Gianfranco Balboni

Summary

Affiliation: University of Cagliari
Country: Italy

Publications

  1. ncbi request reprint Evaluation of the Dmt-Tic pharmacophore: conversion of a potent delta-opioid receptor antagonist into a potent delta agonist and ligands with mixed properties
    Gianfranco Balboni
    Department of Toxicology, University of Cagliary, I09126 Cagliary, Italy
    J Med Chem 45:713-20. 2002
  2. ncbi request reprint Crystal structures of dipeptides containing the Dmt-Tic pharmacophore
    Sharon D Bryant
    Peptide Neurochemistry, LCBRA, National Institute of Environmental Health Sciences, P O Box 12233, Mail Drop C3 04, Research Triangle Park, North Carolina 27709, USA
    J Med Chem 45:5506-13. 2002
  3. doi request reprint Flavones and structurally related 4-chromenones inhibit carbonic anhydrases by a different mechanism of action compared to coumarins
    Gianfranco Balboni
    Dipartimento di Scienze della Vita e dell Ambiente, Universita degli Studi di Cagliari, Via Ospedale 72, I 09124 Cagliari, Italy
    Bioorg Med Chem Lett 22:3063-6. 2012
  4. pmc Further studies on lead compounds containing the opioid pharmacophore Dmt-Tic
    Gianfranco Balboni
    Department of Toxicology, University of Cagliari, I 09124 Cagliari, Italy
    J Med Chem 51:5109-17. 2008
  5. doi request reprint Triazine compounds as antagonists at Bv8-prokineticin receptors
    Gianfranco Balboni
    Department of Pharmaceutical Sciences, University of Ferrara, I 44100 Ferrara, Italy
    J Med Chem 51:7635-9. 2008
  6. doi request reprint Influence of the side chain next to C-terminal benzimidazole in opioid pseudopeptides containing the Dmt-Tic pharmacophore
    Gianfranco Balboni
    Department of Toxicology, University of Cagliari, Cagliari, Italy
    J Med Chem 52:5556-9. 2009
  7. ncbi request reprint From the potent and selective mu opioid receptor agonist H-Dmt-d-Arg-Phe-Lys-NH(2) to the potent delta antagonist H-Dmt-Tic-Phe-Lys(Z)-OH
    Gianfranco Balboni
    Department of Toxicology, University of Cagliari, I 09124, Cagliari, Italy
    J Med Chem 48:5608-11. 2005
  8. pmc Further studies on the effect of lysine at the C-terminus of the Dmt-Tic opioid pharmacophore
    Gianfranco Balboni
    Department of Toxicology, University of Cagliari, I 09124 Cagliari, Italy
    Bioorg Med Chem 15:3143-51. 2007
  9. pmc Opioid bifunctional ligands from morphine and the opioid pharmacophore Dmt-Tic
    Gianfranco Balboni
    Department of Toxicology, University of Cagliari, Via Ospedale 72, I 09124 Cagliari, Italy
    Eur J Med Chem 46:799-803. 2011
  10. pmc Effect of lysine at C-terminus of the Dmt-Tic opioid pharmacophore
    Gianfranco Balboni
    Department of Toxicology, University of Cagliari, I 09124, Cagliari, Italy
    J Med Chem 49:5610-7. 2006

