Although protein tyrosine phosphatases(PTPs)do not contain any metals,their activities can be inhibited by some metal complexes.Here we investigated the inhibition of two zinc complexes with Schiff base ligands agains...Although protein tyrosine phosphatases(PTPs)do not contain any metals,their activities can be inhibited by some metal complexes.Here we investigated the inhibition of two zinc complexes with Schiff base ligands against PTPs activity to explore their effect on the cellular metabolism.It has been found that they are potent inhibitors against four recombinant PIPs5 including protein tyrosine phosphatase 1B(PTP1B),T cell protein tyrosine phosphatase(TCPTP),megakaryocyte protein tyrosine phosphatase 2(PTP-MEG2)S and Src-homology phosphatase 1(SHP-1),with exception of Src-homology phosphatase 2(SHP-2).Moreover,tlaey showed moderate selective inhibition against PTP1B with the IG50 values of 0.15 and 0.36μmol/L.Meanwhile,the complexes also inhibited cellular phosphatase activities efficiently.Comparing the inhibitory potency over PTPs mediated by the zinc ion,we found that zinc complexes might be easily developed into potent and selective inhibitors against certain PTP by rationally modifying the organic ligands moieties.展开更多
基金the National Natural Science Foundation of China(Nos.21471092,21571118)the Project of the Scientific Instrument Center of Shanxi University of China.
文摘Although protein tyrosine phosphatases(PTPs)do not contain any metals,their activities can be inhibited by some metal complexes.Here we investigated the inhibition of two zinc complexes with Schiff base ligands against PTPs activity to explore their effect on the cellular metabolism.It has been found that they are potent inhibitors against four recombinant PIPs5 including protein tyrosine phosphatase 1B(PTP1B),T cell protein tyrosine phosphatase(TCPTP),megakaryocyte protein tyrosine phosphatase 2(PTP-MEG2)S and Src-homology phosphatase 1(SHP-1),with exception of Src-homology phosphatase 2(SHP-2).Moreover,tlaey showed moderate selective inhibition against PTP1B with the IG50 values of 0.15 and 0.36μmol/L.Meanwhile,the complexes also inhibited cellular phosphatase activities efficiently.Comparing the inhibitory potency over PTPs mediated by the zinc ion,we found that zinc complexes might be easily developed into potent and selective inhibitors against certain PTP by rationally modifying the organic ligands moieties.
