Claudiu T Supuran

Summary

Affiliation: University of Florence
Country: Italy

Publications

  1. ncbi Hydroxyurea is a carbonic anhydrase inhibitor
    Andrea Scozzafava
    , Dipartimento di Chimica, Laboratorio di Chimica Bioinorganica, Via della Lastruccia 3, Rm. 188, I-50019 Sesto Fiorentino, Firenze, Italy
    Bioorg Med Chem 11:2241-6. 2003
  2. ncbi Structure-based drug discovery of carbonic anhydrase inhibitors
    Claudiu T Supuran
    Universita degli Studi di Firenze, Polo Scientifico, Laboratorio di Chimica Bioinorganica, Via della Lastruccia, Sesto Fiorentino, Florence, Italy
    J Enzyme Inhib Med Chem 27:759-72. 2012
  3. ncbi Amide derivatives of benzene-sulfonanilide, pharmaceutical composition thereof and method for cancer treatment using the same (US20120095092)
    Claudiu T Supuran
    Universita degli Studi di Firenze, Dipartimento di Scienze Farmaceutiche, Via Ugo Schiff 6, 50019 Sesto Fiorentino Florence, Italy
    Expert Opin Ther Pat 22:1251-5. 2012
  4. ncbi Sulfonamides: a patent review (2008 - 2012)
    Fabrizio Carta
    Universita degli Studi di Firenze, Laboratorio di Chimica Bioinorganica, Rm 188, Via della Lastruccia 3, I 50019 Sesto Fiorentino Florence, Italy
    Expert Opin Ther Pat 22:747-58. 2012
  5. ncbi Carbonic anhydrase inhibitors as emerging drugs for the treatment of obesity
    Claudiu T Supuran
    Universita degli Studi di Firenze, Polo Scientifico, Laboratorio di Chimica Bioinorganica, Rm 188, Via della Lastruccia 3, 50019 Sesto Fiorentino Florence, Italy 39 055 4573005 39 055 4573385
    Expert Opin Emerg Drugs 17:11-5. 2012
  6. ncbi Inhibition of V-ATPase and carbonic anhydrases as interference strategy with tumor acidification processes
    Mario Perez-Sayans
    Oral Medicine, Oral Surgery and Implantology Unit, Faculty of Medicine and Dentistry, Instituto de Investigación Sanitaria de Santiago IDIS, Santiago de Compostela, Spain
    Curr Pharm Des 18:1407-13. 2012
  7. ncbi Inhibition of bacterial carbonic anhydrases and zinc proteases: from orphan targets to innovative new antibiotic drugs
    C T Supuran
    Universita degli Studi di Firenze, Dipartimento di Chimica, Laboratorio di Chimica Inorganica e Bioinorganica, Via della Lastruccia 3, 50019 Sesto Fiorentino Firenze, Italy
    Curr Med Chem 19:831-44. 2012
  8. ncbi Modification of carbonic anhydrase II with acetaldehyde, the first metabolite of ethanol, leads to decreased enzyme activity
    Fatemeh Bootorabi
    Institute of Medical Technology, Tampere University Hospital, 33520 Tampere, Finland
    BMC Biochem 9:32. 2008
  9. ncbi Characterization of the first beta-class carbonic anhydrase from an arthropod (Drosophila melanogaster) and phylogenetic analysis of beta-class carbonic anhydrases in invertebrates
    Leo Syrjänen
    Institute of Medical Technology, University of Tampere and Tampere University Hospital, Finland
    BMC Biochem 11:28. 2010
  10. ncbi Carbonic anhydrase inhibition with natural products: novel chemotypes and inhibition mechanisms
    Claudiu T Supuran
    Laboratorio di Chimica Bioinorganica, Universita degli Studi di Firenze, Rm 188, Via della Lastruccia 3, 50019, Sesto Fiorentino, Florence, Italy
    Mol Divers 15:305-16. 2011

Detail Information

Publications123 found, 100 shown here

  1. ncbi Hydroxyurea is a carbonic anhydrase inhibitor
    Andrea Scozzafava
    , Dipartimento di Chimica, Laboratorio di Chimica Bioinorganica, Via della Lastruccia 3, Rm. 188, I-50019 Sesto Fiorentino, Firenze, Italy
    Bioorg Med Chem 11:2241-6. 2003
    ..Indeed, such inhibitors of the sulfonylated amino acid hydroxamate type have been generated, with potencies in the low nanomolar range for both type of enzymes, CAs and MMPs...
  2. ncbi Structure-based drug discovery of carbonic anhydrase inhibitors
    Claudiu T Supuran
    Universita degli Studi di Firenze, Polo Scientifico, Laboratorio di Chimica Bioinorganica, Via della Lastruccia, Sesto Fiorentino, Florence, Italy
    J Enzyme Inhib Med Chem 27:759-72. 2012
    ..Promising compounds that inhibit CAs from bacterial and fungal pathogens, of the DTC and carboxylate types, will be also reviewed...
  3. ncbi Amide derivatives of benzene-sulfonanilide, pharmaceutical composition thereof and method for cancer treatment using the same (US20120095092)
    Claudiu T Supuran
    Universita degli Studi di Firenze, Dipartimento di Scienze Farmaceutiche, Via Ugo Schiff 6, 50019 Sesto Fiorentino Florence, Italy
    Expert Opin Ther Pat 22:1251-5. 2012
    ..As these compounds incorporate a methanesulfonamide moiety it is not unexpected that they may also appreciably inhibit tumor-associated carbonic anhydrases (CAs), such as isoforms CA IX and XII...
  4. ncbi Sulfonamides: a patent review (2008 - 2012)
    Fabrizio Carta
    Universita degli Studi di Firenze, Laboratorio di Chimica Bioinorganica, Rm 188, Via della Lastruccia 3, I 50019 Sesto Fiorentino Florence, Italy
    Expert Opin Ther Pat 22:747-58. 2012
    ..This privileged structural motif is likely to be present in other drugs in the future...
  5. ncbi Carbonic anhydrase inhibitors as emerging drugs for the treatment of obesity
    Claudiu T Supuran
    Universita degli Studi di Firenze, Polo Scientifico, Laboratorio di Chimica Bioinorganica, Rm 188, Via della Lastruccia 3, 50019 Sesto Fiorentino Florence, Italy 39 055 4573005 39 055 4573385
    Expert Opin Emerg Drugs 17:11-5. 2012
    ..This Editorial discusses the biochemical and biological rationale for the use of CAIs in the management of obesity...
  6. ncbi Inhibition of V-ATPase and carbonic anhydrases as interference strategy with tumor acidification processes
    Mario Perez-Sayans
    Oral Medicine, Oral Surgery and Implantology Unit, Faculty of Medicine and Dentistry, Instituto de Investigación Sanitaria de Santiago IDIS, Santiago de Compostela, Spain
    Curr Pharm Des 18:1407-13. 2012
    ....
  7. ncbi Inhibition of bacterial carbonic anhydrases and zinc proteases: from orphan targets to innovative new antibiotic drugs
    C T Supuran
    Universita degli Studi di Firenze, Dipartimento di Chimica, Laboratorio di Chimica Inorganica e Bioinorganica, Via della Lastruccia 3, 50019 Sesto Fiorentino Firenze, Italy
    Curr Med Chem 19:831-44. 2012
    ....
