The thyroid disruptor 1,1,1-trichloro-2,2-bis(p-chlorophenyl)-ethane appears to be an uncompetitive inverse agonist for the thyrotropin receptor

Journal of Pharmacology and Experimental Therapeutics

Volumn 320, Issue 1, 2007, Pages 465-474

  Rossi, Mario ^a   Dimida, Antonio ^a   Dell'anno, Maria Teresa ^a   Trincavelli, Maria Letizia ^a   Agretti, Patrizia ^a   Giorgi, Franco ^a   Corsini, Giovanni U ^a   Pinchera, Aldo ^a   Vitti, Paolo ^a   Tonacchera, Massimo ^a   Maggio, Roberto ^a,b  

^a UNIVERSITY OF PISA   (Italy)

^b UNIVERSITY OF L'AQUILA   (Italy)

Author keywords

[No Author keywords available]

Indexed keywords

1,1,1 TRICHLORO 2,2 BIS(4 CHLOROPHENYL) ETHANE; ADENOSINE 5' (N ETHYLCARBOXAMIDE); ADENOSINE A2 RECEPTOR; AROCLOR 1254; BETA 2 ADRENERGIC RECEPTOR; CYCLIC AMP; DOPAMINE 1 RECEPTOR; DOPAMINE RECEPTOR STIMULATING AGENT; FORSKOLIN; INSECTICIDE; ISOPRENALINE; STILBENE DERIVATIVE; THYROTROPIN RECEPTOR; TRYPSIN; UNCLASSIFIED DRUG;

ANIMAL CELL; ARTICLE; CELL STRAIN COS7; CERCOPITHECIDAE; CHO CELL; DRUG ACTIVITY; DRUG EFFECT; DRUG MECHANISM; ENZYME INHIBITION; GENETIC TRANSFECTION; HOMEOSTASIS; INHIBITION KINETICS; NONHUMAN; PRIORITY JOURNAL; PROTEIN FUNCTION; PROTEIN INTERACTION; THYROID GLAND;

ADENOSINE-5'-(N-ETHYLCARBOXAMIDE); ADENYLATE CYCLASE; ANIMALS; AROCLOR 1254; CERCOPITHECUS AETHIOPS; CHO CELLS; COS CELLS; CRICETINAE; CYCLIC AMP; DDT; FORSKOLIN; PHENOLS; RECEPTORS, THYROTROPIN; THYROTROPIN;

EID: 33845966395     PISSN: 00223565     EISSN: 15210103     Source Type: Journal    
DOI: 10.1124/jpet.106.113613     Document Type: Article

References (35)

