Structurally related to the known CK2 inhibitors, 2,6-disubstituted pyrazine and 4,6-disubstituted pyrimidine derivatives were synthesized and their inhibitory activities toward CK2alpha and CK2alpha' were evaluated. Structure-activity relationship study has revealed that several pyrazine derivatives bearing a (pyrrol-3-yl)acetic acid and a monosubstituted aniline possess potent inhibitory activities.

Download full-text PDF

Source
http://dx.doi.org/10.1002/ardp.200700269DOI Listing

Publication Analysis

Top Keywords

ck2 inhibitors
8
inhibitory activities
8
structure-activity relationships
4
relationships pyrazine-based
4
pyrazine-based ck2
4
inhibitors synthesis
4
synthesis evaluation
4
evaluation 26-disubstituted
4
26-disubstituted pyrazines
4
pyrazines 46-disubstituted
4

Similar Publications

Placental malaria is characterized by the massive accumulation and sequestration of infected erythrocytes in the placental intervillous blood spaces, causing severe birth outcomes. The variant surface antigen VAR2CSA is associated with Plasmodium falciparum sequestration in the placenta via its capacity to adhere to chondroitin sulfate A. We have previously shown that the extracellular region of VAR2CSA is phosphorylated on several residues and that the phosphorylation enhances the adhesive properties of CSA-binding infected erythrocytes.

View Article and Find Full Text PDF

The serine/threonine kinase CK2 (formerly known as casein kinase II) plays a crucial role in various CNS disorders and is highly expressed in various types of cancer. Therefore, inhibiting this key kinase could be promising for the treatment of these diseases. The CK2 holoenzyme is formed by the recruitment of two catalytically active CK2α and/or CK2α' subunits by a regulatory CK2β dimer.

View Article and Find Full Text PDF

T-cell acute lymphoblastic leukemia (T-ALL) is an aggressive hematological malignancy with a poor prognosis and limited options for targeted therapies. Identifying new molecular targets to develop novel therapeutic strategies is the pressing immediate issue in T-ALL. Here, we observed high expression of WD Repeat-Containing Protein 5 (WDR5) in T-ALL; with in vitro and in vivo models we demonstrated the oncogenic role of WDR5 in T-ALL by activating cell cycle signaling through its new downstream effector, ATPase family AAA domain-containing 2 (ATAD2).

View Article and Find Full Text PDF

Background: Clear cell renal cell carcinoma (ccRCC) is a type of cancer characterized by a vast intracellular accumulation of lipids that are critical to sustain growth and viability of the cells in the tumour microenvironment. Stearoyl-CoA 9-desaturase 1 (SCD-1) is an essential enzyme for the synthesis of monounsaturated fatty acids and consistently overexpressed in all stages of ccRCC growth.

Methods: Human clear cell renal cell carcinoma lines were treated with small-molecule inhibitors of protein kinase CK2.

View Article and Find Full Text PDF

Polyamines Protect Porcine Sperm from Lipopolysaccharide-induced Mitochondrial Dysfunction and Apoptosis via Casein Kinase 2 Activation.

J Anim Sci

December 2024

Key Laboratory for Animal Genetics, Breeding and Reproduction of Shaanxi Province, College of Animal Science and Technology, Northwest A&F University, Yangling, 712100, Shaanxi, China.

Bacterial contamination is an inevitable issue during the processing of semen preservation in pigs. As a prototypical endotoxin from Gram-negative bacteria in semen, lipopolysaccharide (LPS) undermines sperm function during liquid preservation. Spermine and spermidine could protect cells against LPS-induced injury, and the content of spermine and spermidine in seminal plasma is positively correlated with sperm quality.

View Article and Find Full Text PDF

Want AI Summaries of new PubMed Abstracts delivered to your In-box?

Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!