  8. ncbi Modification of carbonic anhydrase II with acetaldehyde, the first metabolite of ethanol, leads to decreased enzyme activity
    Fatemeh Bootorabi
    Institute of Medical Technology, Tampere University Hospital, 33520 Tampere, Finland
    BMC Biochem 9:32. 2008
    ....
  9. ncbi Characterization of the first beta-class carbonic anhydrase from an arthropod (Drosophila melanogaster) and phylogenetic analysis of beta-class carbonic anhydrases in invertebrates
    Leo Syrjänen
    Institute of Medical Technology, University of Tampere and Tampere University Hospital, Finland
    BMC Biochem 11:28. 2010
    ..g., Drosophila melanogaster...
  10. ncbi Carbonic anhydrase inhibition with natural products: novel chemotypes and inhibition mechanisms
    Claudiu T Supuran
    Laboratorio di Chimica Bioinorganica, Universita degli Studi di Firenze, Rm 188, Via della Lastruccia 3, 50019, Sesto Fiorentino, Florence, Italy
    Mol Divers 15:305-16. 2011
    ..Possible applications for these new chemotypes in drug design of CA inhibitors are envisaged and discussed in detail in this review...
  11. ncbi Phosphodiesterase 5 inhibitors--drug design and differentiation based on selectivity, pharmacokinetic and efficacy profiles
    Claudiu T Supuran
    Universita degli Studi di Firenze, Dipartimento di Chimica, Laboratorio di Chimica Bioinorganica, Via della Lastruccia, 3, Rm 188, I 50019 Sesto Fiorentino Florence, Italy
    Curr Pharm Des 12:3459-65. 2006
    ..There are pharmacological interactions between these drugs and other medications metabolized by the cytochrome P450 (P3A4 isoform), such as the azole antifungals, erythromycin and the HIV protease inhibitors...
  12. ncbi Carbonic anhydrase inhibition/activation: trip of a scientist around the world in the search of novel chemotypes and drug targets
    Claudiu T Supuran
    Universita degli Studi di Firenze, Laboratorio di Chimica Bioinorganica, Via della Lastruccia 3, Sesto Fiorentino, Florence, Italy
    Curr Pharm Des 16:3233-45. 2010
    ..Possible applications for these new chemotypes are envisaged and discussed in detail, based on a chemo-geographical approach which took the author around the world and the chemical space...
  13. ncbi Antiviral sulfonamide derivatives
    Claudiu T Supuran
    Universita degli Studi di Firenze, Dipartimento di Chimica, Laboratorio di Chimica Bioinorganica, Via della Lastruccia, 3, Rm 188, I 50019 Sesto Fiorentino, Florence, Italy
    Mini Rev Med Chem 4:189-200. 2004
    ..Finally, some small molecule chemokine antagonists acting as HIV entry inhibitors also possess sulfonamide functionalities in their scaffold...
  14. ncbi COX-2 selective inhibitors, carbonic anhydrase inhibition and anticancer properties of sulfonamides belonging to this class of pharmacological agents
    Claudiu T Supuran
    Universita degli Studi di Firenze, Dipartimento di Chimica, Laboratorio di Chimica Bioinorganica, Via della Lastruccia, 3, Rm 188, I 50019 Sesto Fiorentino Florence, Italy
    Mini Rev Med Chem 4:625-32. 2004
    ....
  15. ncbi Designing of novel carbonic anhydrase inhibitors and activators
    Claudiu T Supuran
    Universita degli Studi di Firenze, Dipartimento di Chimica, Laboratorio di Chimica Bioinorganica, Via della Lastruccia, 3, Rm 188, 1 50019 Sesto Fiorentino Florence, Italy
    Curr Med Chem Cardiovasc Hematol Agents 2:49-68. 2004
    ..e., CA I, II, III and IV. The possible physiologic relevance of CA activation will also be addressed, together with the recent pharmacological applications of blood CA isozymes activators, as potential memory enhancing drugs...
  16. ncbi Carbonic anhydrase inhibitors
    Claudiu T Supuran
    Universita degli Studi di Firenze, Laboratorio di Chimica Bioinorganica, Sesto Fiorentino, Firenze, Italy
    Bioorg Med Chem Lett 20:3467-74. 2010
    ..This class of enzyme inhibitors shows promise for designing interesting pharmacological agents and understanding in detail protein-drug interactions at molecular level...
  17. ncbi Recent advances in structural studies of the carbonic anhydrase family: the crystal structure of human CA IX and CA XIII
    Claudiu T Supuran
    Universita degli Studi di Firenze, Laboratorio di Chimica Bioinorganica, Via della Lastruccia 3, Sesto Fiorentino, Florence, Italy
    Curr Pharm Des 16:3246-54. 2010
    ....
  18. ncbi Quantum theoretic QSAR of benzene derivatives: some enzyme inhibitors
    Claudiu T Supuran
    Universita degli Studi, Laboratorio di Chimica Inorganica e Bioinorganica, Via Gino Capponi 7, 1 50121, Florence, Italy
    J Enzyme Inhib Med Chem 19:237-48. 2004
    ..The resulting equations give better fits, better predictivity and are more easily interpretable than those resulting from traditional QSAR methods...
  19. ncbi Benzolamide is not a membrane-impermeant carbonic anhydrase inhibitor
    Claudiu T Supuran
    Universita degli Studi di Firenze, Polo Scientifico, Laboratorio di Chimica Bioinorganica, Rm 188, Via della Lastruccia 3, 50019 Sesto Fiorentino, Italy
    J Enzyme Inhib Med Chem 19:269-73. 2004
    ..Selective inhibition of membrane-associated CA isozymes is relevant indeed in many physiological studies and also pharmacologically, since the tumor-associated isozymes (CA IX and XII) are both membrane-bound...
  20. ncbi Therapeutic compounds: patent evaluation of WO2011011652A1
    Claudiu T Supuran
    University of Florence, Dipartimento di Chimica, Via della Lastruccia 3, Rm 188, 50019 Sesto Fiorentino, Florence, Italy
    Expert Opin Ther Pat 21:1491-5. 2011
    ....
  21. ncbi Diuretics: from classical carbonic anhydrase inhibitors to novel applications of the sulfonamides
    Claudiu T Supuran
    Universita degli Studi di Firenze, Laboratorio di Chimica Bioinorganica, Rm 188, Via della Lastruccia 3, I 50019 Sesto Fiorentino Firenze, Italy
    Curr Pharm Des 14:641-8. 2008
    ..Thus, these old drugs may be useful as leads for new applications...
  22. ncbi Carbonic anhydrase inhibitors
    Claudiu T Supuran
    Dipartimento di Chimica, University of Florence, Via della Lastruccia 3, Rm 188, Polo Scientifico, 50019 Sesto Fiorentino Firenze, Italy
    Med Res Rev 23:146-89. 2003
    ..Future prospects for drug design applications for inhibitors of these ubiquitous enzymes are also discussed...
