@article{e113abcab82b43698a7ff2dc9e5d86bd,
title = "ON01910, a non-ATP-competitive small molecule inhibitor of Plk1, is a potent anticancer agent",
abstract = "Elevated expression of polo-like kinase1 (Plk1) has been reported in many human tumors, and inhibition of Plk1 activity results in their mitotic arrest and apoptosis. Here we describe the profile of ON01910, a small molecule inhibitor of Plk1 activity, which induces mitotic arrest of tumor cells characterized by spindle abnormalities leading to their apoptosis. This compound was not ATP-competitive, but competed for the substrate binding site of the enzyme. In vivo, this compound did not exhibit hematotoxicity, liver damage, or neurotoxicity, and was a potent inhibitor of tumor growth in a variety of xenograft nude mouse models. ON01910 showed strong synergy with several chemotherapeutic agents, often inducing complete regression of tumors.",
author = "Kiranmai Gumireddy and Reddy, {M. V.Ramana} and Cosenza, {Stephen C.} and Nathan, {R. Boomi} and Baker, {Stacey J.} and Nabisa Papathi and Jiandong Jiang and James Holland and Reddy, {E. Premkumar}",
note = "Funding Information: We gratefully acknowledge the help of Dr. Raymond Erikson, who provided us with the sf9 cells expressing Plk1. This work was supported by grants from Onconova Therapeutics Inc. and the Fels Foundation. We thank Dr. Ramesh Kumar for helpful advice. This work was supported by a grant from Onconova Therapeutics Inc. drug discovery program, and E.P.R. and M.V.R.R. are stockholders of Onconova Therapeutics Inc. E.P.R., S.C.C., and M.V.R.R. are consultants to Onconova Therapeutics Inc. ",
year = "2005",
month = mar,
doi = "10.1016/j.ccr.2005.02.009",
language = "English",
volume = "7",
pages = "275--286",
journal = "Cancer Cell",
issn = "1535-6108",
publisher = "Cell Press",
number = "3",
}