D Sugden

Summary

Affiliation: King's College London
Country: UK

Publications

  1. ncbi request reprint Design, synthesis, and melatoninergic activity of new azido- and isothiocyanato-substituted indoles
    Andrew Tsotinis
    Faculty of Pharmacy, Department of Pharmaceutical Chemistry, University of Athens, Panepistimioupoli Zografou, 157 71 Athens, Greece
    J Med Chem 50:6436-40. 2007
  2. pmc Sleep-promoting action of IIK7, a selective MT2 melatonin receptor agonist in the rat
    Simon P Fisher
    Division of Reproduction and Endocrinology, School of Biomedical and Health Sciences, King s College London, London SE1 1UL, UK
    Neurosci Lett 457:93-6. 2009
  3. ncbi request reprint Melatonin, melatonin receptors and melanophores: a moving story
    David Sugden
    Division of Reproductive Health, Endocrinology and Development, School of Biomedical Sciences, New Hunts House, Kings College London, London Bridge, London SE1 1UL, UK
    Pigment Cell Res 17:454-60. 2004
  4. ncbi request reprint Expression of mt(1) melatonin receptor subtype mRNA in the entrained rat suprachiasmatic nucleus: a quantitative RT-PCR study across the diurnal cycle
    D Sugden
    Department of Physiology, Division of Biomedical Sciences, King s College London, Campden Hill Road, London, UK
    Brain Res Mol Brain Res 72:176-82. 1999
  5. ncbi request reprint Design of subtype selective melatonin receptor agonists and antagonists
    D Sugden
    Physiology Division, GKT School of Biomedical Science, King s College London, UK
    Reprod Nutr Dev 39:335-44. 1999
  6. ncbi request reprint Comparison of circadian expression of tryptophan hydroxylase isoform mRNAs in the rat pineal gland using real-time PCR
    David Sugden
    Centre for Reproduction, Endocrinology and Diabetes, School of Biomedical Sciences, Kings College London, London Bridge, London SE1 1UL, UK
    J Neurochem 86:1308-11. 2003
  7. pmc An endogenous 5-HT(7) receptor mediates pigment granule dispersion in Xenopus laevis melanophores
    M T Teh
    Endocrinology and Reproduction Research Group, GKT School of Biomedical Science, King's College London, London, SE1 1UL
    Br J Pharmacol 132:1799-808. 2001
  8. ncbi request reprint Phosphoprotein phosphatases regulate steroidogenesis by influencing StAR gene transcription
    C J Burns
    Endocrinology and Reproduction Research Group, Guy s, King s and St Thomas School of Biomedical Sciences, Guy s Campus, London Bridge, London, SE1 9RT, United Kingdom
    Biochem Biophys Res Commun 273:35-9. 2000
  9. ncbi request reprint A key role for beta-cell cytosolic phospholipase A(2) in the maintenance of insulin stores but not in the initiation of insulin secretion
    Shanta J Persaud
    Endocrinology and Reproduction Research Group, King s College London, London, UK
    Diabetes 51:98-104. 2002
  10. ncbi request reprint Desensitization of pigment granule aggregation in Xenopus leavis melanophores: melatonin degradation rather than receptor down-regulation is responsible
    Muy Teck Teh
    Endocrinology and Reproduction Research Group, School of Biomedical Sciences, New Hunts House, Kings College London, Guy s Campus, London Bridge, London SE1 1UL, UK
    J Neurochem 81:719-27. 2002

