Dopamine receptor microdomains involved in molecular recognition and the regulation of drug affinity and function

Journal of Receptors and Signal Transduction

Volumn 24, Issue 3, 2004, Pages 207-239

  Floresca, Christina Z ^a   Schetz, John A ^a  

^a UNIVERSITY OF NORTH TEXAS HEALTH SCIENCE CENTER   (United States)

Author keywords

Antipsychotics; G protein coupled receptors (GPCR); Molecular recognition; Neurological disorders; Psychiatric disorders; Structure activity relationships (SAR); Structure function; Subtype selective drugs

Indexed keywords

AMINE; AMINO ACID; AROMATIC AMINO ACID; ASPARTIC ACID; BENZAZEPINE DERIVATIVE; BUTYROPHENONE; CHLORPROMAZINE; CHLORPROTHIXENE; CLOZAPINE; DOMPERIDONE; DOPAMINE RECEPTOR; DOPAMINE RECEPTOR BLOCKING AGENT; DOPAMINE RECEPTOR STIMULATING AGENT; DROPERIDOL; FLUPENTIXOL; HALOPERIDOL; LIGAND; LOXAPINE; METOCLOPRAMIDE; MOLINDONE; PERPHENAZINE; PIMOZIDE; QUETIAPINE; REMOXIPRIDE; RISPERIDONE; SERTINDOLE; SULPIRIDE; THIORIDAZINE; UNINDEXED DRUG; ZIPRASIDONE;

BINDING AFFINITY; BINDING SITE; CHEMICAL BOND; CONFERENCE PAPER; DRUG BINDING; HUMAN; HYDROGEN BOND; LIPID MEMBRANE; MENTAL DISEASE; MOLECULAR RECOGNITION; NEUROLOGIC DISEASE; NONHUMAN; RECEPTOR SENSITIVITY; STRUCTURE ACTIVITY RELATION;

ANIMALS; ARGININE; ASPARTIC ACID; BINDING SITES; CLOZAPINE; DOPAMINE; DOPAMINE ANTAGONISTS; HALOPERIDOL; HUMANS; LIGANDS; PROTEIN STRUCTURE, TERTIARY; RECEPTORS, DOPAMINE; RISPERIDONE; SERINE;

EID: 4944266918     PISSN: 10799893     EISSN: 15324281     Source Type: Journal    
DOI: 10.1081/RRS-200032088     Document Type: Conference Paper

References (47)

