Expansive discovery of chemically diverse structured macrocyclic oligoamides

PJ Salveson, AP Moyer, MY Said, G Gӧkçe, X Li… - Science, 2024 - science.org
Small macrocycles with four or fewer amino acids are among the most potent natural
products known, but there is currently no way to systematically generate such compounds …

[HTML][HTML] Generation of 3D molecules in pockets via a language model

W Feng, L Wang, Z Lin, Y Zhu, H Wang… - Nature Machine …, 2024 - nature.com
Generative models for molecules based on sequential line notation (for example, the
simplified molecular-input line-entry system) or graph representation have attracted an …

[HTML][HTML] Complex peptide macrocycle optimization: combining NMR restraints with conformational analysis to guide structure-based and ligand-based design

AN Jain, AC Brueckner, C Jorge, AE Cleves… - Journal of Computer …, 2023 - Springer
Systematic optimization of large macrocyclic peptide ligands is a serious challenge. Here,
we describe an approach for lead-optimization using the PD-1/PD-L1 system as a …

Lingo3dmol: Generation of a pocket-based 3d molecule using a language model

L Wang, Z Lin, Y Zhu, R Bai, W Feng, H Wang… - arXiv preprint arXiv …, 2023 - arxiv.org
Structure-based drug design powered by deep generative models have attracted increasing
research interest in recent years. Language models have demonstrated a robust capacity for …

Unmasking the True Identity of Rapamycin's Minor Conformer

EB Crull, AN Jain, PCD Hawkins… - Journal of Natural …, 2023 - ACS Publications
Rapamycin, a well-known macrocyclic natural product with myriad biological activities, has
been the subject of intense study since its first isolation and characterization over five …

[HTML][HTML] Exploring protein–ligand binding affinity prediction with electron density-based geometric deep learning

C Isert, K Atz, S Riniker, G Schneider - RSC advances, 2024 - pubs.rsc.org
Rational structure-based drug design relies on accurate predictions of protein–ligand
binding affinity from structural molecular information. Although deep learning-based …