AIMC Topic: Dose-Response Relationship, Drug

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Drug repurposing identifies novel Wee1 kinase inhibitors for triple negative breast cancer therapeutics.

European journal of medicinal chemistry
Triple-negative breast cancer (TNBC) is an aggressive subtype of breast cancer with limited treatment options. Wee1 kinase, a critical regulator of the G2/M checkpoint and DNA replication, is a promising therapeutic target. However, dose dependent as...

4-Hydroxy-2,5-dihydrothiazole derivatives as a new class of small-molecule antibiotics for MRSA: AI-integrated design, chemical synthesis and biological evaluation.

European journal of medicinal chemistry
Staphylococcus aureus (S. aureus) is one of the most concerned Gram-positive bacteria due to its resistance to the commonly used antibiotics, methicillin. To address the threat of methicillin-resistant S. aureus (MRSA), new classes of antibiotics are...

Identification of a novel Aurora B inhibitor using the AI-driven drug screening and docking-based traditional screening.

Bioorganic & medicinal chemistry
Aurora B, a subtype of Aurora kinases that functions as a serine/threonine kinase, playing a vital role in the process of mitosis, is often overexpressed in certain tumor cells leading to tumorigenesis and progression. Therefore, the development of s...

PyaiVS unifies AI workflows to accelerate ligand discovery and yields ABCG2 inhibitors.

European journal of medicinal chemistry
Developing optimized AI models for virtual screening requires coordinated selection of algorithms, molecular representations, and data splitting strategies, yet lacks integrated tools. We present PyaiVS, a Python package that integrates nine machine ...

A dual-view deep learning-driven discovery of cinnamoyl anthranilic acid derivatives against orthopoxvirus through targeting host ITGB3.

European journal of medicinal chemistry
The orthopoxvirus genus, particularly the monkeypox virus (MPXV), continues to pose a significant global public health threat. Therefore, the development of novel anti-orthopoxvirus agents remains an urgent priority. Machine learning has proven to be...

Prediction of High-Dose Methotrexate Blood Concentration in Osteosarcoma Patients Using Machine Learning.

Drug design, development and therapy
INTRODUCTION: High-dose methotrexate is a typical chemotherapy that is widely used in the treatment of osteosarcoma. However, the unique dose-response relationship of methotrexate makes its treatment window relatively narrow, and its clinical use is ...

Toxicological evaluation of Artocarpus lacucha ethyl acetate extract: in vitro and in vivo assessment.

Journal of ethnopharmacology
ETHNOPHARMACOLOGICAL RELEVANCE: Artocarpus lacucha Buch. -Ham. (syn. Artocarpus lakoocha) (A. lacucha), is a tropical fruit tree and a member of the Moraceae family. Fruit, bark, foliage, and roots of A. lacucha are broadly utilized in folklore medic...

The efficacy and toxicity equilibrium of emodin for liver injury: A bidirectional meta-analysis and machine learning.

Phytomedicine : international journal of phytotherapy and phytopharmacology
BACKGROUND: Emodin, a hepatoprotective agent derived from various herbs, exhibits dual effects on liver injury, necessitating further investigation into its therapeutic and toxic properties. Traditional meta-analyses lack predictive capability for do...

Safety assessment of the ethanolic extract of Siparuna guianensis: Cell viability, molecular risk predictions and toxicity risk for acute and sub-chronic oral ingestion.

Journal of ethnopharmacology
ETHNOPHARMACOLOGICAL RELEVANCE: The species Siparuna guianensis Aublet (family Siparunaceae) is traditionally used by indigenous peoples and riverine communities in Central and South America to treat migraines, flu, respiratory diseases, fever, pain,...