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July 6, 2026Journal of Medicinal Chemistry

Discovery of a Potent NAMPT-Targeting PROTAC for the Suppression of Triple-Negative Breast Cancer via Macrophage Reprogramming

Yingqi Song Chengjie Yang Qingjun Li Shijie Huang Shaojie Chen Zhewei Xia Xiaojun Yao Chunquan Sheng Guoqiang Dong

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Key Points

The aim is to evaluate the effects of NAMPT-targeting PROTAC on tumor growth and metastasis in triple-negative breast cancer.
Significant tumor growth inhibition observed (TGI = 82.7%) with low toxicity reported.
Investigated the role of macrophage reprogramming in tumor suppression.
Evaluated the impact on lung metastasis alongside primary tumor growth.
NAMPT degradation leads to an 82.7% reduction in tumor growth.
Effective suppression of lung metastasis was noted without obvious toxicity.
Identified as a promising lead compound for future therapeutic strategies.

Implication

Demonstrates tumor growth inhibition in triple-negative breast cancer, suggesting a new treatment strategy.

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Cite This Study

Song et al. (2026) studied this question.

synapsesocial.com/papers/6a4de976d2ea289ef6283a85 https://doi.org/10.1021/acs.jmedchem.6c00454

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Keep reading

Synapse has enriched 5 closely related papers on similar clinical questions. Consider them for comparative context:

1Development of PROTACs Targeting the Moonlighting Enzyme Nicotinamide Phosphoribosyltransferase (NAMPT) for Breast Cancer TherapyOriginal Research · 2026 · 2 citations
2Mixed Lineage Kinase Suppression in Triple-Negative Breast Cancer: Identification of a Dual Inhibitor Targeting MLK3 and NAMPTOriginal Research · 2026 · 1 citations
3Translational Research on the Oral Delivery of the Cytotoxic PROTAC Molecule via Tumor-Targeting Prodrug Strategy for Triple-Negative Breast Cancer Treatment.2025 · 4 citations
4PROTACs Targeting Molecular Targets in Triple-Negative Breast Cancer2025 · 1 citations
5Abstract 7151: Targeting metabolic pathway in triple negative breast cancer with a small molecule inhibitor2024