Strategies of targeting CK2 in drug discovery: challenges, opportunities, and emerging prospects

Y Chen, Y Wang, J Wang, Z Zhou, S Cao… - Journal of Medicinal …, 2023 - ACS Publications
CK2 (casein kinase 2) is a serine/threonine protein kinase that is ubiquitous in eukaryotic
cells and plays important roles in a variety of cellular functions, including cell growth …

Role of CK2 inhibitor CX-4945 in anti-cancer combination therapy–potential clinical relevance

C D'Amore, C Borgo, S Sarno, M Salvi - Cellular Oncology, 2020 - Springer
Background Protein kinase CK2 inhibition has long been considered as an attractive anti-
cancer strategy based on the following considerations: CK2 is a pro-survival kinase, it is …

Silmitasertib (CX-4945), a clinically used CK2-kinase inhibitor with additional effects on GSK3β and DYRK1A kinases: A structural perspective

P Grygier, K Pustelny, J Nowak, P Golik… - Journal of medicinal …, 2023 - ACS Publications
A clinical casein kinase 2 inhibitor, CX-4945 (silmitasertib), shows significant affinity toward
the DYRK1A and GSK3β kinases, involved in down syndrome phenotypes, Alzheimer's …

Inactivation of paracellular cation-selective claudin-2 channels attenuates immune-mediated experimental colitis in mice

P Raju, N Shashikanth, PY Tsai… - The Journal of …, 2020 - Am Soc Clin Investig
The tight junction protein claudin-2 is upregulated in disease. Although many studies have
linked intestinal barrier loss to local and systemic disease, these have relied on …

Comparative efficacy and selectivity of pharmacological inhibitors of DYRK and CLK protein kinases

MF Lindberg, E Deau, J Arfwedson… - Journal of medicinal …, 2023 - ACS Publications
Dual-specificity, tyrosine phosphorylation-regulated kinases (DYRKs) and cdc2-like kinases
(CLKs) play a large variety of cellular functions and are involved in several diseases …

Inhibition of protein kinase CK2 by flavonoids and tyrphostins. A structural insight

G Lolli, G Cozza, M Mazzorana, E Tibaldi, L Cesaro… - Biochemistry, 2012 - ACS Publications
Sixteen flavonoids and related compounds have been tested for their ability to inhibit three
acidophilic Ser/Thr protein kinases: the Golgi apparatus casein kinase (G-CK) recently …

Unprecedented selectivity and structural determinants of a new class of protein kinase CK2 inhibitors in clinical trials for the treatment of cancer

R Battistutta, G Cozza, F Pierre, E Papinutto, G Lolli… - Biochemistry, 2011 - ACS Publications
5-(3-Chlorophenylamino) benzo [c][2, 6] naphthyridine-8-carboxylic acid (CX-4945), the first
clinical stage inhibitor of protein kinase CK2 for the treatment of cancer, is representative of …

The casein kinase 2 inhibitor, CX-4945, as an anti-cancer drug in treatment of human hematological malignancies

HJ Chon, KJ Bae, Y Lee, J Kim - Frontiers in pharmacology, 2015 - frontiersin.org
The casein kinase 2 (CK2) protein kinase is a pro-survival kinase and therapeutic target in
treatment of various human cancers. CK2 overexpression has been demonstrated in …

Simultaneous CK2/TNIK/DYRK1 inhibition by 108600 suppresses triple negative breast cancer stem cells and chemotherapy-resistant disease

K Sato, AA Padgaonkar, SJ Baker, SC Cosenza… - Nature …, 2021 - nature.com
Triple negative breast cancer (TNBC) remains challenging because of heterogeneous
responses to chemotherapy. Incomplete response is associated with a greater risk of …

Pre-clinical characterization of CX-4945, a potent and selective small molecule inhibitor of CK2 for the treatment of cancer

F Pierre, PC Chua, SE O'Brien, A Siddiqui-Jain… - Molecular and cellular …, 2011 - Springer
In this article we describe the preclinical characterization of 5-(3-chlorophenylamino) benzo
[c][2, 6] naphthyridine-8-carboxylic acid (CX-4945), the first orally available small molecule …