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Receptors, Cytoplasmic and Nuclear

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Oleanolic acid protects against pathogenesis of atherosclerosis, possibly via FXR-mediated angiotensin (Ang)-(1-7) upregulation.

Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie
Atherosclerosis, the leading cause of cardiovascular diseases in the world, is a chronic inflammatory disorder characterized by the dysfunction of arteries. Oleanolic acid (OA) is a bioactive nature product which exists in various plants and herbs. P...

Development of pharmacophore-based classification model for activators of constitutive androstane receptor.

Drug metabolism and pharmacokinetics
Constitutive androstane receptor (CAR) is predominantly expressed in the liver and is important for regulating drug metabolism and transport. Despite its biological importance, there have been few attempts to develop in silico models to predict the a...

Identification of New Fungal Peroxisomal Matrix Proteins and Revision of the PTS1 Consensus.

Traffic (Copenhagen, Denmark)
The peroxisomal targeting signal type 1 (PTS1) is a seemingly simple peptide sequence at the C-terminal end of most peroxisomal matrix proteins. PTS1 can be described as a tripeptide with the consensus motif [S/A/C] [K/R/H] L. However, this descripti...

Modern drug design: the implication of using artificial neuronal networks and multiple molecular dynamic simulations.

Journal of computer-aided molecular design
We report the implementation of molecular modeling approaches developed as a part of the 2016 Grand Challenge 2, the blinded competition of computer aided drug design technologies held by the D3R Drug Design Data Resource ( https://drugdesigndata.org...

Chemogenomic Active Learning's Domain of Applicability on Small, Sparse qHTS Matrices: A Study Using Cytochrome P450 and Nuclear Hormone Receptor Families.

ChemMedChem
Computational models for predicting the activity of small molecules against targets are now routinely developed and used in academia and industry, partially due to public bioactivity databases. While models based on bigger datasets are the trend, rec...

Mathematical deep learning for pose and binding affinity prediction and ranking in D3R Grand Challenges.

Journal of computer-aided molecular design
Advanced mathematics, such as multiscale weighted colored subgraph and element specific persistent homology, and machine learning including deep neural networks were integrated to construct mathematical deep learning models for pose and binding affin...

Prediction of Farnesoid X Receptor Disruptors with Machine Learning Methods.

Chemical research in toxicology
The farnesoid X receptor (FXR) emerges as a promising drug target involved in regulating various metabolic pathways, yet some xenobiotic compounds binding to FXR would be an important determinant to induce the receptor dysfunctions that lead to undes...