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Proceedings of the National Academy of Sciences of the United States of America logoLink to Proceedings of the National Academy of Sciences of the United States of America
. 1981 Apr;78(4):2218–2220. doi: 10.1073/pnas.78.4.2218

beta-Endorphin: characteristics of binding sites in a neuroblastoma--glioma hybrid cell.

R G Hammonds Jr, P Ferrara, C H Li
PMCID: PMC319315  PMID: 6264469

Abstract

Specific binding of human beta-endorphin to NG108-15 cells is described; human beta-[Tyr27-3H2] endorphin was used as the ligand. The binding is time dependent and saturable; Kd = 0.3 nM and ka = 1.8 x 10(8) M-1 min-1. Under the conditions optimal for beta-endorphin binding, leucine-enkephalin has one-fourth to one-third as many binding sites as beta-endorphin and its affinity is 7--10% that of beta-endorphin. Monovalent and divalent cations potently inhibit binding. Trypsin, phospholipase A, and N-ethylmaleimide reduce the ability of NG108-15 cells to bind beta-endorphin. beta-Endorphin analogs are able to fully inhibit the binding of beta-[Tyr27-3H2]endorphin, although enkephalins, morphine, and naloxone inhibit only 50--80%.

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Selected References

These references are in PubMed. This may not be the complete list of references from this article.

