G Milligan

Summary

Affiliation: University of Glasgow
Country: UK

Publications

  1. pmc A single amino acid determines preference between phospholipids and reveals length restriction for activation of the S1P4 receptor
    Gill Holdsworth
    Department of NCE Biology, Celltech R and D Ltd, 216 Bath Road, Slough, Berks, SL1 4EN, U K
    BMC Biochem 5:12. 2004
  2. ncbi request reprint Protein-protein interactions at G-protein-coupled receptors
    G Milligan
    Molecular Pharmacology Group, Division of Biochemistry and Molecular Biology, Institute of Biomedical and Life Sciences, University of Glasgow, G12 8QQ, Glasgow, UK
    Trends Pharmacol Sci 22:513-8. 2001
  3. ncbi request reprint G protein-coupled receptors for free fatty acids
    Graeme Milligan
    Molecular Pharmacology Group, Division of Biochemistry and Molecular Biology, Institute of Biomedical and Life Sciences, University of Glasgow, Glasgow G12 8QQ, Scotland, UK
    Cell Signal 18:1360-5. 2006
  4. ncbi request reprint G-protein-coupled receptor heterodimers: pharmacology, function and relevance to drug discovery
    Graeme Milligan
    Molecular Pharmacology Group, Division of Biochemistry and Molecular Biology, Institute of Biomedical and Life Sciences, University of Glasgow, Glasgow, G12 8QQ, Scotland, UK
    Drug Discov Today 11:541-9. 2006
  5. pmc Heterotrimeric G-proteins: a short history
    Graeme Milligan
    Molecular Pharmacology Group, Division of Biochemistry and Molecular Biology, Institute of Biomedical and Life Sciences, University of Glasgow, Glasgow G12 8QQ
    Br J Pharmacol 147:S46-55. 2006
  6. ncbi request reprint Opioid receptors and their interacting proteins
    Graeme Milligan
    Molecular Pharmacology Group, Division of Biochemistry and Molecular Biology, Institute of Biomedical and Life Sciences, University of Glasgow, Glasgow G12 8QQ, Scotland, UK
    Neuromolecular Med 7:51-9. 2005
  7. ncbi request reprint Interactions between G-protein-coupled receptors and periplakin: a selective means to regulate G-protein activation
    G Milligan
    Molecular Pharmacology Group, Division of Biochemistry and Molecular Biology, Institute of Biomedical and Life Sciences, University of Glasgow, Davidson Building, Glasgow G12 8QQ, Scotland, UK
    Biochem Soc Trans 32:878-80. 2004
  8. ncbi request reprint Strategies to identify ligands for orphan G-protein-coupled receptors
    G Milligan
    Molecular Pharmacology Group, Division of Biochemistry and Molecular Biology, Institute of Biomedical and Life Sciences, Davidson Building, University of Glasgow, Glasgow G12 8QQ, Scotland, UK
    Biochem Soc Trans 30:789-93. 2002
  9. ncbi request reprint Constitutive activity and inverse agonists of G protein-coupled receptors: a current perspective
    Graeme Milligan
    Davidson Building, University of Glasgow, Glasgow G12 8QQ, Scotland, UK
    Mol Pharmacol 64:1271-6. 2003
  10. ncbi request reprint Principles: extending the utility of [35S]GTP gamma S binding assays
    Graeme Milligan
    Molecular Pharmacology Group, Division of Biochemistry and Molecular Biology, Institute of Biomedical and Life Sciences, University of Glasgow, Scotland, UK
    Trends Pharmacol Sci 24:87-90. 2003

Detail Information

Publications111 found, 100 shown here

  1. pmc A single amino acid determines preference between phospholipids and reveals length restriction for activation of the S1P4 receptor
    Gill Holdsworth
    Department of NCE Biology, Celltech R and D Ltd, 216 Bath Road, Slough, Berks, SL1 4EN, U K
    BMC Biochem 5:12. 2004
    ....
  2. ncbi request reprint Protein-protein interactions at G-protein-coupled receptors
    G Milligan
    Molecular Pharmacology Group, Division of Biochemistry and Molecular Biology, Institute of Biomedical and Life Sciences, University of Glasgow, G12 8QQ, Glasgow, UK
    Trends Pharmacol Sci 22:513-8. 2001
    ....
  3. ncbi request reprint G protein-coupled receptors for free fatty acids
    Graeme Milligan
    Molecular Pharmacology Group, Division of Biochemistry and Molecular Biology, Institute of Biomedical and Life Sciences, University of Glasgow, Glasgow G12 8QQ, Scotland, UK
    Cell Signal 18:1360-5. 2006
    ....
  4. ncbi request reprint G-protein-coupled receptor heterodimers: pharmacology, function and relevance to drug discovery
    Graeme Milligan
    Molecular Pharmacology Group, Division of Biochemistry and Molecular Biology, Institute of Biomedical and Life Sciences, University of Glasgow, Glasgow, G12 8QQ, Scotland, UK
    Drug Discov Today 11:541-9. 2006
    ....
  5. pmc Heterotrimeric G-proteins: a short history
    Graeme Milligan
    Molecular Pharmacology Group, Division of Biochemistry and Molecular Biology, Institute of Biomedical and Life Sciences, University of Glasgow, Glasgow G12 8QQ
    Br J Pharmacol 147:S46-55. 2006
    ..Finally, further modifications of such chimeras have generated a range of G-protein alpha-subunits with greater promiscuity to interact across GPCR classes and initiated the use of such modified G-proteins in drug discovery programmes...
  6. ncbi request reprint Opioid receptors and their interacting proteins
    Graeme Milligan
    Molecular Pharmacology Group, Division of Biochemistry and Molecular Biology, Institute of Biomedical and Life Sciences, University of Glasgow, Glasgow G12 8QQ, Scotland, UK
    Neuromolecular Med 7:51-9. 2005
    ....
  7. ncbi request reprint Interactions between G-protein-coupled receptors and periplakin: a selective means to regulate G-protein activation
    G Milligan
    Molecular Pharmacology Group, Division of Biochemistry and Molecular Biology, Institute of Biomedical and Life Sciences, University of Glasgow, Davidson Building, Glasgow G12 8QQ, Scotland, UK
    Biochem Soc Trans 32:878-80. 2004
    ..In each case, the site of interaction is within helix VIII of the receptor and periplakin limits agonist-mediated G-protein activation potentially by competing with G-protein for this region of the receptor...