1. Emilien G, Maloteaux JM, Geurts M, Hoogenberg K, Cragg S. Dopamine receptors-physiological understanding to therapeutic intervention potential. Pharmacol Ther 1999; 84(2):133-156.
2. McDougle CJ, Scahill L, McCracken JT, Aman MG, Tierney E, Arnold LE, Freeman BJ, Martin A, McGough JJ, Cronin P, Posey DJ, Riddle MA, Ritz L, Swiezy NB, Vitiello B, Volkmar FR, Votolato NA, Walson P. Research Units on Pediatric Psychopharmacology (RUPP) Autism Network. Background and rationale for an initial controlled study of risperidone. Child Adolesc Psychiatry Clin North Am 2000; 9(1):201-224.
3. Sultzer DL. Psychosis and antipsychotic medications in Alzheimer's disease: clinical management and research perspectives. Dement Geriatr Cogn Disord 2004; 17(1-2):78-90.
4. Schetz JA. Pharmacotherapeutic principles of neurological and psychiatric disorders. In: Tarazi F, Schetz JA, eds. Neurological and Psychiatric Disorders: From Bench to Bedside. Humana Press Inc.: Totowa, New Jersey, 2004. In press.
5. Schetz JA. Structure-activity relationships. In: Enna SJ, Bylund DB, eds. xPharm. Elsevier Inc.: New York, 2004. In press.
6. Palczewski K, Kumasaka T, Hori T, Behnke CA, Motoshima H, Fox BA, Le Trong I, Teller DC, Okada T, Stenkamp RE, Yamamoto M, Miyano M. Crystal structure of rhodopsin: A G protein-coupled receptor. Science 2000; 289:739-745.
7. Schetz JA. Allosteric modulation of dopamine receptors. Med Chem 2004. In press.
8. Boldry R, Chang Y, Miller DD, Uretsky NJ. Behavioral effects of a dimethylsulfonium analog of dopamine after injection into the nucleus accumbens and the striatum. Pharmacol Biochem and Behav 1986; 24:223-228.
9. Wallace RA, Farooqui T, Wallace L, Ares J, Chang YA, Miller D, Uretsky N. Interaction of permanently charged analogs of dopamine with the D-2 dopaminergic receptor. Biochem Pharm 1987; 36:3903-3910.
10. Sabol B, Boldry R, Farooqui T, Chang YA, Miller D, Uretsky N. Effect of permanently charged and uncharged dopaminergic agonists on the potassium induced release of [3H]acetylcholine from striatal slices. Gen Pharmacol 1987; 36(10):1679-1685.
11. Wallace RA, Farooqui T, Wallace L, Ares J, Chang YA, Miller D, Uretsky N. Interaction of permanently uncharged dopamine analogs with the D-2 dopaminergic receptor. Biochem Pharm 1988; 37:2077-2084.
12. Harrold MW, Chang Y-A., Wallace RA, Farooqui T, Wallace LJ, Uretsky N, Miller DD. Charged analogs of chlorpromazine as dopamine anatagonists. J Med Chem 1987; 30:1631-1635.
13. Harrold MW, Wallace RA, Farooqui T, Wallace LJ, Uretsky N, Miller DD. Synthesis and dopaminergic activity of pyrrolidinium, tetrahydrothiophenium and tetrahydrothiophene analogs of sulpiride. J Med Chem 1989; 32:874-880.
14. Harrold MW, Sriburi A, Matsumoto K, Miller DD, Farooqui T, Uretsky N. The interaction of ammonium, sulfonium and sulfide analogues of metoclopramide with the dopamine D-2 receptor. J Med Chem 1993; 36:3166-3170.
15. Farooqui T, Brooks K, Harrold MW, Miller DD, Wallace LJ, Uretsky NJ. Interaction of permanently charged metoclopramide analogs with D-2 dopamine receptors. Gen Pharmacol 1994; 25:1577-1584.
16. Mansour A, Meng F, Meador-Woodruff JH, Taylor LP, Civelli O, Akil H. Site-directed mutagenesis of the human dopamine D2 receptor. Eur J Pharm Mol Pharm 1992; 227:205-214.
17. Javitch JA, Fu D, Chen J, Karlin A. Mapping the binding site crevice of the dopamine D2 receptor by the substituted-cysteine accessibility method. Neuron 1995; 14:825-831.
18. Stradet CD, Condelore MR, Hills WS, Sigel IS, Dixon RAF. Identification of two serine residents involved in agonist activation of the β-adrenergic receptor. J Biol Chem 1989; 264:13572-13578.
19. Liapakis G, Bollesteros JA, Papachristou S, Chou WC, Chen X, Javitch JA. The forgotten serine: a critical role for ser-203 5.42 in ligand binding to and activation of the β2-adrenergic receptor. J Biol Chem 2000; 275:37779-37788.
20. Woodward R, Coley C, Daniell S, Naylor LH, Strange PG. Investigation of the role of conserved serine residues in the long form of the rat D2 dopamine receptor using site directed mutagenesis. J Neurochem 1996; 66:394-402.
21. Wilcox RE, Huang W.-H., Brusniak M.-Y.K., Wilcox DM, Pearlman RS, Teeter MM, DuRand CJ, Wiens BL, Neve KA. CoMFA-based prediction of agonist affinities at recombinant wild type versus serine to alanine point mutated D2 dopamine receptors. J Med Chem 2000; 43:3005-3019.
22. Cox BA, Henningsen RA, Spanoyannis A, Neve RL, Neve KA. Contributions of conserved serine residues to the interactions of ligands with dopamine D2 receptors. J Neurochem 1992; 59:627-635.
23. Wiens BL, Nelson CS, Neve KA. Contribution of serine residues to constitutive and agonist-induced signaling via the D2S dopamine receptor: evidence for multiple, agonist-specific active conformations. Mol Pharm 1998; 54:435-444.