Collaborators

Detail Information

Publications25

  1. ncbi request reprint Evaluation of the Dmt-Tic pharmacophore: conversion of a potent delta-opioid receptor antagonist into a potent delta agonist and ligands with mixed properties
    Gianfranco Balboni
    Department of Toxicology, University of Cagliary, I09126 Cagliary, Italy
    J Med Chem 45:713-20. 2002
    ....
  2. ncbi request reprint Crystal structures of dipeptides containing the Dmt-Tic pharmacophore
    Sharon D Bryant
    Peptide Neurochemistry, LCBRA, National Institute of Environmental Health Sciences, P O Box 12233, Mail Drop C3 04, Research Triangle Park, North Carolina 27709, USA
    J Med Chem 45:5506-13. 2002
    ..Furthermore, the structural results support the hypothesis that expanded dimensions between aromatic nuclei is important for acquiring mu-agonism...
  3. doi request reprint Flavones and structurally related 4-chromenones inhibit carbonic anhydrases by a different mechanism of action compared to coumarins
    Gianfranco Balboni
    Dipartimento di Scienze della Vita e dell Ambiente, Universita degli Studi di Cagliari, Via Ospedale 72, I 09124 Cagliari, Italy
    Bioorg Med Chem Lett 22:3063-6. 2012
    ..These derivatives inhibited these CAs in the submicromolar-low micromolar range. Flavones, although not as active as the coumarins, may be considered as interesting leads for the design of non-sulfonamide CA inhibitors...
  4. pmc Further studies on lead compounds containing the opioid pharmacophore Dmt-Tic
    Gianfranco Balboni
    Department of Toxicology, University of Cagliari, I 09124 Cagliari, Italy
    J Med Chem 51:5109-17. 2008
    ..4 and 10 had opposite behaviours in mice; 4 caused agitation, 10 gave sedation and convulsions...
  5. doi request reprint Triazine compounds as antagonists at Bv8-prokineticin receptors
    Gianfranco Balboni
    Department of Pharmaceutical Sciences, University of Ferrara, I 44100 Ferrara, Italy
    J Med Chem 51:7635-9. 2008
    ..New compounds were assessed for PKR1 and PKR2 affinity. Antagonist properties were evaluated as inhibition of 1 nM Bv8-induced intracellular Ca2+ mobilization...
  6. doi request reprint Influence of the side chain next to C-terminal benzimidazole in opioid pseudopeptides containing the Dmt-Tic pharmacophore
    Gianfranco Balboni
    Department of Toxicology, University of Cagliari, Cagliari, Italy
    J Med Chem 52:5556-9. 2009
    ..Interesting results were obtained: (1) only Gly, Ala, and Asp resulted in delta agonism, (2) Phe yielded delta antagonism, (3) and all other residues except Glu (devoid of any activity) gave mu agonism...
  7. ncbi request reprint From the potent and selective mu opioid receptor agonist H-Dmt-d-Arg-Phe-Lys-NH(2) to the potent delta antagonist H-Dmt-Tic-Phe-Lys(Z)-OH
    Gianfranco Balboni
    Department of Toxicology, University of Cagliari, I 09124, Cagliari, Italy
    J Med Chem 48:5608-11. 2005
    ..Such a delta antagonist could be used as a pharmacological tool...
  8. pmc Further studies on the effect of lysine at the C-terminus of the Dmt-Tic opioid pharmacophore
    Gianfranco Balboni
    Department of Toxicology, University of Cagliari, I 09124 Cagliari, Italy
    Bioorg Med Chem 15:3143-51. 2007
    ....
  9. pmc Opioid bifunctional ligands from morphine and the opioid pharmacophore Dmt-Tic
    Gianfranco Balboni
    Department of Toxicology, University of Cagliari, Via Ospedale 72, I 09124 Cagliari, Italy
    Eur J Med Chem 46:799-803. 2011
    ..Partial κ agonism is evidenced only for compound 4. Finally, both compounds showed potent δ antagonism...
  10. pmc Effect of lysine at C-terminus of the Dmt-Tic opioid pharmacophore
    Gianfranco Balboni
    Department of Toxicology, University of Cagliari, I 09124, Cagliari, Italy
    J Med Chem 49:5610-7. 2006
    ..0)]. The presence of a Lys linker provides new lead compounds in the formation of opioid peptidomimetics containing the Dmt-Tic pharmacophore with distinct agonist and/or antagonist properties...
  11. ncbi request reprint Direct influence of C-terminally substituted amino acids in the Dmt-Tic pharmacophore on delta-opioid receptor selectivity and antagonism
    Gianfranco Balboni
    Department of Toxicology, University of Cagliary, I 09126 Cagliary, Italy
    J Med Chem 47:4066-71. 2004
    ....
  12. ncbi request reprint Potent delta-opioid receptor agonists containing the Dmt-Tic pharmacophore
    Gianfranco Balboni
    Department of Toxicology, University of Cagliari, I 09126 Cagliari, Italy
    J Med Chem 45:5556-63. 2002
    ....
  13. ncbi request reprint Highly selective fluorescent analogue of the potent delta-opioid receptor antagonist Dmt-Tic
    Gianfranco Balboni
    Department of Toxicology, University of Cagliary, I 09126, Cagliary, Italy
    J Med Chem 47:6541-6. 2004
    ..This probe should prove useful in the study of the distribution of delta-opioid receptors in tissues and the internalization of opioid peptides during signal transduction...
  14. ncbi request reprint Anxiolytic- and antidepressant-like activities of H-Dmt-Tic-NH-CH(CH2-COOH)-Bid (UFP-512), a novel selective delta opioid receptor agonist
    Raffaella Vergura
