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http://hdl.handle.net/2445/44121
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DC Field | Value | Language |
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dc.contributor.author | Barragán, Flavia | - |
dc.contributor.author | Carrión-Salip, Dolors | - |
dc.contributor.author | Gómez-Pinto, Irene | - |
dc.contributor.author | González-Cantó, Alejandro | - |
dc.contributor.author | Sadler, Peter | - |
dc.contributor.author | Llorens Duran, Rafael de | - |
dc.contributor.author | Moreno Martínez, Virtudes | - |
dc.contributor.author | González, Carlos | - |
dc.contributor.author | Massaguer i Vall-llovera, Anna | - |
dc.contributor.author | Marchán Sancho, Vicente | - |
dc.date.accessioned | 2013-06-07T11:15:31Z | - |
dc.date.available | 2013-12-31T23:02:04Z | - |
dc.date.issued | 2012 | - |
dc.identifier.issn | 1043-1802 | - |
dc.identifier.uri | http://hdl.handle.net/2445/44121 | - |
dc.description.abstract | Conjugates of a dicarba analogue of octreotide, a potent somatostatin agonist whose receptors are overexpressed on tumor cells, with [PtCl2(dap)] (dap = 1-(carboxylic acid)-1,2-diaminoethane) (3), [(η6-bip)Os(4-CO2-pico)Cl] (bip = biphenyl, pico = picolinate) (4), [(η6-p-cym)RuCl(dap)]+ (p-cym = p-cymene) (5), and [(η6-p-cym)RuCl(imidazole-CO2H)(PPh3)]+ (6), were synthesized by using a solid-phase approach. Conjugates 3-5 readily underwent hydrolysis and DNA binding, whereas conjugate 6 was inert to ligand substitution. NMR spectroscopy and molecular dynamics calculations showed that conjugate formation does not perturb the overall peptide structure. Only 6 exhibited antiproliferative activity in human tumor cells (IC50 = 63 ± 2 μM in MCF-7 cells and IC50 = 26 ± 3 μM in DU-145 cells) with active participation of somatostatin receptors in cellular uptake. Similar cytotoxic activity was found in a normal cell line (IC50 = 45 ± 2.6 μM in CHO cells), which can be attributed to a similar level of expression of somatostatin subtype-2 receptor. These studies provide new insights into the effect of receptor-binding peptide conjugation on the activity of metal-based anticancer drugs, and demonstrate the potential of such hybrid compounds to target tumor cells specifically. | - |
dc.format.extent | 56 p. | - |
dc.format.mimetype | application/pdf | - |
dc.language.iso | eng | - |
dc.publisher | American Chemical Society | - |
dc.relation.isformatof | Versió postprint del document publicat a: http://dx.doi.org/10.1021/bc300173h | - |
dc.relation.ispartof | Bioconjugate Chemistry, 2012, vol. 23, num. 9, p. 1838-1855 | - |
dc.relation.uri | http://dx.doi.org/10.1021/bc300173h | - |
dc.rights | (c) American Chemical Society , 2012 | - |
dc.source | Articles publicats en revistes (Química Inorgànica i Orgànica) | - |
dc.subject.classification | Cèl·lules canceroses | - |
dc.subject.classification | Càncer | - |
dc.subject.classification | Quimioteràpia del càncer | - |
dc.subject.classification | Pèptids | - |
dc.subject.classification | Receptors cel·lulars | - |
dc.subject.other | Cancer cells | - |
dc.subject.other | Cancer | - |
dc.subject.other | Cancer chemotherapy | - |
dc.subject.other | Peptides | - |
dc.subject.other | Cell receptors | - |
dc.title | Somatostatin Subtype‑2 Receptor-Targeted Metal-Based Anticancer Complexes | eng |
dc.type | info:eu-repo/semantics/article | - |
dc.type | info:eu-repo/semantics/acceptedVersion | - |
dc.identifier.idgrec | 617636 | - |
dc.date.updated | 2013-06-07T10:33:54Z | - |
dc.relation.projectID | info:eu-repo/grantAgreement/EC/FP7/247450/EU//BIOINCMED | - |
dc.rights.accessRights | info:eu-repo/semantics/openAccess | - |
Appears in Collections: | Articles publicats en revistes (Química Inorgànica i Orgànica) |
Files in This Item:
File | Description | Size | Format | |
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617636.pdf | 1.71 MB | Adobe PDF | View/Open |
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