  23. ncbi Indisulam: an anticancer sulfonamide in clinical development
    Claudiu T Supuran
    Universita degli Studi di Firenze, Dipartimento di Chimica, Laboratorio di Chimica Bioinorganica, Via della Lastruccia, 3, Rm 188, I 50019 Sesto Fiorentino, Florence, Italy
    Expert Opin Investig Drugs 12:283-7. 2003
    ..Four Phase I clinical trials gave promising results, showing the compound to possess nonlinear pharmacokinetics. Presently this compound is in Phase II trials in Europe and USA for the treatment of solid tumours...
  24. ncbi Carbonic anhydrases as targets for medicinal chemistry
    Claudiu T Supuran
    Universita degli Studi di Firenze, Laboratorio di Chimica Bioinorganica, Rm 188, Via della Lastruccia 3, I 50019 Sesto Fiorentino Firenze, Italy
    Bioorg Med Chem 15:4336-50. 2007
    ....
  25. ncbi Bacterial protease inhibitors
    Claudiu T Supuran
    University of Florence, Dipartimento di Chimica, Laboratorio di Chimica Inorganica e Bioinorganica, Firenze, Italy
    Med Res Rev 22:329-72. 2002
    ..This review presents the state of the art in the design of such enzyme inhibitors with potential therapeutic applications, as well as recent advances in the use of some of these proteases in therapy...
  26. ncbi Carbonic anhydrase inhibitors: the X-ray crystal structure of the adduct of N-hydroxysulfamide with isozyme II explains why this new zinc binding function is effective in the design of potent inhibitors
    Claudia Temperini
    Universita degli Studi di Firenze, Polo Scientifico, Laboratorio di Chimica Bioinorganica, Rm 188, Via della Lastruccia 3, 50019 Sesto Fiorentino Florence, Italy
    Bioorg Med Chem Lett 17:2795-801. 2007
    ....
  27. ncbi Carbonic anhydrases: novel therapeutic applications for inhibitors and activators
    Claudiu T Supuran
    Laboratorio di Chimica Bioinorganica, Universita degli Studi di Firenze, Rm 188, Via della Lastruccia 3, I 50019 Sesto Fiorentino, Firenze, Italy
    Nat Rev Drug Discov 7:168-81. 2008
    ....
  28. ncbi Dithiocarbamates: a new class of carbonic anhydrase inhibitors. Crystallographic and kinetic investigations
    Fabrizio Carta
    Universita degli Studi di Firenze, Laboratorio di Chimica Bioinorganica, Rm 188, Via della Lastruccia 3, I 50019 Sesto Fiorentino Firenze, Italy
    Chem Commun (Camb) 48:1868-70. 2012
    ..They coordinate to the zinc ion from the enzyme active site in monodentate manner and establish many favorable interactions with amino acid residues nearby. Several low nanomolar CA I, II and IX inhibitors were detected...
  29. ncbi Protease inhibitors of the sulfonamide type: anticancer, antiinflammatory, and antiviral agents
    Claudiu T Supuran
    Universita degli Studi di Firenze, Dipartimento di Chimica, Via della Lastruccia, 3, Rm 188, I 50019 Sesto Fiorentino Florence, Italy
    Med Res Rev 23:535-58. 2003
    ..Other viral proteases, such as those isolated from several types of herpes viruses may be inhibited by sulfonamide derivatives, leading thus to more effective classes of antiviral drugs...
  30. ncbi Carbonic anhydrases--an overview
    Claudiu T Supuran
    Universita degli Studi di Firenze, Laboratorio di Chimica Bioinorganica, Rm 188, Via della Lastruccia 3, I 50019 Sesto Fiorentino Firenze, Italy
    Curr Pharm Des 14:603-14. 2008
    ..The presence of these ubiquitous enzymes in so many tissues and in so different isoforms, represents an attractive goal for the design of inhibitors or activators with biomedical applications...
  31. ncbi Carbonic anhydrase inhibitors and activators for novel therapeutic applications
    Claudiu T Supuran
    Universita degli Studi di Firenze, Laboratorio di Chimica Bioinorganica, Room 188, Via della Lastruccia 3, I 50019 Sesto Fiorentino, Firenze, Italy
    Future Med Chem 3:1165-80. 2011
    ..Activation of some CAs may also have applications in therapy. Bacterial and fungal β-CA inhibitors or nematode α-CA inhibitors have been described that may lead to novel classes of anti-infectives...
  32. ncbi Carbonic anhydrases as drug targets--an overview
    Claudiu T Supuran
    Universita degli Studi di Firenze, Laboratorio di Chimica Bioinorganica, Sesto Fiorentino Firenze, Italy
    Curr Top Med Chem 7:825-33. 2007
    ....
  33. ncbi Carbonic anhydrase inhibitors: novel sulfonamides incorporating 1,3,5-triazine moieties as inhibitors of the cytosolic and tumour-associated carbonic anhydrase isozymes I, II and IX
    Vladimir Garaj
    , Polo Scientifico, Laboratorio di Chimica Bioinorganica, Rm. 188, Via della Lastruccia 3, 50019 Sesto Fiorentino (Florence, Italy
    Bioorg Med Chem Lett 15:3102-8. 2005
    ..33-32.00), thus constituting excellent leads for the development of novel approaches for the management of hypoxic tumours...
  34. ncbi Carbonic anhydrase inhibitors: design of spin-labeled sulfonamides incorporating TEMPO moieties as probes for cytosolic or transmembrane isozymes
    Alessandro Cecchi
    Universita degli Studi di Firenze, Laboratorio di Chimica Bioinorganica, Room 188, Via della Lastruccia 3, I 50019 Sesto Fiorentino, Firenze, Italy
    Bioorg Med Chem Lett 18:3475-80. 2008
    ....
  35. ncbi Carbonic anhydrase inhibitors: synthesis and inhibition of cytosolic/membrane-associated carbonic anhydrase isozymes I, II, and IX with sulfonamides incorporating hydrazino moieties
    Jean-Yves Winum
    Polo Scientifico, Laboratorio di Chimica Bioinorganica, , Room 188, Via della Lastruccia 3, 50019 Sesto Fiorentino (Florence, Italy
    J Med Chem 48:2121-5. 2005
    ..SAR is discussed for the diverse types of inhibitors and their affinity for different isozymes, with the aim of obtaining isozyme-specific CA IX inhibitors, with putative applications as antitumor drugs...
  36. ncbi Carbonic anhydrase inhibitors: synthesis and inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, and IX with bis-sulfamates
    Jean-Yves Winum
    , Polo Scientifico, Laboratorio di Chimica Bioinorganica, Rm. 188, Via della Lastruccia 3, 50019 Sesto Fiorentino (Florence, Italy
    Bioorg Med Chem Lett 15:579-84. 2005
    ....
  37. ncbi Carbonic anhydrase inhibitors: synthesis and topical intraocular pressure lowering effects of fluorine-containing inhibitors devoid of enhanced reactivity
    Xavier de Leval
    Natural and Synthetic Drug Research Center, Polo Scientifico, Laboratorio di Chimica Bioinorganica, Rm. 188, , Via della Lastruccia 3, 50019 Sesto Fiorentino, Florence, Italy
    J Med Chem 47:2796-804. 2004
    ..These compounds constitute valuable candidates for obtaining topically acting antiglaucoma CA inhibitors of a new generation, with enhanced efficacy, prolonged duration of action, and reduced side effects...
