Article

Identification of Suitable Target/E3 Ligase Pairs for PROTAC Development using a Rapamycin-induced Proximity Assay (RiPA)

2024-04-25

Abstract excerpt

The development of proteolysis targeting chimeras (PROTACs), which induce the degradation of target proteins by bringing them into proximity with cellular E3 ubiquitin ligases, has revolutionized drug development. While the human genome encodes more than 600 different E3 ligases, current PROTACs use only a handful of them, drastically limiting their full potential. Furthermore, many PROTAC development campaigns fa...

Topics

Open a Topic to create a Post that cites this publication.

Identifiers and source

Literature Corpus work: 325faf50-77ab-5ff4-a9b4-ce877a2df1c6
DOI: 10.1101/2024.04.24.590940

Open publication

Related research

Semantic proximity does not establish scientific evidence.

Click a neighbor to travelStep 1 · 12 closest

Identification of Suitable Target/E3 Ligase Pairs for PROTAC Development using a Rapamycin-induced Proximity Assay (RiPA)DOI 10.1101/2024.04.24.590940Read

PROTACs: great opportunities for academia and industrySemantic proximity Read

Expanding PROTACtable genome universe of E3 ligasesSemantic proximity Read

Hijacking Methyl Reader Proteins for Nuclear-Specific Protein DegradationSemantic proximity Read

A CRISPR activation screen identifies FBXO22 as an E3 ligase supporting targeted protein degradationSemantic proximity Read

Synthesis, biological evaluation and clinical trials of Cereblon-based PROTACsSemantic proximity Read

Design of a Cereblon construct for crystallographic and biophysical studies of protein degradersSemantic proximity Read

Targeting the Interplay of Proteins through PROTACs for the Management of Cancer and Associated DisordersSemantic proximity Read

Breaking Bad Proteins – Discovery Approaches and the Road to Clinic for DegradersSemantic proximity Read

Identification of KLHDC2 as an efficient proximity-induced degrader of K-RAS, STK33, β-catenin, and FoxP3Semantic proximity Read

Destruction of DNA-binding proteins by programmable O’PROTAC: Oligonucleotide-based PROTACSemantic proximity Read

Structure-Based Survey of the Human Proteome for Opportunities in Proximity PharmacologySemantic proximity Read

PROTACs: Current and Future Potential as a Precision Medicine Strategy to Combat CancerSemantic proximity Read