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Magnoflorine increased the systemic exposure and metabolicstability and suppressed the transport of luteolin. CaCO-2 cell transwell assay was employed for transport evaluation, and the metabolicstability of luteolin and CYP3A activity were assessed in rat liver microsomes.
The co-administration of cryptotanshinone with ophiopogonin D induced pharmacokinetic interaction prolonging the systemic exposure and improving metabolicstability of cryptotanshinone. The Caco-2 cells were employed to evaluate the transport of cryptotanshinone, and the metabolicstability was studied in the rat liver microsomes.
However, the aldehyde functional group metabolic instability has severly hampered their development, except for voxelotor, which was approved in 2019 for SCD treatment.
One way of doing this is to build models for predicting biological activity and other pharmaceutically relevant properties such as aqueous solubility, permeability and metabolicstability.
Complex challenges such as metabolicstability or absorption, distribution, metabolism or excretion (ADME) properties could be better predicted, accurately filtering out poor candidates and streamlining discovery. He has published 22 scientific articles and has a h-index of 13. Matthew is a chartered chemist.
I'll examine an article entitled ‘Mapping the Efficiency and Physicochemical Trajectories of Successful Optimizations’ (YL2018) in this post and I should note that the article title reminded me that abseiling has been described as the second fastest way down the mountain.
Not only this, the reduction in rotatable bonds and consequent reduction in susceptibility to metabolism is an additional benefit [4]. The resulting macrocyclic structure was found to be associated with improved metabolicstability and low propensity for P-gp efflux compared to the acyclic analog [13]. Balazs et al.,
Not only this, the reduction in rotatable bonds and consequent reduction in susceptibility to metabolism is an additional benefit [4]. The resulting macrocyclic structure was found to be associated with improved metabolicstability and low propensity for P-gp efflux compared to the acyclic analog [13]. Balazs et al.,
Review articles 2023 was a bit of a mixed bag for AI in drug discovery. Prospective Validation of Machine Learning Algorithms for Absorption, Distribution, Metabolism, and Excretion Prediction: An Industrial Perspective [link] One of my favorite papers of 2023 provided a tour de force in method comparison.
Cyclic Peptide Design, Chapter 2: Strategies to Enhance MetabolicStabilities. Cyclic peptides in pipeline: What future for these great molecules? Pharmaceuticals , 16(7):996, 2023. Khatri B, Nuthakki VR, Chatterjee J. Springer, 2019. Jain AN, Cleves AE, Gao Q, et al. Journal of Computer-Aided Molecular Design , 33:531558, 2019.
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