caa a22 4500 445321318 CHVBK 20180317142705.0 cr unu---uuuuu 170323e20111201xx s 000 0 eng 10.1007/s10534-011-9460-3 doi (NATIONALLICENCE)springer-10.1007/s10534-011-9460-3 Potent inhibition of protein tyrosine phosphatases by copper complexes with multi-benzimidazole derivatives [Elektronische Daten] [Ying Li, Liping Lu, Miaoli Zhu, Qingming Wang, Caixia Yuan, Shu Xing, Xueqi Fu, Yuhua Mei] A series of copper complexes with multi-benzimidazole derivatives, including mono- and di-nuclear, were synthesized and characterized by Fourier transform IR spectroscopy, UV-Vis spectroscopy, elemental analysis, electrospray ionization mass spectrometry. The speciation of Cu/NTB in aqueous solution was investigated by potentiometric pH titrations. Their inhibitory effects against human protein tyrosine phosphatase 1B (PTP1B), T-cell protein tyrosine phosphatase (TCPTP), megakaryocyte protein tyrosine phosphatase 2 (PTP-MEG2), srchomology phosphatase 1 (SHP-1) and srchomology phosphatase 2 (SHP-2) were evaluated in vitro. The five copper complexes exhibit potent inhibition against PTP1B, TCPTP and PTP-MEG2 with almost same inhibitory effects with IC50 at submicro molar level and about tenfold weaker inhibition versus SHP-1, but almost no inhibition against SHP-2. Kinetic analysis indicates that they are reversible competitive inhibitors of PTP1B. Fluorescence study on the interaction between PTP1B and complex 2 or 4 suggests that the complexes bind to PTP1B with the formation of a 1:1 complex. The binding constant are about 1.14×106 and 1.87×106 M−1 at 310K for 2 and 4, respectively. Springer Science+Business Media, LLC., 2011 Copper complex nationallicence Protein tyrosine phosphatases nationallicence Inhibition nationallicence Fluorescence nationallicence Li Ying Institute of Molecular Science, Key Laboratory of Chemical Biology and Molecular Engineering of the Education Ministry, Shanxi University, 030006, Taiyuan, People's Republic of China aut Lu Liping Institute of Molecular Science, Key Laboratory of Chemical Biology and Molecular Engineering of the Education Ministry, Shanxi University, 030006, Taiyuan, People's Republic of China aut Zhu Miaoli Institute of Molecular Science, Key Laboratory of Chemical Biology and Molecular Engineering of the Education Ministry, Shanxi University, 030006, Taiyuan, People's Republic of China aut Wang Qingming Institute of Molecular Science, Key Laboratory of Chemical Biology and Molecular Engineering of the Education Ministry, Shanxi University, 030006, Taiyuan, People's Republic of China aut Yuan Caixia Institute of Molecular Science, Key Laboratory of Chemical Biology and Molecular Engineering of the Education Ministry, Shanxi University, 030006, Taiyuan, People's Republic of China aut Xing Shu Edmond H. Fischer Signal Transduction Laboratory, College of Life Sciences, Jilin University, 130023, Changchun, People's Republic of China aut Fu Xueqi Edmond H. Fischer Signal Transduction Laboratory, College of Life Sciences, Jilin University, 130023, Changchun, People's Republic of China aut Mei Yuhua State Key Laboratory of Coordination Chemistry, Nanjing University, 210093, Nanjing, People's Republic of China aut BioMetals Springer Netherlands 24/6(2011-12-01), 993-1004 0966-0844 24:6<993 2011 24 10534 https://doi.org/10.1007/s10534-011-9460-3 text/html Onlinezugriff via DOI 1 research-article jats NATIONALLICENCE 856 40 https://doi.org/10.1007/s10534-011-9460-3 text/html Onlinezugriff via DOI NATIONALLICENCE 700 1- Li Ying Institute of Molecular Science, Key Laboratory of Chemical Biology and Molecular Engineering of the Education Ministry, Shanxi University, 030006, Taiyuan, People's Republic of China aut NATIONALLICENCE 700 1- Lu Liping Institute of Molecular Science, Key Laboratory of Chemical Biology and Molecular Engineering of the Education Ministry, Shanxi University, 030006, Taiyuan, People's Republic of China aut NATIONALLICENCE 700 1- Zhu Miaoli Institute of Molecular Science, Key Laboratory of Chemical Biology and Molecular Engineering of the Education Ministry, Shanxi University, 030006, Taiyuan, People's Republic of China aut NATIONALLICENCE 700 1- Wang Qingming Institute of Molecular Science, Key Laboratory of Chemical Biology and Molecular Engineering of the Education Ministry, Shanxi University, 030006, Taiyuan, People's Republic of China aut NATIONALLICENCE 700 1- Yuan Caixia Institute of Molecular Science, Key Laboratory of Chemical Biology and Molecular Engineering of the Education Ministry, Shanxi University, 030006, Taiyuan, People's Republic of China aut NATIONALLICENCE 700 1- Xing Shu Edmond H. Fischer Signal Transduction Laboratory, College of Life Sciences, Jilin University, 130023, Changchun, People's Republic of China aut NATIONALLICENCE 700 1- Fu Xueqi Edmond H. Fischer Signal Transduction Laboratory, College of Life Sciences, Jilin University, 130023, Changchun, People's Republic of China aut NATIONALLICENCE 700 1- Mei Yuhua State Key Laboratory of Coordination Chemistry, Nanjing University, 210093, Nanjing, People's Republic of China aut NATIONALLICENCE 773 0- BioMetals Springer Netherlands 24/6(2011-12-01), 993-1004 0966-0844 24:6<993 2011 24 10534 Metadata rights reserved Springer special CC-BY-NC licence nationallicence BK010053 XK010053 XK010000 NATIONALLICENCE NATIONALLICENCE NL-springer