  8. ncbi request reprint Strategies to identify ligands for orphan G-protein-coupled receptors
    G Milligan
    Molecular Pharmacology Group, Division of Biochemistry and Molecular Biology, Institute of Biomedical and Life Sciences, Davidson Building, University of Glasgow, Glasgow G12 8QQ, Scotland, UK
    Biochem Soc Trans 30:789-93. 2002
    ..A range of currently employed and developing strategies to identify ligands that interact with these orphan receptors and to validate them as drug targets are described and discussed...
  9. ncbi request reprint Constitutive activity and inverse agonists of G protein-coupled receptors: a current perspective
    Graeme Milligan
    Davidson Building, University of Glasgow, Glasgow G12 8QQ, Scotland, UK
    Mol Pharmacol 64:1271-6. 2003
    ..Considerable attention has recently been devoted to the presence and roles of endogenous antagonist/inverse agonists and the concept that inverse agonists may have specific therapeutic benefits compared with neutral antagonists...
  10. ncbi request reprint Principles: extending the utility of [35S]GTP gamma S binding assays
    Graeme Milligan
    Molecular Pharmacology Group, Division of Biochemistry and Molecular Biology, Institute of Biomedical and Life Sciences, University of Glasgow, Scotland, UK
    Trends Pharmacol Sci 24:87-90. 2003
    ..Here, the reasons for this restriction are discussed and recent approaches that have extended the utility of this method such that it is now suitable for analysis of the activation of any heterotrimeric G protein are reviewed...
  11. ncbi request reprint G protein-coupled receptor fusion proteins in drug discovery
    G Milligan
    Division of Biochemistry and Molecular Biology, Institute of Biomedical and Life Sciences, University of Glasgow, Glasgow G12 8QQ, Scotland UK
    Curr Pharm Des 10:1989-2001. 2004
    ..Introduction of N-terminal tags to receptors has also allowed the introduction of novel assay techniques based on a pH-sensitive cyanine dye. These have the capacity to overcome certain limitations of GPCR-fluorescent protein fusions...
  12. ncbi request reprint G protein-coupled receptor dimerization: function and ligand pharmacology
    Graeme Milligan
    Molecular Pharmacology Group, Davidson Building, University of Glasgow, Glasgow G12 8QQ Scotland, UK
    Mol Pharmacol 66:1-7. 2004
    ..Key questions that remain to be addressed effectively include the prevalence and relevance of these in native tissues and the implications of heterodimerization for pharmacology and, potentially, for drug design...
  13. ncbi request reprint The use of receptor G-protein fusion proteins for the study of ligand activity
    Graeme Milligan
    Molecular Pharmacology Group, Division of Biochemistry and Molecular Biology, Institute of Biomedical and Life Sciences, University of Glasgow, Scotland, UK
    Receptors Channels 8:309-17. 2002
    ....
  14. ncbi request reprint Selectivity in the oligomerisation of G protein-coupled receptors
    Graeme Milligan
    Molecular Pharmacology Group, Division of Biochemistry and Molecular Biology, Institute of Biomedical and Life Sciences, University of Glasgow, Glasgow G12 8QQ, Scotland, UK
    Semin Cell Dev Biol 15:263-8. 2004
    ..Knowledge of the basis and selectivity of GPCR hetero-dimerisation is thus vital. Current understanding of these areas is reviewed...
  15. ncbi request reprint High-content assays for ligand regulation of G-protein-coupled receptors
    Graeme Milligan
    Molecular Pharmacology Group, Division of Biochemistry and Molecular Biology, Institute of Biomedical and Life Sciences, University of Glasgow, Glasgow, UK G12 8QQ
    Drug Discov Today 8:579-85. 2003
    ..Recent improvements in throughput using high-content screening platforms means that such assays are now an integral element of functional analysis in the drug discovery process...
  16. ncbi request reprint Applications of bioluminescence- and fluorescence resonance energy transfer to drug discovery at G protein-coupled receptors
    Graeme Milligan
    Molecular Pharmacology Group, Division of Biochemistry and Molecular Biology, University of Glasgow, Glasgow G12 8QQ, Scotland, UK
    Eur J Pharm Sci 21:397-405. 2004
    ..Specific applications of resonance energy transfer techniques to the identification of ligands for this class of protein are highlighted to illustrate general principles...
  17. ncbi request reprint GPCR dimerisation
    Graeme Milligan
    Molecular Pharmacology Group, Division of Biochemistry and Molecular Biology, Institute of Biomedical and Life Sciences, University of Glasgow, Davidson Building, G12 8QQ, Scotland, Glasgow, UK
    Life Sci 74:181-8. 2003
    ..Much remains to be examined, however, on the specificity and mechanisms of these interactions and to develop techniques to monitor the function only of hetero-dimers when the corresponding homo-dimers must also be present...
  18. ncbi request reprint Oligomeric structure of the alpha1b-adrenoceptor: comparisons with rhodopsin
    Graeme Milligan
    Molecular Pharmacology Group, Division of Biochemistry and Molecular Biology, Institute of Biomedical and Life Sciences, University of Glasgow, Glasgow G12 8QQ, Scotland, UK
    Vision Res 46:4434-41. 2006
    ..The mutated alpha(1b)-adrenoceptor was unable to reach the cell surface, did not become terminally N-glycosylated and was unable to signal...
  19. ncbi request reprint Ligand rescue of constitutively active mutant receptors
    Graeme Milligan
    Molecular Pharmacology Group, Division of Biochemistry and Molecular Biology, Institute of Biomedical and Life Sciences, University of Glasgow, Scotland, UK
    Neurosignals 11:29-33. 2002
    ..The application of these observations to the development of a high-throughput reporter assay suitable for ligand identification is also discussed...
  20. ncbi request reprint The role of GPCR dimerisation/oligomerisation in receptor signalling
    G Milligan
    Molecular Pharmacology Group, Division of Biochemistry and Molecular Biology, Institute of Biomedical and Life Sciences, University of Glasgow, G12 8QQ Glasgow, Scotland, UK
    Ernst Schering Found Symp Proc . 2006
    ....
  21. ncbi request reprint Novel pharmacological applications of G-protein-coupled receptor-G protein fusions
    Graeme Milligan
    Molecular Pharmacology Group, Division of Biochemistry and Molecular Biology, Institute of Biomedical and Life Sciences, University of Glasgow, Glasgow G12 8QQ, Scotland, UK
    Curr Opin Pharmacol 7:521-6. 2007
    ....
