TY - CHAP
T1 - Screening of DTP compound libraries for CK2 inhibitors with focus on natural products
AU - Rasmussen, Tine D. L.
AU - Guerra, Barbara
AU - Issinger, Olaf-Georg
PY - 2015
Y1 - 2015
N2 - Various compound libraries of the Drug Therapeutic Program (DTP) of the NIH/NCI were screened against the catalytic subunit and the tetrameric holoenzyme of protein kinase CK2. Different IC50 values were obtained for the two CK2 molecules. In the case of nortangeretin, the IC50 value was 0.34 μM for the catalytic subunit and 15 μM for the holoenzyme. In the case of coumestrol, opposite results were obtained, i.e., high IC50 for the CK2α subunit (2.7 μM) and a lower IC50 value for the holoenzyme (0.19 μM). From the many compounds identified to inhibit CK2, we have selected 14 different compounds and listed them according to their CK2α/CK2 holoenzyme IC50 ratio. Four compounds were tested on a panel of seven cell lines revealing considerable differences in the degree of CK2 inhibition inside the cells.
AB - Various compound libraries of the Drug Therapeutic Program (DTP) of the NIH/NCI were screened against the catalytic subunit and the tetrameric holoenzyme of protein kinase CK2. Different IC50 values were obtained for the two CK2 molecules. In the case of nortangeretin, the IC50 value was 0.34 μM for the catalytic subunit and 15 μM for the holoenzyme. In the case of coumestrol, opposite results were obtained, i.e., high IC50 for the CK2α subunit (2.7 μM) and a lower IC50 value for the holoenzyme (0.19 μM). From the many compounds identified to inhibit CK2, we have selected 14 different compounds and listed them according to their CK2α/CK2 holoenzyme IC50 ratio. Four compounds were tested on a panel of seven cell lines revealing considerable differences in the degree of CK2 inhibition inside the cells.
KW - CMGC kinases
KW - Casein kinase 2
KW - DTP compound libraries
KW - Eukaryotic protein kinases
KW - Protein kinase CK2
KW - Protein kinase inhibitors
KW - Signal transduction pathways
KW - Small molecule compounds
U2 - 10.1007/978-3-319-14544-0_18
DO - 10.1007/978-3-319-14544-0_18
M3 - Book chapter
SN - 978-3-319-14543-3
T3 - Advances in Biochemistry in Health and Disease
SP - 319
EP - 340
BT - Protein Kinase CK2 Cellular Function in Normal and Disease States
A2 - Ahmed, Khalil
A2 - Issinger, Olaf-Georg
A2 - Szyszka, Ryszard
PB - Springer
ER -