scholarly journals Preparation of poly(thiophene-alt-pyrrole) bearing chiral LC group

2020 ◽  
Vol 60 (2) ◽  
pp. 226-232
Author(s):  
Akiko Yatsu ◽  
Takuya Yonehara ◽  
Hiromasa Goto
Keyword(s):  
Chiral Lc

scholarly journals Catalytic activity and stereoselectivity of engineered phosphotriesterases towards structurally different nerve agents in vitro

2021 ◽  
Author(s):  
Anja Köhler ◽  
Benjamin Escher ◽  
Laura Job ◽  
Marianne Koller ◽  
Horst Thiermann ◽  
...  
Keyword(s):  
Plasma Clearance ◽  
Nerve Agents ◽  
Inhibition Assay ◽  
Ache Inhibition ◽  
Catalytic Activities ◽  
Chiral Lc ◽  
Hydrolysis Of ◽  
Medical Countermeasures

AbstractHighly toxic organophosphorus nerve agents, especially the extremely stable and persistent V-type agents such as VX, still pose a threat to the human population and require effective medical countermeasures. Engineered mutants of the Brevundimonas diminuta phosphotriesterase (BdPTE) exhibit enhanced catalytic activities and have demonstrated detoxification in animal models, however, substrate specificity and fast plasma clearance limit their medical applicability. To allow better assessment of their substrate profiles, we have thoroughly investigated the catalytic efficacies of five BdPTE mutants with 17 different nerve agents using an AChE inhibition assay. In addition, we studied one BdPTE version that was fused with structurally disordered PAS polypeptides to enable delayed plasma clearance and one bispecific BdPTE with broadened substrate spectrum composed of two functionally distinct subunits connected by a PAS linker. Measured kcat/KM values were as high as 6.5 and 1.5 × 108 M−1 min−1 with G- and V-agents, respectively. Furthermore, the stereoselective degradation of VX enantiomers by the PASylated BdPTE-4 and the bispecific BdPTE-7 were investigated by chiral LC–MS/MS, resulting in a several fold faster hydrolysis of the more toxic P(−) VX stereoisomer compared to P(+) VX. In conclusion, the newly developed enzymes BdPTE-4 and BdPTE-7 have shown high catalytic efficacy towards structurally different nerve agents and stereoselectivity towards the toxic P(−) VX enantiomer in vitro and offer promise for use as bioscavengers in vivo.

Choice of chiral LC systems

1989 ◽  
pp. 223-234
Author(s):  
W. J. Lough ◽  
I. W. Wainer
Keyword(s):  
Chiral Lc

Quantitation of ivosidenib in human plasma via LC–MS/MS and its application in clinical trials

Bioanalysis ◽  
2021 ◽  
Author(s):  
Feng Yin ◽  
Shaoxia Yu ◽  
Rohini Narayanaswamy ◽  
Heidi Mangus ◽  
Erin McCourt ◽  
...  
Keyword(s):  
Clinical Trials ◽  
Human Plasma ◽  
Internal Standard ◽  
Clinical Samples ◽  
Isocitrate Dehydrogenase 1 ◽  
Bioanalytical Method ◽  
Molecule Inhibitor ◽  
Chiral Lc ◽  
First Time

Aim: Ivosidenib is a potent and selective small molecule inhibitor of mutant isocitrate dehydrogenase 1. Accurate measurement of ivosidenib is the key to ivosidenib pharmacokinetics in clinical trials. Materials & methods: Quantitation of ivosidenib was conducted by using a stable isotope labeled compound (ivosidenib-d4) as the internal standard. Results: This assay was validated and successfully applied to support multiple clinical trials. Selected clinical samples were also tested by a chiral LC–MS/MS method against four ivosidenib isomer standards to exclude the possibility of in vivo racemization of ivosidenib. Conclusion: A robust LC–MS/MS method was validated for ivosidenib in human plasma. This is the first time for ivosidenib bioanalytical method in any human matrix to be reported.

Enantioselective analysis of citalopram and demethylcitalopram in human and rat plasma by chiral LC-MS/MS: Application to pharmacokinetics

Chirality ◽  
2007 ◽  
Vol 19 (10) ◽  
pp. 793-801 ◽  
Author(s):  
Adriana Rocha ◽  
Maria P. Marques ◽  
Eduardo B. Coelho ◽  
Vera L. Lanchote
Keyword(s):  
Rat Plasma ◽  
Enantioselective Analysis ◽  
Chiral Lc

scholarly journals Development of a sensitive and rapid method for quantitation of ( S )-(−)- and ( R )-(+)-metoprolol in human plasma by chiral LC–ESI–MS/MS

2014 ◽  
Vol 4 (1) ◽  
pp. 63-79 ◽  
Author(s):  
Primal Sharma ◽  
Pritesh Contractor ◽  
Swati Guttikar ◽  
Daxesh P. Patel ◽  
Pranav S. Shrivastav
Keyword(s):  
Human Plasma ◽  
Rapid Method ◽  
Esi Ms ◽  
Chiral Lc
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