  22. ncbi request reprint Uncovering the pharmacology of the G protein-coupled receptor GPR40: high apparent constitutive activity in guanosine 5'-O-(3-[35S]thio)triphosphate binding studies reflects binding of an endogenous agonist
    Leigh A Stoddart
    Davidson Building University of Glasgow, Glasgow G12 8QQ, Scotland, UK
    Mol Pharmacol 71:994-1005. 2007
    ....
  23. ncbi request reprint Allosteric modulation of heterodimeric G-protein-coupled receptors
    Graeme Milligan
    Molecular Pharmacology Group, Division of Biochemistry and Molecular Biology, Institute of Biomedical and Life Sciences, University of Glasgow, Glasgow, Scotland, UK
    Trends Pharmacol Sci 28:615-20. 2007
    ..In our opinion, this will require the development of new approaches for screening and a return to the use of physiologically relevant cell systems at an early stage in compound identification...
  24. ncbi request reprint Insights into ligand pharmacology using receptor-G-protein fusion proteins
    G Milligan
    Molecular Pharmacology Group, Division of Biochemistry and Molecular Biology, Institute of Biomedical and Life Sciences, University of Glasgow, Glasgow, UK G12 8QQ
    Trends Pharmacol Sci 21:24-8. 2000
    ..In addition, the effects of point mutations, in both receptors and G proteins, on ligand function are particularly amenable to the types of robust quantitative analyses that can be produced using such fusion proteins...
  25. ncbi request reprint G protein-coupled receptor dimerisation: molecular basis and relevance to function
    Graeme Milligan
    Molecular Pharmacology Group, Division of Biochemistry and Molecular Biology, Institute of Biomedical and Life Sciences, University of Glasgow, Glasgow, Scotland, UK
    Biochim Biophys Acta 1768:825-35. 2007
    ..The relevance of this to physiology and function is only beginning to be unravelled but may offer great potential for more selective therapeutic intervention...
  26. doi request reprint G protein coupling and ligand selectivity of the D2L and D3 dopamine receptors
    J Robert Lane
    Davidson Building, University of Glasgow, Glasgow G12 8QQ, Scotland, UK
    J Pharmacol Exp Ther 325:319-30. 2008
    ..This chimera displayed D(3)-like affinity for [(3)H]spiperone and potency for agonists but gained D(2)-like ability to couple to each of Galpha(i1-3) as well as Galpha(o1)...
  27. pmc G protein-coupled receptor hetero-dimerization: contribution to pharmacology and function
    Graeme Milligan
    Molecular Pharmacology Group, Neuroscience and Molecular Pharmacology, Faculty of Biomedical and Life Sciences, University of Glasgow, Glasgow, UK
    Br J Pharmacol 158:5-14. 2009
    ..The current review summarizes key recent developments in these topics...
  28. ncbi request reprint Dimerization of alpha1-adrenoceptors
    G Milligan
    Molecular Pharmacology Group, Division of Biochemistry and Molecular Biology, Institute of Biomedical and Life Sciences, University of Glasgow, Glasgow G12 8QQ, Scotland, UK
    Biochem Soc Trans 32:847-50. 2004
    ..Key studies in this field are reviewed and the approaches that have been applied to monitoring the selectivity and the basis of alpha(1)-adrenoceptor dimerization are discussed...
  29. pmc Agonism and allosterism: the pharmacology of the free fatty acid receptors FFA2 and FFA3
    Graeme Milligan
    Molecular Pharmacology Group, Neuroscience and Molecular Pharmacology, Faculty of Biomedical and Life Sciences, University of Glasgow, Glasgow, UK
    Br J Pharmacol 158:146-53. 2009
    ....
  30. ncbi request reprint Oligomerisation of G-protein-coupled receptors
    G Milligan
    Molecular Pharmacology Group, Division of Biochemistry and Molecular Biology, Institute of Biomedical and Life Sciences, University of Glasgow, Glasgow, G12 8QQ, UK
    J Cell Sci 114:1265-71. 2001
    ..However, the majority of studies have relied largely on co-immunoprecipitation techniques, and there is still little direct information on the fraction of receptors existing as oligomers in intact cells...
  31. doi request reprint The role of dimerisation in the cellular trafficking of G-protein-coupled receptors
    Graeme Milligan
    Faculty of Biomedical and Life Sciences, University of Glasgow, Glasgow, Scotland, UK
    Curr Opin Pharmacol 10:23-9. 2010
    ..Although dimer/oligomer formation appears to be essential for cell surface delivery of class A and class C GPCRs, this may not be the case for class B receptors...
  32. ncbi request reprint The specificity and molecular basis of alpha1-adrenoceptor and CXCR chemokine receptor dimerization
    Graeme Milligan
    Molecular Pharmacology Group, Division of Biochemistry and Molecular Biology, Institute of Biomedical and Life Sciences, University of Glasgow, Glasgow G12 8QQ, Scotland
    J Mol Neurosci 26:161-8. 2005
    ....
  33. pmc A day in the life of a G protein-coupled receptor: the contribution to function of G protein-coupled receptor dimerization
    G Milligan
    Molecular Pharmacology Group, Division of Biochemistry and Molecular Biology, Institute of Biomedical and Life Sciences, University of Glasgow, Glasgow, Scotland, UK
    Br J Pharmacol 153:S216-29. 2008
    ....
  34. ncbi request reprint The human delta opioid receptor activates G(i1)alpha more efficiently than G(o1)alpha
    H E Moon
    Molecular Pharmacology Group, Division of Biochemistry and Molecular Biology, Institute of Biomedical and Life Sciences, University of Glasgow, Glasgow, UK
    J Neurochem 76:1805-13. 2001
    ....
  35. pmc Ligand regulation of green fluorescent protein-tagged forms of the human beta(1)- and beta(2)-adrenoceptors; comparisons with the unmodified receptors
    A J McLean
    Molecular Pharmacology Group, Division of Biochemistry and Molecular Biology, Institute of Biomedical and Life Sciences, University of Glasgow, Glasgow G12 8QQ
    Br J Pharmacol 130:1825-32. 2000
    ....
  36. ncbi request reprint Differential capacities of the RGS1, RGS16 and RGS-GAIP regulators of G protein signaling to enhance alpha2A-adrenoreceptor agonist-stimulated GTPase activity of G(o1)alpha
    M Hoffmann
    Molecular Pharmacology Group, Division of Biochemistry and Molecular Biology, Institute of Biomedical and Life Sciences, University of Glasgow, Glasgow, UK
    J Neurochem 78:797-806. 2001
    ....
