Henning, Ryan K. published the artcileDegradation of Akt using protein-catalyzed capture agents, Safety of Dbco-maleimide, the publication is Journal of Peptide Science (2016), 22(4), 196-200, database is CAplus and MEDLINE.
Abnormal signaling of the protein kinase Akt has been shown to contribute to human diseases such as diabetes and cancer, but Akt has proven to be a challenging target for drugging. Using iterative in situ click chem., we recently developed multiple protein-catalyzed capture (PCC) agents that allosterically modulate Akt enzymic activity in a protein-based assay. Here, we utilize similar PCCs to exploit endogenous protein degradation pathways. We use the modularity of the anti-Akt PCCs to prepare proteolysis targeting chimeric mols. that are shown to promote the rapid degradation of Akt in live cancer cells. These novel proteolysis targeting chimeric mols. demonstrate that the epitope targeting selectivity of PCCs can be coupled with non-traditional drugging moieties to inhibit challenging targets.
Journal of Peptide Science published new progress about 1395786-30-7. 1395786-30-7 belongs to catalysis-chemistry, auxiliary class Inhibitor, name is Dbco-maleimide, and the molecular formula is C25H21N3O4, Safety of Dbco-maleimide.
Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia