Cereblon|Recruiting PROTACs

Current strategies for the design of PROTAC linkers: a critical review

However, the option to target different ligases is important: changing the recruited ligase has been shown to alter the degradation profile of PROTACs [30]; ...

Molecular glue CELMoD compounds are regulators of cereblon ...

Humphreys, Modeling the CRL4A ligase complex to predict target protein ubiquitination induced by cereblon-recruiting PROTACs. J. Biol. Chem ...

A beginner's guide to current synthetic linker strategies towards VHL ...

In this review, we focus on the current synthetic linker strategies employed in the assembly of VHL-recruiting PROTACs.

E3 Ligase Ligands for PROTACs: How They Were Found and How ...

PROTACs consist of a ligand for recruiting a target protein of interest (POI) and a ligand for an E3 ubiquitin ligase, joined with an ...

Tubulin Resists Degradation by Cereblon-Recruiting PROTACs

Our results indicate, that although previously reported covalent tubulin binders led to tubulin degradation, in our hands, cereblon-recruiting PROTACs were not ...

An overview of PROTACs: a promising drug discovery paradigm

Finally, the Ub-tagged E2 and target protein are recruited by E3 ligase to facilitate ubiquitin labeling on target proteins [13]. Such ...

Major advances in targeted protein degradation: PROTACs, LYTACs ...

PROTACs and molecular glues hijack the E3 ligase and recruit neosubstrates for ubiquitination and subsequent degradation. In 2001, our ...

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PROTAC degraders with ligands recruiting MDM2 E3 ubiquitin ligase

MDM2-based PROTACs selectively bind the p53 site on the surface of MDM2, thereby stabilizing p53 and degrading target proteins with favorable ...

Next-Generation Drugs Targeting the Cereblon Ubiquitin Ligase

Understanding the Pathway article: https://ascopubs.org/doi/full/10.1200/JCO.2018.77.9637 The Journal of Clinical Oncology's "Understanding ...

PROTAC-induced Protein Functional Dynamics in Targeted ... - eLife

PROTACs recruit the target protein and E3 ligase; a critical first step is forming a ternary complex. However, while the formation a ternary ...

AlphaLISA Human Cereblon Binding Kit, 500 Assay Points - Revvity

... ) binding kit, the accelerated solution using Alpha technology to bind Cereblon E3 ligase in targeted protein degradation and PROTAC drug discovery.

PROTACs and Molecular Glues - AstraZeneca

... recruits a cellular enzyme, an E3 ubiquitin ligase. This enables the PROTAC to bring the ligase enzyme into close contact with the target ...

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Chemical Inactivation-E3 Ubiquitin Ligase Cereblon By ... - YouTube

Chemical Inactivation-E3 Ubiquitin Ligase Cereblon By Homo-PROTACs l Protocol Preview. 111 views · 1 year ago ...more. JoVE (Journal of ...

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Uncovering new pathways for targeted protein degradation

... recruiting a single E3 ligase, Cereblon. Arising resistance ... PROTACs and Molecular Glues (MGs) are a new class of therapeutic small ...

Developments of CRBN-based PROTACs as potential therapeutic ...

Heterogeneous bifunctional PROTACs contain a ligand for recruiting E3 ligase, a linker, and another ligand to bind to the target protein for degradation. A ...

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