  37. pmc Detection of receptor ligands by monitoring selective stabilization of a Renilla luciferase-tagged, constitutively active mutant, G-protein-coupled receptor
    D Ramsay
    Molecular Pharmacology Group, Division of Biochemistry and Molecular Biology, Institute of Biomedical and Life Sciences, University of Glasgow, Glasgow, G12 8QQ, UK
    Br J Pharmacol 133:315-23. 2001
    ..As no prior knowledge of receptor ligands is required this approach may be suitable to identify ligands at orphan G protein-coupled receptors...
  38. ncbi request reprint S 14506: novel receptor coupling at 5-HT(1A) receptors
    G Milligan
    Molecular Pharmacology Group, Division of Biochemistry and Molecular Biology, University of Glasgow, G12 8QQ, Glasgow, UK
    Neuropharmacology 40:334-44. 2001
    ..Thus it is possible to synthesise ligands at G-protein-coupled receptors which are highly potent agonists, but which are structurally related to inverse agonists and show some features of antagonist/inverse agonist binding...
  39. ncbi request reprint Control of the efficiency of agonist-induced information transfer and stability of the ternary complex containing the delta opioid receptor and the alpha subunit of G(i1) by mutation of a receptor/G protein contact interface
    H E Moon
    Molecular Pharmacology Group, Division of Biochemistry and Molecular Biology, Institute of Biomedical and Life Sciences, University of Glasgow, Davidson Building, Glasgow G12 8QQ, UK
    Neuropharmacology 41:321-30. 2001
    ....
  40. ncbi request reprint Selective interactions between helix VIII of the human mu-opioid receptors and the C terminus of periplakin disrupt G protein activation
    Giu Jie Feng
    Molecular Pharmacology Group, Division of Biochemistry and Molecular Biology, Institute of Biomedical and Life Sciences, University of Glasgow, Glasgow G12 8QQ, Scotland, United Kingdom
    J Biol Chem 278:33400-7. 2003
    ..This represents the first example of an opioid receptor-interacting protein that functions to disrupt agonist-mediated G protein activation...
  41. ncbi request reprint Monitoring receptor oligomerization using time-resolved fluorescence resonance energy transfer and bioluminescence resonance energy transfer. The human delta -opioid receptor displays constitutive oligomerization at the cell surface, which is not regulate
    M McVey
    Molecular Pharmacology Group, Division of Biochemistry and Molecular Biology, Institute of Biomedical and Life Sciences, University of Glasgow, Glasgow G12 8QQ, Scotland
    J Biol Chem 276:14092-9. 2001
    ..However, these are not regulated by ligand occupancy. They also indicate that time-resolved fluorescence resonance energy transfer represents a means to detect such oligomers at the cell surface in populations of intact cells...
  42. ncbi request reprint Analysis of function of receptor-G-protein and receptor-RGS fusion proteins
    Richard J Ward
    Molecular Pharmacology Group, University of Glasgow, Scotland, United Kingdom
    Methods Mol Biol 259:225-47. 2004
    ..Recently we have begun to supplement this approach with the use of fusions between G-protein-coupled receptors and regulator of G-protein signaling proteins to examine the function of this important group of signaling molecules...
  43. ncbi request reprint Periplakin interferes with G protein activation by the melanin-concentrating hormone receptor-1 by binding to the proximal segment of the receptor C-terminal tail
    Hannah Murdoch
    Molecular Pharmacology Group, Division of Biochemistry and Molecular Biology, Institute of Biomedical and Life Sciences, University of Glasgow, Glasgow G12 8QQ, Scotland, United Kingdom
    J Biol Chem 280:8208-20. 2005
    ..Periplakin is the first protein described to modify the capacity of the melanin-concentrating hormone-1 receptor to initiate signal transduction...
  44. ncbi request reprint Analysis of the C-terminal tail of the rat thyrotropin-releasing hormone receptor-1 in interactions and cointernalization with beta-arrestin 1-green fluorescent protein
    D A Groarke
    Molecular Pharmacology Group, Division of Biochemistry and Molecular Biology, Institute of Biomedical and Life Sciences, University of Glasgow, Glasgow Scotland, United Kingdom
    Mol Pharmacol 59:375-85. 2001
    ....
  45. ncbi request reprint The CXCR1 and CXCR2 receptors form constitutive homo- and heterodimers selectively and with equal apparent affinities
    Shirley Wilson
    Molecular Pharmacology Group, Division of Biochemistry and Molecular Biology, Institute of Biomedical and Life Sciences, University of Glasgow, Glasgow G12 8QQ, Scotland, United Kingdom
    J Biol Chem 280:28663-74. 2005
    ..Di Bartolomeo, S., Lauro, C., Catalano, M., Ciotti, M. T., and Limatola, C. (2003) J. Biol. Chem. 278, 40980-40988)...
  46. pmc Cell surface delivery and structural re-organization by pharmacological chaperones of an oligomerization-defective alpha(1b)-adrenoceptor mutant demonstrates membrane targeting of GPCR oligomers
    Meritxell Canals
    Molecular Pharmacology Group, Neuroscience and Molecular Pharmacology, Faculty of Biomedical and Life Sciences, University of Glasgow, Glasgow G128QQ, Scotland, UK
    Biochem J 417:161-72. 2009
    ....
  47. ncbi request reprint The human muscarinic M1 acetylcholine receptor, when express in CHO cells, activates and downregulates both Gq alpha and G11 alpha equally and non-selectively
    I Mullaney
    Department of Biochemistry, University of Glasgow, Scotland, UK
    FEBS Lett 324:241-5. 1993
    ..These data indicate that the HM1 receptor interacts with the activates both Gq alpha and G11 alpha equivalently and non-selectively in a whole cell system in which the receptor has access to both G-proteins...
  48. pmc Efficacy of inverse agonists in cells overexpressing a constitutively active beta2-adrenoceptor and type II adenylyl cyclase
    P A Stevens
    Division of Biochemistry and Molecular Biology, Institute of Biomedical and Life Sciences, University of Glasgow, Scotland
    Br J Pharmacol 123:335-43. 1998
    ..6 These data demonstrate that inverse agonist efficacy can be modulated by receptor availability and also indicate why in physiological systems, inverse agonism can be difficult to detect...
  49. pmc CXCR2 chemokine receptor antagonism enhances DOP opioid receptor function via allosteric regulation of the CXCR2-DOP receptor heterodimer
    Geraldine Parenty
    Molecular Pharmacology Group, Division of Biochemistry and Molecular Biology, Institute of Biomedical and Life Sciences, University of Glasgow, Glasgow G12 8QQ, Scotland, UK
    Biochem J 412:245-56. 2008
    ..These results have novel and important implications for the development and use of small-molecule therapeutics...
