Two drug-enzyme conjugates of dexamethasone-subtilisin and dexamethasone-cellulase have been synthesized and characterized to study their drug-protein incorporation ratio, immunoreactivity, enzyme activity and stability and these studies proved that a variety of drug enzyme conjugates could also be synthesized and characterized.
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Microbiol Res
December 2024
Jiangsu Key Laboratory for Pathogens and Ecosystems, Jiangsu Engineering and Technology Research Center for Microbiology, College of Life Sciences, Nanjing Normal University, Nanjing, China. Electronic address:
The airborne fungus Aspergillus fumigatus is a major pathogen that poses a serious health threat to humans by causing aspergillosis. Azole antifungals inhibit sterol 14-demethylase (encoded by cyp51A), an enzyme crucial for fungal cell survival. However, the most common mechanism of azole resistance in A.
View Article and Find Full Text PDFMethods Mol Biol
August 2021
The Wallace H. Coulter Department of Biomedical Engineering, Georgia Institute of Technology and Emory University, Atlanta, GA, USA.
Intracellular drug metabolism involves transport, bioactivation, conjugation, and other biochemical steps. The dynamics of these steps are each dependent on a number of other cellular factors that can ultimately lead to unexpected behavior. In this review, we discuss the confounding processes and coupled reactions within bioactivation networks that require a systems-level perspective in order to fully understand the time-varying behavior.
View Article and Find Full Text PDFMethods Mol Biol
September 2014
Division of Cardiology, Department of Medicine, Emory University, Atlanta, GA, USA.
Intracellular drug metabolism involves transport, bioactivation, conjugation, and other biochemical steps. The dynamics of these steps are each dependent on a number of other cellular factors that can ultimately lead to unexpected behavior. In this review, we discuss the confounding processes and coupled reactions within bioactivation networks that require a systems-level perspective in order to fully understand the time-varying behavior.
View Article and Find Full Text PDFPLoS One
March 2013
Indian Institute of Science Education and Research Kolkata, Mohanpur Campus, Mohanpur, Nadia, India.
Oxime drugs translocate through the 20 Å active-site gorge of acetylcholinesterase in order to liberate the enzyme from organophosphorus compounds' (such as tabun) conjugation. Here we report bidirectional steered molecular dynamics simulations of oxime drug (Ortho-7) translocation through the gorge of tabun intoxicated enzyme, in which time dependent external forces accelerate the translocation event. The simulations reveal the participation of drug-enzyme hydrogen bonding, hydrophobic interactions and water bridges between them.
View Article and Find Full Text PDFJ Drug Target
June 2011
Department of Biological Chemistry, Weizmann Institute of Science, Rehovot, Israel.
Human ovarian cancer cells specifically bind the isoflavone daidzein. A chemical conjugate between daidzein and the garlic enzyme alliinase was prepared. The conjugate specifically bound to ovarian cancer cells and upon addition of the prodrug alliin, it effectively produced cytotoxic allicin molecules which killed the cancer cells.
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