1. Birnbaumer M (1995) Mutation and diseases of G-protein coupled receptors. J Recept Signal Transduct Res 15:131-160.
2. Brucker-Davis F (1998) Effects of environmental synthetic chemicals on thyroid function. Thyroid 8:827-856.
3. Cetani F, Tonacchera M, and Vassart G (1996) Differential effect of NaCl concentration on the constitutive activity of the thyrotropin and the luteinizing hormone/chorionic gonadotropin receptor. FEBS Lett 378:27-31.
4. Chen A, Zhang J, Zhou L, Gao ES, Chen L, Rogan WJ, and Wolff MS (2005) DDT serum concentration and menstruation among young Chinese women. Environ Res 99:397-402.
5. Chen C-R, Chazenbalk GD, McLachlan SM, and Rapoport B (2003) Evidence that the C terminus of the A subunit suppresses thyrotropin receptor constitutive activity. Endocrinology 144:3821-3827.
6. Costa T and Cotecchia S (2005) Historical review: negative efficacy and the constitutive activity of G-protein coupled receptors. Trends Pharmacol Sci 26:618-624.
7. De Jager C, Farias P, Barraza-Villarreal A, Avila MH, Ayotte P, Dewailly E, Dombrowski C, Rousseau F, Sanchez VD, and Bailey JL (2006) Reduced seminal parameters associated with environmental DDT exposure and p,p′-DDE concentrations in men in Chiapas, Mexico: a cross-sectional study. J Androl 27:16-27.
8. 2+/calmodulin insensitive adenylyl cyclase from rat brain. Proc Natl Acad Sci USA 88:10173-10177.
9. Fisher DA, Smith JF, Pillar JS, St Denis SH, and Cheng JB (1998) Isolation and characterization of PDE8A, a novel human cAMP-specific phosphodiesterase. Biochem Biophys Res Commun 246:570-577.
10. Gao B and Gilman AG (1991) Cloning and expression of a widely distributed (type IV) adenylyl cyclase. Proc Natl Acad Sci USA 88:10178- 10182.
11. Gasparini F, Kuhn R, and Pin J-P (2002) Allosteric modulators of group I metabotropic glutamate receptors: novel subtype-selective ligands and therapeutic perspectives. Curr Opin Pharmacol 2:43-49.
12. Hanke S, Nurnberg B, Groll DH, and Liebmann C (2001) Cross talk between beta-adrenergic and bradykinin B(2) receptors results in cooperative regulation of cyclic AMP accumulation and mitogen-activated protein kinase activity. Mol Cell Biol 21:8452-8460.
13. Johnson RA and Salomon Y (1991) Assay of adenylyl cyclase catalytic activity. Methods Enzymol 195:3-27.
14. Karmaus W, Huang S, and Cameron L (2002) Parental concentration of dichlorodiphenyl dichloroethene and polychlorinated biphenyls in Michigan fish eaters and sex ratio in offsprings. J Occup Environ Med 44:8-13.
15. 2A-adenosine receptor blunts constitutive activity: differential effect on cAMP accumulation and MAP kinase stimulation. Naunyn-Schmiedeberg's Arch Pharmacol 366:287-298.
16. + channels as targets of insecticides. Trends Pharmacol Sci 13:236-241.
17. Parma J, Duprez L, Van Sande J, Cochaux P, Gervy C, Mockel J, Dumont J, and Vassart G (1993) Somatic mutations in the thyrotropin receptor gene cause hyperfunctioning thyroid adenomas. Nature (Lond) 365:649-651.
18. Parnot C, Miserey-Lenkei S, Bardin S, Corvol P, and Clauser E (2002) Lessons from constitutively active mutants of G protein-coupled receptors. Trends Endocrinol Metab 13:336-343.
19. Patton JS, Stone B, Papa C, Abramowitz R, and Yalkowsky SH (1984) Solubility of fatty acids and other hydrophobic molecules in liquid trioleoylglycerol. J Lipid Res 25:189-197.
20. Perret J, Ludgate M, Libert F, Gerard C, Dumont JE, Vassart G, and Parmentier M (1990) Stable expression of the human TSH receptor in CHO cells and characterization of differentially expressing clones. Biochem Biophys Res Commun 171:1044-1050.
21. Pin J-P, Pin JP, Kniazeff J, Goudet C, Bessis AS, Liu J, Galvez T, Acher F, Rondard P, and Prezeau L (2004) The activation mechanism of class-C G-protein coupled receptors. Biol Cell 96:335-342.
22. Queiroz EK and Waissmann W (2006) Occupational exposure and effects on the male reproductive system. Cad Saude Publica 22:485-493.
23. Rosenkilde MM, Waldhoer M, Luttichau HR, and Schwartz TW (2001) Virally encoded 7TM receptors. Oncogene 20:1582-1593.
24. Santini F, Vitti P, Ceccarini G, Mammoli C, Rosellini V, Pelosini C, Marsili A, Tonacchera M, Agretti P, Santoni T, et al. (2003) In vitro assay of thyroid disruptors affecting TSH-stimulated adenylate cyclase activity. J Endocrinol Investig 26:950-955.
25. Seetharamaiah GS, Kurosky A, Desai RK, Dallas JS, and Prabhakar BS (1994) A recombinant extracellular domain of the thyrotropin (TSH) receptor binds TSH in the absence of membranes. Endocrinology 134:549-554.
26. Smit MJ, Vink C, Verzijl D, Casarosa P, Bruggeman CA, and Leurs R (2003) Virally encoded G protein-coupled receptors: targets for potentially innovative anti-viral drug development. Curr Drug Targets 4:431-441.
27. Smits G, Campillo M, Govaerts C, Janssens V, Richter C, Vassrt G, Pardo L, and Costagliola S (2003) Glycoprotein hormone receptors: determinants in leucine-rich repeats responsible for ligand specificity. EMBO (Eur Mol Biol Organ) J 22:2692-2703.
28. Taussig R, Tang WJ, Hepler JR, and Gilman AG (1994) Distinct patterns of bidirectional regulation of mammalian adenylylcyclases. J Biol Chem 269:6093-6100.
29. Tonacchera M, Chiovato L, Pinchera A, Agretti P, Fiore E, Cetani F, Rocchi R, Viacava P, Miccoli P, and Vitti P (1998) Hyperfunctioning thyroid nodules in toxic multinodular goiter share activating thyrotropin receptor mutations with solitary toxic adenoma. J Clin Endocrinol Metab 83:492-498.
30. Van Sande J, Massart C, Costagliola S, Allgeier A, Cetani F, Vassart G, and Dumont J (1996) Specific activation of the thyrotropin receptor by trypsin. Mol Cell Endocrinol 119:161-168.
31. Vassart G, Pardo L, and Costagliola S. A molecular dissection of the glycoprotein hormone receptors. Trends Biochem Sci 29:119-126, 2004.
32. Vitti P, Elisei R, Tonacchera M, Chiovato L, Mancusi F, Rago T, Mammoli C, Ludgate M, Vassart G, and Pinchera A (1993) Detection of thyroid stimulating antibody using Chinese hamster ovary cells transfected with the cloned human thyrotropin receptor. J Clin Endocrinol Metab 76:499-503.
33. Vlaeminck V, Ho SC, Rodien P, Vassart G, and Costagliola S (2002) Activation of the cAMP pathway by the TSH receptor involves switching of the ectodomain from a tethered inverse agonist to an agonist. Mol Endocrinol 16:736-746.
34. Younis HM, Abo-El-Saad MM, Abdel-Razik RK, and Abo-Seda SA (2002) Resolving the DDT target protein in insects as a subunit of the ATP synthase. Biotechnol Appl Biochem 35:9-17.
35. Zhang M, Tong KPT, Fremont V, Chen J, Narayan P, Puett D, Weintraub BD, and Szkudlinski MW (2000) The extracellular domain suppresses constitutive activity of the transmembrane domain of the human TSH receptor: implication for hormone-receptor interaction and antagonist design. Endocrinology 141:3514-3517.