Tunable Methacrylamides for Covalent Ligand Directed Release Chemistry
Rambabu Reddi, Efrat Resnick, Adi Rogel, Boddu Venkateswara Rao, Ronen Gabizon, Kim Goldenberg, Neta Gurwicz, Daniel Zaidman, A.N. Plotnikov, Haim Barr, Ziv Shulman, Nir London
Abstract
. We further demonstrate a BTK CoLDR chemiluminescent probe that enabled a high-throughput screen for BTK inhibitors. Altogether we show that α-substituted methacrylamides represent a new and versatile addition to the toolbox of targeted covalent inhibitor design.
Topics & Concepts
ChemistryCovalent bondElectrophileCombinatorial chemistryCysteineConjugateSubstituentLigand (biochemistry)Bruton's tyrosine kinaseReactivity (psychology)StereochemistryBiochemistryOrganic chemistryTyrosine kinaseEnzymeSignal transductionAlternative medicineMedicinePathologyMathematical analysisReceptorCatalysisMathematicsChronic Lymphocytic Leukemia ResearchLymphoma Diagnosis and TreatmentClick Chemistry and Applications