E3 ligase Ligand-Linker Conjugates 10

E3 ligase Ligand-Linker Conjugates 10 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 10 uses the VHL ligand[1]. The linker is 6-2-2. 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 10 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.

E3 ligase Ligand-Linker Conjugates 14 | E3 Ligase Ligand-Linker Conjugates 1 | E3 ligase Ligand-Linker Conjugates 17 | E3 ligase Ligand-Linker Conjugates 16 | (SRS)-AHPC-PEG3-NH2 hydrochloride | E3 ligase Ligand-Linker Conjugates 6 | E3 ligase Ligand-Linker Conjugates 18 | E3 Ligase Ligand-Linker Conjugates 2 | E3 ligase Ligand-Linker Conjugates 4 | (SRS)-AHPC-PEG4-NH2 hydrochloride | E3 Ligase Ligand-Linker Conjugates 22 | E3 ligase Ligand-Linker Conjugates 13 | E3 Ligase Ligand-Linker Conjugates 24 TFA | E3 ligase Ligand-Linker Conjugates 11