GX-BP1: Targeting SOX2 to Prevent Resistance in mCRPC

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GX-BP1, a bioPROTAC-based SOX2 degrader, selectively targets SOX2, an undruggable protein, for ubiquitin-proteasome elimination, overcoming limitations of prior inhibition strategies. In preclinical models, GX-BP1 monotherapy delivered approximately 70% tumor growth inhibition, while combinations with agents like carboplatin/paclitaxel achieved 87-96% inhibition and near-complete tumor suppression at optimal doses. Notably, GX-BP1 paired with osimertinib eradicated cancer stem […]

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ITRI-148: A Next-Generation AR Degrader Targeting Resistance at Its Core

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A new experimental compound, ITRI-148, may represent a meaningful shift in how advanced prostate cancer is treated, particularly in patients who develop resistance to current androgen receptor (AR)-targeted therapies. Resistance to drugs like enzalutamide is frequently driven by AR splice variants such as AR-V7, which lack the ligand-binding domain (LBD) targeted by existing therapies, allowing […]

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A nano-PROTAC on the horizon: combining targeted protein degradation and ferroptosis for advanced prostate cancer

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A new study from Wuhan University and the Renmin Hospital of Wuhan University has reported a promising preclinical strategy for advanced prostate cancer, especially castration-resistant prostate cancer (CRPC). The work was published online in Angewandte Chemie International Edition, one of the leading international journals in chemistry. The study describes a new nano-PROTAC platform designed to […]

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CBPD‑409, an Oral CBP/p300 Degrader for Advanced Prostate Cancer

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CBPD‑409 is an experimental, oral medicine designed to remove two helper proteins, CBP and p300, that prostate tumors use to turn cancer‑driving genes on. These proteins partner with the androgen receptor (AR), the key signal that fuels most prostate cancers, especially in the advanced, treatment‑resistant setting. By tagging CBP and p300 for destruction, a strategy […]

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Self-Assembled Nano-PROTAC to Improve Targeted Therapy in Castration-Resistant Prostate Cancer

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A new study published in Nature Signal Transduction and Targeted Therapy reports a major leap in the design of targeted cancer therapies through the development of an in vivo self-assembled nano-PROTAC (proteolysis targeting chimera) system capable of delivering dual-targeted degradation in castration-resistant prostate cancer (CRPC).​ PROTACs have reshaped the drug discovery landscape by inducing selective […]

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