http://www.cnr.it/ontology/cnr/individuo/prodotto/ID38430
Emerging Protein Targets for Anticancer Metallodrugs: Inhibition of Thioredoxin Reductase and Cathepsin B by Antitumor Ruthenium (II)-Arene Compounds. (Articolo in rivista)
- Type
- Label
- Emerging Protein Targets for Anticancer Metallodrugs: Inhibition of Thioredoxin Reductase and Cathepsin B by Antitumor Ruthenium (II)-Arene Compounds. (Articolo in rivista) (literal)
- Anno
- 2008-01-01T00:00:00+01:00 (literal)
- Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#doi
- 10.1021/jm8006678 (literal)
- Alternative label
Casini A, Gabbiani C, Sorrentino F, Rigobello M.P., Bindoli A, Geldbach TJ, Marrone A, Re N, Hartinger CG , Dyson PJ, Messori L. (2008)
Emerging Protein Targets for Anticancer Metallodrugs: Inhibition of Thioredoxin Reductase and Cathepsin B by Antitumor Ruthenium (II)-Arene Compounds.
in Journal of medicinal chemistry
(literal)
- Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#autori
- Casini A, Gabbiani C, Sorrentino F, Rigobello M.P., Bindoli A, Geldbach TJ, Marrone A, Re N, Hartinger CG , Dyson PJ, Messori L. (literal)
- Pagina inizio
- Pagina fine
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- Rivista
- Note
- ISI Web of Science (WOS) (literal)
- Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#affiliazioni
- Department of Chemistry, UniVersity of Florence, Via della Lastruccia 3, 50019 Sesto Fiorentino, Firenze, Italy, Department of Biological
Chemistry, UniVersity of PadoVa, Viale G. Colombo 3, 35121 PadoVa, Italy, Institute of Neurosciences (CNR), Section of PadoVa, Viale G.
Colombo 3, 35121 PadoVa, Italy, Institut des Sciences et Inge´nierie Chimiques, Ecole Polytechnique Fe´de´rale de Lausanne (EPFL), CH-1015
Lausanne, Switzerland, and Dipartimento di Scienze del Farmaco, UniVersity G. d'Annunzio, Via dei Vestini 31, 66100 Chieti, Italy (literal)
- Titolo
- Emerging Protein Targets for Anticancer Metallodrugs: Inhibition of Thioredoxin Reductase and Cathepsin B by Antitumor Ruthenium (II)-Arene Compounds. (literal)
- Abstract
- A series of ruthenium(II)-arene (RAPTA) compounds were evaluated for their ability to inhibit thioredoxin
reductase (either cytosolic or mitochondrial) and cathepsin B, two possible targets for anticancer metallodrugs.
In general, inhibition of the thioredoxin reductases was lower than that of cathepsin B, although selected
compounds were excellent inhibitors of both classes of enzymes in comparison to other metal-based drugs.
Some initial structure-activity relationships could be established. On the basis of the obtained data, different
mechanisms of binding/inhibition appear to be operative; remarkably the selectivity of the ruthenium
compounds toward solid metastatic tumors also correlates to the observed trends. Notably, docking studies
of the interactions of representative RAPTA compounds with cathepsin B were performed that provided
realistic structures for the resulting protein-metallodrug adducts. Good agreement was generally found
between the inhibiting potency of the RAPTA compounds and the computed stability of the corresponding
cat B/RAPTA adducts. (literal)
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- Autore CNR
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