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Discovery of an Aldo-Keto reductase 1C3 (AKR1C3) degrader

Medicine and Health

Discovery of an Aldo-Keto reductase 1C3 (AKR1C3) degrader

A. V. Carmona, S. Jonnalagadda, et al.

Discover the groundbreaking research by Angelica V. Carmona and colleagues on the first-in-class AKR1C3 PROTAC degrader that shows promise in targeting prostate cancer by reducing AKR1C3 expression and degrading ARv7. This innovative approach could change the landscape of prostate cancer treatment.

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Playback language: English
Abstract
Aldo-keto reductase 1C3 (AKR1C3) is a protein upregulated in prostate cancer, contributing to proliferation and chemotherapeutic resistance. This study reports the discovery of the first-in-class AKR1C3 PROTAC degrader, which potently reduced AKR1C3 expression in prostate cancer cells, also degrading ARv7 and other AKR1C isoforms. This compound is a promising strategy for prostate cancer intervention.
Publisher
Communications Chemistry
Published On
Mar 14, 2024
Authors
Angelica V. Carmona, Shirisha Jonnalagadda, Alfie M. Case, Krishnaiah Maddeboina, Sravan K. Jonnalagadda, Louise F. Dow, Ling Duan, Trevor M. Penning, Paul C. Trippier
Tags
AKR1C3
PROTAC
prostate cancer
chemotherapy resistance
ARv7
degrader
therapeutic strategy

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