  38. ncbi Anion inhibition studies of the fastest carbonic anhydrase (CA) known, the extremo-CA from the bacterium Sulfurihydrogenibium azorense
    Daniela Vullo
    Universita degli Studi di Firenze, Polo Scientifico, Laboratorio di Chimica Bioinorganica, Rm 188, Via della Lastruccia 3, 50019 Sesto Fiorentino Florence, Italy
    Bioorg Med Chem Lett 22:7142-5. 2012
    ....
  39. ncbi Carbonic anhydrase inhibitors. Inhibition and homology modeling studies of the fungal beta-carbonic anhydrase from Candida albicans with sulfonamides
    Alessio Innocenti
    Universita degli Studi di Firenze, Polo Scientifico, Laboratorio di Chimica Bioinorganica, Sesto Fiorentino, Florence, Italy
    Bioorg Med Chem 17:4503-9. 2009
    ..Such compounds may be useful for the design of antifungal agents possessing a new mechanism of action...
  40. ncbi Carbonic anhydrase inhibitors: topically acting antiglaucoma sulfonamides incorporating esters and amides of 3- and 4-carboxybenzolamide
    Angela Casini
    Universita degli Studi, Laboratorio di Chimica Inorganica e Bioinorganica, Via della Lastruccia 3, Rm 188 50019 Sesto Fiorentino, Florence, Italy
    Bioorg Med Chem Lett 13:2867-73. 2003
    ..Efficacy of several of the new sulfonamides reported was better than that of the standard drugs dorzolamide and brinzolamide, whereas their duration of action was prolonged as compared to that of the clinically used drugs...
  41. ncbi Carbonic anhydrase inhibitors: E7070, a sulfonamide anticancer agent, potently inhibits cytosolic isozymes I and II, and transmembrane, tumor-associated isozyme IX
    Francesco Abbate
    , Polo Scientifico, Dipartimento di Chimica, Laboratorio di Chimica Bioinorganica, Via della Lastruccia 3, Rm. 188, I-50019 Sesto Fiorentino, Florence, Italy
    Bioorg Med Chem Lett 14:217-23. 2004
    ..A superimposition of these conformations with those of other sulfonamide/sulfamate CA inhibitors indicated that similar regions of the hCA II active site could be involved in the interaction with inhibitors...
  42. ncbi Carbonic anhydrase inhibitors. Inhibition of transmembrane isozymes XII (cancer-associated) and XIV with anions
    Alessio Innocenti
    Universita degli Studi di Firenze, Laboratorio di Chimica Bioinorganica, Via della Lastruccia 3, I 50019 Sesto Fiorentino Florence, Italy
    Bioorg Med Chem Lett 17:1532-7. 2007
    ..Chloride and bicarbonate showed K(I)s in the range of 0.75-0.77 mM for this isoform. The best hCA XIV anion inhibitors were sulfate, phenylarsonic, and phenylboronic acid (K(I) in the range of 10-92 microM)...
  43. ncbi Carbonic anhydrase inhibitors: synthesis and inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, and IX with sulfonamides incorporating 1,2,4-triazine moieties
    Vladimir Garaj
    , Polo Scientifico, Laboratorio di Chimica Bioinorganica, Rm. 188, Via della Lastruccia 3, 50019 Sesto Fiorentino (Florence, Italy
    Bioorg Med Chem Lett 14:5427-33. 2004
    ..Clear renal cell carcinoma, which is the most lethal urologic malignancy and is both characterized by very high CA IX expression and chemotherapy unresponsiveness, could be the leading candidate of such novel therapies...
  44. ncbi Carbonic anhydrase inhibitors. Inhibition of isozymes I, II, IV, V and IX with complex fluorides, chlorides and cyanides
    Alessio Innocenti
    Universita degli Studi di Firenze, Laboratorio di Chimica Bioinorganica, Rm 188, Via della Lastruccia 3, I 50019 Sesto Fiorentino Firenze, Italy
    Bioorg Med Chem Lett 15:1909-13. 2005
    ..The best hCA IX inhibitors were on the other hand cyanide, heptafluoroniobate and dicyanoargentate (K(I)s in the range of 4 microM-0.33 mM), whereas the worst ones were hexacyanoferrate(III) and hexacyanoferrate(II)...
  45. ncbi Carbonic anhydrase inhibitors: synthesis of water soluble sulfonamides incorporating a 4-sulfamoylphenylmethylthiourea scaffold, with potent intraocular pressure lowering properties
    Angela Casini
    , Polo Scientifico, Dipartimento di Chimica, Laboratorio di Chimica Bioinorganica, Via della Lastruccia, 3, Rm. 188, 1-50019 Sesto Fiorentino (Firenze, Italy
    J Enzyme Inhib Med Chem 17:333-43. 2002
    ..5-7.0. Furthermore, in normotensive rabbits, some of them showed an effective and prolonged intraocular pressure (IOP) lowering when administered topically, as 2% solutions...
  46. ncbi Carbonic anhydrase inhibitors with strong topical antiglaucoma properties incorporating a 4-(2-aminopyrimidin-4-yl-amino)-benzenesulfonamide scaffold
    Angela Casini
    , Polo Scientifico, Laboratorio di Chimica Bioinorganica, Italy
    J Enzyme Inhib Med Chem 17:9-18. 2002
    ..Furthermore, in normotensive and hypertensive rabbits, some of them showed an effective and prolonged intraocular pressure (IOP) lowering when administered topically, as 2% suspensions/solutions...
  47. ncbi Dithiocarbamates strongly inhibit carbonic anhydrases and show antiglaucoma action in vivo
    Fabrizio Carta
    Laboratorio di Chimica Bioinorganica, Polo Scientifico, Universita degli Studi di Firenze, Room 188, Via della Lastruccia 3, 50019 Sesto Fiorentino, Florence, Italy
    J Med Chem 55:1721-30. 2012
    ..Some dithiocarbamates showed an effective intraocular pressure lowering activity in an animal model of glucoma...
  48. ncbi Carbonic anhydrase inhibitors: SAR and X-ray crystallographic study for the interaction of sugar sulfamates/sulfamides with isozymes I, II and IV
    Angela Casini
    Dipartimento di Chimica, Laboratorio di Chimica Bioinorganica, , Rm. 188, Via della Lastruccia 3, I-50019 Sesto Fiorentino, Florence, Italy
    Bioorg Med Chem Lett 13:841-5. 2003
    ..Structural changes in this series of sugar derivatives led to compounds with diminished CA inhibitory properties as compared to topiramate...
  49. ncbi Carbonic anhydrase inhibitors. Interaction of the antiepileptic drug sulthiame with twelve mammalian isoforms: kinetic and X-ray crystallographic studies
    Claudia Temperini
    Universita degli Studi di Firenze, Polo Scientifico, Laboratorio di Chimica Bioinorganica, Rm 188, Via della Lastruccia 3, 50019 Sesto Fiorentino Florence, Italy
    Bioorg Med Chem Lett 17:4866-72. 2007
    ....
