000295842 001__ 295842
000295842 005__ 20241214120757.0
000295842 037__ $$aDKFZ-2024-02659
000295842 1001_ $$0P:(DE-He78)9bc7437d3c410002e64b4b6133d0102d$$aHanne, Malte$$b0$$udkfz
000295842 245__ $$aSynthesis of Targeted Degraders and Inhibitors for Branched-Chain Amino Acid Aminotransferase 1
000295842 260__ $$c2024
000295842 3367_ $$2DataCite$$aOutput Types/Supervised Student Publication
000295842 3367_ $$02$$2EndNote$$aThesis
000295842 3367_ $$2BibTeX$$aMASTERSTHESIS
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000295842 3367_ $$0PUB:(DE-HGF)19$$2PUB:(DE-HGF)$$aMaster Thesis$$bmaster$$mmaster$$s1734096629_9063
000295842 3367_ $$2ORCID$$aSUPERVISED_STUDENT_PUBLICATION
000295842 502__ $$aMasterarbeit, University of Heidelberg, 2024$$bMasterarbeit$$cUniversity of Heidelberg$$gFaculty of Chemistry and Earth Sciences
000295842 520__ $$aBranched-chain amino acid transferase 1 (BCAT1), the cytosolic isozyme of BCAT, is an enzyme that catalyzes the transamination reaction of branched-chain amino acids, such as leucine or valine, towards α-keto acids to fuel the citric acid cycle, while also being suspected of showing a moonlighting function in mitosis. In the literature, a high abundance of BCAT1 in a number of cancer types has been reported, with BCAT1 knock-out cells showing reduced cell proliferation. These findings make it a promising target in medicinal chemistry, with a number of recent approaches targeting the enzyme.In this thesis, a number of different targeted degraders (PROTACs) and inhibitors for BCAT1 is reported, with different structural modifications being screened to improve activity and cell permeability. The obtained inhibitors are tested for activity against BCAT1 in an enzyme assay, and for cell permeability using a Caco-2 assay.
000295842 536__ $$0G:(DE-HGF)POF4-311$$a311 - Zellbiologie und Tumorbiologie (POF4-311)$$cPOF4-311$$fPOF IV$$x0
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000295842 9101_ $$0I:(DE-588b)2036810-0$$6P:(DE-He78)9bc7437d3c410002e64b4b6133d0102d$$aDeutsches Krebsforschungszentrum$$b0$$kDKFZ
000295842 9131_ $$0G:(DE-HGF)POF4-311$$1G:(DE-HGF)POF4-310$$2G:(DE-HGF)POF4-300$$3G:(DE-HGF)POF4$$4G:(DE-HGF)POF$$aDE-HGF$$bGesundheit$$lKrebsforschung$$vZellbiologie und Tumorbiologie$$x0
000295842 9141_ $$y2024
000295842 9201_ $$0I:(DE-He78)A390-20160331$$kA390$$lAG Wirkstoffforschung$$x0
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