1129-28-8Relevant articles and documents
Dioxygenation of flavonol catalyzed by Copper(II)complexes supported by carboxylate-containing ligands: Structural and functional models of quercetin 2,4-dioxygenase
Sun, Ying-Ji,Li, Pei,Huang, Qian-Qian,Zhang, Jian-Jun,Itoh, Shinobu
, p. 1845 - 1854 (2017)
To obtain insights into the role of the carboxylate group of Glu73 in the active site of quercetin 2,4-dioxygenase (2,4-QD), the copper(Icomplexes [CuIILn(AcO)] [1 (Ln = L1), 2 (Ln = L2), 3 (Ln = L3), and 4 (Ln = L4)] supported by a series of carboxylate-containing ligands [L1H = 2-{[bis(pyridin-2-ylmethyl)amino]methyl}benzoic acid L2H = 3-{[bis(pyridin-2-ylmethyl)amino]methyl}benzoic acid, L3H = 2-({bis[2-(pyridin-2-yl)ethyl]amino}methyl)benzoic acid L4H = 3-({bis[2-(pyridin-2-yl)ethyl]amino}methyl)benzoic acid] as well as the ternary CuII flavonolate (fla-) complexes [CuIILn(fla)] [5 (Ln = L1), 6 (Ln = L2), 7 (Ln = L3), and 8 (Ln = L4)] were synthesized and characterized as structural and functional models for the active site of 2,4-QD. The ternary complexes [CuIILn(fla)] showed different reactivities in the dioxygenation of bound flavonolate to benzoic acid, salicylic acid, and N,N-dimethylbenzamide at 75-90 °C (single-turnover reactioin the order 5 >> 7 > 8 ≈ 6. A similar reactivity tendency was found in the catalytic dioxygenation of the substrate flavonol (multiturnover reactioby the binary complexes. The different reactivities of the copper complexes could be attributed to the different Lewis acidities of the copper(Iions induced by the different coordination environments of the ligands. The results will provide important insights into the pivotal catalytic role of the carboxylate group of Glu73 in 2,4-QD.
Cation-Transporting Peptides: Scaffolds for Functionalized Pores?
Behera, Harekrushna,Ramkumar, Venkatachalam,Madhavan, Nandita
, p. 10179 - 10184 (2015)
Protein pores that selectively transport ions across membranes are among nature's most efficient machines. The selectivity of these pores can be exploited for ion sensing and water purification. Since it is difficult to reconstitute membrane proteins in their active form for practical applications it is desirable to develop robust synthetic compounds that selectively transport ions across cell membranes. One can envision tuning the selectivity of pores by incorporating functional groups inside the pore. Readily accessible octapeptides containing (aminomethyl)benzoic acid and alanine are reported here that preferentially transport cations over halides across the lipid bilayer. Ion transport is hypothesized through pores formed by stable assemblies of the peptides. The aromatic ring(s) appear to be proximal to the pore and could be potentially utilized for functionalizing the pore interior.
1-benzylisatin derivative as well as synthesis method and application thereof
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Paragraph 0017-0018; 0021-0022, (2020/10/20)
The invention relates to a 1-benzylisatin derivative as well as a synthesis method and application thereof, belongs to the technical field of medicines, and relates to a general formula (I) in which R1, R2 and R3 are different substituents. The invention discloses structures of the compounds, a synthesis method of the compounds, inhibitory activity of acetylcholin esterase and inhibitory activityof histone deacetylase 6; and the compounds can be further developed into drugs for treating Alzheimer's disease.
The development of a novel transforming growth factor-β (TGF-β) inhibitor that disrupts ligand-receptor interactions
Wu, Han,Sun, Yu,Wong, Wee Lin,Cui, Jiajia,Li, Jingyang,You, Xuefu,Yap, Lee Fah,Huang, Yu,Hong, Wei,Yang, Xinyi,Paterson, Ian C.,Wang, Hao
, (2020/01/21)
Transforming growth factor-β (TGF-β) plays an important role in regulating epithelial to mesenchymal transition (EMT) and the TGF-β signaling pathway is a potential target for therapeutic intervention in the development of many diseases, such as fibrosis and cancer. Most currently available inhibitors of TGF-β signaling function as TGF-β receptor I (TβR-I) kinase inhibitors, however, such kinase inhibitors often lack specificity. In the present study, we targeted the extracellular protein binding domain of the TGF-β receptor II (TβR-II) to interfere with the protein-protein interactions (PPIs) between TGF-β and its receptors. One compound, CJJ300, inhibited TGF-β signaling by disrupting the formation of the TGF-β-TβR-I-TβR-II signaling complex. Treatment of A549 cells with CJJ300 resulted in the inhibition of downstream signaling events such as the phosphorylation of key factors along the TGF-β pathway and the induction of EMT markers. Concomitant with these effects, CJJ300 significantly inhibited cell migration. The present study describes for the first time a designed molecule that can regulate TGF-β-induced signaling and EMT by interfering with the PPIs required for the formation of the TGF-β signaling complex. Therefore, CJJ300 can be an important lead compound with which to study TGF-β signaling and to design more potent TGF-β signaling antagonists.