Protein Tyrosine Phosphatase Inhibition by Metals and Metal Complexes

Abstract

Investigating the structural basis of the interactions between metal complexes and PTPs would facilitate a comprehensive understanding of the structure-activity relationship and accelerate the development of promising metal-based drugs targeting specific PTPs.

Gold(I) NHC-based homo- and heterobimetallic complexes: synthesis, characterization and evaluation as potential anticancer agents

“…Interestingly, in contrast to what we observed for 7, other Ru-arene complexes of the (p-cymene)(NHC)RuCl 2 type have been reported to be good inhibitors of TrxR [65]. Moreover, the cathepsins cysteine proteases have been shown to be inhibited by other families of Ru-arene complexes, [31] while protein tyrosine phosphatases are good targets for Cu compounds [66].…”

“…The gold(I) mono-and polynuclear compounds were also shown to be potent TrxR inhibitors in the nM range in vitro. In the case of the mononuclear Cu(II) complex 6 the fact that there is no correlation between its marked cytotoxic activity and the poor TrxR inhibition is not unexpected, since other mechanisms are known to be responsible for Cu(II) complex cytotoxic effects, including the inhibition of protein tyrosine phosphatases [66] and the influence on cell redox pathways, [67,68] as well as DNA damage [69].…”

“…These cores were stored in ice-cold UW until they were sliced with a pre-cooled Krumdieck tissue slicer in ice-cold Krebs-Henseleit buffer saturated with carbogen (95 % O 2 /5 % CO 2 ). PCLS (average of 5 mm diameter, 250 μm thickness and 5 mg wet weight) were stored in ice-cold UW solution until incubation [66,70]. Incubation of PCLS took place in Williams medium E glutamax (WME, Gibco) supplemented with additional d-glucose monohydrate (1.375 g/500 mL) and gentamicin solution (50 mg/mL; 500 µL/500 mL).…”

1,4-Bis(1H-1,2,4-triazol-1-yl)benzene

“…Their copper complexes can inhibit the activity of protein tyrosine phosphatase (Lu & Zhu, 2014). Thus, we reacted 2,5-bis(1H-1,2,4-triazol-1-yl)terephthalic acid with CuCl 2 under hydrothermal conditions in an attempt to form a complex, but instead crystals of the title compound, (I), were obtained.…”

Vanadyl complexes with dansyl-labelled di-picolinic acid ligands: synthesis, phosphatase inhibition activity and cellular uptake studies

“…These observations suggest that the complexes show some selectivity towards certain PTPs compared to others. There also seems to be an effect on the inhibitory properties of the complex on increasing the length of the linker from diethanolamine (14) to dipropanolamine (15) Table 2. We also carried out the inhibition studies using VOSO 4 as a control.…”