Functionalized Warhead Ligands

Literature (1)
Cat. No. Product Name / Activity
6588 (+)-JQ1 carboxylic acid
Carboxylic acid-functionalized BET bromodomain inhibitor; target ligand for PROTACs
6589 (+)-JQ1 PA
Functionalized BET bromodomain inhibitor; 'click' target ligand for PROTACs

Literature for Functionalized Warhead Ligands

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Targeted Protein Degradation

Targeted Protein Degradation Poster

Degraders (e.g. PROTACs) are bifunctional small molecules, that harness the Ubiquitin Proteasome System (UPS) to selectively degrade target proteins within cells. They consist of three covalently linked components: an E3 ubiquitin ligase ligand, a linker and a ligand for the target protein of interest. Authored in-house, this poster outlines the generation of a toolbox of building blocks for the development of Degraders. The characteristics and selection of each of these components are discussed. Presented at EFMC 2018, Ljubljana, Slovenia