Linked Life Data

21607272

Source:http://linkedlifedata.com/resource/pubmed/id/21607272

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
24
pubmed:dateCreated
2011-6-9
pubmed:abstractText
Six copper complexes of Schiff base ligands containing 3,5-substituted-4-salicylideneamino-3,5-dimethyl-1,2,4-triazole have been synthesized and well characterized. The structures of complexes 1 and 2 were determined by X-ray crystal analysis. Fluorescence and potentiometric study indicated that in the physiological pH range, one ligand was dissociated from the complexes to form 1:1 mononucleus copper complexes. The complexes potently inhibit protein tyrosine phosphatase 1B (PTP1B), T-cell protein tyrosine phosphatase (TCPTP), megakaryocyte protein tyrosine phosphatase 2 (PTP-MEG2) and Src homology phosphatase 1 (SHP-1) with 3-4 fold selectivity against PTP1B over TCPTP and PTP-MEG2, and 3-9 fold over SHP-1, but display almost no inhibition against Src homology phosphatase 2 (SHP-2). Complex 1 inhibits PTP1B with a competitive model with K(i) of 30 nM. Substitution with small groups at the phenyl of the ligand does not obviously influence the inhibitory ability of the complexes.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Jun
pubmed:issn
1477-9234
pubmed:author
pubmed:copyrightInfo
This journal is © The Royal Society of Chemistry 2011
pubmed:issnType
Electronic
pubmed:day
28
pubmed:volume
40
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
6532-40
pubmed:meshHeading
pubmed-meshheading:21607272-Coordination Complexes, pubmed-meshheading:21607272-Copper, pubmed-meshheading:21607272-Crystallography, X-Ray, pubmed-meshheading:21607272-Enzyme Inhibitors, pubmed-meshheading:21607272-Hydrogen Bonding, pubmed-meshheading:21607272-Hydrogen-Ion Concentration, pubmed-meshheading:21607272-Kinetics, pubmed-meshheading:21607272-Molecular Conformation, pubmed-meshheading:21607272-Protein Tyrosine Phosphatase, Non-Receptor Type 1, pubmed-meshheading:21607272-Protein Tyrosine Phosphatase, Non-Receptor Type 2, pubmed-meshheading:21607272-Protein Tyrosine Phosphatase, Non-Receptor Type 6, pubmed-meshheading:21607272-Protein Tyrosine Phosphatases, pubmed-meshheading:21607272-Schiff Bases, pubmed-meshheading:21607272-Stereoisomerism, pubmed-meshheading:21607272-Triazoles
pubmed:year
2011
pubmed:articleTitle
Mononuclear copper(II) complexes with 3,5-substituted-4-salicylidene-amino-3,5-dimethyl-1,2,4-triazole: synthesis, structure and potent inhibition of protein tyrosine phosphatases.
pubmed:affiliation
Institute of Molecular Science, Key Laboratory of Chemical Biology and Molecular Engineering of the Education Ministry, Shanxi University, Taiyuan, Shanxi 030006, PR China.
pubmed:publicationType
Journal Article, Research Support, Non-U.S. Gov't