Identification of two serine residues essential for agonist-induced 5-HT2A receptor desensitization

Biochemistry

Volumn 42, Issue 36, 2003, Pages 10853-10862

  Gray, John A ^a   Compton Toth, Beth A ^a   Roth, Bryan L ^a  

^a CASE WESTERN RESERVE UNIVERSITY SCHOOL OF MEDICINE   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

CYTOLOGY; DISEASE CONTROL; DRUG PRODUCTS; MUTAGENESIS; PATHOLOGY;

PATHOGENESIS;

BIOCHEMISTRY;

G PROTEIN COUPLED RECEPTOR; GUANINE NUCLEOTIDE BINDING PROTEIN; SERINE; SEROTONIN 2A AGONIST; SEROTONIN 2A RECEPTOR;

ARTICLE; CARBOXY TERMINAL SEQUENCE; DESENSITIZATION; PRIORITY JOURNAL; PROTEIN ANALYSIS; PROTEIN DOMAIN; PROTEIN PHOSPHORYLATION; RECEPTOR AFFINITY; RECEPTOR DOWN REGULATION; RESIDUE ANALYSIS; SECOND MESSENGER; SINGLE NUCLEOTIDE POLYMORPHISM; SMOOTH MUSCLE CONTRACTION; THROMBOCYTE AGGREGATION;

AMINO ACID SEQUENCE; AMINO ACID SUBSTITUTION; ANIMALS; CELLS, CULTURED; ENZYME INHIBITORS; HUMANS; MOLECULAR SEQUENCE DATA; PHORBOL ESTERS; PHOSPHATIDYLINOSITOLS; PROTEIN KINASE C; QUIPAZINE; RATS; RECEPTOR, SEROTONIN, 5-HT2A; RECEPTORS, SEROTONIN; RECOMBINANT PROTEINS; SERINE; SEROTONIN; SEROTONIN AGONISTS; THREONINE; TRANSFECTION;

EID: 0042318792     PISSN: 00062960     EISSN: None     Source Type: Journal    
DOI: 10.1021/bi035061z     Document Type: Article

References (30)

