Drug-induced liver injury (DILI) is a major challenge in drug development, often leading to clinical trial failures and market withdrawals due to liver toxicity. This study presents StackDILI, a computational framework designed to accelerate toxicity assessment by predicting DILI risk. StackDILI integrates multiple molecular descriptors to extract structural and physicochemical features, including the constitution, pharmacophore, MACCS, and E-state descriptors. Additionally, a genetic algorithm is employed for feature selection and optimization, ensuring that the most relevant features are used. These optimized features are processed through a stacking ensemble model comprising multiple tree-based machine learning models, improving prediction accuracy and interpretability. Notably, StackDILI demonstrates a strong performance on the DILIrank test set and maintains robustness across cross-validation. Moreover, interpretability analysis reveals key molecular features associated with DILI risks, providing valuable insights into toxicity prediction. To further improve accessibility, a user-friendly web interface is developed, allowing users to input SMILES strings and receive rapid predictions with ease. The StackDILI model provides a powerful tool for efficient DILI assessment, supporting safer drug development. The web interface is accessible at https://awi.cuhk.edu.cn/biosequence/StackDILI/.
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http://dx.doi.org/10.1021/acs.jcim.4c02079 | DOI Listing |
Zhonghua Gan Zang Bing Za Zhi
December 2024
With the widespread application of systemic treatments for hepatocellular carcinoma, liver injury caused by molecular targeted drugs and immune checkpoint inhibitors has become a common clinical problem. The Chinese Society of Hepatology organized relevant domestic experts to summarize and analyze the adverse liver reactions and diagnosis and treatment progress related to systemic treatment of liver cancer at home and abroad, and formulated the "Consensus on the management of liver injury associated with targeted drugs and immune checkpoint inhibitors for hepatocellular carcinoma," aiming to provide reasonable suggestions and decision-making references for clinical physicians in liver disease and related specialties in the monitoring, diagnosis, prevention and treatment of liver injury during the treatment of targeted drugs and immune checkpoint inhibitors for hepatocellular carcinoma, so as to enable more liver cancer patients to benefit from targeted immune therapy.
View Article and Find Full Text PDFAnal Chem
January 2025
College of Chemistry, Jilin Province Research Center for Engineering and Technology of Spectral Analytical Instruments, Jilin University, Qianjin Street 2699, Changchun 130012, China.
Vanin-1 is a pantetheine hydrolase that plays a key role in inflammatory diseases. Effective tools for noninvasive, real-time monitoring of Vanin-1 are lacking, largely due to background fluorescence interference in existing probes. To address this issue, we developed a dual-modal fluorescent and colorimetric probe, MB-Van1, to detect Vanin-1 with high sensitivity and selectivity.
View Article and Find Full Text PDFJ Chem Inf Model
January 2025
Kobilka Institute of Innovative Drug Discovery, School of Medicine, The Chinese University of Hong Kong, Shenzhen, 2001 Longxiang Road, 518172 Shenzhen, China.
Drug-induced liver injury (DILI) is a major challenge in drug development, often leading to clinical trial failures and market withdrawals due to liver toxicity. This study presents StackDILI, a computational framework designed to accelerate toxicity assessment by predicting DILI risk. StackDILI integrates multiple molecular descriptors to extract structural and physicochemical features, including the constitution, pharmacophore, MACCS, and E-state descriptors.
View Article and Find Full Text PDFToxicol Sci
January 2025
Takeda Development Center Americas, Inc, Cambridge, MA, USA.
The frequency of drug-induced liver injury (DILI) in clinical trials remains a challenge for drug developers despite advances in human hepatotoxicity models and improvements in reducing liver-related attrition in preclinical species. TAK-994, an oral orexin receptor 2 agonist, was withdrawn from phase II clinical trials due to the appearance of severe DILI. Here, we investigate the likely mechanism of TAK-994 DILI in hepatic cell culture systems examined cytotoxicity, mitochondrial toxicity, impact on drug transporter proteins, and covalent binding.
View Article and Find Full Text PDFCureus
January 2025
Genetics Clinic, Karaiskakio Foundation, Nicosia, CYP.
Metabolic-dysfunction-associated steatotic liver disease (MASLD) is the most common chronic liver disease in the Western world. MASLD-associated cirrhosis prevalence is on the rise along with the obesity and metabolic syndrome epidemic. Genetic factors are included in the multi-hit model of MASLD pathogenesis and insulin-like growth factor-1 (IGF-1) has an important role.
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