Receptor antagonists targeting transmembrane domains

Expert Opinion on Emerging Drugs

Volumn 5, Issue 2, 2000, Pages 221-229

  Tarasova, Nadya I ^a  

^a NATIONAL CANCER INSTITUTE   (United States)

Author keywords

chemokine receptors; GPCR; membrane proteins; receptor antagonist; transmembrane domains

Indexed keywords

CHEMOKINE RECEPTOR CXCR4; G PROTEIN COUPLED RECEPTOR; MEMBRANE PROTEIN; RECEPTOR BLOCKING AGENT;

PROTEIN DOMAIN; RECEPTOR BLOCKING; REVIEW; STRUCTURE ACTIVITY RELATION;

EID: 0033948269     PISSN: 14728214     EISSN: None     Source Type: Journal    
DOI: 10.1517/14728214.5.2.221     Document Type: Review

References (39)

1. WATSON S, ARKINSTALL S: The G-Protein Linked Receptor-Facts Book. Academic Press, London, UK (1994).
2. PEBAY-PEYROULA E, RUMMEL G, ROSENBUSCH JP, LANDAU EM: X-ray structure of bacteriorhodopsin at 2.5 angstroms from microcrystals grown in lipidic cubic phases. Science (1997) 277:1676-1681. (Pubitemid 27446232)
3. LUECKE H, SCHOBERT B, RICHTER HT, CARTAILLER JP, LANYI JK: Structure of bacteriorhodopsin at 1.55 A resolution.J. Mol. Biol. (1999) 291(4):899-911.
4. ESSEN L, SIEGERT OR, LEHMANN WD, OESTERHELT D: Lipid patches in membrane protein oligomers: crystal structure of the bacteriorhodopsin-lipid complex. Proc. Natl. Acad. Sci. USA (1998) 95:11673-11678. (Pubitemid 28460473)
5. DEISENHOFERJ, EPP O, SINNIN G I, MICHEL H: Crystallo-graphic refinement at 2.3 A resolution and refined model of the photosynthetic reaction centre from Rhodopseudomonas viridis. J. Mol. Biol. (1995) 246:429-457.
6. YOSHIKAWA S, SHINZAWA-ITOH K, NAKASHIMA R et al.: Redox-coupled crystal structural changes in bovine heart cytochrome c oxidase. Science (1998) 280:1723-1729. (Pubitemid 28283490)
7. XIA D, YU CA, KIM H et al.: Crystal structure of the cytochrome bc1 complex from bovine heart mitochondria. Science (1997) 277:60-66 (Pubitemid 27450644)
8. DOYLE DA, MORAIS CABRAL J, PFUETZNER RA et al: The structure of the potassium channel: molecular basis of K+conduction and selectivity. Science(1998) 280:69-77 (Pubitemid 28169082)
9. LEMMON MA, FLANAGAN JM, TREUTLEIN HR, ZHANG J, ENGELMAN DM: Sequence specificity in the dimeriza-tion of transmembrane alpha-helices. Biochemistry (1992) 31:12719-12725. (Pubitemid 23027049)
10. MACKENZIE KR, PRESTEGARD JH, ENGELMAN DM: A transmembrane helix dimer: structure and implica tions. Science (1997) 276:131-133. (Pubitemid 27161261)
11. BALDWIN JM, SCHERTLER GF, UNGER VM: An alpha-carbon template for the transmembrane helices in the rhodopsin family of G-protein-coupled receptors. J. Mol. Biol. (1997) 272:144-164. (Pubitemid 27395544)
12. PEITSCH MC, HERZYK P, WELL TN, HUBBARD RE: Automated modelling of the transmembrane region of G-protein coupled receptor by Swiss-model. Rec. Channels (1996) 4:161-164. (Pubitemid 27032382)
13. KOBILKA BK, KOBILKA TS, DANIEL K et al: Chimeric alpha 2-, beta2-adrenergic receptors: delineation of domains involved in effector coupling and ligand binding specificity. Science (1988) 240:1310-1316.
14. SCHONENBERG T, LIU J, WESS J: Plasma membrane localization and functional rescue of truncated forms of a G protein-coupled receptor. J. Biol. Chem. (1995) 270:18000-18006.
15. JAKUBIK J, WESS J: Use of a sandwich enzyme-linked immunosorbent assay strategy to study mechanisms of G protein-coupled receptor assembly. J. Biol. Chem. (1999) 274:1349-1358.
16. RIDGE KD, LEE SS, YAO LL: In vivo assembly of rhodopsin from expressed polypeptide fragments. Proc. Natl. Acad. Sci. USA (1995) 91:3204-3208.
17. HUANG KS, BAYLEY H, LIAO MJ, LONDON E, KHORANA HG: Refolding of an integral membrane protein. Denaturation, renaturation and reconstitution of intact bacteriorhodopsin and two proteolytic fragments. J. Biol. Chem. (1981) 256:3802-3809.
18. KAHN TW, ENGELMAN DM: Bacteriorhodopsin can be refolded from two independently stable transmem-brane helices and the complementary five-helix fragment. Biochemistry (1992) 31:6144-6151.