Collaborators

Detail Information

Publications31

  1. ncbi request reprint Design, synthesis, and melatoninergic activity of new azido- and isothiocyanato-substituted indoles
    Andrew Tsotinis
    Faculty of Pharmacy, Department of Pharmaceutical Chemistry, University of Athens, Panepistimioupoli Zografou, 157 71 Athens, Greece
    J Med Chem 50:6436-40. 2007
    ..All active compounds were partial agonists or antagonists in the Xenopus melanophore assay, the most potent being the 5-OMe C3-substituted azido 45 and isothiocyanato 46 analogues...
  2. pmc Sleep-promoting action of IIK7, a selective MT2 melatonin receptor agonist in the rat
    Simon P Fisher
    Division of Reproduction and Endocrinology, School of Biomedical and Health Sciences, King s College London, London SE1 1UL, UK
    Neurosci Lett 457:93-6. 2009
    ..The acute and transient changes in the sleep-wake cycle mimic the changes seen with melatonin and suggest that its sleep-promoting activity is mediated by activation of the MT2 receptor subtype...
  3. ncbi request reprint Melatonin, melatonin receptors and melanophores: a moving story
    David Sugden
    Division of Reproductive Health, Endocrinology and Development, School of Biomedical Sciences, New Hunts House, Kings College London, London Bridge, London SE1 1UL, UK
    Pigment Cell Res 17:454-60. 2004
    ....
  4. ncbi request reprint Expression of mt(1) melatonin receptor subtype mRNA in the entrained rat suprachiasmatic nucleus: a quantitative RT-PCR study across the diurnal cycle
    D Sugden
    Department of Physiology, Division of Biomedical Sciences, King s College London, Campden Hill Road, London, UK
    Brain Res Mol Brain Res 72:176-82. 1999
    ..These results indicate that changes in the level of mt(1) mRNA do not underlie the diurnal and/or circadian variation in the response of the SCN circadian clock to the phase-resetting effects of melatonin...
  5. ncbi request reprint Design of subtype selective melatonin receptor agonists and antagonists
    D Sugden
    Physiology Division, GKT School of Biomedical Science, King s College London, UK
    Reprod Nutr Dev 39:335-44. 1999
    ..In binding assays, K185 is 140-fold selective for the MT2 subtype...
  6. ncbi request reprint Comparison of circadian expression of tryptophan hydroxylase isoform mRNAs in the rat pineal gland using real-time PCR
    David Sugden
    Centre for Reproduction, Endocrinology and Diabetes, School of Biomedical Sciences, Kings College London, London Bridge, London SE1 1UL, UK
    J Neurochem 86:1308-11. 2003
    ..TPH2 expression within the gland showed no significant variation with time of day and was very low (approximately 300 copies/gland) indicating expression in the small proportion of "non-pinealocyte" cells in the gland...
  7. pmc An endogenous 5-HT(7) receptor mediates pigment granule dispersion in Xenopus laevis melanophores
    M T Teh
    Endocrinology and Reproduction Research Group, GKT School of Biomedical Science, King's College London, London, SE1 1UL
    Br J Pharmacol 132:1799-808. 2001
    ..Conceivably some of the effects attributed to pharmacological doses of melatonin in mammals may be mediated by activation of 5-HT(7) receptors...
  8. ncbi request reprint Phosphoprotein phosphatases regulate steroidogenesis by influencing StAR gene transcription
    C J Burns
    Endocrinology and Reproduction Research Group, Guy s, King s and St Thomas School of Biomedical Sciences, Guy s Campus, London Bridge, London, SE1 9RT, United Kingdom
    Biochem Biophys Res Commun 273:35-9. 2000
    ..These results suggest that cyclic AMP-induced increases in StAR mRNA levels are dependent upon phosphoprotein phosphatase activities...
  9. ncbi request reprint A key role for beta-cell cytosolic phospholipase A(2) in the maintenance of insulin stores but not in the initiation of insulin secretion
    Shanta J Persaud
    Endocrinology and Reproduction Research Group, King s College London, London, UK
    Diabetes 51:98-104. 2002
    ..These data are consistent with a role for cPLA(2) in the maintenance of insulin stores, but they suggest that it is not required for the initiation of insulin secretion from beta-cells...
  10. ncbi request reprint Desensitization of pigment granule aggregation in Xenopus leavis melanophores: melatonin degradation rather than receptor down-regulation is responsible
    Muy Teck Teh
    Endocrinology and Reproduction Research Group, School of Biomedical Sciences, New Hunts House, Kings College London, Guy s Campus, London Bridge, London SE1 1UL, UK
    J Neurochem 81:719-27. 2002
    ....
  11. doi request reprint Function and expression of melatonin receptors on human pancreatic islets
    Reshma D Ramracheya
    Beta Cell Development and Function Group, School of Biomedical and Health Sciences, King s College London, London, UK
