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@MASTERSTHESIS{Hanne:295842,
author = {M. Hanne$^*$},
title = {{S}ynthesis of {T}argeted {D}egraders and {I}nhibitors for
{B}ranched-{C}hain {A}mino {A}cid {A}minotransferase 1},
school = {University of Heidelberg},
type = {Masterarbeit},
reportid = {DKFZ-2024-02659},
year = {2024},
note = {Masterarbeit, University of Heidelberg, 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.},
cin = {A390},
cid = {I:(DE-He78)A390-20160331},
pnm = {311 - Zellbiologie und Tumorbiologie (POF4-311)},
pid = {G:(DE-HGF)POF4-311},
typ = {PUB:(DE-HGF)19},
url = {https://inrepo02.dkfz.de/record/295842},
}