scholarly journals A Chemical Probe Strategy for Interrogating Inhibitor Selectivity Across the MEK Kinase Family

2017 ◽  
Vol 12 (5) ◽  
pp. 1245-1256 ◽  
Author(s):  
Kristine K. Deibler ◽  
Rama K. Mishra ◽  
Matthew R. Clutter ◽  
Aleksandar Antanasijevic ◽  
Raymond Bergan ◽  
...  
Keyword(s):  
Chemical Probe ◽  
Kinase Family ◽  
Inhibitor Selectivity ◽  
Mek Kinase

Wavelength-specific Activation of MAP Kinase Family Proteins by Monochromatic UV Irradiation¶

2001 ◽  
Vol 73 (2) ◽  
pp. 147 ◽  
Author(s):  
Yukihito Kabuyama ◽  
Miwako K. Homma ◽  
Masayuki Sekimata ◽  
Yoshimi Homma
Keyword(s):  
Map Kinase ◽  
Uv Irradiation ◽  
Kinase Family

SGC-CK2-1: The First Selective Chemical Probe for the Pleiotropic Kinase CK2

2020 ◽  
Author(s):  
Carrow Wells ◽  
David Drewry ◽  
Julie E. Pickett ◽  
Alison D. Axtman
Keyword(s):  
Cell Lines ◽  
Small Molecule ◽  
Chemical Probe ◽  
High Quality ◽  
Extensive Evaluation ◽  
Key Driver ◽  
Selective Chemical ◽  
Kinase Ck2 ◽  
Ck2 Inhibitors

Building upon a wealth of published knowledge surrounding the pyrazolopyrimidine scaffold, we designed a small library around the most selective small molecule CK2 inhibitors reported. Through extensive evaluation of this library we identified inhibitor 24 (SGC-CK2-1) as a potent, selective, and cell-active CK2 chemical probe. Remarkably, despite years of research pointing to CK2 as a key driver in cancer, our probe did not elicit an antiproliferative phenotype in cell lines tested. While many publications have attempted tocharacterize CK2 function, CK2 biology is complex and a high-quality chemical tool like SGC-CK2-1 will aid in connecting CK2 functions to phenotypes.

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