MARD-Mol: A Hybrid Autoregressive-Diffusion Paradigm for Coarse-Grained Molecular Modeling

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ID: 324299
2026
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Abstract
MOTIVATION: Deep generative models have transformed drug molecule generation. However, molecules exhibit complex hierarchical structures, requiring models to simultaneously balance macroscopic topological coherence and microscopic chemical self-consistency. Although autoregressive and discrete diffusion paradigms are highly complementary, integrating their advantages within a unified architecture remains severely limited by traditional "atom-by-atom" fine-grained modeling. RESULTS: We propose MARD-Mol, a hybrid autoregressive-diffusion framework based on motif-inspired units. By elevating the representation granularity from atoms to motif-inspired units and introducing a dual-stream hierarchical attention mechanism, it couples inter-unit autoregressive global scaffold planning with intra-unit discrete diffusion generation. To support goal-directed drug discovery, we reformulate property optimization into an iterative "diagnose-and-repair" process, enabling targeted optimization of defective motifs while preserving the global scaffold. Extensive experiments demonstrate that MARD-Mol achieves an 86.0% Quality score in de novo generation and exhibits superior performance in fragment-constrained and multi-objective optimization, establishing a new paradigm for high-quality drug design. AVAILABILITY AND IMPLEMENTATION: The source code and datasets used in this study are available at GitHub: https://github.com/CSUBioGroup/MARD-Mol.
Reference Key
openalex_W7196934256 Use this key to autocite in the manuscript while using SciMatic Manuscript Manager or Thesis Manager
Authors Sizhe Zhang, Gang Luo, Wei Fan, Xiaoyi Lv, Min Li
Journal BMC Bioinformatics
Year 2026
DOI
10.1093/bioinformatics/btag586
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