  50. ncbi request reprint Engineering a V(2) vasopressin receptor agonist- and regulator of G-protein-signaling-sensitive G protein
    Gui Jie Feng
    Molecular Pharmacology Group, Division of Biochemistry and Molecular Biology, Institute of Biomedical and Life Sciences, University of Glasgow, Glasgow, Scotland, United Kingdom
    Anal Biochem 300:212-20. 2002
    ..This approach provides a sensitive assay for V(2) receptor agonist ligands and may be amenable to many other G(s)alpha-coupled receptors...
  51. ncbi request reprint Methods to monitor the quaternary structure of G protein-coupled receptors
    Graeme Milligan
    Molecular Pharmacology Group, Division of Biochemistry and Molecular Biology, Institute of Biomedical and Life Sciences, University of Glasgow, UK
    FEBS J 272:2914-25. 2005
    ..Herein we assess the widely applied techniques and discuss the relative benefits and limitations of these approaches...
  52. ncbi request reprint Tailoring cAMP-signalling responses through isoform multiplicity
    M D Houslay
    Division of Biochemistry and Molecular Biology, University of Glasgow, Scotland, UK
    Trends Biochem Sci 22:217-24. 1997
    ..The ability to breach the PKA activation threshold can depend upon either or both the activation of adenylate cyclase and inhibition of specific PDE isoforms...
  53. ncbi request reprint Coordinated agonist regulation of receptor and G protein palmitoylation and functional rescue of palmitoylation-deficient mutants of the G protein G11alpha following fusion to the alpha1b-adrenoreceptor: palmitoylation of G11alpha is not required for inte
    P A Stevens
    Molecular Pharmacology Group, Division of Biochemistry and Molecular Biology, Institute of Biomedical and Life Sciences, University of Glasgow, Glasgow G12 8QQ, Scotland, United Kingdom
    J Biol Chem 276:35883-90. 2001
    ..gamma complex upon agonist stimulation whether or not the G protein can be palmitoylated. They also demonstrate that Ca(2+) signaling in EF88 cells by such fusion proteins is mediated via release of the G protein beta.gamma complex...
  54. pmc Analysis of the relative interactions between the alpha 2C10 adrenoceptor and the guanine-nucleotide-binding proteins G(o)1 alpha and Gi 2 alpha following co-expression of these polypeptides in rat 1 fibroblasts
    M A Grassie
    Molecular Pharmacology Group, University of Glasgow, Scotland, U K
    Biochem J 306:525-30. 1995
    ....
  55. ncbi request reprint The alpha1b-adrenoceptor exists as a higher-order oligomer: effective oligomerization is required for receptor maturation, surface delivery, and function
    Juan F Lopez-Gimenez
    Molecular Pharmacology Group, Division of Biochemistry and Molecular Biology, Institute of Biomedical and Life Sciences, University of Glasgow, Glasgow, Scotland, United Kingdom
    Mol Pharmacol 71:1015-29. 2007
    ....
  56. ncbi request reprint Concerted stimulation and deactivation of pertussis toxin-sensitive G proteins by chimeric G protein-coupled receptor-regulator of G protein signaling 4 fusion proteins: analysis of the contribution of palmitoylated cysteine residues to the GAP activity o
    Daljit S Bahia
    Molecular Pharmacology Group, Division of Biochemistry and Molecular Biology, Institute of Biomedical and Life Sciences, University of Glasgow, Glasgow, UK
    J Neurochem 85:1289-98. 2003
    ....
  57. pmc β-Arrestin 1 inhibits the GTPase-activating protein function of ARHGAP21, promoting activation of RhoA following angiotensin II type 1A receptor stimulation
    D F Anthony
    Neuroscience and Molecular Pharmacology, Division of Integrative Biology, IBLS, Wolfson Building, University of Glasgow, Glasgow G12 8QQ, Scotland, United Kingdom
    Mol Cell Biol 31:1066-75. 2011
    ....
  58. ncbi request reprint Molecular manipulation of G-protein-coupled receptors: a new avenue into drug discovery
    M Sautel
    Division of Biochemistry and Molecular Biology, Institute of Biomedical and Life Sciences, University of Glasgow, UK
    Curr Med Chem 7:889-96. 2000
    ....
  59. ncbi request reprint The alpha 2B adrenergic receptor of undifferentiated neuroblastoma x glioma hybrid NG108-15 cells, interacts directly with the guanine nucleotide binding protein, Gi2
    S J McClue
    Department of Biochemistry, University of Glasgow, Scotland, UK
    FEBS Lett 269:430-4. 1990
    ..These results demonstrate a direct interaction of the alpha 2B adrenergic receptor of NG108-15 cells with Gi2...
  60. ncbi request reprint Inverse agonism at adrenergic and opioid receptors: studies with wild type and constitutively active mutant receptors
    G Milligan
    Division of Biochemistry and Molecular Biology, University of Glasgow, U K
    Receptors Channels 5:209-13. 1997
    ..In the stable cells lines this effect was prevented by co-incubation with neutral antagonists but could not be reproduced by an adenylyl cyclase P-site ligand which also inhibited basal adenylyl cyclase levels...
  61. ncbi request reprint Agonist-induced transfer of the alpha subunits of the guanine-nucleotide-binding regulatory proteins Gq and G11 and of muscarinic m1 acetylcholine receptors from plasma membranes to a light-vesicular membrane fraction
    P Svoboda
    Department of Biochemistry, University of Glasgow, Scotland
    Eur J Biochem 224:455-62. 1994
    ..The second step is represented by an agonist-specific down-regulation pathway. Both the Hm1 receptor and Gq alpha/G11 alpha appear to follow similar sequestration and down-regulation patterns...
  62. doi request reprint International Union of Pharmacology. LXXI. Free fatty acid receptors FFA1, -2, and -3: pharmacology and pathophysiological functions
    Leigh A Stoddart
    Molecular Pharmacology Group, Neuroscience and Molecular Pharmacology, Faculty of Biomedical and Life Sciences, University of Glasgow, Glasgow, Scotland, United Kingdom
    Pharmacol Rev 60:405-17. 2008
    ..The aim of this review is to provide a comprehensive overview of the current understanding of the pharmacology and physiological role of these fatty acid receptors...
