Design, Synthesis, and Biological Evaluation of Novel cRGD- Paclitaxel Conjugates for Integrin-Assisted Drug Delivery (Articolo in rivista)

Type
Label
  • Design, Synthesis, and Biological Evaluation of Novel cRGD- Paclitaxel Conjugates for Integrin-Assisted Drug Delivery (Articolo in rivista) (literal)
Anno
  • 2012-01-01T00:00:00+01:00 (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#doi
  • 10.1021/bc300164t (literal)
Alternative label
  • Michael Pilkington-Miksa; Daniela Arosio; Lucia Battistini; Laura Belvisi; Marilenia De Matteo; Francesca Vasile; Paola Burreddu; Paola Carta; Gloria Rassu; Paola Perego; Nives Carenini; Franco Zunino; Michelandrea De Cesare; Vittoria Castiglioni; Eugenio Scanziani; Carlo Scolastico; Giovanni Casiraghi; Franca Zanardi; and Leonardo Manzoni (2012)
    Design, Synthesis, and Biological Evaluation of Novel cRGD- Paclitaxel Conjugates for Integrin-Assisted Drug Delivery
    in Bioconjugate chemistry
    (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#autori
  • Michael Pilkington-Miksa; Daniela Arosio; Lucia Battistini; Laura Belvisi; Marilenia De Matteo; Francesca Vasile; Paola Burreddu; Paola Carta; Gloria Rassu; Paola Perego; Nives Carenini; Franco Zunino; Michelandrea De Cesare; Vittoria Castiglioni; Eugenio Scanziani; Carlo Scolastico; Giovanni Casiraghi; Franca Zanardi; and Leonardo Manzoni (literal)
Pagina inizio
  • 1610 (literal)
Pagina fine
  • 1622 (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#numeroVolume
  • 23 (literal)
Rivista
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#pagineTotali
  • 13 (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#numeroFascicolo
  • 8 (literal)
Note
  • ISI Web of Science (WOS) (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#affiliazioni
  • Michael Pilkington-Miksa; Marilenia De Matteo; Francesca Vasile; Centro Interdipartimentale Studi Biomolecolari e Applicazioni Industriali, Universita? degli Studi di Milano, Via Fantoli 16/15, I-20138 Milano, Italy Daniela Arosio; Leonardo Manzoni; Istituto di Scienze e Tecnologie Molecolari, Consiglio Nazionale delle Ricerche, Via Golgi 19, I-20133 Milano, Italy Lucia Battistini; Giovanni Casiraghi; Franca Zanardi; Dipartimento Farmaceutico, Universita? degli Studi di Parma, Parco Area delle Scienze 27A, I-43124 Parma, Italy Laura Belvisi; Dipartimento di Chimica Organica e Industriale, Universita? degli Studi di Milano, Via Venezian 21, I-20133 Milano, Italy Paola Burreddu; Gloria Rassu; Istituto di Chimica Biomolecolare, Consiglio Nazionale delle Ricerche, Traversa La Crucca 3, I-07100 Li Punti, Sassari, Italy Paola Carta; Porto Conte Ricerche Srl, I-07041 Tramariglio Alghero, Sassari, Italy Paola Perego; Nives Carenini; Franco Zunino; Michelandrea De Cesare; Dipartimento di Oncologia Sperimentale e Medicina Molecolare, Fondazione IRCCS Istituto Nazionale Tumori, Via Amadeo 42, I-20133 Milano, Italy Vittoria Castiglioni; Eugenio Scanziani; Dipartimento di Patologia Animale, Igiene e Sanita?Pubblica Veterinaria (DIPAV), Facolta?di Medicina Veterinaria, Universita? degli Studi di Milano, Via Celoria 10, I-20133 Milano, Italy and Mouse and Animal Pathology Laboratory, Fondazione Filarete, Viale Ortles 22/4, I-20139 Milano, Italy (literal)
Titolo
  • Design, Synthesis, and Biological Evaluation of Novel cRGD- Paclitaxel Conjugates for Integrin-Assisted Drug Delivery (literal)
Abstract
  • The efficacy of taxane-based antitumor therapy is limited by several drawbacks which result in poor therapeutic index. Thus, the development of approaches that may favor selective delivery of taxane drugs (e.g. paclitaxel, PTX) to the disease district represents a truly challenging goal. Based on the strategic role of integrins in tumor cell survival and tumor progression, as well as on integrin expression in tumors, novel molecular conjugates were prepared where PTX is covalently attached to either cyclic AbaRGD (Azabicycloalkane-RGD) or AmproRGD (Aminoproline-RGD) integrin-recognizing matrices via structurally diverse connections. Receptor-binding assays indicated satisfactory-to-excellent ?V?3 binding capabilities for most conjugates, while in vitro growth inhibition assays on a panel of human tumor cell lines revealed outstanding cell sensitivity values. Among the nine conjugate ensemble, derivative 21, bearing a robust triazole ring connected to ethyleneglycol units by an amide function and showing excellent cell sensitivity properties, was selected for in vivo studies in an ovarian carcinoma model xenografted in immunodeficient mice. A remarkable antitumor activity was attained, superior to PTX itself, which was associated with a marked induction of aberrant mitoses, consistent with the mechanism of action of spindle poisons. Overall, the novel cRGD-PTX conjugates here disclosed represent promising candidates for further advancement in the domain of targeted anti-tumor therapy. (literal)
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