E3 ligase Ligand-Linker Conjugates 9

E3 ligase Ligand-Linker Conjugates 9 is a synthesized compound that incorporates an E3 ligase ligand and a linker used in PROTAC technology.

Signaling Pathways >> PROTAC >> E3 Ligase Ligand-Linker Conjugate

Research Areas >> Cancer

E3 Ligase Ligand-Linker Conjugate[1]

E3 ligase Ligand-Linker Conjugates 9 uses the VHL ligand[1]. The linker is 6-2-2-2-2-2-2. The linkers contain a mixture of hydrophobic and hydrophilic moieties to balance the hydrophobicity/hydrophilicity of the resulting hybrid compounds. PROTACs that induce the degradation of an oncogenic tyrosine kinase, BCR-ABL has been developed. E3 ligase Ligand-Linker Conjugates 9 can be attached to potent TKIs (bosutinib and dasatinib) that mediate the degradation of c-ABL and BCR-ABL by hijacking either CRBN or VHL E3 ubiquitin ligase [2].

[1]. US 20170121321 A1

[2]. Lai AC, et al. Modular PROTAC Design for the Degradation of Oncogenic BCR-ABL. Angew Chem Int Ed Engl. 2016 Jan 11;55(2):807-10.

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