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Updated: Jan 11, 2026

Establishing Cell Lines Overexpressing DR3 to Assess the Apoptotic Response to Anti-mitotic Therapeutics
Published on: January 11, 2019
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.
Abstract:
Therapeutic peptides offer high specificity and low toxicity, but rational design remains difficult due to their vast chemical diversity and conformational flexibility. In oncology, B-cell lymphoma-extra large (BCL-xL), a key anti-apoptotic protein, is overexpressed in various cancers, making it an important target for peptide-based therapeutics. Existing generative models for anticancer peptide design often neglect detailed receptor structural context, limiting biological plausibility. We present a target-aware latent diffusion framework (T-LDM) that conditions sequence denoising on receptor pocket context encoded by a graph-based structural model. Conditioning is fused into the U-Net denoiser via lightweight modulation and cross attention, enabling the Latent Diffusion Model to align sampling with the local interaction topology of the binding groove while preserving protein language model priors. We evaluate distributional calibration with Jensen-Shannon divergence across key physicochemical properties, sequence quality with perplexity, motif overlap with BLEU, and structural compatibility via protein-peptide docking. A controlled ablation was performed that varies the scope of structural conditioning (none, global, pocket) and the fusion into the denoiser, letting us assess the marginal effect of pocket-aware guidance and fusion on generation quality. Overall, the study indicates that explicit pocket conditioning yields peptides that are syntactically fluent, physicochemically realistic, and more compatible with the intended BCL-xL target, while maintaining diversity and novelty. Source code is available at https://github.com/tiaranatashasayuti/T-LDM.
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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