Tumor-targeting ligands

Pasqualini, R., Koivunen, E., and Ruoslahti, E. (1997). Alpha V integrins as receptors for tumor targeting by circulating ligands. Nat. Biotechnol. 15, 542-546. 

An pFl-dependent coordination isomerism has been observed for the tumor targeting rhenium(V) 0x0 complex [ReO(DMSA)2] (DMSA = 2,3-mercaptosuccinate). In solution the crystallo-graphically characterized syn,endo-isomQx (87a) slowly isomerizes into the anti- (87b) and the iyn,exo-isomers (87c) which has consequences for the biodistribution of the potential pharmaceutical (Scheme 10). The conversion rate decreases with increasing pH suggesting an acid catalyzed reaction. The syn,exo-comy> ex is favored in alkaline solutions (pH > 8.4) which can be understood in terms of the repulsions between the deprotonated carboxylic groups and the 0x0 ligand. 

Kircheis, R., Blessing, T., Brunner, S., Wightman, L., Wagner, E. (2001). Tumor targeting with surface-shielded ligand-polycation DNA complexes. J. Control Release, 72, 165-170. 

Agus DB, Akita RW, Fox WD, Lewis GD, Higgins B, et al. 2002. Targeting ligand-activated ErbB2 signaling inhibits breast and prostate tumor growth. Cancer Cell 2 127-137. 

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