Target-aware latent diffusion model for design of apoptosis-inducing anticancer peptides

Tiara Natasha Binte Sayuti1, Kakuly Mittal1, Tan Lai Heng2

  • 1College of Computing and Data Science, Nanyang Technological University, 50 Nanyang Ave, 639798, Singapore.

PubMed

Insights

We developed a target-aware latent diffusion model (T-LDM) to design anticancer peptides. This approach improves peptide design by considering the B-cell lymphoma-extra large (BCL-xL) protein

Area of Science:

  • Computational chemistry and drug discovery
  • Bioinformatics and structural biology
  • Oncology therapeutics

Background:

  • Therapeutic peptide design is challenging due to chemical diversity and flexibility.
  • B-cell lymphoma-extra large (BCL-xL) is a key anti-apoptotic target in cancer.
  • Current generative models lack detailed receptor structural context.

Purpose of the Study:

  • To present a target-aware latent diffusion framework (T-LDM) for designing anticancer peptides.
  • To condition peptide generation on specific receptor pocket structural information.
  • To improve the biological plausibility and target specificity of designed peptides.

Main Methods:

  • Developed a target-aware latent diffusion framework (T-LDM).
  • Conditioned sequence denoising on receptor pocket context using graph-based structural models.
  • Fused conditioning into a U-Net denoiser via modulation and cross-attention.
  • Evaluated peptide properties using Jensen-Shannon divergence, perplexity, BLEU, and protein-peptide docking.

Main Results:

  • T-LDM generates peptides that are syntactically fluent and physicochemically realistic.
  • Explicit pocket conditioning enhances compatibility with the BCL-xL target.
  • The model maintains peptide diversity and novelty.
  • Ablation studies confirmed the benefit of pocket-aware guidance.

Conclusions:

  • Target-aware latent diffusion models offer a promising approach for rational peptide drug design.
  • Conditioning generative models on structural context improves therapeutic potential.
  • This framework advances the design of targeted peptide therapeutics for oncology.

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