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| Home > Publications database > Synthesis of Targeted Degraders and Inhibitors for Branched-Chain Amino Acid Aminotransferase 1 |
| Master Thesis | DKFZ-2024-02659 |
2024
Abstract: Branched-chain amino acid transferase 1 (BCAT1), the cytosolic isozyme of BCAT, is an enzyme that catalyzes the transamination reaction of branched-chain amino acids, such as leucine or valine, towards α-keto acids to fuel the citric acid cycle, while also being suspected of showing a moonlighting function in mitosis. In the literature, a high abundance of BCAT1 in a number of cancer types has been reported, with BCAT1 knock-out cells showing reduced cell proliferation. These findings make it a promising target in medicinal chemistry, with a number of recent approaches targeting the enzyme.In this thesis, a number of different targeted degraders (PROTACs) and inhibitors for BCAT1 is reported, with different structural modifications being screened to improve activity and cell permeability. The obtained inhibitors are tested for activity against BCAT1 in an enzyme assay, and for cell permeability using a Caco-2 assay.
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