    Department of Experimental and Clinical Medicine, Section of Pharmacology, and National Institute of Neuroscience, University of Ferrara, via Fossato di Mortara 19, 44100 Ferrara, Italy
    Peptides 29:93-103. 2008
    ....
  15. pmc A new opioid designed multiple ligand derived from the micro opioid agonist endomorphin-2 and the delta opioid antagonist pharmacophore Dmt-Tic
    Severo Salvadori
    Department of Pharmaceutical Science and Biotechnology Center, University of Ferrara, I 44100 Ferrara, Italy
    Bioorg Med Chem 15:6876-81. 2007
    ..As predicted, the resulting bivalent ligand showed a micro agonist/delta antagonist profile deriving from the corresponding activities of each pharmacophore...
  16. ncbi request reprint Synthesis and opioid activity of N,N-dimethyl-Dmt-Tic-NH-CH(R)-R' analogues: acquisition of potent delta antagonism
    Gianfranco Balboni
    Department of Toxicology, University of Cagliary, I 09126, Cagliary, Italy
    Bioorg Med Chem 11:5435-41. 2003
    ..With the exception of compound 1', the change in the hydrophobic environment at the N-terminus and formation of a tertiary amine by N,N-dimethylation in analogues of the Dmt-Tic pharmacophore produced potent delta-selective antagonists...
  17. pmc Conversion of the potent delta-opioid agonist H-Dmt-Tic-NH-CH(2)-bid into delta-opioid antagonists by N(1)-benzimidazole alkylation(1)
    Gianfranco Balboni
    Department of Toxicology, University of Cagliari, I 09124, Cagliari, Italy
    J Med Chem 48:8112-4. 2005
    ..44-1.42 nM). Only delta antagonism (pA(2)=8.52-10.14) was observed; micro agonism (IC(50)=30-450 nM) was not correlated with changes in alkylating agent or delta antagonism, and some compounds yielded mixed delta antagonism/micro agonism...
  18. pmc Role of benzimidazole (Bid) in the delta-opioid agonist pseudopeptide H-Dmt-Tic-NH-CH(2)-Bid (UFP-502)
    Severo Salvadori
    Department of Pharmaceutical Sciences and Biotechnology Center, University of Ferrara, I 44100 Ferrara, Italy
    Bioorg Med Chem 16:3032-8. 2008
    ..Phenyl ring of benzimidazole is not important for delta-agonism; in fact 1H-imidazole-2-yl retains delta-agonist activity...
  19. pmc Role of 2',6'-dimethyl-l-tyrosine (Dmt) in some opioid lead compounds
    Gianfranco Balboni
    Department of Toxicology, University of Cagliari, I 09124 Cagliari, Italy
    Bioorg Med Chem 18:6024-30. 2010
    ..Antagonists containing the Dmt-Tic pharmacophore do not support the exchange of Dmt with Dft or Tyr...
  20. ncbi request reprint Dmt-Tic-NH-CH2-Bid (UFP-502), a potent DOP receptor agonist: in vitro and in vivo studies
    Raffaella Vergura
    Department of Experimental and Clinical Medicine, Section of Pharmacology, and Neuroscience Centre, University of Ferrara, via Fossato di Mortara 19, 44100 Ferrara, Italy
    Peptides 27:3322-30. 2006
    ..In conclusion, UFP-502 represents a novel and useful chemical template for the design of selective agonists for the DOP receptor...
  21. pmc Synthesis of a potent and selective (18)F-labeled delta-opioid receptor antagonist derived from the Dmt-Tic pharmacophore for positron emission tomography imaging
    Eun Kyoung Ryu
    Molecular Imaging Program at Stanford, Department of Radiology and Bio X Program, Stanford University School of Medicine, Stanford, CA 94305, USA
    J Med Chem 51:1817-23. 2008
    ..Noninvasive microPET imaging studies revealed the absence of [(18)F]- 1 in rat brain, since it fails to cross the blood-brain barrier. This study demonstrates the suitability of [ (18)F]- 1 for imaging peripheral delta-opioid receptors...
  22. pmc New 2',6'-dimethyl-L-tyrosine (Dmt) opioid peptidomimetics based on the Aba-Gly scaffold. Development of unique mu-opioid receptor ligands
    Steven Ballet
    Department of Organic Chemistry, Vrije Universiteit Brussels, Pleinlaan 2, B 1050 Brussels, Belgium
    J Med Chem 49:3990-3. 2006
    ..48, and 19.9 nM, respectively), selectivity, and bioactivity to micro-opioid receptors. These compounds represent templates for a new class of lead opioid agonists that are easily synthesized and suitable for therapeutic pain relief...
  23. pmc 6-N,N-dimethylamino-2,3-naphthalimide: a new environment-sensitive fluorescent probe in delta- and mu-selective opioid peptides
    M Eugenio Vazquez
    Departamento de Química Orgánica y Unidad Asociada al CSIC, Universidad de Santiago de Compostela, 15782 Santiago de Compostela, Spain
    J Med Chem 49:3653-8. 2006
    ....
  24. pmc Peptidic delta opioid receptor agonists produce antidepressant-like effects in the forced swim test and regulate BDNF mRNA expression in rats
    Mary M Torregrossa
    Neuroscience Program, University of Michigan, Ann Arbor, MI 48109, USA
    Brain Res 1069:172-81. 2006
    ....
  25. pmc New opioid designed multiple ligand from Dmt-Tic and morphinan pharmacophores
    John L Neumeyer
    Alcohol and Drug Abuse Research Center, McLean Hospital, Harvard Medical School, 115 Mill Street, Belmont, Massachusetts 02478, USA
    J Med Chem 49:5640-3. 2006
    ..MCL 450 represents a useful starting point for the synthesis of other multiple opioid ligands endowed with analgesic properties with low tolerance and dependence...