Tracking the PROTAC degradation pathway in living cells highlights the importance of ternary complex measurement for PROTAC optimization

Schwalm, MP; Krämer, A; Dölle, A; Weckesser, J; Yu, XF; Jin, J; Saxena, K; Knapp, S

Knapp, S (通讯作者),Goethe Univ Frankfurt, Inst Pharmazeut Chem, Biozentrum, Max von Laue Str 9, D-60438 Frankfurt, Germany.;Knapp, S (通讯作者),Goethe Univ Frankfurt, Buchmann Inst Life Sci, Struct Genom Consortium, Max von Laue Str 15, D-60438 Frankfurt, Germany.;Knapp, S (通讯作者),German Canc Consortium DKTK, German Canc Res Ctr DKFZ, DKTK Site Frankfurt Mainz, D-69120 Heidelberg, Germany.

CELL CHEMICAL BIOLOGY, 2023; 30 (7): 753

Abstract

The multi-step degradation process of PROteolysis TArgeting Chimeras (PROTACs) poses a challenge for their rational development, as the rate-limiting ......

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