
Bioorganic and Medicinal Chemistry p. 3016 - 3020 (2018)
Update date:2022-07-30
Topics:
Brear, Paul
North, Andrew
Iegre, Jessica
Hadje Georgiou, Kathy
Lubin, Alexandra
Carro, Laura
Green, William
Sore, Hannah F.
Hyv?nen, Marko
Spring, David R.
Increased CK2 levels are prevalent in many cancers. Combined with the critical role CK2 plays in many cell-signaling pathways, this makes it a prime target for down regulation to fight tumour growth. Herein, we report a fragment-based approach to inhibiting the interaction between CK2α and CK2β at the α-β interface of the holoenzyme. A fragment, CAM187, with an IC50 of 44 μM and a molecular weight of only 257 gmol?1 has been identified as the most promising compound. Importantly, the lead fragment only bound at the interface and was not observed in the ATP binding site of the protein when co-crystallised with CK2α. The fragment-like molecules discovered in this study represent unique scaffolds to CK2 inhibition and leave room for further optimisation.
View MoreChengdu ZY Biochemical Technology Co., LTD
Contact:0086-28-88680086
Address:170 Qingpu Road, Shouan Town, Pujiang County
Hangzhou J&H Chemical Co., Ltd.
website:http://www.jhechem.com/
Contact:+86-571-87396432
Address:No.200 Zhenhua Rd.Xihu Industrial Park, Hangzhou 310030, China
Chengdu Boon Stream Chemical Industry Co.,Ltd.
Contact:+86-28-83156758
Address:No.859,Dongzikou Road,Jinniu District,Chengdu,Sichuan,P.R.China
website:http://www.shengmaochem.com
Contact:86-27-82853423, 82819281
Address:Rm 202, A Unit Huaqiao Building No. 2, Lihuangpi Road, Wuhan, China
Shanghai PotentPharm Science and Technology Co.,Ltd
Contact:86-021-51969655
Address:Unit B, Building 18, No.300, Chuantu Rd,Pudong District, Shanghai 201202, China
Doi:10.1016/S0277-5387(99)00129-1
(1999)Doi:10.1002/anie.201407477
(2014)Doi:10.1016/S0040-4020(99)00709-7
(1999)Doi:10.1039/C39790000749
(1979)Doi:10.1016/S0040-4039(99)01499-9
(1999)Doi:10.1021/jo0200466
(2002)