19. SCHONENBERG T, YUN J, WENKERT D, WESS J: Functional rescue of mutant V2 vasopressin receptors causing nephrogenic diabetes insipidus by a co-expressed receptor polypeptide. EMBO J. (1996) 15:1283-1291. (Pubitemid 26093464)
20. OSUGA Y, HAYASHI M, KUDO M et al.: Co-expression of defective luteinizing hormone receptor fragments partially reconstitutes ligand-induced signal generation. J. Biol. Chem. (1997) 272:25006-25012. (Pubitemid 27415680)
21. HEBERT TE, MOFFETT S, MORELLO JP et al.: A peptide derived from a beta2-adrenergic receptor transmem-branedomain inhibits both receptor dimerization and activation. J. Biol. Chem. (1996) 271:16384-16392. (Pubitemid 26236264)
22. GEORGE SR, LEE SP, VARGHESE G et al.: A transmem-brane domain-derived peptide inhibits D1 dopamine receptor function without affecting receptor oligomerization. J. Biol. Chem. (1998) 273:30244-30248. (Pubitemid 28545490)
23. TARASOVA NI, RICE WG, MICHEJDA CJ: Inhibition of G-protein coupled receptor function by disruption of transmembrane domain interactions. J. Biol. Chem. (1999) 274:34911-34915. (Pubitemid 129509538)
24. HUNT JF, RATH P, ROTHSCHILD KJ, ENGELMAN DM: Spontaneous, pH-dependent membrane insertion of a transbilayer alpha-helix. Biochemistry (1997) 36(49):15177-15179.
25. BAYLE D, WEEKS D, SACHS G: Identification of membrane insertion sequences of the rabbit gastric cholecystokinin-A receptor by in vitro translation. J. Biol. Chem. (1997) 272:19697-19707. (Pubitemid 27340058)
26. VON HEIJNE G: Membrane protein structure predic tion. Hydrophobicity analysis and the positive-inside rule. J. Mol. Biol. (1992) 225(2):487-494.
27. HARTMANN E, RAPOPORT TA, LODISN HF: Predicting the orientation of eukaryotic membrane-spanning proteins. Proc. Natl. Acad. Sci. USA (1989) 86:5786-5790. (Pubitemid 19217538)
28. WALLIN E, VON HEIJNE G: Genome-wide analysis of integral membrane proteins from eubacterial, archaean and eukaryotic organisms. Protein. Sci. (1998) 7(4):1029-1038. (Pubitemid 28216544)
29. SATO M, HRESKO R, MUECKLER M: Testing the charge difference hypothesis for the assembly of a eucaryotic multispanning membrane protein. J. Biol. Chem. (1998) 273:25203-25208. (Pubitemid 28443282)
30. WU Y, HUANG HW, OLAH GA: Method of oriented circular dichroism Biophys. J. (1990) 57:797-806. (Pubitemid 20111238)
31. ROST B, CASADIO R, FARISELLI P et al.: Transmembrane helices predicted at 95% accuracy. Protein Sci. (1995) 4(3):521-533.
32. LE T, TSENG TT, SAIER MH, JR.: Flexible programs for the prediction of average amphipathicity of multiply aligned homologous proteins: application to integral membrane transport proteins. Mol. Membr. Biol. (1999) 16(2):173-179.
33. ROST B, FARISELLI P, CASADIO R: Topology prediction for helical transmembrane proteins at 86% accuracy. Protein Sci. (1996) 5(8):1704-1718. (Pubitemid 26257233)
34. GROMIHA MM: A simple method for predicting transmembrane alpha helices with better accuracy. Protein Eng. (1999) 12(7):557-561. (Pubitemid 29368962)
35. PILPEL Y, BEN-TAL N, LANCET D: kPROT: a knowledge-based scale for the propensityofresidue orientation in transmembrane segments. Application to membrane protein structure prediction. J. Mol. Biol. (1999) 294(4):921-935. (Pubitemid 30000385)
36. PASQUIER C, PROMPONAS VJ, PALAIOS GA, HAMODRAKAS JS, HAMODRAKAS SJ: Anovel method for predicting transmembrane segments in proteins based on a statistical analysis of the SwissProt database: the PRED-TMR algorithm. Protein Eng. (1999) 12(5):381-385. (Pubitemid 29265394)
37. MORGENSTERN B, WERNER T, DRESS AWM: Multiple DNA and protein sequence alignment based on segment-to-segment comparison. Proc. Natl. Acad. Sci. USA (1996) 93:12098-12103. (Pubitemid 26367101)
38. KIEBER-EMMONS T, MURALI R, GREENE MI: Therapeutic peptides and peptidomimetics. Curr. Opin. Biotechnol. (1997) 8:435-441. (Pubitemid 27351280)
39. HARIS PI: Synthetic peptide fragments as probes for structure determination of potassium ion-channel proteins. Biosci. Rep. (1998) 18:299-312. (Pubitemid 29248728)