  50. ncbi Carbonic anhydrase inhibitors: Inhibition of the new membrane-associated isoform XV with phenols
    Alessio Innocenti
    Universita degli Studi di Firenze, Polo Scientifico, Laboratorio di Chimica Bioinorganica, Rm 188, Via della Lastruccia 3, 50019 Sesto Fiorentino Florence, Italy
    Bioorg Med Chem Lett 18:3593-6. 2008
    ..Phenols show a different inhibition mechanism as compared to sulfonamides and their isosteres, and may lead to the design of compounds with selectivity for inhibiting different CA isozymes with medicinal chemistry applications...
  51. ncbi Carbonic anhydrase inhibitors. Sulfonamide diuretics revisited--old leads for new applications?
    Claudia Temperini
    Universita degli Studi di Firenze, Laboratorio di Chimica Bioinorganica, Rm 188, Via della Lastruccia 3, I 50019 Sesto Fiorentino Firenze, Italy
    Org Biomol Chem 6:2499-506. 2008
    ..Indapamide binds to CA II in a manner not seen earlier for any other CA inhibitor, which might be important for the design of compounds with a different inhibition profile...
  52. ncbi Carbonic anhydrase inhibitors. Inhibition of isozymes I, II, IV, V, and IX with anions isosteric and isoelectronic with sulfate, nitrate, and carbonate
    Alessio Innocenti
    Universita degli Studi di Firenze, Laboratorio di Chimica Bioinorganica, Rm 188, Via della Lastruccia 3, I 50019 Sesto Fiorentino Firenze, Italy
    Bioorg Med Chem Lett 15:567-71. 2005
    ..Bromate and chlorate are quite weak CA IX inhibitors (K(I) s of 147-274 mM)...
  53. ncbi Dissecting the inhibition mechanism of cytosolic versus transmembrane carbonic anhydrases by ESR
    Laura Ciani
    Dipartimento di Chimica and CSGI, Universita degli Studi di Firenze, Via della Lastruccia 3, I 50019 Sesto Fiorentino, Firenze, Italy
    J Phys Chem B 113:13998-4005. 2009
    ..Combining the sulfonamide zinc-binding group with the TEMPO moiety thus allowed to dissect the selective inhibition mechanism of different cytosolic and transmembrane carbonic anhydrases...
  54. ncbi Carbonic anhydrase inhibitors: synthesis and inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, IX, and XII with N-hydroxysulfamides--a new zinc-binding function in the design of inhibitors
    Jean-Yves Winum
    , Polo Scientifico, Laboratorio di Chimica Bioinorganica, Rm. 188, Via della Lastruccia 3, 50019 Sesto Fiorentino, Florence, Italy
    Bioorg Med Chem Lett 15:2353-8. 2005
    ....
  55. ncbi Carbonic anhydrase inhibitors: synthesis and inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, and IX with sulfonamides derived from 4-isothiocyanato-benzolamide
    Alessandro Cecchi
    Universita degli Studi di Firenze, Polo Scientifico, Laboratorio di Chimica Bioinorganica, Rm 188, Via della Lastruccia 3, 50019 Sesto Fiorentino Florence, Italy
    Bioorg Med Chem Lett 14:5775-80. 2004
    ..6-62 nM against hCA I, 0.5-1.7 nM against hCA II and 3.2-23 nM against hCA IX, respectively. These derivatives are interesting candidates for the development of novel therapies targeting hypoxic tumors...
  56. ncbi Carbonic anhydrase activators: L-Adrenaline plugs the active site entrance of isozyme II, activating better isoforms I, IV, VA, VII, and XIV
    Claudia Temperini
    Universita degli Studi di Firenze, Laboratorio di Chimica Bioinorganica, Rm 188, Via della Lastruccia 3, I 50019 Sesto Fiorentino Firenze, Italy
    Bioorg Med Chem Lett 17:628-35. 2007
    ..The X-ray crystal structure of the CA II-L-adrenaline adduct revealed that the activator plugs the entrance of the active site cavity, obstructing it almost completely...
  57. ncbi Carbonic anhydrase activators: Activation of the beta-carbonic anhydrase from the pathogenic yeast Candida glabrata with amines and amino acids
    Alessio Innocenti
    Universita degli Studi di Firenze, Laboratorio di Chimica Bioinorganica, Rm 188, Via della Lastruccia 3, I 50019 Sesto Fiorentino Firenze, Italy
    Bioorg Med Chem Lett 20:1701-4. 2010
    ..1-16.7microM). The best activators were l-/d-Tyr, with activation constants of 7.1-9.5microM. This study may bring a better understanding of the catalytic/activation mechanisms of beta-CAs from pathogenic fungi...
  58. ncbi Carbonic anhydrase inhibitors. Design of fluorescent sulfonamides as probes of tumor-associated carbonic anhydrase IX that inhibit isozyme IX-mediated acidification of hypoxic tumors
    Alessandro Cecchi
    Polo Scientifico, Laboratorio di Chimica Bioinorganica, Rm. 188, , Via della Lastruccia 3, 50019 Sesto Fiorentino, Florence, Italy
    J Med Chem 48:4834-41. 2005
    ..These inhibitors represent promising candidates for developing anticancer therapies based on tumor-associated CA isozyme inhibition and offer interesting tools for imaging and further investigation of hypoxic tumors...
  59. ncbi Carbonic anhydrase activators: Activation of the human cytosolic isozyme III and membrane-associated isoform IV with amino acids and amines
    Daniela Vullo
    Universita degli Studi di Firenze, Laboratorio di Chimica Bioinorganica, Rm 188, Via della Lastruccia 3, I 50019 Sesto Fiorentino, Firenze, Italy
    Bioorg Med Chem Lett 18:4303-7. 2008
    ..The activation profiles of CA III and IV are distinct from those of all other mammalian CA isoforms investigated so far for their interaction with amino acids and amines...
  60. ncbi Carbonic anhydrase inhibitors. Inhibition of the membrane-bound human and bovine isozymes IV with sulfonamides
    Alessio Innocenti
    , Laboratorio di Chimica Bioinorganica, Rm. 188, Via della Lastruccia 3, I-50019 Sesto Fiorentino (Firenze, Italy
    Bioorg Med Chem Lett 15:1149-54. 2005
    ..The membrane-associated isozyme which probably is critical for aqueous humor secretion is hCA XII and not hCA IV...
  61. ncbi The proteoglycan region of the tumor-associated carbonic anhydrase isoform IX acts as anintrinsic buffer optimizing CO2 hydration at acidic pH values characteristic of solid tumors
    Alessio Innocenti
    Universita degli Studi di Firenze, Laboratorio di Chimica Bioinorganica, Rm 188, Via della, Lastruccia 3, I 50019, Sesto Fiorentino Firenze, Italy
    Bioorg Med Chem Lett 19:5825-8. 2009
    ..The proteoglycan domain of CA IX (present only in this transmembrane isoform) may thus act as an intrinsic buffer promoting efficient CO2 hydration at acidic pH values found in hypoxic tumors...
