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September 29, 2024Journal of Medicinal Chemistry

Discovery of a Highly Potent PROTAC Degrader of p300/CBP Proteins for the Treatment of Enzalutamide-Resistant Prostate Cancer

Mengjun Ma Mengyao Li Chengwei Zhang Zixuan Yang Xiaoyu Chen Penghui Lu Shuangshuang Nie Siqi Zhang Shumin Ma Chong Qin

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Abstract

Prostate cancer therapies against androgen receptor (AR) eventually develop lethal resistance; thus, exploring new therapeutic approaches is urgent for prostate cancer treatment. Acetyltransferase p300/CBP are key coactivators for AR-mediated transcription and represent promising therapeutic targets to inhibit AR activity in prostate cancer. We describe the design synthesis and evaluation of a new class of p300/CBP PROTAC degraders. We identified an excellent p300/CBP degrader

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Ma et al. (2024) studied this question.

synapsesocial.com/papers/68e57074b6db643587511482 https://doi.org/10.1021/acs.jmedchem.4c01100

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

1Abstract 6048: Targeting AR positive prostate cancer cells by the novel P300/CBP oral available PROTAC degrader2024
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