High-throughput screening assay for new ligands at human melatonin receptors

Acta Pharmacologica Sinica

Volumn 29, Issue 12, 2008, Pages 1515-1521

  Yan, Jian Hua ^a   Su, Hao Ran ^a   Boutin, Jean A ^b   Renard, M Pierre ^b   Wang, Ming Wei ^a  

^a SHANGHAI INSTITUTE OF MATERIA MEDICA   (China)

^b INSTITUT DE RECHERCHES INTERNATIONALES SERVIER   (France)

Author keywords

Agonist; Antagonist; Melatonin; Receptor; Selectivity

Indexed keywords

GUANOSINE TRIPHOSPHATE; HORMONE RECEPTOR BLOCKING AGENT; HORMONE RECEPTOR STIMULATING AGENT; LIGAND; MELATONIN; MELATONIN 1 RECEPTOR; MELATONIN 2 RECEPTOR; NATURAL PRODUCT; NC 00004068; NC 00076880; NC 00080421; NC 00085323; NC 00085862; NC 00085864; NC 00085892; NC 00086791; NC 00087441; NC 00089216; NC 00090038; NC 00090702; NC 00094488; NC 00096199; NC 00096661; NC 00098918; NC 00099763; NC 00100636; RECEPTOR SUBTYPE; UNCLASSIFIED DRUG;

AGONIST; ANIMAL CELL; ARTICLE; CHO CELL; CONTROLLED STUDY; DRUG IDENTIFICATION; DRUG POTENCY; DRUG RECEPTOR BINDING; DRUG SCREENING; DRUG STRUCTURE; FEMALE; HIGH THROUGHPUT SCREENING; NONHUMAN; STRUCTURE ACTIVITY RELATION; ANIMAL; CHEMICAL STRUCTURE; CHEMISTRY; DRUG ANTAGONISM; HUMAN; METABOLISM; METHODOLOGY; RADIOASSAY;

ANIMALS; HUMANS; LIGANDS; MELATONIN; MOLECULAR STRUCTURE; RADIOLIGAND ASSAY; RECEPTOR, MELATONIN, MT1; RECEPTOR, MELATONIN, MT2;

EID: 64549116824     PISSN: 16714083     EISSN: 17457254     Source Type: Journal    
DOI: 10.1111/j.1745-7254.2008.00903.x     Document Type: Article

References (39)

