- Integrin-targeted nano-sized polymeric systems for paclitaxel conjugation: a comparative study
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The generation of rationally designed polymer therapeutics via the conjugation of low molecular weight anti-cancer drugs to water-soluble polymeric nanocarriers aims to improve the therapeutic index. Here, we focus on applying polymer therapeutics to targ
- Eldar-Boock, Anat,Blau, Rachel,Ryppa, Claudia,Baabur-Cohen, Hemda,Many, Ariel,Vicent, María Jesús,Kratz, Felix,Sanchis, Joaquin,Satchi-Fainaro, Ronit
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p. 829 - 844
(2017/10/06)
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- POLYMERIC SYSTEMS AND USES THEREOF IN THERANOSTIC APPLICATIONS
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Polymeric systems useful for theranostic applications are disclosed. The polymeric systems comprise a fluorescent or fluorogenic moiety and a therapeutically active agent, each attached to the same or different polymeric moiety. The polymeric systems are designed such that a fluorescent signal is generated in response to a chemical event, preferably upon contacting an analyte (e.g., an enzyme) that is over- expressed in a diseased tissue or organ. Probes useful for inclusion in such polymeric systems, processes of preparing such probes and the polymeric systems, and uses thereof in diagnostic and/or theranostic applications are also disclosed.
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- CONJUGATES OF A POLYMER, A BISPHOSPHONATE AND AN ANTI-ANGIOGENESIS AGENT AND USES THEREOF IN THE TREATMENT AND MONITORING OF BONE RELATED DISEASES
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Conjugates of polymers or copolymers having attached thereto an anti-angiogenesis agent and a bisphosphonate bone targeting agent, and processes of preparing same, are disclosed. Pharmaceutical compositions containing these conjugates and uses thereof in
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Paragraph 0402-0405
(2016/01/26)
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- Conjugates of a novel 7-substituted camptothecin with RGD-peptides as αvβ3 integrin ligands: An approach to tumor-targeted therapy
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Eight conjugates of a novel camptothecin derivative (Namitecan, NMT) with RGD peptides have been synthesized and biologically evaluated. This study focused on factors that optimize the drug linkage to the transport vector. The different linkages investigated consist of heterofunctional glycol fragments and a lysosomally cleavable peptide. The linkage length and conformation were systematically modified with the purpose to understand their effect on receptor affinity, systemic stability, cytotoxicity, and solubility of the corresponding conjugates. Among the new conjugates prepared, C6 and C7 showed high receptor affinity and tumor cell adhesion, acceptable stability in murine blood, and high cytotoxic activity (IC50 = 8 nM). The rationale, synthetic strategy, and preliminary biological results will be presented.
- Dal Pozzo, Alma,Esposito, Emiliano,Ni, Minghong,Muzi, Laura,Pisano, Claudio,Bucci, Federica,Vesci, Loredana,Castorina, Massimo,Penco, Sergio
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p. 1956 - 1967
(2011/08/21)
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