  63. ncbi request reprint Protean agonism at the dopamine D2 receptor: (S)-3-(3-hydroxyphenyl)-N-propylpiperidine is an agonist for activation of Go1 but an antagonist/inverse agonist for Gi1,Gi2, and Gi3
    J Robert Lane
    Molecular Pharmacology Group, Division of Biochemistry and Molecular Biology, Institute of Biomedical and Life Sciences, University of Glasgow, Glasgow, Scotland, United Kingdom
    Mol Pharmacol 71:1349-59. 2007
    ..These results demonstrate (S)-(-)-3-(3-hydroxyphenyl)-N-propylpiperidine to be a protean agonist at the D(2) receptor and may explain in vivo actions of this ligand...
  64. doi request reprint Conserved polar residues in transmembrane domains V, VI, and VII of free fatty acid receptor 2 and free fatty acid receptor 3 are required for the binding and function of short chain fatty acids
    Leigh A Stoddart
    Molecular Pharmacology Group, Neuroscience and Molecular Pharmacology, Faculty of Biomedical and Life Sciences, University of Glasgow, Glasgow G12 8QQ, Scotland
    J Biol Chem 283:32913-24. 2008
    ..The development of small molecule ligands that interact selectively with these receptors will allow further details of the binding pockets to be elucidated...
  65. ncbi request reprint Beta-arrestin-dependent spontaneous alpha1a-adrenoceptor endocytosis causes intracellular transportation of alpha-blockers via recycling compartments
    John D Pediani
    Autonomic Physiology Unit, Institute of Biomedical and Life Sciences, University of Glasgow, Glasgow G12 8QQ, Scotland, UK
    Mol Pharmacol 67:992-1004. 2005
    ..We conclude that alpha(1a)-ARs recycle rapidly by an agonist-independent, constitutive, beta-arrestin-dependent process and that this can transport "alpha-blockers" into cells carrying these receptors...
  66. doi request reprint Mutations of beta-arrestin 2 that limit self-association also interfere with interactions with the beta2-adrenoceptor and the ERK1/2 MAPKs: implications for beta2-adrenoceptor signalling via the ERK1/2 MAPKs
    Tian Rui Xu
    Sir Henry Welcome Functional Genomics Facility, Division of Biochemistry and Molecular Biology, Institute of Biomedical and Life Sciences, University of Glasgow, Glasgow G12 8QQ, Scotland, UK
    Biochem J 413:51-60. 2008
    ..Regulation of beta-arrestin 2 self-association may therefore control beta-arrestin 2-mediated beta2-adrenoceptor-ERK1/2 MAPK signalling...
  67. ncbi request reprint Opioid regulation of mu receptor internalisation: relevance to the development of tolerance and dependence
    Juan F Lopez-Gimenez
    Molecular Pharmacology Group, Neuroscience and Molecular Pharmacology, Faculty of Biomedical and Life Sciences, University of Glasgow, Glasgow G12 8QQ, Scotland, UK
    CNS Neurol Disord Drug Targets 9:616-26. 2010
    ..Although aspects of this model are controversial, such observations suggest a number of approaches to further enhance the use of morphine as an analgesic...
  68. ncbi request reprint Expression of Gsalpha, connexin-43, connexin-26, and EP1, 3, and 4 receptors in myometrium of prelabor singleton versus multiple gestations and the effects of mechanical stretch and steroids on Gsalpha
    Fiona Lyall
    Institute of Medical Genetics, Yorkhill, Glasgow, United Kingdom
    J Soc Gynecol Investig 9:299-307. 2002
    ....
  69. ncbi request reprint Measurement of agonist-dependent and -independent signal initiation of alpha(1b)-adrenoceptor mutants by direct analysis of guanine nucleotide exchange on the G protein galpha(11)
    Juan J Carrillo
    Molecular Pharmacology Group, Division of Biochemistry and Molecular Biology, University of Glasgow, Glasgow G12 8QQ, Scotland, United Kingdom
    J Pharmacol Exp Ther 302:1080-8. 2002
    ....
  70. doi request reprint When simple agonism is not enough: emerging modalities of GPCR ligands
    Nicola J Smith
    Molecular Pharmacology Group, Neuroscience and Molecular Pharmacology, Faculty of Biomedical and Life Sciences, University of Glasgow, Glasgow G12 8QQ, Scotland, UK
    Mol Cell Endocrinol 331:241-7. 2011
    ..Finally, the concept that efficacy should be defined by the activity of an endogenous ligand will be challenged by the discovery that some ligands act as 'super-agonists' in specific pathways or at certain receptor mutations...
  71. ncbi request reprint Why are there so many adrenoceptor subtypes?
    G Milligan
    Department of Biochemistry, University of Glasgow, Scotland, U K
    Biochem Pharmacol 48:1059-71. 1994
  72. pmc Hormonal regulation of Gi2 alpha-subunit phosphorylation in intact hepatocytes
    M Bushfield
    Department of Biochemistry, University of Glasgow, Scotland, U K
    Biochem J 268:449-57. 1990
    ..We suggest that there are two possible sites for the phosphorylation of alpha-Gi2; one for C-kinase and the other for an unidentified kinase whose action is triggered by A-kinase activation...
  73. ncbi request reprint Interaction of the G-protein G11alpha with receptors and phosphoinositidase C: the contribution of G-protein palmitoylation and membrane association
    A Wise
    Division of Biochemistry and Molecular Biology, Institute of Biomedical and Life Sciences, University of Glasgow, Scotland, UK
    FEBS Lett 407:257-60. 1997
    ..The degree of stimulation produced by TRH following co-transfection of the palmitoylation-resistant forms of G11alpha compared to the wild-type protein correlated with the amount of membrane-associated G protein...
  74. pmc Mapping binding sites for the PDE4D5 cAMP-specific phosphodiesterase to the N- and C-domains of beta-arrestin using spot-immobilized peptide arrays
    George S Baillie
    Molecular Pharmacology Group, Division of Biochemistry and Molecular Biology, Institute of Biomedical and Life Sciences, University of Glasgow, Glasgow G12 8QQ, Scotland, UK
    Biochem J 404:71-80. 2007
    ..These data show that the interaction of PDE4D5 with both the N- and C-domains of beta-arrestin 2 are essential for beta2-AR regulation...
  75. pmc The action and mode of binding of thiazolidinedione ligands at free fatty acid receptor 1
    Nicola J Smith
    Molecular Pharmacology Group, Neuroscience and Molecular Pharmacology, Faculty of Biomedical and Life Sciences, University of Glasgow, Glasgow G12 8QQ, Scotland, United Kingdom
    J Biol Chem 284:17527-39. 2009
    ....