  1. Blume A. J. Opiate binding to membrane preparations of neuroblastoma x glioma hybrid cells NG108-15: effects of ions and nucleotides. Life Sci. 1978 May 22;22(20):1843–1852. doi: 10.1016/0024-3205(78)90602-1. [DOI] [PubMed] [Google Scholar]
  2. Blume A. J., Shorr J., Finberg J. P., Spector S. Binding of the endogenous nonpeptide morphine-like compound to opiate receptors. Proc Natl Acad Sci U S A. 1977 Nov;74(11):4927–4931. doi: 10.1073/pnas.74.11.4927. [DOI] [PMC free article] [PubMed] [Google Scholar]
  3. Brandt M., Buchen C., Hamprecht B. Endorphins exert opiate-like action on neuroblastoma x glioma hybrid cells. FEBS Lett. 1977 Aug 15;80(2):251–254. doi: 10.1016/0014-5793(77)80451-1. [DOI] [PubMed] [Google Scholar]
  4. Chang K. J., Cuatrecasas P. Multiple opiate receptors. Enkephalins and morphine bind to receptors of different specificity. J Biol Chem. 1979 Apr 25;254(8):2610–2618. [PubMed] [Google Scholar]
  5. Chang K. J., Hazum E., Cuatrecasas P. Possible role of distinct morphine and enkephalin receptors in mediating actins of benzomorphan drugs (putative kappa and sigma agonists). Proc Natl Acad Sci U S A. 1980 Aug;77(8):4469–4473. doi: 10.1073/pnas.77.8.4469. [DOI] [PMC free article] [PubMed] [Google Scholar]
  6. Chang K. J., Miller R. J., Cuatrecasas P. Interaction of enkephalin with opiate receptors in intact cultured cells. Mol Pharmacol. 1978 Nov;14(6):961–970. [PubMed] [Google Scholar]
  7. Ferrara P., Houghten R., Li C. H. beta-Endorphin: characteristics of binding sites in the rat brain. Biochem Biophys Res Commun. 1979 Aug 13;89(3):786–792. doi: 10.1016/0006-291x(79)91847-3. [DOI] [PubMed] [Google Scholar]
  8. Gerber L. D., Stein S., Rubinstein M., Wideman J., Udenfriend S. Binding assay for opioid peptides with neuroblastoma x glioma hybrid cells: specificity of the receptor site. Brain Res. 1978 Jul 28;151(1):117–126. doi: 10.1016/0006-8993(78)90954-x. [DOI] [PubMed] [Google Scholar]
  9. Houghten R. A., Chang W. C., Li C. H. Human beta-endorphin: synthesis and characterization of analogs iodinated and tritiated at tyrosine residues 1 and 27. Int J Pept Protein Res. 1980 Oct;16(4):311–320. doi: 10.1111/j.1399-3011.1980.tb02592.x. [DOI] [PubMed] [Google Scholar]
  10. Houghten R. A., Li C. H. Preparation and properties of tritiated human beta-endorphin with high specific radioactivity. Int J Pept Protein Res. 1978 Nov;12(5):325–326. doi: 10.1111/j.1399-3011.1978.tb02904.x. [DOI] [PubMed] [Google Scholar]
  11. Klee W. A., Nirenberg M. A neuroblastoma times glioma hybrid cell line with morphine receptors. Proc Natl Acad Sci U S A. 1974 Sep;71(9):3474–3477. doi: 10.1073/pnas.71.9.3474. [DOI] [PMC free article] [PubMed] [Google Scholar]
  12. Law P. Y., Loh H. H., Li C. H. Properties and localization of beta-endorphin receptor in rat brain. Proc Natl Acad Sci U S A. 1979 Nov;76(11):5455–5459. doi: 10.1073/pnas.76.11.5455. [DOI] [PMC free article] [PubMed] [Google Scholar]
  13. Li C. H., Chung D. Isolation and structure of an untriakontapeptide with opiate activity from camel pituitary glands. Proc Natl Acad Sci U S A. 1976 Apr;73(4):1145–1148. doi: 10.1073/pnas.73.4.1145. [DOI] [PMC free article] [PubMed] [Google Scholar]
  14. Li C. H., Lemaire S., Yamashiro D., Doneen B. A. The synthesis and opiate activity of beta-endorphin. Biochem Biophys Res Commun. 1976 Jul 12;71(1):19–25. doi: 10.1016/0006-291x(76)90243-6. [DOI] [PubMed] [Google Scholar]
  15. Li C. H., Yamashiro D., Tseng L. F., Loh H. H. Synthesis and analgesic activity of human beta-endorphin. J Med Chem. 1977 Mar;20(3):325–328. doi: 10.1021/jm00213a001. [DOI] [PubMed] [Google Scholar]
  16. Loh H. H., Tseng L. F., Wei E., Li C. H. beta-endorphin is a potent analgesic agent. Proc Natl Acad Sci U S A. 1976 Aug;73(8):2895–2898. doi: 10.1073/pnas.73.8.2895. [DOI] [PMC free article] [PubMed] [Google Scholar]
  17. Maelicke A., Fulpius B. W., Klett R. P., Reich E. Acetylcholine receptor. Responses to drug binding. J Biol Chem. 1977 Jul 25;252(14):4811–4830. [PubMed] [Google Scholar]
  18. Pasternak G. W., Snowman A. M., Snyder S. H. Selective enhancement of [3H]opiate agonist binding by divalent cations. Mol Pharmacol. 1975 Nov;11(6):735–744. [PubMed] [Google Scholar]
  19. Pert C. B., Pasternak G., Snyder S. H. Opiate agonists and antagonists discriminated by receptor binding in brain. Science. 1973 Dec 28;182(4119):1359–1361. doi: 10.1126/science.182.4119.1359. [DOI] [PubMed] [Google Scholar]
  20. Sharma S. K., Nirenberg M., Klee W. A. Morphine receptors as regulators of adenylate cyclase activity. Proc Natl Acad Sci U S A. 1975 Feb;72(2):590–594. doi: 10.1073/pnas.72.2.590. [DOI] [PMC free article] [PubMed] [Google Scholar]
  21. Simantov R., Snowman A. M., Snyder S. H. Temperature and ionic influences on opiate receptor binding. Mol Pharmacol. 1976 Nov;12(6):977–986. [PubMed] [Google Scholar]
  22. Simantov R., Snyder S. H. Morphine-like peptides, leucine enkephalin and methionine enkephalin: interactions with the opiate receptor. Mol Pharmacol. 1976 Nov;12(6):987–998. [PubMed] [Google Scholar]
  23. Swann R. W., Li C. H. Characterization of turkey myelin basic protein isolated by a simple procedure. Int J Pept Protein Res. 1979;14(5):495–503. doi: 10.1111/j.1399-3011.1979.tb01961.x. [DOI] [PubMed] [Google Scholar]
  24. Yamashiro D., Li C. H., Tseng L. F., Loh H. H. beta-Endorphin: synthesis and analgesic activity of several analogs modified in positions 2 and 5. Int J Pept Protein Res. 1978 Apr;11(4):251–257. doi: 10.1111/j.1399-3011.1978.tb02847.x. [DOI] [PubMed] [Google Scholar]

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