24. Pollock NJ, Manelli AM, Hutchins CW, Steffey ME, Mackenzie RG, Frail DE. Serine mutations in transmembrane V of the dopamine D1 receptor affect ligand interactions and receptor activation. J Biol Chem 1992; 267:17780-17786.
25. Sartania N, Strange PG. Role of conserved serine residues in the interaction of agonists with D3 dopamine receptors. J Neurochem 1999; 72:2621-2624.
26. Coley C, Woodward R, Johansson AM, Strange PG, Naylor LH. Effect of multiple serine/alanine mutations in the transmembrane spanning region V of the D2 dopamine receptor on ligand binding. J Neurochem 2000; 74:358-366.
27. Payne SL, Johansson AM, Strange PG. Mechanisms of ligand binding and efficacy at the human D2(short) dopamine receptor. J Neurochem 2002; 82:1106-1117.
28. Javitch JA, Fu D, Chen J. Residues in the fifth membrane-spanning segment of the dopamine D2 receptor exposed in the binding site crevice. Biochemistry 1995; 34:16433-16439.
29. Javitch JA, Shi L, Liapakis G. Use of the substituted cysteine accessibility method to study the structure and function of G protein-coupled receptors. Methods Enzymol 2002; 343:137-156.
30. Javitch JA, Ballesteros JA, Weinstein H, Chen J. A cluster of aromatic residues in the sixth membrane-spanning segment of the dopamine D2 receptor is accessible in the binding-site crevice. Biochemistry 1998; 37:998-1006.
31. Zhang D, Weinstein H. Polarity conserved positions in transmembrane domains of G-protein coupled receptors and bacteriorhodopsin. FEBS Lett 1994; 337:207-212.
32. Farrens DL, Altenbach C, Yang K, Hubbell WL, Khorana HG. Requirement of rigid-body motion of transmembrane helices for light activation of rhodopsin. Science 1996; 274:768-770.
33. Sheikh SP, Viladarga JP, Baranski TJ, Lichtarge O, Iiri T, Meng EC, Nissenson RA, Bourne HR. Similar structures and shared switch mechanisms of the beta2-adrenoreceptor and the parathyroid hormone receptor. Zn(II) bridges between helices III and IV block activation. J Biol Chem 1999; 274: 17033-17041.
34. Gether U, Ballesteros JA, Seifert R, Sanders-Bush E, Weinstein H, Kobilka BK. Structural instability of a constitutively active G protein-coupled receptor. Agonist-independent activation due to conformational flexibility. J Biol Chem 1997; 272:2587-2590.
35. Visiers I, Ballesteros JA, Weinstein H. Three-dimensional representations of G protein-coupled receptor structures and mechanisms. Meth Enzymol 2002; 343:329-371.
36. Cho W, Taylor LP, Mansour A, Akil H. Hydrophobie residues of the D2 dopamine receptor are important for binding and signal transduction. J Neurochem 1995; 65(5):2105-2115.
37. Woodward R, Daniell SJ, Strange PG, Naylor LH. Structural studies on D2 dopamine receptors: mutation of a histidine residue specifically affects the binding of a subgroup of substituted benzamide drugs. J Neurochem 1994; 62:1664-1669.
38. Ballesteros J, Jensen AD, Liapakis G, Rasmussen S.G.F., Shi L, Gether U, Javitch JA. Activation of the β2-adrenergic receptor involves disruption of an ionic lock between the cytoplasmic ends of transmembrane segments e and 6. J Biol Chem 2001; 276:29171-29177.
39. Ballesteros J, Kitanovic S, Guarnieri F, Davies P, Fromme BJ, Konvicka K, Chi L, Millar RP, Davidson JS, Weinstein H, Sealfon SC. Functional microdomains in G-protein-coupled receptors. The conserved arginine-cage motif in the gonadotropin-releasing hormone receptor. J Biol Chem 1998; 273:10445-10453.
40. Schetz JA, Benjamin PS, Sibley DR. Nonconserved residues in the second transmembrane-spanning domain of the D(4) dopamine receptor are molecular determinants of D(4)-selective pharmacology. Mol Pharm 2000; 57:144-152.
41. Simpson MM, Ballesteros JA, Chiappa V, Chen J, Suehiro M, Hartman DS, Godel T, Snyder LA, Sakmar TP, Javitch JA. Dopamine D4/D2 receptor selectivity is determined by a divergent aromatic microdomain contained within the second, third, and seventh membrane-spanning segments. Mol Pharmacol 1999; 56:1116-1126.
42. Schetz JA. unpublished results, 2004.
43. Van Tol HH, Bunzow JR, Guan HC, Sunahara RK, Seeman P, Niznik HB, Civelli O. Cloning of the gene for a human dopamine D4 receptor with high affinity for the antipsychotic clozapine. Nature 1991; 350:610-614.
44. Psychoactive Drug Screening Program (PDSP) certified data, 2004. http://pdsp.cwru.edu/pdsp.asp.
45. Liu IS, Seeman P, Sanyal S, Ulpian C, Rodgers-Johnson PE, Serjeant GR, Van ToI HH. Dopamine D4 receptor variant in Africans, D4valine194glycine, is insensitive to dopamine and clozapine: report of a homozygous individual. Am J Med Genet 1996; 61:277-282.
46. Cravchik A, Gejman PV. Functional analysis of the human D5 dopamine receptor missense and nonsense variants: differences in dopamine binding affinities. Pharmacogenetics 1999; 9:199-206.
47. Schetz JA, Sibley DR. The binding-site crevice of the D4 dopamine receptor is coupled to three distinct sites of allosteric modulation. J Pharmacol Exp Ther 2001; 296:359-363.