    J Pineal Res 44:273-9. 2008
    ..This study also indicates that the effects of melatonin are species-specific with primarily an inhibitory role in rodent beta-cells and a stimulatory effect in human islets...
  12. ncbi request reprint Early activation of the p42/p44MAPK pathway mediates adenosine-induced nitric oxide production in human endothelial cells: a novel calcium-insensitive mechanism
    Amanda W Wyatt
    Centre for Cardiovascular Biology and Medicine, GKT School of Biomedical Sciences, King s College London, Guy s Campus, London SE1 1UL, UK
    FASEB J 16:1584-94. 2002
    ....
  13. ncbi request reprint Characterization of alpha1-adrenoceptor subtypes mediating noradrenaline-induced contraction of rat epididymal vas deferens in calcium-free medium
    N I Amobi
    Physiology Division, King s College London, Great Britain, UK
    Life Sci 65:187-96. 1999
    ..These results suggest that NA contracts the tissue in Ca2+-free medium by the stimulation of alpha1A-adrenoceptors. Two factors affecting CEC-sensitivity of NA-induced contractions in this tissue are discussed...
  14. ncbi request reprint ACTH stimulates insulin secretion from MIN6 cells and primary mouse and human islets of Langerhans
    H T Al-Majed
    Centre for Reproduction, Endocrinology and Diabetes, GKT School of Biomedical Sciences, King s College London, Guy s Campus, London SE1 1UL, UK
    J Endocrinol 180:155-66. 2004
    ..Overall the results demonstrate that the MC2-R is expressed in beta-cells and suggest that activation of the receptor by ACTH initiates insulin secretion through the activation of PKA in association with Ca2+ influx into beta-cells...
  15. pmc Endogenous melatonin is not obligatory for the regulation of the rat sleep-wake cycle
    Simon P Fisher
    Division of Reproduction and Endocrinology, School of Biomedical and Health Sciences, King s College London, London, UK
    Sleep 33:833-40. 2010
    ..Some clinical case reports suggest that reduced nocturnal melatonin secretion is linked to sleep disruption, but pineal-gland removal in experimental animals has given variable results...
  16. ncbi request reprint Dietary soy isoflavone induced increases in antioxidant and eNOS gene expression lead to improved endothelial function and reduced blood pressure in vivo
    Katharina Mahn
    Cardiovascular Division, School of Biomedical and Health Sciences, King s College London, London, UK
    FASEB J 19:1755-7. 2005
    ..The improvement in endothelial function, increased gene expression, and reduced blood pressure by soy isoflavones have implications for alternative therapy for postmenopausal women and patients at risk of coronary heart disease...
  17. ncbi request reprint Identification of PAC1 receptor isoform mRNAs by real-time PCR in rat suprachiasmatic nucleus
    Supaporn Ajpru
    Endocrinology and Reproduction Research Group, GKT School of Biomedical Sciences, Kings College London, London SE1 1UL, UK
    Brain Res Mol Brain Res 105:29-37. 2002
    ....
  18. ncbi request reprint Mechanical stretch induces monocyte chemoattractant activity via an NF-kappaB-dependent monocyte chemoattractant protein-1-mediated pathway in human mesangial cells: inhibition by rosiglitazone
    Gabriella Gruden
    Department of Diabetes and Endocrinology, Cardiovascular Division, King s College, London, UK
    J Am Soc Nephrol 16:688-96. 2005
    ..In conclusion, stretching of mesangial cells stimulates their monocyte chemoattractant activity via an NF-kappaB-mediated, MCP-1-dependent pathway, and this effect is prevented by rosiglitazone...
  19. doi request reprint Acute sleep-promoting action of the melatonin agonist, ramelteon, in the rat
    Simon P Fisher
    Division of Reproduction and Endocrinology, School of Biomedical and Health Sciences, King s College London, London, UK
    J Pineal Res 45:125-32. 2008
    ..In conclusion, ramelteon administration, like melatonin, exerted an acute, short-lasting sleep-promoting effect in the rat, the model most commonly used to evaluate the activity of novel hypnotic drugs...
  20. ncbi request reprint Protease-activated receptors upregulate cyclooxygenase-2 expression in human endothelial cells
    Rebecca A Houliston
    Department of Veterinary Basic Sciences, Royal Veterinary College, University of London, Royal College Street, London, UK
    Thromb Haemost 88:321-8. 2002
    ..These results demonstrate that regulation of COX-2 induction is an important functional response of HUVEC to PAR activation and suggest that PARs promote sustained upregulation of prostanoid production in human endothelium...
  21. pmc Gene deletion reveals roles for annexin A1 in the regulation of lipolysis and IL-6 release in epididymal adipose tissue
    James P Warne
