AMD3100 conjugates as components of targeted nonviral gene delivery systems: synthesis and in vitro transfection efficiency of CXCR4-expressing cells.

We describe the synthesis of a series of AMD3100-lipid and AMD3100-polycationic conjugates which were used as components of targeted lipoplexes (in conjunction with (poly)cationic lipids) and polyplexes, respectively, for mediating specific gene transfer into cells expressing CXCR4 which displays a high affinity for AMD3100. Transfection studies were investigated with suspension CXCR4(+) human lymphoma Jurkat cells and with adherent CXCR4(-) human glioblastoma T98G and human lung carcinoma A549 cells lines in order to demonstrate a receptor-mediated endocytosis pathway and to minimize nonspecific transfection pathways. Altogether, our results show that polyplexes formulated with AMD-labeled polymers constitute, under certain conditions, specific gene transfer systems into suspension CXCR4(+) Jurkat cells.

Polycationic diblock and random polyethylene glycol- or tris(hydroxymethyl)methyl-grafted (co)telomers for gene transfer: synthesis and evaluation of their in vitro transfection efficiency.

We report on the synthesis of a series of polycationic telomers, polycationic diblock and random polyethylene glycol (PEG)-grafted (co)telomers, and polycationic random tris(hydroxymethyl)methyl (THM) cotelomers, and on their in vitro gene transfer capability. These compounds were obtained by a telomerization process of various amino-, tetraethylene glycol-, or THM-acrylamide taxogens with thiols which might derive from PEG2000. For N/P ratios [N is the number of (co)telomer amine equivalents; P is the number of DNA phosphate equivalents] from 0.

Polycationic telomers and cotelomers for gene transfer: synthesis and evaluation of their an vitro transfection efficiency.

We report on the synthesis of a series of lipopolyamine telomers, [I(Asp)-14,n(A)(NH), I(His)-18,n(A)(NH), I-18,n(B)(NMe), Gal-n(A)(NH)], and random cotelomers, [I-18,n(A)(NH)-n(B)(NMe) and I-18,n(A)(NH)-n(C)(OH)], and on their in vitro gene transfer capability. They were obtained by a telomerization process of various amino-acrylamide taxogens with various lipophilic thiol telogens which might also contain an aspartic or a histidine residue or with a thiogalactosyle derivative. For N/P ratios (N = number of (co)telomer amine equivalents, P = number of DNA phosphates) from 0.