1932

Abstract

This article considers early work from the author’s laboratory on muscarinic receptor specificity, subtypes, and conformational variability, with the use of nuclear magnetic resonance in pharmacology and the conformational variants of dihydrofolate reductase and general questions of receptors. It also considers some current approaches to drug development and receptor function, particularly as influenced by increasing knowledge of three-dimensional structure of receptors.

Loading

Article metrics loading...

/content/journals/10.1146/annurev.pharmtox.40.1.1
2000-04-01
2024-10-09
Loading full text...

Full text loading...

/deliver/fulltext/pharmtox/40/1/annurev.pharmtox.40.1.1.html?itemId=/content/journals/10.1146/annurev.pharmtox.40.1.1&mimeType=html&fmt=ahah

Literature Cited

  1. Goldstein A. 1997. A rewarding research pathway. Annu. Rev. Pharmacol. Toxicol. 37:1–28
  2. Burgen ASV, Dickens F, Zatman LJ. 1949. The action of botulinum toxin on the neuromuscular junction. J. Physiol. 109:10–24
  3. Burgen ASV, Terroux KG. 1953. On the negative inotropic effect in the cat’s auricle. J. Physiol. 120:449–64
  4. Burgen ASV. 1956. The secretion of non-electrolytes in the parotid saliva. J. Cell Comp. Physiol. 48:113–38
  5. Martin K, Burgen ASV. 1962. Changes in the permeability of the salivary gland caused by sympathetic stimulation and by catecholamines. J. Gen. Physiol. 46:225–43
  6. Burgen ASV, Kuffler SW. 1957. Two inhibitory fibres forming synapses with a single nerve cell in the lobster. Nature 180:1490–91
  7. Enger PES, Burgen ASV. 1957. The effects of some anino acids on the perfused lobster heart. Biol. Bull. 113:345– 46
  8. Burgen ASV. 1966. The drug-receptor complex. J. Pharm. Pharmacol. 18:137– 49
  9. Taylor PW, King RW, Burgen ASV. 1970. Kinetics of complex formation between human carbonic anhydrase and aromatic sulphonamides. Biochemistry 9:2638–45
  10. King RW, Burgen ASV. 1976. Kinetic aspects of structure-activity relations; the binding of sulphonamides by carbonic anhydrase. Proc. R. Soc. London Ser. B 193:107–25
  11. Taylor PW, King RW, Burgen ASV. 1970. Inflence of pH on the kinetics of complex formation between sulphonamides and human carbonic anhydrase. Biochemistry 9:3894–903
  12. Burgen ASV, Spero L. 1968. The action of acetylcholine and other drugs on the efflux of potassium and rubidium from smooth muscle of guinea-pig ileum. Br. J. Pharmacol. 34:99–115
  13. Burgen ASV, Spero L. 1970. The effects of calcium and magnesium on the response of intestinal smooth muscle to drugs. Br. J. Pharmacol. 40:492–500
  14. Hulme EC, Birdsall NJM, Burgen ASV, Mehta P. 1978. The binding of antagonists to brain muscarinic receptors. Mol. Pharmacol. 14:737–50
  15. Birdsall NJM, Burgen ASV, Hulme EC. 1978. The binding of agonists to brain muscarinic receptors. Mol. Pharmacol. 14:723–36
  16. Birdsall NJM, Hulme EC, Burgen ASV. 1980. The character of muscarinic receptors in different areas of the brain. Proc. R. Soc. London Ser. B 207:1–12
  17. Burgen ASV. 1986. The effects of ionic strength on cardiac muscarinic receptors. Br. J. Pharmacol. 88:451–55
  18. Birdsall NJM, Berrie CP, Burgen ASV, Hulme EC. 1980. Modulation of the binding properties of muscarinic receptors: evidence for receptor-effector coupling. In Receptors for Neurotransmitters and Peptide Hormones, ed. G Pepeu, MJ Kuhar, SJ Enna, pp. 107–16. New York: Raven
  19. Hammer R, Berrie R, Birdsall NJM, Burgen ASV, Hulme EC. 1980. Pirenzipine distinguishes between different subclasses of muscarinic receptors. Nature 283:90–92
  20. Stockton JM, Birdsall NJM, Burgen ASV, Hulme EC. 1983. Modification of the binding properties of muscarinic receptors by gallamine. Mol. Pharmacol. 23:551–57
  21. Burgen ASV, Jardetzky O, Metcalfe JC, Wade-Jardetzky N. 1967. Investigation of a hapten-antibody complex by nuclear magnetic resonance. Proc. Natl. Acad. Sci. USA 58:447–53
  22. Feeney J, Roberts GCR, Brown JP, Burgen ASV, Gregory H. 1972. Conformational studies of some component peptides of pentagastrin. J. Chem. Soc. PII:601–4