  76. doi request reprint Localization of the succinate receptor in the distal nephron and its signaling in polarized MDCK cells
    Joris H Robben
    Molecular Pharmacology Group, Division of Neuroscience and Molecular Pharmacology, Faculty of Biomedical and Life Sciences, University of Glasgow, Glasgow, UK
    Kidney Int 76:1258-67. 2009
    ..Our study suggests that changes in the luminal succinate concentration may regulate several aspects of renal function...
  77. ncbi request reprint Orexin-1 receptor-cannabinoid CB1 receptor heterodimerization results in both ligand-dependent and -independent coordinated alterations of receptor localization and function
    James Ellis
    Molecular Pharmacology Group, Division of Biochemistry and Molecular Biology, Institute of Biomedical and Life Sciences, University of Glasgow, Glasgow G12 8QQ, Scotland, United Kingdom
    J Biol Chem 281:38812-24. 2006
    ..These studies introduce an entirely novel pharmacological paradigm, whereby ligands modulate the function of receptors for which they have no significant inherent affinity by acting as regulators of receptor heterodimers...
  78. doi request reprint Antibodies that identify only the active conformation of G(i) family G protein alpha subunits
    J Robert Lane
    Molecular Pharmacology Group, Division of Biochemistry and Molecular Biology, Institute of Biomedical and Life Sciences, University of Glasgow, Glasgow, UK
    FASEB J 22:1924-32. 2008
    ..Such reagents allow the specific identification of activated G proteins in a native environment and may allow the development of label-free screening assays for G protein-coupled receptor-mediated activation of G(i) family G proteins...
  79. ncbi request reprint A key serine for the GTPase-activating protein function of regulator of G protein signaling proteins is not a general target for 14-3-3 interactions
    Richard J Ward
    Molecular Pharmacolofy Group, Division of Biochemistry and Molecular Biology, Institute of Biomedical and Life Sciences, Davidson Building, University of Glasgow, Glasgow G12 8QQ, Scotland, United Kingdom
    Mol Pharmacol 68:1821-30. 2005
    ..Although interactions between 14-3-3 proteins and many RGS proteins can be observed, this does not involve this conserved serine and does not inherently modify GAP function...
  80. pmc Regulation of the avidity of ternary complexes containing the human 5-HT(1A) receptor by mutation of a receptor contact site on the interacting G protein alpha subunit
    Philip J Welsby
    Molecular Pharmacology Group, Division of Biochemistry and Molecular Biology, Institute of Biomedical and Life Sciences, University of Glasgow, Glasgow G12 8QQ
    Br J Pharmacol 137:345-52. 2002
    ..7 These results indicate that a higher avidity ternary complex is formed between 8-OH-DPAT, the 5-HT(1A) receptor and G proteins when isoleucine rather than glycine is located at residue(351) of the interacting G protein...
  81. pmc The sustainability of interactions between the orexin-1 receptor and beta-arrestin-2 is defined by a single C-terminal cluster of hydroxy amino acids and modulates the kinetics of ERK MAPK regulation
    Sandra Milasta
    Molecular Pharmacology Group, Division of Biochemistry and Molecular Biology, Institute of Biomedical and Life Sciences, University of Glasgow, Glasgow G12 8QQ, Scotland, UK
    Biochem J 387:573-84. 2005
    ....
  82. pmc Activation of an alpha2A-adrenoceptor-Galphao1 fusion protein dynamically regulates the palmitoylation status of the G protein but not of the receptor
    Elaine Barclay
    Molecular Pharmacology Group, Division of Biochemistry and Molecular Biology, University of Glasgow, Glasgow G12 8QQ, Scotland, UK
    Biochem J 385:197-206. 2005
    ....
  83. ncbi request reprint Reciprocal mutations of highly conserved residues in transmembrane helices 2 and 7 of the alpha(2A)-adrenoceptor restore agonist activation of G(i1)alpha
    Richard J Ward
    Molecular Pharmacology Group, Division of Biochemistry and Molecular Biology, Institute of Biomedical and Life Sciences, University of Glasgow, Glasgow G12 8QQ, Scotland, UK
    Cell Signal 14:139-44. 2002
    ..By examining alterations in this helix 2-helix 7 microdomain, we further demonstrate the utility of receptor-G-protein fusion proteins to quantitate mutational effects on receptor-G-protein interactions and information transfer...
  84. ncbi request reprint Dimers of class A G protein-coupled receptors function via agonist-mediated trans-activation of associated G proteins
    Juan J Carrillo
    Molecular Pharmacology Group, Division of Biochemistry and Molecular Biology, Institute of Biomedical and Life Sciences, University of Glasgow, Glasgow G12 8QQ, Scotland, U K
    J Biol Chem 278:42578-87. 2003
    ..These data demonstrate that dimers of these class A receptors function via trans-activation of associated G proteins...
  85. ncbi request reprint Functional interactions between the alpha1b-adrenoceptor and Galpha11 are compromised by de-palmitoylation of the G protein but not of the receptor
    Jiri Novotny
    Molecular Pharmacology Group, Division of Biochemistry and Molecular Biology, Institute of Biomedical and Life Sciences, University of Glasgow, Glasgow G12 8QQ, Scotland, UK
    Cell Signal 18:1244-51. 2006
    ....
  86. doi request reprint Chapter 10. Hetero-oligomerization of chemokine receptors
    Shirley Appelbe
    Neuroscience and Molecular Pharmacology, University of Glasgow, Glasgow, Scotland, United Kingdom
    Methods Enzymol 461:207-25. 2009
    ..This chapter highlights some of the most common techniques used to investigate chemokine receptor oligomerization...
  87. ncbi request reprint Construction and analysis of function of G protein-coupled receptor-G protein fusion proteins
    Graeme Milligan
    Molecular Pharmacology Group, Division of Biochemistry and Molecular Biology, Institute of Biomedical and Life Sciences, University of Glasgow, Glasgow G12 8QQ, Scotland, United Kingdom
    Methods Enzymol 343:260-73. 2002
  88. ncbi request reprint Generation and analysis of constitutively active and physically destabilized mutants of the human beta(1)-adrenoceptor
    Alison J McLean
    Molecular Pharmacology Group, Division of Biochemistry and Molecular Biology, Institute of Biomedical and Life Sciences, University of Glasgow, Glasgow, Scotland, United Kingdom
    Mol Pharmacol 62:747-55. 2002
    ....
