Protein kinase CK2: a potential therapeutic target for diverse human diseases

C Borgo, C D'Amore, S Sarno, M Salvi… - Signal transduction and …, 2021 - nature.com
CK2 is a constitutively active Ser/Thr protein kinase, which phosphorylates hundreds of
substrates, controls several signaling pathways, and is implicated in a plethora of human …

A review on anticancer potential of bioactive heterocycle quinoline

O Afzal, S Kumar, MR Haider, MR Ali, R Kumar… - European Journal of …, 2015 - Elsevier
The advent of Camptothecin added a new dimension in the field anticancer drug
development containing quinoline motif. Quinoline scaffold plays an important role in …

Hybrid drugs—a strategy for overcoming anticancer drug resistance?

M Szumilak, A Wiktorowska-Owczarek, A Stanczak - Molecules, 2021 - mdpi.com
Despite enormous progress in the treatment of many malignancies, the development of
cancer resistance is still an important reason for cancer chemotherapy failure. Increasing …

CX-4945, an orally bioavailable selective inhibitor of protein kinase CK2, inhibits prosurvival and angiogenic signaling and exhibits antitumor efficacy

A Siddiqui-Jain, D Drygin, N Streiner, P Chua, F Pierre… - Cancer research, 2010 - AACR
Malignant transformation and maintenance of the malignant phenotype depends on
oncogenic and non-oncogenic proteins that are essential to mediate oncogene signaling …

Thiazole in the targeted anticancer drug discovery

A Ayati, S Emami, S Moghimi… - Future medicinal …, 2019 - Taylor & Francis
Cancer is known as one of the main causes of death in the world; and many compounds
have been synthesized to date with potential use in cancer therapy. Thiazole is a versatile …

The RNA polymerase I transcription machinery: an emerging target for the treatment of cancer

D Drygin, WG Rice, I Grummt - Annual review of pharmacology …, 2010 - annualreviews.org
The RNA polymerase I (Pol I) transcription machinery in the nucleolus is the key
convergence point that collects and integrates a vast array of information from cellular …

Discovery and SAR of 5-(3-Chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic Acid (CX-4945), the First Clinical Stage Inhibitor of Protein Kinase CK2 for the …

F Pierre, PC Chua, SE O'Brien… - Journal of medicinal …, 2011 - ACS Publications
Herein we chronicle the discovery of CX-4945 (25n), a first-in-class, orally bioavailable ATP-
competitive inhibitor of protein kinase CK2 in clinical trials for cancer. CK2 has long been …

Addiction to protein kinase CK2: a common denominator of diverse cancer cells?

M Ruzzene, LA Pinna - Biochimica et Biophysica Acta (BBA)-Proteins and …, 2010 - Elsevier
At variance with most oncogenic protein kinases whose malignancy is generally due to
genetic alterations conferring constitutive activity, CK2 is a highly pleiotropic Ser/Thr protein …

Protein kinase CK2 in health and disease: CK2: a key player in cancer biology

JH Trembley, G Wang, G Unger, J Slaton… - Cellular and molecular …, 2009 - Springer
Elevated levels of protein kinase CK2 (formerly casein kinase 2 or II) have long been
associated with increased cell growth and proliferation both in normal and cancer cells. The …

A large-scale method to measure absolute protein phosphorylation stoichiometries

R Wu, W Haas, N Dephoure, EL Huttlin, B Zhai… - Nature …, 2011 - nature.com
The functional role of protein phosphorylation is impacted by its fractional stoichiometry.
Thus, a comprehensive strategy to study phosphorylation dynamics should include an …