: A novel piperazinylpyrimidine compound, Q12, was synthesized and tested for its potential to selectively inhibit the growth of certain tumor cell lines within the NCI-60 cell line panel. Q12 is an ATP competitive inhibitor of cyclin dependent kinase 8 (CDK 8). We studied Q12 in the context of sensitive cell lines MDA-MB-468 (GI50 0.06 μM) and HCT- 116 (GI50 0.27 μM) and a non-sensitive cell line COLO 205 (GI50 30 μM). The MDA-MD-468 cell line represents triple negative breast cancer, a difficult type of cancer to treat because of lacking HER2, estrogen and progesterone receptors. HCT- 116 and COLO 205 are human colon cancer cell lines, which harbor β- catenin and APC mutations respectively
The landscape of genetic alterations that can lead to cancer is vast and complex. Precancerous cells...
Cyclin-dependent kinase 8 (CDK8) plays a vital role in regulating cell transcription either through ...
Background: Hepatocellular carcinoma (HCC) is a lethal malignancy lacking effective treatment. The C...
Over the past two decades, protein kinases have been intensively investigated as targets to treat ne...
Cyclin-dependent kinases (CDKs) and cyclins (Cyclins) are the core molecules in the regulation mecha...
Cyclin-dependent kinase 8 (CDK8) has been identified as a colon cancer oncogene. Since this initial ...
Aberrant activity of cyclin-dependent kinase (CDK) 8 is implicated in various cancers. While CDK8-ta...
Background: Cyclin-dependent kinases (CDKs) control cell cycle progression, RNA transcription and ap...
Cyclin-dependent kinases (CDKs) drive cell cycle progression and control transcriptional pro-cesses....
The mediator complex-associated cyclin dependent kinase CDK8 regulates β-catenin-dependent transcrip...
Kinase inhibitors constitute an important new class of cancer drugs, whose selective efficacy is lar...
Deregulation of the cyclin-dependent kinases (CDKs) has been implicated in the pathogenesis of multi...
Introduction: Cell cycle and gene transcription are under the control of cyclin-dependent kinases (C...
Cyclin-dependent kinase 8 (CDK8) plays a vital role in regulating cell transcription either through ...
The main difficulty in the development of ATP antagonist kinase inhibitors is target specificity, si...
The landscape of genetic alterations that can lead to cancer is vast and complex. Precancerous cells...
Cyclin-dependent kinase 8 (CDK8) plays a vital role in regulating cell transcription either through ...
Background: Hepatocellular carcinoma (HCC) is a lethal malignancy lacking effective treatment. The C...
Over the past two decades, protein kinases have been intensively investigated as targets to treat ne...
Cyclin-dependent kinases (CDKs) and cyclins (Cyclins) are the core molecules in the regulation mecha...
Cyclin-dependent kinase 8 (CDK8) has been identified as a colon cancer oncogene. Since this initial ...
Aberrant activity of cyclin-dependent kinase (CDK) 8 is implicated in various cancers. While CDK8-ta...
Background: Cyclin-dependent kinases (CDKs) control cell cycle progression, RNA transcription and ap...
Cyclin-dependent kinases (CDKs) drive cell cycle progression and control transcriptional pro-cesses....
The mediator complex-associated cyclin dependent kinase CDK8 regulates β-catenin-dependent transcrip...
Kinase inhibitors constitute an important new class of cancer drugs, whose selective efficacy is lar...
Deregulation of the cyclin-dependent kinases (CDKs) has been implicated in the pathogenesis of multi...
Introduction: Cell cycle and gene transcription are under the control of cyclin-dependent kinases (C...
Cyclin-dependent kinase 8 (CDK8) plays a vital role in regulating cell transcription either through ...
The main difficulty in the development of ATP antagonist kinase inhibitors is target specificity, si...
The landscape of genetic alterations that can lead to cancer is vast and complex. Precancerous cells...
Cyclin-dependent kinase 8 (CDK8) plays a vital role in regulating cell transcription either through ...
Background: Hepatocellular carcinoma (HCC) is a lethal malignancy lacking effective treatment. The C...