  89. ncbi request reprint High-affinity interactions between human alpha1A-adrenoceptor C-terminal splice variants produce homo- and heterodimers but do not generate the alpha1L-adrenoceptor
    Douglas Ramsay
    Division of Biochemistry and Molecular Biology, Institute of Biomedical and Life Sciences, University of Glasgow, Scotland, United Kingdom
    Mol Pharmacol 66:228-39. 2004
    ....
  90. pmc Ligand regulation of the quaternary organization of cell surface M3 muscarinic acetylcholine receptors analyzed by fluorescence resonance energy transfer (FRET) imaging and homogeneous time-resolved FRET
    Elisa Alvarez-Curto
    Molecular Pharmacology Group, Neuroscience and Molecular Pharmacology, Faculty of Biomedical and Life Sciences, University of Glasgow, Glasgow G12 8QQ, Scotland, United Kingdom
    J Biol Chem 285:23318-30. 2010
    ..However, conclusions as to the effect of ligands on such complexes may depend on the approach used...
  91. doi request reprint Applications of fluorescence and bioluminescence resonance energy transfer to drug discovery at G protein coupled receptors
    Elisa Alvarez-Curto
    Molecular Pharmacology Group, Neuroscience and Molecular Pharmacology, Faculty of Biomedical and Life Sciences, University of Glasgow, Glasgow G12 8QQ, UK
    Anal Bioanal Chem 398:167-80. 2010
    ..In this review we highlight the latest advances in these technologies to illustrate general principles...
  92. ncbi request reprint Functional complementation and the analysis of opioid receptor homodimerization
    Geraldine Pascal
    Davidson Building, University of Glasgow, Glasgow G12 8QQ, Scotland, UK
    Mol Pharmacol 68:905-15. 2005
    ..Because the amino acids modified in the opioid receptors are highly conserved in most rhodopsin-like receptors, this approach should be widely applicable to study the existence and molecular basis of receptor dimerization...
  93. ncbi request reprint Enhanced detection of receptor constitutive activity in the presence of regulators of G protein signaling: applications to the detection and analysis of inverse agonists and low-efficacy partial agonists
    Philip J Welsby
    Molecular Pharmacology Group, Division of Biochemistry and Molecular Biology, Institute of Biomedical and Life Sciences, University of Glasgow, Glasgow, Scotland, United Kingdom
    Mol Pharmacol 61:1211-21. 2002
    ..By so doing, it also greatly enhances the ability to detect and analyze the effects of inverse agonists and to discriminate between neutral ligands and those with low levels of positive intrinsic efficacy...
  94. ncbi request reprint Interactions between the Mas-related receptors MrgD and MrgE alter signalling and trafficking of MrgD
    Sandra Milasta
    Molecular Pharmacology Group, Division of Biochemistry and Molecular Biology, Institute of Biomedical and Life Sciences, University of Glasgow, Scotland, UK
    Mol Pharmacol 69:479-91. 2006
    ..Because the Mrg receptors are potential therapeutic targets in pain, these results suggest that efforts to understand the function and regulation of individual Mrg family receptors may require coexpression of relevant pairs...
  95. pmc GPR35 as a Novel Therapeutic Target
    A E MacKenzie
    Molecular Pharmacology Group, Institute of Neuroscience and Psychology, College of Medical, Veterinary and Life Sciences, University of Glasgow Glasgow, UK
    Front Endocrinol (Lausanne) 2:68. 2011
    ....
  96. pmc Angiotensin1-9 antagonises pro-hypertrophic signalling in cardiomyocytes via the angiotensin type 2 receptor
    M Flores-Muñoz
    Institute of Cardiovascular and Medical Sciences, BHF GCRC, University of Glasgow, 126 University Place, Glasgow G12 8TA, UK
    J Physiol 589:939-51. 2011
    ..28 ± 0.1). In summary, we ascribe a direct biological role for Ang1-9 acting via the AT2R. This has implications for RAS function and identifying new therapeutic targets in cardiovascular disease...
  97. ncbi request reprint Identification of a novel site within G protein alpha subunits important for specificity of receptor-G protein interaction
    Arne Heydorn
    Laboratory for Molecular Pharmacology, The Panum Institute, University of Copenhagen, Copenhagen, Denmark
    Mol Pharmacol 66:250-9. 2004
    ....
  98. ncbi request reprint Mechanism of action of Gq to inhibit G beta gamma modulation of CaV2.2 calcium channels: probed by the use of receptor-G alpha tandems
    Federica Bertaso
    Department of Pharmacology, University College London, London, United Kingdom
    Mol Pharmacol 63:832-43. 2003
    ..The potential sites of phosphorylation are discussed...
  99. ncbi request reprint Palmitoylation regulates regulators of G-protein signaling (RGS) 16 function. I. Mutation of amino-terminal cysteine residues on RGS16 prevents its targeting to lipid rafts and palmitoylation of an internal cysteine residue
    Abel Hiol
    Metabolic Diseases Branch, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, Maryland 20892, USA
    J Biol Chem 278:19301-8. 2003
    ..L., Waheed, A. A., Hiol, A., Ward, R. J., Davey, P. C., Nini, L., Wang, J., Milligan, G., Jones, T. L. Z., and Druey, K. M. (2003) J. Biol. Chem. 278, 19309-19316) was critical for RGS16 and RGS4 GAP activity...
  100. ncbi request reprint Palmitoylation regulates regulator of G-protein signaling (RGS) 16 function. II. Palmitoylation of a cysteine residue in the RGS box is critical for RGS16 GTPase accelerating activity and regulation of Gi-coupled signalling
    James L Osterhout
    Molecular Signal Transduction Section, Laboratory of Allergic Diseases, National Institute of Allergy and Infectious Diseases, National Institutes of Health, Rockville, Maryland 20892, USA
    J Biol Chem 278:19309-16. 2003
    ..These results suggest that palmitoylation of a Cys residue in the RGS box is critical for RGS16 and RGS4 GAP activity and their ability to regulate Gi-coupled signaling in mammalian cells...
  101. ncbi request reprint Allosteric modulation and constitutive activity of fusion proteins between the adenosine A1 receptor and different 351Cys-mutated Gi alpha-subunits
    Elisabeth Klaasse
    Division of Medicinal Chemistry, Leiden Amsterdam Center for Drug Research, Leiden University, P O Box 9502, 2300 RA Leiden, The Netherlands
    Eur J Pharmacol 499:91-8. 2004
    ..In conclusion, A1-Gialpha fusion proteins, especially with 351Cys and 351Ile, can be used as research tools to investigate inverse agonism, due to their increased readout window in [35S]GTPgammaS binding experiments...