1. Reiter RJ. Pineal melatonin: cell biology of its synthesis and of its physiological interactions. Endocr Rev 1991; 12: 151-80.
2. Lerner AB, Case JD. Structure of melatonin. J Am Chem Soc 1959; 81: 6084-5.
3. Cassone VM. Melatonin's role in vertebrate circadian rhythms. Chronobiol Int 1998; 15: 457-73.
4. Krause DN, Geary GG, Doolen S, Duckles SP. Melatonin and cardiovascular function. Adv Exp Med Biol 1999; 460: 299-310.
5. Reiter RJ. Melatonin and human reproduction. Ann Med 1998; 30: 103-8.
6. Jones MP, Melan MA, Witt-Enderby PA. Melatonin decreases cell proliferation and transformation in a melatonin receptor-dependent manner. Cancer Lett 2000; 151: 133-43.
7. Dubocovich ML. Characterization of a retinal melatonin receptor. J Pharmacol Exp Ther 1985; 234: 395-401.
8. 125I]iodomelatonin to characterize melatonin binding sites in chicken retina. Proc Natl Acad Sci USA 1987; 84: 3916-20.
9. Reppert SM, Weaver DR, Ebisawa T. Cloning and characterization of a mammalian melatonin receptor that mediates reproductive and circadian responses. Neuron 1994; 13: 1177-85.
10. Reppert SM, Godson C, Mahle CD, Weaver DR, Slaugenhaupt SA, Gusella JF. Molecular characterization of a second melatonin receptor expressed in human retina and brain: the Mel1b melatonin receptor. Proc Natl Acad Sci USA 1995; 92: 8734-8.
11. Hunt AE, Ghoul WM, Dubocovich ML. Activation of melatonin MT2 receptors in rat suprachiasmatic nucleus phase advances the circadian clock. Am J Physiol Cell Physiol 2001; 280: C110-C8.
12. 3 as the quinone reductase 2. J Biol Chem 2000; 257: 31 311-7.
13. 2. Biochem Pharmacol 2001; 61: 1369-79.
14. Dubocovich ML, Cardinali DP, Delagrange P, Krause DN, Strosberg D, Sugden D, et al. The IUPHAR compendium of receptor characterization and classifcation. IUPHAR Media, London 2000: 270-7.
15. Al-Ghoul WM, Herman MD, Dubocovich ML. Melatonin receptor subtype expression in human cerebellum. Neuroreport 1998; 9: 4063-8.
16. 1 melatonin receptor subtype in tail artery of juvenile Wistar rats. Br J Pharmacol 1999; 127: 987-95.
17. Mazzucchelli C, Pannacci M, Nonno R, Lucini V, Fraschini F, Stankov BM. The melatonin receptor in the human brain: cloning experiments and distribution studies. Brain Res Mol Brain Res 1996; 39: 117-26.
18. Weaver DR, Reppert SM. The Mel1a melatonin receptor gene is expressed in human suprachiasmatic nuclei. Neuroreport 1996; 8: 109-12.
19. Song Y, Chan CW, Brown GM, Pang SF, Silverman M. Studies of the renal action of melatonin: evidence that the effects are mediated by 37 kDa receptors of the Mel1a subtype localized primarily to the basolateral membrane of the proximal tubule. FASEB J 1997; 11: 93-100.
20. Delagrange P, Guardiola-Lemaitre B. Melatonin, its receptors and relationships with biological rhythms disorders. Clin Neuropharmacol 1997; 20: 482-510.
21. Mahle CD, Takaki KS, Watson AJ. Melatonin receptor ligands and their potential clinical applications. Annu Rep Med Chem 1997: 31-40.
22. Wu B, Gao J, Wang MW. Development of a complex scintillation proximity assay for high-throughput screening of PPARγ modulators. Acta Pharmacol Sin 2005; 26: 339-44.
23. 35S]GTPγS binding assay: approaches and applications in pharmacology. Life Sci 2003; 74: 489-508.
24. 2 receptors. Naunyn Schmiedeberg's Arch Pharmacol 2003; 367: 553-61.
25. Bradford MM. A rapid and sensitive method for the quantitation of microgram quantities of protein utilizing the principle of protein-dye binding. Anal Biochem 1976; 72: 248-54.
26. 50) of an enzymatic reaction. Biochem Pharmacol 1973; 22: 3099-108.
27. Cohen FR, Lazareno S, Birdsall NJM. The effects of saponin on the binding and functional properties of the human adenosine A1 receptor. Br J Pharmacol 1996; 117: 1521-9.
28. Zhang J-H, Chung TDY, Oldenburg KR. A simple statistical parameter for use in evaluation and validation of high throughput screening assays. J Biomol Screen 1999; 4: 67-73.
29. Dubocovich ML, Masana MI, Iacob S, Sauri DM. Melatonin receptor antagonists that differentiate between the human Mel1a and Mel1b recombinant subtypes are used to assess the pharmacological profle of the rabbit retina ML1 presynaptic heteroreceptor. Naunyn- Schmiedeberg's Arch Pharmacol 1997; 355: 365-75.
30. 2 receptor models. J Med Chem 2005; 48: 4049-60.
31. Lewy AJ, Emens J, Jackman A, Yuhas K. Circadian uses of melatonin in humans. Chronobiol Int 2006; 23: 403-12.
32. Srinivasan V, Smits M, Spence W, Lowe AD, Kayumov L, Pandi- Perumal SR, et al. Melatonin in mood disorders. World J Biol Psychiatry 2006; 7: 138-51.
33. Poeggeler B. Melatonin, aging, and age-related diseases: perspectives for prevention, intervention, and therapy. Endocrine 2005; 27: 201-12.
34. Srinivasan V, Maestroni G, Cardinali D, Esquifino A, Perumal SP, Miller S. Melatonin, immune function and aging. Immun Ageing 2005; 2: 17.
35. 1 and MT2 are decreased in Alzheimer's disease. Eur J Histochem 2006; 50: 311-6.
36. Naguib M, Gottumukkala V, Goldstein PA. Melatonin and anesthesia: a clinical perspective. J Pineal Res 2007; 42: 12-21.
37. Banki MC. Agomelatin: the first "melatoninergic" antidepressant. Neuropsychopharmacol Hung 2006; 8: 105-12.
38. Hussein MR, Ahmed OG, Hassan AF, Ahmed MA. Intake of melatonin is associated with amelioration of physiological changes, both metabolic and morphological pathologies associated with obesity: an animal model. Int J Exp Pathol 2007; 88: 19-29.
39. Delagrange P, Boutin JA. Therapeutic potential of melatonin ligands. Chronobiol Int 2006; 23: 413-8.