  62. ncbi Carbonic anhydrase activators: kinetic and X-ray crystallographic study for the interaction of D- and L-tryptophan with the mammalian isoforms I-XIV
    Claudia Temperini
    Universita degli Studi di Firenze, Laboratorio di Chimica Bioinorganica, Room 188, Via della Lastruccia 3, I 50019 Sesto Fiorentino Firenze, Italy
    Bioorg Med Chem 16:8373-8. 2008
    ..These findings explain the strong affinity of D-Trp for CA II and may be useful for designing novel classes of CA activators by using this compound as lead molecule...
  63. ncbi Carbonic anhydrase inhibitors. Inhibition of the transmembrane isozyme XII with sulfonamides-a new target for the design of antitumor and antiglaucoma drugs?
    Daniela Vullo
    Universita degli Studi di Firenze, Laboratorio di Chimica Bioinorganica, Rm 188, Via della Lastruccia 3, I 50019 Sesto Fiorentino Firenze, Italy
    Bioorg Med Chem Lett 15:963-9. 2005
    ..7-566.7. Apparently, hCA XII is a target of the antiglaucoma sulfonamides, and potent hCA XII inhibitors may be developed/used for the management of hypoxic tumors, together with inhibitors of the other tumor-associated isozyme, CA IX...
  64. ncbi Polyamines inhibit carbonic anhydrases by anchoring to the zinc-coordinated water molecule
    Fabrizio Carta
    Universita degli Studi di Firenze, Polo Scientifico, Laboratorio di Chimica Bioinorganica, Sesto Fiorentino Florence, Italy
    J Med Chem 53:5511-22. 2010
    ..Spermine binds differently compared to sulfonamides, phenols, or coumarins, rendering possible to develop CAIs with a diverse inhibition mechanism, profile, and selectivity for various isoforms...
  65. ncbi Carbonic anhydrase inhibitors. Synthesis and inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, and IX with boron-containing sulfonamides, sulfamides, and sulfamates: toward agents for boron neutron capture therapy of hypoxic tumo
    Jean-Yves Winum
    , Polo Scientifico, Laboratorio di Chimica Bioinorganica, Rm. 188, Via della Lastruccia 3, 50019 Sesto Fiorentino (Florence, Italy
    Bioorg Med Chem Lett 15:3302-6. 2005
    ....
  66. ncbi Carbonic anhydrase activators. Activation of the membrane-associated isoform XV with amino acids and amines
    Alessio Innocenti
    Universita degli Studi di Firenze, Laboratorio di Chimica Bioinorganica, Rm 188, Via della Lastruccia 3, I 50019 Sesto Fiorentino, Firenze, Italy
    Bioorg Med Chem Lett 19:3430-3. 2009
    ....
  67. ncbi Sulfonamides incorporating 1,3,5-triazine moieties selectively and potently inhibit carbonic anhydrase transmembrane isoforms IX, XII and XIV over cytosolic isoforms I and II: Solution and X-ray crystallographic studies
    Fabrizio Carta
    Universita degli Studi di Firenze, Polo Scientifico, Laboratorio di Chimica Bioinorganica, Florence, Italy
    Bioorg Med Chem 19:3105-19. 2011
    ..The 1,3,5-triazinyl-substituted benzenesulfonamides constitute thus a class of compounds with great potential for obtaining inhibitors targeting both α-class mammalian, tumor-associated, and β-class from pathogenic organisms CAs...
  68. ncbi Investigations of the esterase, phosphatase, and sulfatase activities of the cytosolic mammalian carbonic anhydrase isoforms I, II, and XIII with 4-nitrophenyl esters as substrates
    Alessio Innocenti
    Universita degli Studi di Firenze, Laboratorio di Chimica Bioinorganica, Rm 188, Via della Lastruccia 3, I 50019 Sesto Fiorentino, Firenze, Italy
    Bioorg Med Chem Lett 18:2267-71. 2008
    ..CA XIII was the most effective esterase and phosphatase. CA XIII might catalyze other physiological reactions than CO(2) hydration, based on its relevant phosphatase activity...
  69. ncbi Carbonic anhydrase inhibitors: inhibition of human cytosolic isozyme II and mitochondrial isozyme V with a series of benzene sulfonamide derivatives
    Alessio Innocenti
    Universita degli Studi di Firenze, Laboratorio di Chimica Bioinorganica, Rm 188, Via della Lastruccia 3, I 50019 Sesto Fiorentino, Florence, Italy
    Bioorg Med Chem Lett 14:5703-7. 2004
    ..39), whereas all other derivatives investigated here were much better hCA II inhibitors (selectivity ratios CA II/CA V in the range of 0.0008-0.73) than hCA V inhibitors...
  70. ncbi Carbonic anhydrase inhibitors: thioxolone versus sulfonamides for obtaining isozyme-selective inhibitors?
    Alessio Innocenti
    Universita degli Studi di Firenze, Polo Scientifico, Laboratorio di Chimica Bioinorganica, Room 188, Via della Lastruccia 3, 50019 Sesto Fiorentino Florence, Italy
    Bioorg Med Chem Lett 18:3938-41. 2008
    ..The sulfonamide zinc-binding group is thus superior to the thiol one for generating CA inhibitors with a varied and sometimes isozyme-selective inhibition profile against the mammalian enzymes...
  71. ncbi N-hydroxyurea--a versatile zinc binding function in the design of metalloenzyme inhibitors
    Claudia Temperini
    , Laboratorio di Chimica Bioinorganica, Sesto Fiorentino (Firenze, Italy
    Bioorg Med Chem Lett 16:4316-20. 2006
    ..This simple zinc binding function may be exploited for obtaining potent metalloenzyme inhibitors, due to its versatility of binding to the metal ion present in the active site of such enzymes...
  72. ncbi Carbonic anhydrase inhibitors. Interaction of the antitumor sulfamate EMD 486019 with twelve mammalian carbonic anhydrase isoforms: Kinetic and X-ray crystallographic studies
    Claudia Temperini
    Universita degli Studi di Firenze, Polo Scientifico, Laboratorio di Chimica Bioinorganica, Rm 188, Via della Lastruccia 3, 50019 Sesto Fiorentino, Florence, Italy
    Bioorg Med Chem Lett 18:4282-6. 2008
    ..CA II/IX potent inhibitors belonging to the sulfamate class are thus valuable clinical candidates with potential for development as antitumor agents with a multifactorial mechanism of action...
  73. ncbi Carbonic anhydrase inhibitors. Inhibition of mitochondrial isozyme V with aromatic and heterocyclic sulfonamides
    Daniela Vullo
    Laboratorio di Chimica Bioinorganica, Universita degli Studi di Firenze, Rm 188, Via della Lastruccia 3, I 50019 Sesto Fiorentino Firenze, Italy
    J Med Chem 47:1272-9. 2004
    ....
  74. ncbi Carbonic anhydrase inhibitors. Interaction of 2-N,N-dimethylamino-1,3,4-thiadiazole-5-methanesulfonamide with 12 mammalian isoforms: kinetic and X-ray crystallographic studies
    Claudia Temperini
    Universita degli Studi di Firenze, Polo Scientifico, Laboratorio di Chimica Bioinorganica, Rm 188, Via della Lastruccia 3, 50019 Sesto Fiorentino Florence, Italy
    Bioorg Med Chem Lett 18:999-1005. 2008
    ....
