The invention discloses a
target protein degradation agent based on ethacrynic acid and application thereof, relates to the technical field of
drug development, and comprises a
target protein degradation agent based on ethacrynic acid, which has a structure as shown in the following formula (I): R1LR2 formula (I), wherein R1 is ethacrynic acid EA; r2 is a ligand JQ1 of a
bromodomain protein 4; l is a connecting chain, and R1 and R2 are connected through L; according to the
target protein degradation agent based on ethacrynic acid and the application thereof, E3 ubiquitinase HECTD1 is recruited through ethacrynic acid to realize degradation of target
protein BRD4, and the process is realized through
ubiquitin-
proteasome, so that
drug resistance caused by target
mutation is avoided, a new choice is provided for recruiting molecules of the target
protein degradation agent, and the target
protein degradation agent has the advantages that the target
protein degradation agent is simple and convenient to operate, and the application prospect is wide. Meanwhile, a new E3 ubiquitination
enzyme is also provided, a new construction thought is provided for a degradation agent of tumor protein difficult to target, and the E3 ubiquitination
enzyme has good application in preparation of anti-
cancer drugs.