Ligandability of E3 Ligases for Targeted Protein Degradation Applications
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https://figshare.com/articles/dataset/Ligandability_of_E3_Ligases_for_Targeted_Protein_Degradation_Applications/16563893
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资源简介：
Targeted
protein degradation (TPD) using proteolysis targeting
chimeras (PROTACs) and molecular glue degraders has arisen as a powerful
therapeutic modality for eliminating disease-causing proteins from
cells. PROTACs and molecular glue degraders employ heterobifunctional
or monovalent small molecules, respectively, to chemically induce
the proximity of target proteins with E3 ubiquitin ligases to ubiquitinate
and degrade specific proteins via the proteasome. Whereas TPD is an
attractive therapeutic strategy for expanding the druggable proteome,
only a relatively small number of E3 ligases out of the >600 E3
ligases
encoded by the human genome have been exploited by small molecules
for TPD applications. Here we review the existing E3 ligases that
have thus far been successfully exploited for TPD and discuss chemoproteomics-enabled
covalent screening strategies for discovering new E3 ligase recruiters.
We also provide a chemoproteomic map of reactive cysteines within
hundreds of E3 ligases that may represent potential ligandable sites
that can be pharmacologically interrogated to uncover additional E3
ligase recruiters.
创建时间：
2021-09-02
