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@ARTICLE{Zou:142609,
author = {F. Zou and S. Pusch$^*$ and J. Hua and T. Ma and L. Yang
and Q. Zhu and Y. Xu and Y. Gu and A. von Deimling$^*$ and
X. Zha},
title = {{I}dentification of novel allosteric inhibitors of mutant
isocitrate dehydrogenase 1 by cross docking-based virtual
screening.},
journal = {Bioorganic $\&$ medicinal chemistry letters},
volume = {28},
number = {3},
issn = {0960-894X},
address = {Amsterdam [u.a.]},
publisher = {Elsevier Science},
reportid = {DKFZ-2019-00327},
pages = {388 - 393},
year = {2018},
abstract = {IDH1 mutation (mIDH1) occurs in $20-30\%$ of gliomas and is
a promising target for the cancer therapy. In this article,
a cross docking-based virtual screening was employed to
identify seven small molecules for the allosteric site of
mIDH1. Compounds ZX01, ZX05 and ZX06 exhibited the potent
inhibitory activity and the high selectivity against
WT-IDH1, providing a good starting point for the further
development of highly selective mIDH1 inhibitors.
Importantly, the parallel artificial membrane permeation
assay of the blood-brain barrier (PAMPA-BBB) identified ZX06
with a good ability to penetrate BBB. These findings
indicate that ZX06 deserves further optimization as a lead
compound for the treatment of patients with IDH1 mutated
brain cancers.},
cin = {L101 / G380},
ddc = {610},
cid = {I:(DE-He78)L101-20160331 / I:(DE-He78)G380-20160331},
pnm = {317 - Translational cancer research (POF3-317)},
pid = {G:(DE-HGF)POF3-317},
typ = {PUB:(DE-HGF)16},
pubmed = {pmid:29290542},
doi = {10.1016/j.bmcl.2017.12.030},
url = {https://inrepo02.dkfz.de/record/142609},
}