site concentrations of approximately 1 X 10(-9) M and 1 fmol/mg prot and 2 X 10(-8) M and 20 fmol/mg prot, respectively. Specific binding was inhibited by the following agents in descending order of potency: PGE1, PGA2, PGD2, 6-keto-PGF1 alpha, and thromboxane B2. Trypsin treatment or boiling reduced or abolished specific PGE2 binding. PGE2 stimulated cAMP formation in the 2,500-g fraction, with an approximate Km of 1 X 10(-6) M, but stimulation of adenylate cyclase activity by PG was not evident in the 16,000-g or 30,000-g tissue preparations. These results suggest that a specific PGE2-binding site exists in the 16,000-g and 30,000-g fractions of porcine fundic mucosa, although an increase in cAMP-forming capacity could not b of 1 X 10(-6) M, but stimulation of adenylate cyclase activity by PG was not evident in the 16,000-g or 30,000-g tissue preparations. These results suggest that a specific PGE2-binding site exists in the 16,000-g and 30,000-g fractions of porcine fundic mucosa, although an increase in cAMP-forming capacity could not b of 1 X 10(-6) M, but stimulation of adenylate cyclase activity by PG was not evident in the 16,000-g or 30,000-g tissue preparations. These results suggest that a specific PGE2-binding site exists in the 16,000-g and 30,000-g fractions of porcine fundic mucosa, although an increase in cAMP-forming capacity could not be localized in these fractions in vitro.

Subcellular distribution of [3H]-prostaglandin E2 binding sites in porcine gastric mucosa

1983 ◽  
Vol 25 (3) ◽  
pp. 425-441 ◽  
Author(s):  
Barry L. Tepperman ◽  
Brian D. Soper
Keyword(s):  
Gastric Mucosa ◽  
Prostaglandin E2 ◽  
Binding Sites ◽  
Subcellular Distribution

Detailed mapping of prostaglandin E2 binding sites in the brain

1991 ◽  
Vol 14 ◽  
pp. S141
Author(s):  
Kiyoshi Matsumura ◽  
Yumiko Watanabe ◽  
Hirotaka Onoe ◽  
Yoshimasa Koyama ◽  
Michael Connolly ◽  
...  
Keyword(s):  
Prostaglandin E2 ◽  
Binding Sites ◽  
The Brain

Modulation of 3H-prostaglandin E2 binding sites in the rabbit gastric mucosa

1990 ◽  
Vol 39 (2) ◽  
pp. 113-122 ◽  
Author(s):  
M. Tomoi ◽  
M. Matsuo ◽  
T. Ono ◽  
F. Shibayama
Keyword(s):  
Gastric Mucosa ◽  
Prostaglandin E2 ◽  
Binding Sites

scholarly journals Quantitative autoradiographic localization of prostaglandin E2 binding sites in monkey diencephalon

1988 ◽  
Vol 8 (6) ◽  
pp. 2003-2010 ◽  
Author(s):  
Y Watanabe ◽  
Y Watanabe ◽  
O Hayaishi
Keyword(s):  
Prostaglandin E2 ◽  
Binding Sites

scholarly journals Desensitization of P2U receptor in neuronal cell line. Different control by the agonists ATP and UTP, as demonstrated by single-cell Ca2+ responses

1996 ◽  
Vol 320 (1) ◽  
pp. 215-219 ◽  
Author(s):  
Uwe CZUBAYKO ◽  
Georg REISER
Keyword(s):  
Single Cell ◽  
Cell Line ◽  
Binding Sites ◽  
Neuronal Cell ◽  
Nucleotide Receptor ◽  
Maximal Amplitude ◽  
Neuronal Cell Line ◽  
Natural Ligands ◽  
Extracellular Stimuli ◽  
Comparable Size

The neuronal cell line NG108-15 (180CC15) responds to extracellular stimuli of ATP or UTP with a transient increase in the level of cytosolic Ca2+. Desensitization was investigated by recording single-cell Ca2+ responses induced by consecutive, regularly spaced (100 s intervals), brief pulses of the nucleotides. The two natural ligands of the P2U receptor, ATP and UTP, were applied at a concentration that evoked responses of a comparable size. With two pulses of UTP (10 µM), a substantial decrease (of 43%) was observed in the size of the second response. The magnitude of response was determined by measuring either the maximal amplitude or the total response, represented by the area of the Ca2+ transient. The analogous studies with ATP pulses showed a much smaller decrease (of 12%). Comparable experiments performed to investigate the mutual interaction between ATP and UTP revealed that after stimulation with ATP the response to UTP was slightly (12%) diminished, whereas the response to ATP after UTP was greatly (52%) decreased. The different degree of desensitization by either UTP or ATP of P2U receptors could be due to (1) a difference in the mode of activation of the receptor by the two ligands or (2) recruitment of another effector mechanism besides elevated Ca2+. Our results indicate the existence of a novel mechanism of receptor control, involving different modes of the receptor, that are induced by two different, activating ligands. We also investigated the cross-talk between the bradykinin B2 receptor and the nucleotide receptor. ATP and UTP, even when eliciting responses of comparable size in the neuronal cell line, affect the desensitization of the bradykinin receptor differently. This suggests regulatory binding sites for the nucleotides on either the nucleotide receptor or the peptide receptor.

scholarly journals Prostaglandin E2 glyceryl ester is an endogenous agonist of the nucleotide receptor P2Y6

2017 ◽  
Vol 7 (1) ◽  
Author(s):  
Antje Brüser ◽  
Anne Zimmermann ◽  
Brenda C. Crews ◽  
Gregory Sliwoski ◽  
Jens Meiler ◽  
...  
Keyword(s):  
Prostaglandin E2 ◽  
Nucleotide Receptor
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