    Dept of Cellular and Molecular Neuroscience, Division of Neuroscience and Mental Health, Imperial College London, Hammersmith Campus, London, W12 0NN, UK
    Am J Physiol Endocrinol Metab 291:E1264-73. 2006
    ..Collectively, these studies suggest that ANXA1 supports aspects of adipose tissue mass and alters the sensitivity of epididymal adipose tissue to catecholamines, glucocorticoids, and LPS, thereby modulating lipolysis and IL-6 release...
  22. ncbi request reprint Synthesis of N1-phenethyl substituted indole derivatives as new melatoninergic agonists and antagonists
    Andrew Tsotinis
    School of Pharmacy, University of Athens, Greece
    Chem Pharm Bull (Tokyo) 50:31-9. 2002
    ....
  23. ncbi request reprint 7-Substituted-melatonin and 7-substituted-1-methylmelatonin analogues: effect of substituents on potency and binding affinity
    Rüdiger Faust
    Department of Chemistry, University College London, 20 Gordon Street, London WC1H 0AJ, UK
    Bioorg Med Chem 15:4543-51. 2007
    ..These results suggest that the receptor pocket around C-7 favours binding by an electronegative group, suggesting an electropositive region in this area of the receptor...
  24. ncbi request reprint Binding affinity and biological activity of oxygen and sulfur isosteres at melatonin receptors as a function of their hydrogen bonding capability
    David J Davies
    Department of Chemistry, University College London, WC1H 0AJ, UK
    Bioorg Chem 32:1-12. 2004
    ..Using K(B)(H) values from Abraham's equations we have assessed the possibility of estimating EC50 values for sulfur isosteres from the EC50 values of their oxygen analogues...
  25. ncbi request reprint Mapping the melatonin receptor. 7. Subtype selective ligands based on beta-substituted N-acyl-5-methoxytryptamines and beta-substituted N-acyl-5-methoxy-1-methyltryptamines
    Andrew Tsotinis
    Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Athens, Panepistimioupoli Zografou, Athens 157 71, Greece
    J Med Chem 49:3509-19. 2006
    ....
  26. ncbi request reprint Melatonin stimulates cell proliferation in zebrafish embryo and accelerates its development
    Nadia Danilova
    Department of Biology, Massachusetts Institute of Technology, 77 Massachusetts Ave, Cambridge, Massachusetts 02139, USA
    FASEB J 18:751-3. 2004
    ..We propose that melatonin has a role in extending the safe limit of proliferation rate at night to allow more rapid development when potentially damaging ultraviolet light is absent...
  27. ncbi request reprint Design, synthesis and melatoninergic activity of new unsubstituted and beta,beta'-difunctionalised 2,3-dihydro-1H-pyrrolo[3,2,1-ij]quinolin-6-alkanamides
    Andrew Tsotinis
    Faculty of Pharmacy, Department of Pharmaceutical Chemistry, University of Athens, Panepistimioupoli Zografou, 157 71 Athens, Greece
    Eur J Med Chem 42:1004-13. 2007
    ..Last, the new N1-C7 annulated derivatives presented herein are substantially more potent than their respective N1-C2 annulated counterparts, previously reported...
  28. ncbi request reprint Neural adrenergic/cyclic AMP regulation of the immunoglobulin E receptor alpha-subunit expression in the mammalian pinealocyte: a neuroendocrine/immune response link?
    Surajit Ganguly
    Section on Neuroendocrinology, National Institute of Child Health and Human Development, National Institutes of Health, Bethesda, MD 20892, USA
    J Biol Chem 282:32758-64. 2007
    ..Pineal FcepsilonRIalpha and FcepsilonRIgamma may represent a previously unrealized molecular link between the neuroendocrine and immune systems...
  29. ncbi request reprint Design and synthesis of new N1 and C3-substituted 4-fluoroindolic melatoninergics
    Andrew Tsotinis
    Faculty of Pharmacy, Department of Pharmaceutical Chemistry, University of Athens, Panepistimioupoli Zografou, 15771 Athens, Greece
    Curr Drug Discov Technol 4:198-207. 2007
    ..Last, the new C-3 substituted 4-fluorotryptamides presented herein are substantially more potent than their respective N-OMe functionalized congeners, previously reported...
  30. ncbi request reprint Bicyclic melatonin receptor agonists containing a ring-junction nitrogen: Synthesis, biological evaluation, and molecular modeling of the putative bioactive conformation
    Jan Elsner
    Department of Medicinal Chemistry, Emil Fischer Center, Friedrich Alexander University, Schuhstrasse 19, D 91052 Erlangen, Germany
    Bioorg Med Chem 14:1949-58. 2006
    ....
  31. ncbi request reprint Design, synthesis and melatoninergic potency of new N-acyl 8,9-dihydro-4-methoxy-7H-2-benzo[de]quinolinalkanamines
    Andrew Tsotinis
    Faculty of Pharmacy, Department of Pharmaceutical Chemistry, University of Athens, Panepistimioupoli Zografou, 157 71 Athens, Greece
    Bioorg Chem 35:189-204. 2007
    ....