  75. ncbi Carbonic anhydrase inhibitors: X-ray crystallographic structure of the adduct of human isozyme II with a bis-sulfonamide-two heads are better than one?
    Angela Casini
    Universita degli Studi di Firenze, Polo Scientifico, Dipartimento di Chimica, Laboratorio di Chimica Bioinorganica, Via della Lastruccia, 3, Rm 188, I 50019 Firenze, Sesto Fiorentino, Italy
    Bioorg Med Chem Lett 13:2759-63. 2003
    ..All these findings are important for the design of better carboxamido CA inhibitors with applications in clinical medicine...
  76. ncbi Carbonic anhydrase activators: activation of the beta-carbonic anhydrases from the pathogenic fungi Candida albicans and Cryptococcus neoformans with amines and amino acids
    Alessio Innocenti
    Universita degli Studi di Firenze, Laboratorio di Chimica Bioinorganica, Rm 188, Via della Lastruccia 3, I 50019 Sesto Fiorentino Firenze, Italy
    Bioorg Med Chem 18:1034-7. 2010
    ..7-47.2 microM. The best Can2 activator was L-Trp. This study may help to better understand the catalytic/activation mechanisms of the beta-CAs and eventually to design CA activity modulators of such widespread enzymes in pathogenic fungi...
  77. ncbi Carbonic anhydrase activators: an activation study of the human mitochondrial isoforms VA and VB with amino acids and amines
    Daniela Vullo
    Universita degli Studi di Firenze, Laboratorio di Chimica Bioinorganica, Rm 188, Via della Lastruccia 3, I 50019 Sesto Fiorentino, Firenze, Italy
    Bioorg Med Chem Lett 17:1336-40. 2007
    ..The activation pattern of the two mitochondrial isoforms is very different from each other and as compared to those of the cytosolic isoforms hCA I and II...
  78. ncbi Carbonic anhydrase inhibitors: inhibition of the tumor-associated isozyme IX with aromatic and heterocyclic sulfonamides
    Daniela Vullo
    , Laboratorio di Chimica Bioinorganica, Rm. 188, Via della Lastruccia 3, I-50019 Sesto Fiorentino (Firenze, Italy
    Bioorg Med Chem Lett 13:1005-9. 2003
    ....
  79. ncbi Nonaromatic sulfonamide group as an ideal anchor for potent human carbonic anhydrase inhibitors: role of hydrogen-bonding networks in ligand binding and drug design
    Francesco Abbate
    Laboratorio di Chimica Inorganica e Bioinorganica, , Via Gino Capponi 7, I-50121, Florence, Italy
    J Med Chem 45:3583-7. 2002
    ..This study also explains why sulfate is a several-orders-of-magnitude weaker CA inhibitor compared to derivatives incorporating sulfonamide/sulfamide moieties...
  80. ncbi Carbonic anhydrase inhibitors: X-ray crystallographic structure of the adduct of human isozyme II with the perfluorobenzoyl analogue of methazolamide. Implications for the drug design of fluorinated inhibitors
    Francesco Abbate
    Universita degli Studi di Firenze, Polo Scientifico, Dipartimento di Chimica, Laboratorio di Chimica Bioinorganica, Via della Lastruccia, 3, Rm 188, 1 50019 Sesto Fiorentino, Firenze, Italy
    J Enzyme Inhib Med Chem 18:303-8. 2003
    ....
  81. ncbi Carbonic anhydrase inhibitors. Inhibition of cytosolic isozymes I and II and transmembrane, cancer-associated isozyme IX with lipophilic sulfonamides
    Marco Franchi
    , Dipartimento di Biologia Animale e Genetica, Via Romana 17-19, 50122 Firenze, Italy
    J Enzyme Inhib Med Chem 18:333-8. 2003
    ..This may lead to the development of novel anticancer therapies based on the selective inhibition of CA IX...
  82. ncbi Carbonic anhydrase activators. Activation of isoforms I, II, IV, VA, VII, and XIV with L- and D-phenylalanine and crystallographic analysis of their adducts with isozyme II: stereospecific recognition within the active site of an enzyme and its consequenc
    Claudia Temperini
    , Laboratorio di Chimica Bioinorganica, Rm. 188, Via della Lastruccia 3, I-50019 Sesto Fiorentino (Firenze, Italy
    J Med Chem 49:3019-27. 2006
    ..As the blood and brain concentrations of l-Phe are quite variable (30-73 microM), activity of some brain CAs may strongly be influenced by the level of activator(s) present in such tissues...
  83. ncbi Carbonic anhydrase inhibitors. A general approach for the preparation of water-soluble sulfonamides incorporating polyamino-polycarboxylate tails and of their metal complexes possessing long-lasting, topical intraocular pressure-lowering properties
    Andrea Scozzafava
    Laboratorio di Chimica Inorganica e Bioinorganica, , Via Gino Capponi 7, I-50121, Florence, Italy
    J Med Chem 45:1466-76. 2002
    ....
  84. ncbi Carbonic anhydrase inhibitors: inhibition of the human transmembrane isozyme XIV with a library of aromatic/heterocyclic sulfonamides
    Ozen Ozensoy
    , Polo Scientifico, Laboratorio di Chimica Bioinorganica, Rm. 188, Via della Lastruccia 3, 50019 Sesto Fiorentino (Florence, Italy
    Bioorg Med Chem 13:6089-93. 2005
    ..Thus, highly potent hCA XIV inhibitors were detected, but isozyme-specific inhibitors were not discovered for the moment...
  85. ncbi The β-carbonic anhydrases from Mycobacterium tuberculosis as drug targets
    Isao Nishimori
    Department of Gastroenterology, Kochi Medical School, Nankoku, Kochi, Japan
    Curr Pharm Des 16:3300-9. 2010
    ..tuberculosis...
  86. ncbi Carbonic anhydrase inhibitors: inhibition of the tumor-associated isozymes IX and XII with a library of aromatic and heteroaromatic sulfonamides
    Ozen Ozensoy
    , Polo Scientifico, Laboratorio di Chimica Bioinorganica, Room 188, Via della Lastruccia 3, 50019 Sesto Fiorentino (Florence, Italy
    Bioorg Med Chem Lett 15:4862-6. 2005
    ....
  87. ncbi Carbonic anhydrase inhibitors: the very weak inhibitors dithiothreitol, beta-mercaptoethanol, tris(carboxyethyl)phosphine and threitol interfere with the binding of sulfonamides to isozymes II and IX
    Alessio Innocenti
    Universita degli Studi di Firenze, Laboratorio di Chimica Bioinorganica, Room 188, Via della Lastruccia 3, I 50019 Sesto Fiorentino Firenze, Italy
    Bioorg Med Chem Lett 18:1898-903. 2008
    ....
