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Protein Kinase Inhibitors

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Discovery of New HER2 Inhibitors via Computational Docking, Pharmacophore Modeling, and Machine Learning.

Molecular informatics
The human epidermal growth factor receptor 2 (HER2) is a critical oncogene implicated in the development of various aggressive cancers, particularly breast cancer. Discovering novel HER2 inhibitors is crucial for expanding therapeutic options for HER...

Explainable machine learning prediction of edema adverse events in patients treated with tepotinib.

Clinical and translational science
Tepotinib is approved for the treatment of patients with non-small-cell lung cancer harboring MET exon 14 skipping alterations. While edema is the most prevalent adverse event (AE) and a known class effect of MET inhibitors including tepotinib, there...

How Artificial Intelligence Unravels the Complex Web of Cancer Drug Response.

Cancer research
The intersection of precision medicine and artificial intelligence (AI) holds profound implications for cancer treatment, with the potential to significantly advance our understanding of drug responses based on the intricate architecture of tumor cel...

An ensemble machine learning model generates a focused screening library for the identification of CDK8 inhibitors.

Protein science : a publication of the Protein Society
The identification of an effective inhibitor is an important starting step in drug development. Unfortunately, many issues such as the characterization of protein binding sites, the screening library, materials for assays, etc., make drug screening a...

Identification of novel CDK2 inhibitors by a multistage virtual screening method based on SVM, pharmacophore and docking model.

Journal of enzyme inhibition and medicinal chemistry
Cyclin-dependent kinase 2 (CDK2) is the family of Ser/Thr protein kinases that has emerged as a highly selective with low toxic cancer therapy target. A multistage virtual screening method combined by SVM, protein-ligand interaction fingerprints (PLI...

PTML Modeling for Alzheimer's Disease: Design and Prediction of Virtual Multi-Target Inhibitors of GSK3B, HDAC1, and HDAC6.

Current topics in medicinal chemistry
BACKGROUND: Alzheimer's disease is characterized by a progressive pattern of cognitive and functional impairment, which ultimately leads to death. Computational approaches have played an important role in the context of drug discovery for anti-Alzhei...

Machine learning-based chemical binding similarity using evolutionary relationships of target genes.

Nucleic acids research
Chemical similarity searching is a basic research tool that can be used to find small molecules which are similar in shape to known active molecules. Despite its popularity, the retrieval of local molecular features that are critical to functional ac...

Inhibition activity prediction for a dataset of candidates' drug by combining fuzzy logic with MLR/ANN QSAR models.

Chemical biology & drug design
A hybrid of artificial intelligence simple and low computational cost QSAR was used. Approximately 90 pyridinylimidazole-based drug candidates with a range of potencies against p38R MAP kinase were investigated. To obtain more flexibility and effecti...