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Identification and Validation of a Potent Type II Inhibitor of Inactive Polo‐like Kinase 1
Author(s) -
Keppner Sarah,
Proschak Ewgenij,
Schneider Gisbert,
Spänkuch Birgit
Publication year - 2009
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.200900338
Subject(s) - polo like kinase , plk1 , kinase , identification (biology) , apoptosis , homology modeling , virtual screening , chemistry , computational biology , biology , drug discovery , biochemistry , cell cycle , enzyme , botany
Virtual screening using a homology model of human polo‐like kinase 1 (Plk1) in an inactive conformation led to the identification of a selective Plk1 inhibitor that decreases proliferation and induces apoptosis. This suggests that type II Plk1 inhibitors may be considered for the development of cancer therapeutics.