  88. ncbi Protease inhibitors: synthesis of bacterial collagenase and matrix metalloproteinase inhibitors incorporating arylsulfonylureido and 5-dibenzo-suberenyl/suberyl moieties
    Monica Ilies
    , Laboratorio di Chimica Inorganica e Bioinorganica, Via della Lastruccia 3, Rm 188, Polo Scientifico, 50019-Sesto Fiorentino, Firenze, Italy
    Bioorg Med Chem 11:2227-39. 2003
    ..Several of these inhibitors also showed selectivity for the deep pocket enzymes (MMP-2, MMP-8 and MMP-9) over the shallow pocket ones MMP-1 and ChC...
  89. ncbi Anticancer and antiviral sulfonamides
    Andrea Scozzafava
    , Dipartimento di Chimica, Laboratorio di Chimica Bioinorganica, Via della Lastruccia, 3, Rm. 188, I-50019 Sesto Fiorentino, Florence, Italy
    Curr Med Chem 10:925-53. 2003
    ..Some small molecule chemokine antagonists acting as HIV entry inhibitors also possess sulfonamide functionalities in their scaffold...
  90. ncbi Crystal structure of a zinc-activated variant of human carbonic anhydrase I, CA I Michigan 1: evidence for a second zinc binding site involving arginine coordination
    Marta Ferraroni
    Dipartimento di Chimica, Laboratorio di Chimica Bioinorganica, Universita degli Studi di Firenze, Via della Lastruccia, 5, I 50019 Sesto Fiorentino, Italy
    Biochemistry 41:6237-44. 2002
    ..This is, to our knowledge, the first example of a zinc ion coordinating with an arginine residue in a Zn(II) enzyme...
  91. ncbi Carbonic anhydrase inhibitors. Inhibition of mammalian isoforms I-XIV with a series of natural product polyphenols and phenolic acids
    Alessio Innocenti
    Universita degli Studi di Firenze, Polo Scientifico, Laboratorio di Chimica Bioinorganica, 50019 Sesto Fiorentino Florence, Italy
    Bioorg Med Chem 18:2159-64. 2010
    ..As this is the region with the highest variability between the many CA isozymes found in mammals, this class of compounds may lead to isoform-selective inhibitors targeting just one or few of the medicinally relevant CAs...
  92. ncbi Carbonic anhydrase activation and the drug design
    Claudia Temperini
    Universita degli Studi di Firenze, Laboratorio di Chimica Bioinorganica, Rm 188, Via della Lastruccia 3, I 50019 Sesto Fiorentino Firenze, Italy
    Curr Pharm Des 14:708-15. 2008
    ..The physiological relevance of CA activation and the possible application of CAAs in Alzheimer's disease and for other memory therapies are also treated...
  93. ncbi Inhibitors of HIV-1 protease: current state of the art 10 years after their introduction. From antiretroviral drugs to antifungal, antibacterial and antitumor agents based on aspartic protease inhibitors
    Antonio Mastrolorenzo
    Universita degli Studi di Firenze, Dipartimento di Chimica, Laboratorio di Chimica Bioinorganica, I 50019 Sesto Fiorentino, Florence, Italy
    Curr Med Chem 14:2734-48. 2007
    ....
  94. ncbi Coumarins incorporating hydroxy- and chloro-moieties selectively inhibit the transmembrane, tumor-associated carbonic anhydrase isoforms IX and XII over the cytosolic ones I and II
    Alfonso Maresca
    Universita degli Studi di Firenze, Laboratorio di Chimica Bioinorganica, Sesto Fiorentino Firenze, Italy
    Bioorg Med Chem Lett 20:4511-4. 2010
    ..683 microM against CA XII, being thus a selective, efficient inhibitor for the tumor-associated over cytosolic isoforms. These compounds are also excellent leads for designing isoform-selective enzyme inhibitors...
  95. ncbi Carbonic anhydrase inhibitors. Comparison of chlorthalidone, indapamide, trichloromethiazide, and furosemide X-ray crystal structures in adducts with isozyme II, when several water molecules make the difference
    Claudia Temperini
    Universita degli Studi di Firenze, Laboratorio di Chimica Bioinorganica, Rm 188, Via della Lastruccia 3, I 50019 Sesto Fiorentino Firenze, Italy
    Bioorg Med Chem 17:1214-21. 2009
    ..The newly evidenced binding modes of these diuretics may be exploited for designing better CA II inhibitors as well as compounds with selectivity/affinity for various isoforms with medicinal chemistry applications...
  96. ncbi Hypoxia activates the capacity of tumor-associated carbonic anhydrase IX to acidify extracellular pH
    Eliska Svastova
    Centre of Molecular Medicine, Institute of Virology, Slovak Academy of Sciences, Dubravska cesta 9, 845 05 Bratislava, Slovak Republic
    FEBS Lett 577:439-45. 2004
    ..Our findings suggest that hypoxia regulates both expression and activity of CA IX in order to enhance the extracellular acidification, which may have important implications for tumor progression...
  97. ncbi Biochemical characterization of CA IX, one of the most active carbonic anhydrase isozymes
    Mika Hilvo
    Institute of Medical Technology, University of Tampere and Tampere University Hospital, FI 33014 Tampere, Finland
    J Biol Chem 283:27799-809. 2008
    ..This study provides novel information on the biochemical properties of CA IX and may help characterize the various cellular and pathophysiological processes in which this unique enzyme is involved...
  98. ncbi Carbonic anhydrase inhibitors. Inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, IX, and XII with Schiff's bases incorporating chromone and aromatic sulfonamide moieties, and their zinc complexes
    Luca Puccetti
    Ospedale San Lazzaro, Divisione di Urologia, Via Pierino Belli 26, 12051 Alba, Cuneo, Italy
    Bioorg Med Chem Lett 15:3096-101. 2005
    ..Some of these compounds may show applications for the development of therapies targeting hypoxic tumors in which CA IX and XII are often highly overexpressed...
  99. ncbi Sulfamates and their therapeutic potential
    Jean Yves Winum
    Laboratoire de Chimie Biomoleculaire, Universite Montpellier II, UMR 5032, Ecole Nationale Superieure de Chimie de Montpellier, 8 rue de l Ecole Normale, 34296 Montpellier Cedex, France
    Med Res Rev 25:186-228. 2005
    ....
  100. ncbi Carbonic anhydrase inhibitors. Design of selective, membrane-impermeant inhibitors targeting the human tumor-associated isozyme IX
    Joseph R Casey
    Canadian Institutes of Health Research, Membrane Protein Research Group, Department of Physiology, University of Alberta, Edmonton, Alberta, Canada T6G 2H7
    J Med Chem 47:2337-47. 2004
    ..Furthermore, we prove here for the first time that the CA-AE metabolon can be inhibited by the same type of sulfonamide derivative...
  101. ncbi Carbonic anhydrase inhibitors: inhibition of transmembrane, tumor-associated isozyme IX, and cytosolic isozymes I and II with aliphatic sulfamates
    Jean-Yves Winum
    , UMR 5032, , , 8 rue de l'Ecole Normale, 34296 Montpellier Cedex, France
    J Med Chem 46:5471-7. 2003
    ..23-0.51). These data are critical for the design of novel antitumor therapies, mainly for hypoxic tumors that overexpress CA IX, which are nonresponsive to radiation or chemotherapy...