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In this study, we introduce a novel approach for predicting two key drug properties, blood-brain barrier (BBB) permeability and human intestinal absorption via Caco-2 permeability. Our methodology centers around a specialized neural network, the atom transformer-based Message Passing Neural Network (MPNN), which we have combined with contrastive learning techniques to enhance the process of representing and embedding molecular structures for more accurate property prediction. These innovative models focus on predicting BBB and Caco-2 permeability -two critical factors in drug absorption and distribution- which fall under the broader scope of ADMET (absorption, distribution, metabolism, excretion, and toxicity) properties. The models are readily accessible online through the Enalos Cloud Platform which offers a user-friendly, AI-powered, ready-to-use web service that significantly streamlines the drug design process, enabling users to easily predict and understand the behavior of potential drug compounds within the human body.Scientific Contribution Our study combines an atom-attention Message Passing Neural Network (AA-MPNN) with contrastive learning (CL), which significantly improves predictive accuracy. Our model leverages self-supervised learning to expand the chemical space used in training and self-attention mechanisms to focus on critical molecular features, enhancing both model accuracy and interpretability. Additionally, the ready-to-use web service based on our model democratizes access to predictive tools for the scientific and regulatory communities.
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http://dx.doi.org/10.1186/s13321-025-01007-2 | DOI Listing |
Arch Toxicol
September 2025
Department of Toxicology, Faculty of Medicine, Collegium Medicum, Rzeszów University, Al. mjr. W. Kopisto 2a, 35-959, Rzeszow, Poland.
ACP-105 (CAS: 1048998-11-3) is a novel non-steroidal selective androgen receptor modulator (SARM), increasingly detected in anti-doping analyses, yet lacking a comprehensive ADME profile. This study provides the first integrative in silico characterization of ACP-105's ADME properties using seven independent methods (ADMETlab 3.0, ADMET Predictor 12.
View Article and Find Full Text PDFJ Cell Mol Med
September 2025
Department of Obstetrics and Gynecology, Second Hospital of Shanxi Medical University, Taiyuan, Shanxi, China.
This study aims to assess whether endometriosis causally increases the risk of IBD through Mendelian randomisation (MR) analysis and to elucidate potential mechanisms using in vitro experiments. A two-sample Mendelian randomisation (MR) analysis was conducted using genome-wide association study datasets for endometriosis and IBD, including ulcerative colitis and Crohn's disease. Causal inference was assessed using inverse variance weighting, MR-Egger, and weighted median methods, with MR-PRESSO used to detect horizontal pleiotropy.
View Article and Find Full Text PDFJ Med Chem
September 2025
Center for Marine Biotechnology and Biomedicine, Scripps Institution of Oceanography, University of California San Diego, La Jolla, California 92093, United States.
Proteasome inhibitors are effective in treating hematologic cancers but have limited utility in brain tumors due to poor blood-brain barrier (BBB) penetration and metabolic instability. In this study, we developed novel macrocyclic peptide epoxyketone inhibitors with improved drug-like properties. Compounds were screened for cytotoxicity against brain cancer cell lines, permeability (PAMPA-BBB and Caco-2), and metabolic stability.
View Article and Find Full Text PDFSAR QSAR Environ Res
August 2025
Laboratory of Drug Design and Discovery, Department of Pharmaceutical Technology, Jadavpur University, Kolkata, India.
Evaluating the permeability of different molecular structures across the Caco-2 cell line is crucial for drug discovery and development. The present study primarily focuses on developing machine learning-based multiclass classification models for predicting the permeability of molecules across the Caco-2 cell line. However, the class imbalance in permeability datasets poses a significant challenge for developing predictive models in the case of multiclass analysis.
View Article and Find Full Text PDFJ Appl Toxicol
September 2025
The Procter & Gamble Company, Cincinnati, USA.
The in vitro intestinal permeability of straight- and branched-chain parabens has not been extensively investigated. Sixteen parabens were tested in the Caco-2 assay. Passive diffusion was measured using PAMPA.
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