Literature summary for 2.7.11.21 extracted from

Gilmartin, A.G.; Bleam, M.R.; Richter, M.C.; Erskine, S.G.; Kruger, R.G.; Madden, L.; Hassler, D.F.; Smith, G.K.; Gontarek, R.R.; Courtney, M.P.; Sutton, D.; Diamond, M.A.; Jackson, J.R.; Laquerre, S.G.
Distinct concentration-dependent effects of the polo-like kinase 1-specific inhibitor GSK461364A, including differential effect on apoptosis (2009), Cancer Res., 69, 6969-6977.

Search for more literature for 2.7.11.21

Application

Application	Comment	Organism
medicine	GSK461364A is broadly antiproliferative for tumor cell lines in vitro and efficacious in multiple in vivo tumor models	Homo sapiens

Inhibitors

Inhibitors	Comment	Organism	Structure
GSK461364A	ATP-competitive inhibitor	Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates	Organism	Comment (Nat. Sub.)	Natural Products	Comment (Nat. Pro.)	Rev.	Reac.
ATP + a protein	Homo sapiens	-	ADP + a phosphoprotein	-	?

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	-	-	-

Source Tissue

Source Tissue	Comment	Organism	Textmining
A-549 cell	NSCLC line A549	Homo sapiens	-
Colo-205 cell	-	Homo sapiens	-
HCT-116 cell	-	Homo sapiens	-
HT-29 cell	-	Homo sapiens	-
MCF-7 cell	-	Homo sapiens	-
MDA-MB-231 cell	-	Homo sapiens	-
MDA-MB-468 cell	-	Homo sapiens	-
MV-522 cell	-	Homo sapiens	-
MX-1 cell	-	Homo sapiens	-
NCI-H460 cell	-	Homo sapiens	-
SKOV-3 cell	-	Homo sapiens	-
SW-620 cell	-	Homo sapiens	-
U2-OS cell	-	Homo sapiens	-
ZR-75-1 cell	-	Homo sapiens	-

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
ATP + a protein	-	Homo sapiens	ADP + a phosphoprotein	-	?

Synonyms

Synonyms	Comment	Organism
Plk1	-	Homo sapiens
Polo-like kinase 1	-	Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C]	Temperature Optimum Maximum [°C]	Comment	Organism
22	-	Plk scintillation proximity assay at room temperature	Homo sapiens
23	-	kinase assay	Homo sapiens

pH Optimum

pH Optimum Minimum	pH Optimum Maximum	Comment	Organism
7.2	-	Plk scintillation proximity assay	Homo sapiens
7.5	-	kinase assay	Homo sapiens

Cofactor

Cofactor	Comment	Organism	Structure
ATP	-	Homo sapiens

Ki Value [mM]

Ki Value [mM]	Ki Value maximum [mM]	Inhibitor	Comment	Organism	Structure
0.0000005	-	GSK461364A	Ki, apparent dissociation constant, less than 0.0000005	Homo sapiens

Expression

Organism	Comment	Expression
Homo sapiens	Plk1 overexpression is strongly associated with cancer	up

General Information

General Information	Comment	Organism
physiological function	Plk1 plays an essential role in regulating the many processes involved in mitotic entry and progression	Homo sapiens

Use of this online version of BRENDA is free under the CC BY 4.0 license. See terms of use for full details.

Release 2023.1 (January 2023)