AIMC Topic: Structure-Activity Relationship

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Machine learning assisted design of highly active peptides for drug discovery.

PLoS computational biology
The discovery of peptides possessing high biological activity is very challenging due to the enormous diversity for which only a minority have the desired properties. To lower cost and reduce the time to obtain promising peptides, machine learning ap...

Systematic artifacts in support vector regression-based compound potency prediction revealed by statistical and activity landscape analysis.

PloS one
Support vector machines are a popular machine learning method for many classification tasks in biology and chemistry. In addition, the support vector regression (SVR) variant is widely used for numerical property predictions. In chemoinformatics and ...

Types and effects of protein variations.

Human genetics
Variations in proteins have very large number of diverse effects affecting sequence, structure, stability, interactions, activity, abundance and other properties. Although protein-coding exons cover just over 1 % of the human genome they harbor an di...

Three- and four-class classification models for P-glycoprotein inhibitors using counter-propagation neural networks.

SAR and QSAR in environmental research
P-glycoprotein (P-gp) is an ATP binding cassette (ABC) transporter that helps to protect several certain human organs from xenobiotic exposure. This efflux pump is also responsible for multi-drug resistance (MDR), an issue of the chemotherapy approac...

Active-learning strategies in computer-assisted drug discovery.

Drug discovery today
High-throughput compound screening is time and resource consuming, and considerable effort is invested into screening compound libraries, profiling, and selecting the most promising candidates for further testing. Active-learning methods assist the s...

Discovery of novel GluN1/GluN3A NMDA receptor inhibitors using a deep learning-based method.

Acta pharmacologica Sinica
Ligand-based drug discovery methods typically utilize pharmacophore similarities among molecules to screen for potential active compounds. Among these, scaffold hopping is a widely used ligand-based lead identification strategy that facilitates clini...

A deep learning model for structure-based bioactivity optimization and its application in the bioactivity optimization of a SARS-CoV-2 main protease inhibitor.

European journal of medicinal chemistry
Bioactivity optimization is a crucial and technical task in the early stages of drug discovery, traditionally carried out through iterative substituent optimization, a process that is often both time-consuming and expensive. To address this challenge...

Discovery of naturally inspired antimicrobial peptides using deep learning.

Bioorganic chemistry
Non-ribosomal peptides (NRPs) are promising lead compounds for novel antibiotics. Bioinformatic mining of silent microbial NRPS gene clusters provide crucial insights for the discovery and de novo design of bioactive peptides. Here, we describe the e...

Machine Learning Accelerated Discovery of Antimicrobial Inorganic Nanomaterials.

The journal of physical chemistry letters
The growing prevalence of infectious diseases and the increasing threat of bacterial resistance have drawn widespread attention to antimicrobial inorganic nanomaterials. However, the diversity, abundance, and complex mechanisms of these materials pre...

Dumpling GNN: Hybrid GNN Enables Better ADC Payload Activity Prediction Based on the Chemical Structure.

International journal of molecular sciences
Antibody-drug conjugates (ADCs) are promising cancer therapeutics, but optimizing their cytotoxic payloads remains challenging. We present DumplingGNN, a novel hybrid Graph Neural Network architecture for predicting ADC payload activity and toxicity....