Synthesis and Biological Evaluation (in Vitro and in Vivo) of Cyclic Arginine-Glycine-Aspartate (RGD) Peptidomimetic-Paclitaxel Conjugates Targeting Integrin alphaVbeta3 (Articolo in rivista)

Type
Label
  • Synthesis and Biological Evaluation (in Vitro and in Vivo) of Cyclic Arginine-Glycine-Aspartate (RGD) Peptidomimetic-Paclitaxel Conjugates Targeting Integrin alphaVbeta3 (Articolo in rivista) (literal)
Anno
  • 2012-01-01T00:00:00+01:00 (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#doi
  • 10.1021/jm301058f (literal)
Alternative label
  • Raffaele Colombo, Michele Mingozzi, Laura Belvisi, Daniela Arosio, Umberto Piarulli, Nives Carenini, Paola Perego, Nadia Zaffaroni, Michelandrea De Cesare, Vittoria Castiglioni, Eugenio Scanziani, and Cesare Gennari (2012)
    Synthesis and Biological Evaluation (in Vitro and in Vivo) of Cyclic Arginine-Glycine-Aspartate (RGD) Peptidomimetic-Paclitaxel Conjugates Targeting Integrin alphaVbeta3
    in Journal of medicinal chemistry
    (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#autori
  • Raffaele Colombo, Michele Mingozzi, Laura Belvisi, Daniela Arosio, Umberto Piarulli, Nives Carenini, Paola Perego, Nadia Zaffaroni, Michelandrea De Cesare, Vittoria Castiglioni, Eugenio Scanziani, and Cesare Gennari (literal)
Pagina inizio
  • 10460 (literal)
Pagina fine
  • 10474 (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#numeroVolume
  • 55 (literal)
Rivista
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#numeroFascicolo
  • 23 (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#affiliazioni
  • Daniela Arosio: CNR - Istituto di Scienze e Tecnologie Molecolari (ISTM) Raffaele Colombo, Michele Mingozzi, Laura Belvisi, Cesare Gennari: Dipartimento di Chimica, Universita? degli Studi di Milano Umberto Piarulli: Dipartimento di Scienza e Alta Tecnologia, Universita? degli Studi dell'Insubria Nives Carenini, Paola Perego, Nadia Zaffaroni, Michelandrea De Cesare: Molecular Pharmacology Unit, Department of Experimental Oncology and Molecular Medicine, Fondazione IRCCS Istituto Nazionale Tumori Vittoria Castiglioni, Eugenio Scanziani: Dipartimento di Scienze Veterinarie e Sanita? Pubblica, Universita? degli Studi di Milano (literal)
Titolo
  • Synthesis and Biological Evaluation (in Vitro and in Vivo) of Cyclic Arginine-Glycine-Aspartate (RGD) Peptidomimetic-Paclitaxel Conjugates Targeting Integrin alphaVbeta3 (literal)
Abstract
  • A small library of integrin ligand-paclitaxel conjugates 10-13 was synthesized with the aim of using the tumor-homing cyclo[DKP-RGD] peptidomimetics for site-directed delivery of the cytotoxic drug. All the paclitaxel-RGD constructs 10-13 inhibited biotinylated vitronectin binding to the purified ?V?3 integrin receptor at low nanomolar concentration and showed in vitro cytotoxic activity against a panel of human tumor cell lines similar to that of paclitaxel. Among the cell lines, the cisplatin-resistant IGROV-1/Pt1 cells expressed high levels of integrin ?V?3, making them attractive to be tested in in vivo models. cyclo[DKP-f 3-RGD]-PTX 11 displayed sufficient stability in physiological solution and in both human and murine plasma to be a good candidate for in vivo testing. In tumor-targeting experiments against the IGROV-1/Pt1 human ovarian carcinoma xenotransplanted in nude mice, compound 11 exhibited a superior activity compared with paclitaxel, despite the lower (about half) molar dosage used. (literal)
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