Tissue distribution and retention drives efficacy of rapidly clearing VHL-based PROTACs.
Donglu ZhangBin MaPeter S DragovichLi MaShu ChenEugene C ChenXiaofen YeJoyce LiuJennifer PizzanoElizabeth BortolonEmily ChanXing ZhangYi-Chen ChenElizabeth S LevyRobert L YauchS Cyrus KhojastehCornelis E C A HopPublished in: Communications medicine (2024)
Plasma sampling for VHL-PROTAC does not represent the tissue concentrations necessary for efficacy. Understanding of tissue uptake and retention could enable less frequent IV administration to be used for therapeutic dosing.
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