Pillow, Thomas H. published the artcileAntibody Conjugation of a Chimeric BET Degrader Enables in vivo Activity, Application of 2-Methyl-2-sulfanylpropan-1-ol, the publication is ChemMedChem (2020), 15(1), 17-25, database is CAplus and MEDLINE.
The ability to selectively degrade proteins with bifunctional small mols. has the potential to fundamentally alter therapy in a variety of diseases. However, the relatively large size of these chimeric mols. often results in challenging physico-chem. properties (e. g., low aqueous solubility) and poor pharmacokinetics which may complicate their in vivo applications. We recently discovered an exquisitely potent chimeric BET degrader (GNE-987) which exhibited picomolar cell potencies but also demonstrated low in vivo exposures. In an effort to improve the pharmacokinetic properties of this mol., we discovered the first degrader-antibody conjugate by attaching GNE-987 to an anti-CLL1 antibody via a novel linker. A single IV dose of the conjugate afforded sustained in vivo exposures that resulted in antigen-specific tumor regressions. Enhancement of a chimeric protein degrader with poor in vivo properties through antibody conjugation thereby expands the utility of directed protein degradation as both a biol. tool and a therapeutic possibility.
ChemMedChem published new progress about 73303-88-5. 73303-88-5 belongs to alcohols-buliding-blocks, auxiliary class Thiol,Aliphatic hydrocarbon chain,Alcohol, name is 2-Methyl-2-sulfanylpropan-1-ol, and the molecular formula is C4H10OS, Application of 2-Methyl-2-sulfanylpropan-1-ol.
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