scholarly journals Studies of H3K4me3 demethylation by KDM5B/Jarid1B/PLU1 reveals strong substrate recognition in vitro and identifies 2,4-pyridine-dicarboxylic acid as an in vitro and in cell inhibitor

FEBS Journal ◽  
2012 ◽  
Vol 279 (11) ◽  
pp. 1905-1914 ◽  
Author(s):  
Line H. Kristensen ◽  
Anders L. Nielsen ◽  
Charlotte Helgstrand ◽  
Michael Lees ◽  
Paul Cloos ◽  
...  
Keyword(s):  
Dicarboxylic Acid ◽  
Substrate Recognition ◽  
Pyridine Dicarboxylic Acid

scholarly journals Anti-bacterial activity, anti-cancer activity and nanofiber formation of certain poly (ester amides) from 2,5-pyridine dicarboxylic acid

2018 ◽  
Vol 8 (6-s) ◽  
pp. 166-173
Author(s):  
V. Chitra ◽  
D. Roop Singh
Keyword(s):  
Dicarboxylic Acid ◽  
Bacterial Activity ◽  
Composite Fibers ◽  
Thermal Phase Transition ◽  
Anti Cancer ◽  
Pyridine Dicarboxylic Acid ◽  
Nano Fiber ◽  
Human Breast Carcinoma Cells ◽  
Cancer Activity

A new series of four poly(ester amides) were synthesized by direct polycondensation of 2,5-pyridine dicarboxylic acid  with two different varying diols and diamines in pyridine medium using diphenylchlorophosphate as a condensation agent. The two diamines employed in the synthesis were 4,4’-diamino diphenyl methane and 1,4-diamino benzene. The arylidenediols 2,5-bis(4-hydroxy-3-methoxybenzylidene)cyclopentanone and 2,6-bis(4-hydroxy-3-methoxybenzylidene) cyclohexanone were also used. The synthesized poly(ester amides) were characterized by qualitative solubility test, FT-IR, 1H and 13C-NMR spectra. The monomeric moieties were found by spectroscopic analysis to be well incorporated in the polymer back bone. The thermal phase transition behavior of the poly(ester amides) were investigated by differential thermo gravimetry (DTG). The nanofibers of synthesized poly(ester amides) with PVC and composite fibers with PVC/nanoclay were formed by electrospinning.  The morphology of these composite fibers was studied by scanning electron microscopy (SEM). These poly(ester amides) were screened for their anti-bacterial potential in vitro against Pseudomonas aeruginosa, Escherichia coli, Staphylococcus aureus and Bacillus subtilis. In vitro anti-cancer activities of synthesized polymers were also evaluated against MCF7 human breast carcinoma cells. The results show that the polymers exhibited significant anti-bacterial and anti-cancer activity. Keywords: Poly (ester amides), Anti-bacterial activity, Nano fiber, Anticancer activity

Investigation of X-ray crystal structure and in vitro cytotoxicity of two Ga(III) complexes containing pyridine dicarboxylic acid derivatives and 2-aminobenzimidazole

2021 ◽  
Vol 1223 ◽  
pp. 129005
Author(s):  
Alireza Aliabadi ◽  
Mohammad Hakimi ◽  
Fatemeh Hosseinabadi ◽  
Elham Motieiyan ◽  
Vitor Hugo Nunes Rodrigues ◽  
...  
Keyword(s):  
Crystal Structure ◽  
Dicarboxylic Acid ◽  
In Vitro Cytotoxicity ◽  
X Ray ◽  
Pyridine Dicarboxylic Acid

scholarly journals Anionic amino acids support hydrolysis of poly-β-(1,6)-N-acetylglucosamine exopolysaccharides by the biofilm dispersing glycosidase Dispersin B

2020 ◽  
pp. jbc.RA120.015524
Author(s):  
Alexandra P Breslawec ◽  
Shaochi Wang ◽  
Crystal Li ◽  
Myles B Poulin
Keyword(s):  
Amino Acids ◽  
Bacterial Infections ◽  
Substrate Recognition ◽  
Site Directed Mutagenesis ◽  
Binding Surface ◽  
Activity Measurements ◽  
Rate Of Hydrolysis ◽  
Biofilm Dispersal ◽  
Hydrolysis Of

The exopolysaccharide poly-β-(1→6)-N-acetylglucosamine (PNAG) is a major structural determinant of bacterial biofilms responsible for persistent and nosocomial infections. The enzymatic dispersal of biofilms by PNAG-hydrolyzing glycosidase enzymes, such as Dispersin B (DspB), is a possible approach to treat biofilm dependent bacterial infections. The cationic charge resulting from partial de-N-acetylation of native PNAG is critical for PNAG-dependent biofilm formation. We recently demonstrated that DspB has increased catalytic activity on de-N-acetylated PNAG oligosaccharides, but the molecular basis for this increased activity is not known. Here, we analyze the role of anionic amino acids surrounding the catalytic pocket of DspB in PNAG substrate recognition and hydrolysis using a combination of site directed mutagenesis, activity measurements using synthetic PNAG oligosaccharide analogs, and in vitro biofilm dispersal assays. The results of these studies support a model in which bound PNAG is weakly associated with a shallow anionic groove on the DspB protein surface with recognition driven by interactions with the –1 GlcNAc residue in the catalytic pocket. An increased rate of hydrolysis for cationic PNAG was driven, in part, by interaction with D147 on the anionic surface. Moreover, we identified that a DspB mutant with improved hydrolysis of fully acetylated PNAG oligosaccharides correlates with improved in vitro dispersal of PNAG dependent Staphylococcus epidermidis biofilms. These results provide insight into the mechanism of substrate recognition by DspB and suggest a method to improve DspB biofilm dispersal activity by mutation of the amino acids within the anionic binding surface.

Pregn-5-en-3β-ol and androst-5-en-3β-ol dicarboxylic acid esters as potential therapeutics for NMDA hypofunction: In vitro safety assessment and plasma stability

Steroids ◽  
2019 ◽  
Vol 147 ◽  
pp. 4-9 ◽  
Author(s):  
Marika Matousova ◽  
Radko Soucek ◽  
Eva Tloustova ◽  
Barbora Slavikova ◽  
Hana Chodounska ◽  
...  
Keyword(s):  
Dicarboxylic Acid ◽  
Safety Assessment ◽  
Plasma Stability ◽  
Potential Therapeutics ◽  
Acid Esters
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