  23. Feeney J, Roberts GCR, Rockey JH, Burgen ASV. 1971. Conformational studies of oxytocin and lysine vasopressin in aqueous solution using high resolution NMR spectroscopy. Nat. New Biol. 232:108–10
  24. Burgen ASV, Roberts GCR, Feeney J. 1975. Binding of flexible ligands to macromolecules. Nature 253:753–55
  25. Metcalfe JC, Seeman P, Burgen ASV. 1968. The proton relaxation of benzyl alcohol in erythrocyte membranes. Mol. Pharmacol. 4:87–95
  26. Birdsall B, Burgen ASV, Roberts GCR. 1980. Binding of coenzyme analogues to Lactobacillus casei dihydrofolate reductase: binary and ternary complexes. Biochemistry 19:3723–31
  27. Birdsall B, Burgen ASV, Hyde EI, Roberts GCR, Feeney J. 1981. Negative cooperativity between folinic acid and coenzyme in their binding to Lactobacillus casei dihydrofolate reductase. Biochemistry 20:2186–95
  28. Birdsall B, Burgen ASV, Rodrigues de Miranda J, Roberts GCR. 1978. Cooperativity in ligand binding to dihydofolate reductase. Biochemistry 17:2102–10
  29. Gronenborn A, Birdsall B, Hyde E, Roberts G, Feeney J, Burgen A. 1981. 1H and 31P NMR characterization of two conformations of the trimethoprim-NADP+-dihydrofolate reductase complex. Mol. Pharmacol. 20:145–53
  30. Birdsall B, Gronenborn A, Clore GM, Roberts GCR, Feeney J, Burgen ASV. 1981. 13C NMR evidence for three slowly interconverting conformations of the dihydrofolate reductase-NADP+-folate complex. Biochem. Biophys. Res. Commun. 101:1139–44
  31. Gomeza J, Shannon H, Kostenis E, Felder C, Zhang L, et al. 1999. Pronounced pharmacologic deficits in M2 muscarinic receptor knockout mice. Proc. Natl. Acad. Sci. USA 96:1692–97
  32. Rosoff ML, Wei J, Nathanson NM. 1996. Isolation and characterisation of the chicken m2 acetylcholine promoter region. Induction of gene transcription by leukaemia inhibitory factor and ciliary neurotrophic factor. Proc. Natl. Acad. Sci. USA 93:14889–94
  33. Haddad E-B, Russell J. 1998. Regulation of the expression and function of the M2 muscarinic receptor. Trends Pharmacol. Sci. 19:322–27
  34. Weng G, Bhalla US, Iyengar R. 1999. Complexity in biological signalling systems. Science 284:92–96
  35. Büscher R, Herrmann V, Insel PA. 1999. Human adrenoreceptor polymorphisms: evolving recognition of clinical importance. Trends Pharmacol. Sci. 20:94–99
  36. Mahsood E. 1999. A consortium plans free SNP map of human genome. Nature 398:545–46
  37. Luttrell LM, Ferguson SSG, Daaka Y, Miller WE, Maudsley S, et al. 1999. β-Arrestin-dependent formation of β2 adrenergic receptor-Src protein kinase complexes. Science 283:655–61
  38. Ge M, Chen Z, Onishi HR, Kohler J, Silver LL, et al. 1999. Vancomycin derivatives that inhibit peptidoglycan biosynthesis without binding d-Ala-d-Ala. Science 284:507–11
  39. Dooley CT, Chung NN, Wilkes BC, Schiller PW, Bidlack JM, et al. 1994. An all d-amino acid opioid peptide with central analgesic activity from a combinatorial library. Science 266:2019–22
  40. Hünenberger PH, Helms V, Narayama N, Taylor SS, McCammon JA. 1999. Determinants of ligand binding to cAMP-dependent protein kinase. Biochemistry 38:2358–66
  41. Koehler KF, Rao SN, Snyder JP. 1996. Modelling drug-receptor interactions. See Ref. 45, pp. 235–36
  42. Itai A, Mizutani MY, Nishibata Y, Tomioka N. 1996. Computer-assisted new lead design. See Ref. 45, pp. 107–9
  43. Birdsall B, Feeney J, Pascual C, Roberts GCK, Kompis I, et al. 1984. A 1H nmr study of the interactions and conformations of rationally designed brodimoprim analogues in complexes with Lactobacillus casei dihydrofolate reductase. J. Med. Chem. 23:1672–76
  44. Giannis A, Rübsam. 1997. Peptidomimetics in drug design. Adv. Drug Res. 29:1–78
  45. Cohen NC, ed. 1996. Guidebook on Moleculer Modelling in Drug Design. San Diego, CA: Academic
/content/journals/10.1146/annurev.pharmtox.40.1.1
Loading
  • Article Type: Review Article
This is a required field
Please enter a valid email address
Approval was a Success
Invalid data
An Error Occurred
Approval was partially successful, following selected items could not be processed due to error