- MULTI-ARM TARGETING ANTI-CANCER CONJUGATE
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A multi-branched dnig conjugate of formula (I) or a pharmaceutically acceptable salt thereof. In the formula, R is an organic center, POLY is a polymer, L is a multivalent linker, T is a targeting molecule, D is an active agent, and q is any integer between 3 and 8. The symbol “*” in L represents a junction point of the multivalent linker L and the targeting molecule T, “#” represents a junction point of the multivalent linker L and the active agent D, and “%” represents a junction point of the multivalent linker L and POLY. 1 is any integer between 2 and 20, and m and n are each an integer between 0 and 10. T is iRGD, cRGD, tLyp-1, Lyp-1, RPARPAR, Angiopep2, or GE11. D is a camptothecin drug.
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- Integrin receptor targeted anticancer conjugate
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The invention discloses a multi-arm targeted drug conjugate heptane sulfonate modified by a water-soluble polymer. The drug conjugate has the structural formula as shown in the description. The typical heptane sulfonate of the conjugate comprises single-e
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- Small and stable peptidic PEGylated quantum dots to target polyhistidine-tagged proteins with controlled stoichiometry
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The use of the semiconductor quantum dots (QD) as biolabels for both ensemble and single-molecule tracking requires the development of simple and versatile methods to target individual proteins in a controlled manner, ideally in living cells. To address t
- Dif, Aure Lien,Boulmedais, Fouzia,Pinot, Mathieu,Roullier, Victor,Baudy-Floc'h, Michele,Coquelle, Frederic M.,Clarke, Samuel,Neveu, Pierre,Vignaux, Francoise,Le Borgne, Roland,Dahan, Maxime,Gueroui, Zoher,Marchi-Artzner, Valerie
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experimental part
p. 14738 - 14746
(2010/01/06)
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- Synthesis of bifunctional integrin-binding peptides containing PEG spacers of defined length for non-viral gene delivery
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Improving the buffer and serum stability of non-viral gene delivery vectors, and increasing their circulation time in vivo, is an important focus of current research in gene therapy. The most successful strategies to date have involved shielding the complexes with large polydisperse PEG adducts. However, this approach is accompanied by a fall in transfection efficiency. In this paper we describe the solid-phase synthesis of a series of bifunctional peptides bearing short PEG spacers of defined structure as components of lipopolyplex gene delivery vectors. Short, high-yielding routes to a series of PEG-amino acids are described: these PEG-amino acids can be used in varying combinations to afford bifunctional peptides with varying lengths of PEG spacers by using standard solid-phase synthesis techniques. A series of lipopolyplexes were formulated using these bifunctional peptides, and their transfection properties assessed. Dynamic light scattering measurements on the complex with the best transfection properties showed that in phosphate-buffered saline this complex was considerably more stable, and aggregated more slowly, than a complex formulated using a similar peptide lacking the short PEG spacer. Wiley-VCH Verlag GmbH & Co. KGaA, 2008.
- Pilkington-Miksa, Michael A.,Sarkar, Supti,Writer, Michele J.,Barker, Susie E.,Shamlou, Parviz Ayazi,Hart, Stephen L.,Hailes, Helen C.,Tabor, Alethea B.
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experimental part
p. 2900 - 2914
(2009/04/11)
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- Multimeric cyclic RGD peptides as potential tools for tumor targeting: Solid-phase peptide synthesis and chemoselective oxime ligation
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The αvβ3 integrin receptor plays an important role in human metastasis and tumor-induced angiogenesis. Targeting this receptor may provide information about the receptor status of the tumor and enable specific therapeutic planning. Solid-phase peptide synthesis of multimeric cyclo(-RGDfE-)-peptides is described, which offer the possibility of enhanced integrin targeting due to polyvalency effects. These peptides contain an aminooxy group for versatile chemoselective oxime ligation. Conjugation with para-trimethylstannylbenzaldehyde results in a precursor for radioiododestannylation, which would allow them to be used as potential tools for targeting and imaging αvβ3-expressing tumor cells. The conjugates were obtained in good yield without the need of a protection strategy and under mild conditions.
- Thumshirn, Georgette,Hersel, Ulrich,Goodman, Simon L.,Kessler, Horst
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p. 2717 - 2725
(2007/10/03)
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