Ligand Design for E3 Ligase


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As a leading service provider in drug discovery and development, BOC Sciences is fully qualified and committed to providing one-stop PROTAC development services, which has become a promising strategy in the field of small molecular drug discovery. With a comprehensive and advanced platform, we provide Ligand Design for E3 Ligase to customers around the world to meet new drug discovery goals.

Introduction of E3 Ligase and E3 Ligase Ligand

Ubiquitin (UB) is a protein modifier that regulates many important cellular processes. In order to initiate protein modification through UB, E1 enzyme activates the C-terminal carboxylate of UB to transfer to the target protein through E1-E2-E3 cascade. E3 is a ubiquitous protein ligase, which directly or indirectly catalyzes the transfer of ubiquitous proteins to target proteins (substrates) to form heteropeptide bonds. By using small molecular ligands to recruit target proteins and E3 ligand, all small molecular PROTAC has achieved rapid target degradation and better cell permeability. Various small molecules that have been shown to bind to several E3 ligase or substrate receptor proteins of the CRL E3 ligase complex, such as MDM2,cIAP1,CRBN and VHL, have been used in PROTAC development.

Ligand Design for E3 Ligase

Ligand Design Services for E3 Ligase

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Workflow of Ligand Design Services

Ligand Design for E3 Ligase

References:

  1. Buckley, D. L., Gustafson, J. L., Van Molle, I., Roth, A. G., Tae, H. S., Gareiss, P. C., ... & Crews, C. M. (2012). Small‐Molecule Inhibitors of the Interaction between the E3 Ligase VHL and HIF1α. Angewandte Chemie International Edition, 51(46), 11463-11467.
  2. Steinebach, C., Kehm, H., Lindner, S., Vu, L. P., Köpff, S., Mármol, Á. L., ... & Gütschow, M. (2019). PROTAC-mediated crosstalk between E3 ligases. Chemical communications, 55(12), 1821-1824.

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