AI Medical Compendium Topic:
Ligands

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Increase Docking Score Screening Power by Simple Fusion With CNNscore.

Journal of computational chemistry
Scoring functions (SFs) of molecular docking is a vital component of structure-based virtual screening (SBVS). Traditional SFs yield their inherent shortage for idealized approximations and simplifications predicting the binding affinity. Complementa...

Deep learning in GPCR drug discovery: benchmarking the path to accurate peptide binding.

Briefings in bioinformatics
Deep learning (DL) methods have drastically advanced structure-based drug discovery by directly predicting protein structures from sequences. Recently, these methods have become increasingly accurate in predicting complexes formed by multiple protein...

canSAR 2024-an update to the public drug discovery knowledgebase.

Nucleic acids research
canSAR (https://cansar.ai) continues to serve as the largest publicly available platform for cancer-focused drug discovery and translational research. It integrates multidisciplinary data from disparate and otherwise siloed public data sources as wel...

Combining Machine Learning and Electrophysiology for Insect Odorant Receptor Studies.

Methods in molecular biology (Clifton, N.J.)
Insects rely on olfaction in many aspects of their life, and odorant receptors are key proteins in this process. Whereas a plethora of insect odorant receptor sequences is available, most of them are still orphan or uncompletely characterized, since ...

SG-ML-PLAP: A structure-guided machine learning-based scoring function for protein-ligand binding affinity prediction.

Protein science : a publication of the Protein Society
Computational methods to predict binding affinity of protein-ligand complex have been used extensively to design inhibitors for proteins selected as drug targets. In recent years machine learning (ML) is being increasingly used for design of drugs/in...

Leveraging Artificial Intelligence in GPCR Activation Studies: Computational Prediction Methods as Key Drivers of Knowledge.

Methods in molecular biology (Clifton, N.J.)
G protein-coupled receptors (GPCRs) are key molecules involved in cellular signaling and are attractive targets for pharmacological intervention. This chapter is designed to explore the range of algorithms used to predict GPCRs' activation states, wh...

Ligand identification in CryoEM and X-ray maps using deep learning.

Bioinformatics (Oxford, England)
MOTIVATION: Accurately identifying ligands plays a crucial role in the process of structure-guided drug design. Based on density maps from X-ray diffraction or cryogenic-sample electron microscopy (cryoEM), scientists verify whether small-molecule li...

Large-scale prediction of biological activities with Active-IT system.

Biomeditsinskaia khimiia
Traditional testing methods in pharmaceutical development can be time-consuming and costly, but in silico evaluation tools can offer a solution. Our in-house Active-IT system, a Ligand-Based Virtual Screening (LBVS) tool, was developed to predict the...

DiffPROTACs is a deep learning-based generator for proteolysis targeting chimeras.

Briefings in bioinformatics
PROteolysis TArgeting Chimeras (PROTACs) has recently emerged as a promising technology. However, the design of rational PROTACs, especially the linker component, remains challenging due to the absence of structure-activity relationships and experime...

Machine learning-assisted substrate binding pocket engineering based on structural information.

Briefings in bioinformatics
Engineering enzyme-substrate binding pockets is the most efficient approach for modifying catalytic activity, but is limited if the substrate binding sites are indistinct. Here, we developed a 3D convolutional neural network for predicting protein-li...