AIMC Topic: Structure-Activity Relationship

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Discovery of Novel 4,5-Dihydropyrrolo[3,4-]pyrazol-6()-one-Based Tubulin Inhibitors Targeting Colchicine Binding Site with Potent Anti-Ovarian Cancer Activity.

Journal of medicinal chemistry
To address the toxicity of current microtubule inhibitors, we employed the GeminiMol deep learning model to screen the Zinc20 database, identifying a novel 4,5-dihydropyrrolo[3,4-]pyrazol-6(2)-one scaffold () targeting the colchicine binding site. Su...

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 ...

MolAI: A Deep Learning Framework for Data-Driven Molecular Descriptor Generation and Advanced Drug Discovery Applications.

Journal of chemical information and modeling
This study introduces MolAI, a robust deep learning model designed for data-driven molecular descriptor generation. Utilizing a vast training data set of 221 million unique compounds, MolAI employs an autoencoder neural machine translation model to g...

Separation, characterization, AI screening, and bioactivities of marine bioactive peptides: A review.

Food chemistry
Marine bioactive peptides (MBPs) are short-chain amino acid polymers derived from marine sources that possess specific physiological activities. Owing to their unique origins and structural diversity, MBPs have attracted considerable research interes...

Bacterial polysaccharides in the food industry: Synthesis-structure-properties relationships, AI-driven innovations, regulatory challenges, and bioeconomy prospects.

Carbohydrate polymers
Bacterial polysaccharides have attracted considerable interest due to their rapid production, customizable properties, and suitability for large-scale manufacturing. Unlike plant or algal polysaccharides, they can be efficiently synthesized through f...

Knowledge and Structure-Based Drug Design of 15-PGDH Inhibitors.

Journal of medicinal chemistry
PGE2 plays important roles in immune cell function and in potentiating tissue regeneration. 15-PGDH is the key enzyme involved in inactivation of PGE2 and its inhibition therefore provides valuable therapeutic opportunity. We have solved the first co...

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...

Protein Structure-Function Relationship: A Kernel-PCA Approach for Reaction Coordinate Identification.

Journal of chemical theory and computation
In this study, we propose a Kernel-PCA model designed to capture structure-function relationships in a protein. This model also enables the ranking of reaction coordinates according to their impact on protein properties. By leveraging machine learnin...

Machine-Learning-Driven Discovery of -Phenylbenzenesulfonamides as a Novel Chemotype for Lactate Dehydrogenase A Inhibition with Anti-Pancreatic Cancer Activity.

Journal of medicinal chemistry
Lactate dehydrogenase A (LDHA) is a promising target for cancer therapy due to its crucial role in aerobic glycolysis. Despite extensive efforts, the structural diversity of LDHA inhibitors remains limited. Here, we utilized machine learning techniqu...

Decoding tissue complexity: multiscale mapping of chemistry-structure-function relationships through advanced visualization technologies.

Journal of materials chemistry. B
Comprehensively acquiring biological tissue information is pivotal for advancing our understanding of biological systems, elucidating disease mechanisms, and developing innovative clinical strategies. Biological tissues, as nature's archetypal biomat...