1. Roth, B. L., Willins, D. L., Kristiansen, K., and Kroeze, W. K. (1998) 5-Hydroxytryptamine2-family receptors (5-hydroxytryptamine2A, 5-hydroxytryptamine2B, 5-hydroxytryptamine2C): where structure meets function, Pharmacol. Ther. 79, 231-257.
2. Roth, B. L., Baner, K., Westkaemper, R., Siebert, D., Rice, K. C., Steinberg, S., Ernsberger, P., and Rothman, R. B. (2002) Salvinorin A: a potent naturally occurring nonnitrogenous kappa opioid selective agonist, Proc. Natl. Acad. Sci. U.S.A. 99, 11934-11939.
3. Glennon, R. A., Titeler, M., and McKenney, J. D. (1984) Evidence for 5-HT2 involvement in the mechanism of action of hallucinogenic agents, Life Sci. 35, 2505-2511.
4. i values, J. Pharmacol. Exp. Ther. 251, 238-246.
5. Gray, J. A., and Roth, B. L. (2001) Paradoxical trafficking and regulation of 5-HT2A receptors by agonists and antagonists, Brain Res. Bull. 56, 441-451.
6. Roth, B. L., Hamblin, M., and Ciaranello, R. D. (1990) Regulation of 5-HT2 and 5-HT1C serotonin receptor levels. Methodology and mechanisms, Neuropsychopharmacology 3, 427-433.
7. Roth, B. L., Berry, S. A., Kroeze, W. K., Willins, D. L., and Kristiansen, K. (1998) Serotonin 5-HT2A receptors: molecular biology and mechanisms of regulation, Crit. Rev. Neurobiol. 12, 319-338.
8. Roth, B. L., Palvimaki, E. P., Berry, S., Khan, N., Sachs, N., Uluer, A., and Choudhary, M. S. (1995) 5-Hydroxytryptamine2A (5-HT2A) receptor desensitization can occur without down-regulation, J. Pharmacol. Exp. Ther. 275, 1638-1646.
9. Ivins, K. J., and Molinoff, P. B. (1991) Desensitization and down-regulation of 5-HT2 receptors in P11 cells, J. Pharmacol. Exp. Ther. 259, 423-429.
10. Gray, J. A., Sheffler, D. J., Bhatnagar, A., Woods, J. A., Hufeisen, S. J., Benovic, J. L., and Roth, B. L. (2001) Cell-type specific effects of endocytosis inhibitors on 5-hydroxytryptamine(2A) receptor desensitization and resensitization reveal an arrestin-, GRK2-, and GRK5-independent mode of regulation in human embryonic kidney 293 cells, Mol. Pharmacol. 60, 1020-1030.
11. Roth, B. L., Patel, S., Kroeze, W. K., and Lopez, E. (2000) The Multiplicity of Serotonin Receptors: Uselessly Diverse Molecules or an Embarrasment of Riches? Neuroscientist 6, 252-262.
12. Freedman, N. J., and Lefkowitz, R. J. (1996) Desensitization of G protein-coupled receptors, Recent Prog. Horm. Res. 51, 319-353.
13. Ferguson, S. S. (2001) Evolving concepts in G protein-coupled receptor endocytosis: the role in receptor desensitization and signaling, Pharmacol. Rev. 53, 1-24.
14. Bhatnagar, A., Willins, D. L., Gray, J. A., Woods, J., Benovic, J. L., and Roth, B. L. (2001) The dynamin-dependent, arrestin-independent internalization of 5-hydroxytryptamine 2A (5-HT2A) serotonin receptors reveals differential sorting of arrestins and 5-HT2A receptors during endocytosis, J. Biol. Chem. 276, 8269-8277.
15. Vouret-Craviari, V., Auberger, P., Pouyssegur, J., and Van Obberghen-Schilling, E. (1995) Distinct mechanisms regulate 5-HT2 and thrombin receptor desensitization, J. Biol. Chem. 270, 4813-4821.
16. Senanayake, S. D., and Brian, D. A. (1995) Precise large deletions by the PCR-based overlap extension method, Mol. Biotechnol. 4, 13-15.
17. Sanders-Bush, E., and Breeding, M. (1990) Serotonin 1c receptor reserve in choroid plexus masks receptor subsensitivity, J. Pharmacol. Exp. Ther. 252, 984-988.
18. Roth, B. L., Nakaki, T., Chuang, D. M., and Costa, E. (1986) 5-Hydroxytryptamine2 receptors coupled to phospholipase C in rat aorta: modulation of phosphoinositide turnover by phorbol ester, J. Pharmacol. Exp. Ther. 238, 480-485.
19. Rahimian, R., and Hrdina, P. D. (1995) Possible role of protein kinase C in regulation of 5-hydroxytryptamine 2A receptors in rat brain, Can. J. Physiol. Pharmacol. 73, 1686-1691.
20. Rahman, S., McLean, J. H., Darby-King, A., Paterno, G., Reynolds, J. N., and Neuman, R. S. (1995) Loss of cortical serotonin2A signal transduction in senescent rats: reversal following inhibition of protein kinase C, Neuroscience 66, 891-901.
21. Kagaya, A., Mikuni, M., Kusumi, I., Yamamoto, H., and Takahashi, K. (1990) Serotonin-induced acute desensitization of serotonin2 receptors in human platelets via a mechanism involving protein kinase C, J. Pharmacol. Exp. Ther. 255, 305-311.
22. Kagaya, A., Mikuni, M., Muraoka, S., Saitoh, K., Ogawa, T., Shinno, H., Yamawaki, S., and Takahashi, K. (1993) Homologous desensitization of serotonin 5-HT2 receptor-stimulated intracellular calcium mobilization in C6BU-1 glioma cells via a mechanism involving a calmodulin pathway, J. Neurochem. 61, 1050-1056.
23. Toullec, D., Pianetti, P., Coste, H., Bellevergue, P., Grand-Perret, T., Ajakane, M., Baudet, V., Boissin, P., Boursier, E., Loriolle, F., et al. (1991) The bisindolylmaleimide GF 109203X is a potent and selective inhibitor of protein kinase C, J. Biol. Chem. 266, 15771-15781.
24. Herbert, J. M., Augereau, J. M., Gleye, J., and Maffrand, J. P. (1990) Chelerythrine is a potent and specific inhibitor of protein kinase C, Biochem. Biophys. Res. Commun. 172, 993-999.
25. Hill-Eubanks, D., Burstein, E. S., Spalding, T. A., Brauner-Osborne, H., and Brann, M. R. (1996) Structure of a G-protein-coupling domain of a muscarinic receptor predicted by random saturation mutagenesis, J. Biol. Chem. 271, 3058-3065.
26. Oksenberg, D., Havlik, S., Peroutka, S. J., and Ashkenazi, A. (1995) The third intracellular loop of the 5-hydroxytryptamine2A receptor determines effector coupling specificity, J. Neurochem. 64, 1440-1447.
27. Gelber, E. I., Kroeze, W. K., Willins, D. L., Gray, J. A., Sinar, C. A., Hyde, E. G., Gurevich, V., Benovic, J., and Roth, B. L. (1999) Structure and function of the third intracellular loop of the 5-hydroxytryptamine2A receptor: the third intracellular loop is α-helical and binds purified arrestins, J. Neurochem. 72, 2206-2214.
28. Lembo, P. M., Ghahremani, M. H., Morris, S. J., and Albert, P. R. (1997) A conserved threonine residue in the second intracellular loop of the 5-hydroxytryptamine 1A receptor directs signaling specificity, Mol. Pharmacol. 52, 164-171.
29. Lowe, J. D., Celver, J. P., Gurevich, V. V., and Chavkin, C. (2002) μ-Opioid Receptors Desensitize Less Rapidly than δ-Opioid Receptors Due to Less Efficient Activation of Arrestin, J. Biol. Chem. 277, 15729-15735.
30. Celver, J. P., Lowe, J., Kovoor, A., Gurevich, V. V., and Chavkin, C. (2001) Threonine 180 is required for G-protein-coupled receptor kinase 3- and β-arrestin 2-mediated desensitization of the μ-opioid receptor in Xenopus oocytes, J. Biol. Chem. 276, 4894-4900.