Related Experiment Video
Updated: Mar 30, 2026
11:11
Identification of Novel CK2 Kinase Substrates Using a Versatile Biochemical Approach
Published on: February 21, 2019
7.9K
Casein kinases as potential therapeutic targets.
Giorgio Cozza1, Lorenzo A Pinna1,2
1a 1 University of Padova, Department of Biomedical Sciences , Via Ugo Bassi 58B, 35131 Padova, Italy giorgio.cozza@unipd.it.
Expert Opinion on Therapeutic Targets
|November 14, 2015
Summary
This study compares three casein kinase (CK) classes as therapeutic targets. CK1 and CK2 inhibitors show promise for cancer and neurodegeneration, while Fam20C activators may aid mineralization disorders.
Area of Science:
- Biochemistry
- Molecular Biology
- Pharmacology
Background:
- Casein kinases (CKs) encompass three distinct families: CK1, CK2, and Golgi-CK (G-CK)/Fam20C.
- While sharing in vitro casein phosphorylation, these CK families are structurally unrelated.
- All CK families are implicated in various human diseases, necessitating a comparative therapeutic target analysis.
Purpose of the Study:
- To provide a comparative analysis of CK1, CK2, and G-CK/Fam20C as potential therapeutic targets.
- To evaluate the druggability of different casein kinase families for disease treatment.
Main Methods:
- Review and comparative analysis of existing literature on CK1, CK2, and G-CK/Fam20C.
- Examination of therapeutic strategies involving inhibitors and activators for each CK class.
Main Results:
- CK2 is strongly linked to cancer, with inhibitors in clinical trials.
- CK1 inhibitors are being developed for oncology and neurodegenerative diseases.
- G-CK/Fam20C's pathogenic role stems from loss-of-function; activators are under investigation.
Conclusions:
- Optimized CK2 and CK1 inhibitors offer new therapeutic avenues for cancer and neurodegeneration.
- Development of G-CK/Fam20C activators could benefit bio-mineralization and hypophosphatemic diseases.
Related Concept Videos
02:54Protein Kinases and Phosphatases
15.6K
Proteins undergo chemical modifications that trigger changes in the charge, structure, and conformation of the proteins. Phosphorylation, acetylation, glycosylation, nitrosylation, ubiquitination, lipidation, methylation, and proteolysis are various protein modifications that regulate protein activity. Such modifications are usually enzyme-driven.
Protein kinases
Many proteins in the cell are regulated by phosphorylation, the addition of a phosphate group. A family of enzymes called kinases...
Protein kinases
Many proteins in the cell are regulated by phosphorylation, the addition of a phosphate group. A family of enzymes called kinases...
15.6K
02:54Protein Kinases and Phosphatases
4.7K
4.7K
01:27Transducer Mechanism: Enzyme-Linked Receptors
4.9K
Enzyme-linked receptors are cell-surface receptors acting as an enzyme or associating with an enzyme intracellularly. They make excellent drug targets. Drugs can bind to the extracellular ligand-binding domain or directly affect their enzymatic domain and alter their activity.
Major types that are helpful drug targets include:
Major types that are helpful drug targets include:
4.9K
01:25cAMP-dependent Protein Kinase Pathways
9.2K
Cyclic Adenosine Monophosphate (cAMP) is an essential second messenger that activates protein kinase A (PKA) and regulates various biological processes. A single epinephrine molecule binds to GPCR and activates several heterotrimeric G proteins, each stimulating multiple adenylyl cyclase, amplifying the signal, and synthesizing large numbers of cAMP molecules. Small changes in cAMP concentration affect PKA activity. The binding of four cAMP molecules induces a conformational change in PKA,...
9.2K
01:29Pharmacogenomics: Identification of New Drug Targets
76
Advances in genomics have profoundly influenced drug discovery by increasing both the speed and accuracy of pharmaceutical development. Pharmacogenomics, which examines how genetic variation influences drug response, facilitates the identification of novel therapeutic targets and enables patient stratification for personalized treatment. These strategies contribute to improved drug efficacy, minimized adverse effects, and more efficient clinical trial design.Mapping genetic differences...
76
01:22Amplifying Signals via Enzymatic Cascade
19.2K
When a ligand binds to a cell-surface receptor, the receptor's intracellular domain changes shape, which may either activate its enzyme function or allow its binding to other molecules. The initial signal is amplified by most signal transduction pathways. This means that a single ligand molecule can activate multiple molecules of a downstream target. Proteins that relay a signal are most commonly phosphorylated at one or more sites, activating or inactivating the protein. Kinases catalyze...
19.2K