Words 1 and organic cation transporter 1 h at 3 Ufigsten discussed, but it seems to be on certain cell lines. Systematic studies on the relationship of structure can lead to accumulation of Cl Tion of the underlying mechanisms of drug transport. Recently, we investigated the Benazepril Lotensin influence of lipophilicity on cellular Re accumulation of oxaliplatin with known platinum drugs and structurally related compounds with ligands of different amines. We concluded that passive diffusion is the main mechanism for the influx of the first few minutes of incubation. Then, enrichment, independent Dependent and lipophilicity due to transport proteins Be taught. Therefore, it is likely that the reactivity of t, k, of platinum complexes can Play a r Point in the interaction between the platinum complex and the transport protein. For the platinum complexes, the reactivity of t times the F Ability is, to replace the leaving group in nucleophilic defined. The binding of mononucleotides can be a model for the reactivity of t of platinum compounds in general and for the response to DNA in particular. Inert platinum complexes generally have lower power consumption and toxicity Tons of reactive complexes. There are some tricks that reactivity is t the trailer Ufung effect of platinum. Pereira Maia and Garnier Suillerot studied the relationship between the concentration of extracellular Rem cisplatin solvated species and the rate of cellular Ren accumulation. It has been suggested that only solvated species were picked up by active transport. More reactive platinum complexes such as cisplatin, produce green Ere amounts of solvated species and thus faster Nelarabine DNA Synthesis inhibitor than less reactive platinum complexes such as carboplatin made.
In another study with erythrocytes of man, a relationship between the reactivity of t of the various complexes of platinum diammine / diaminocyclohexane and cellular Re accumulation has been shown, however, in this case, the reactivity of t on the basis of the interaction determined by the G -actin, which probably not relevant in vivo. In addition, the relevance of the reactivity of t with the influx of people CTR1 mediates examined. It has been suggested that to stabilize the platinum complexes, a homotrimer of hCTR1 by crosslinking hCTR1 subunits via methionine-rich clusters. The degree of formation homotrimer has been shown that the reactivity of t from the platinum complex. Thus trimerization less effective after treatment with Zoledronate oxaliplatin compared to cisplatin and was even slower after treatment with carboplatin. However, the reactivity of t is also to be something for the binding of methionine-rich clusters appears to be important, the bulky diaminocyclohexane ligand was proposed to the influx of oxaliplatin by an independent mediate Independent CTR1. In addition, the organic components in the group were taught nonleaving as critical to the influx of OCT1 and OCT2. It was the aim of this study, the hypothesis that increased Hte reactivity leads t to an increased Hten accumulation and cytotoxicity t of platinum compounds in human cancer cells tested. Thus we examined the fa There Systematic reactive Ability, cellular Cytotoxicity re t of accumulation and diaminocyclohexane platinum complexes with different leaving groups, additionally Tzlich to the previously studied complexes 2-5 with ligands of different operators.