Integrating Molecular Dynamics and Generative Modeling for Cryptic Pocket Drug Discovery
Abstract
Identifying cryptic pockets and designing ligands that selectively target them could enable safer, more effective drugs. However, this remains a challenge for both traditional physics-based methods, which are computationally expensive, and machine learning approaches, which are constrained by limited training data. Recent flow-matching methods for pocket-conditioned ligand generation have shown promise when the binding pocket is known a priori, but it remains unclear how atomistic molecular dynamics (MD) can be incorporated to improve ligand design. We present a work-in-progress framework that couples MD sampling with a pre-trained generative model to identify relevant pocket conformations, guide ligand generation, and validate generated candidates. Applied to a known cryptic site in KRAS, the workflow produces chemically diverse candidates and identifies stable molecules for subsequent refinement. This provides a modular route toward iterative, simulation-guided molecular design in which generative models and physics-based tools can be composed in a closed loop.