Roscovitine [CY-202, (R)-Roscovitine, Seliciclib] is a small molecule that inhibits cyclin-dependent kinases (CDKs) through direct competition at the ATP-binding site. It is a broad-range purine inhibitor, which inhibits CDK1, CDK2, CDK5 and CDK7, but is a poor inhibitor for CDK4 and CDK6. Roscovitine is widely used as a biological tool in cell cycle, cancer, apoptosis and neurobiology studies. Moreover, it is currently evaluated as a potential drug to treat cancers, neurodegenerative diseases, inflammation, viral infections, polycystic kidney disease and glomerulonephritis. This review focuses on the use of roscovitine in the disease model as well as clinical model research.
Download full-text PDF |
Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4486920 | PMC |
| http://dx.doi.org/10.3978/j.issn.2305-5839.2015.03.61 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Antiproliferative Activity and Molecular Docking of Some Pyrazole-Based Quinazolinone, Benzimidazole, and Tetrazinethione Derivatives.
J Biochem Mol Toxicol
January 2025
Chemistry Department, Faculty of Science, Ain Shams University, Cairo, Egypt.
Researchers are actively looking for novel anticancer medications because cancer is one of the leading causes of mortality worldwide. A fascinating area of study in medicinal chemistry is the screening of antioxidants for novel anticancer medicines, as antioxidants have lately been used as therapeutic candidates to combat a variety of ailments in aerobic species. Additionally, pyrazole-based heterocycle synthesis is a productive approach to the drug development process.
View Article and Find Full Text PDFSerum starvation as the most suitable method for inducing G/G phase cell cycle arrest in six-banded armadillo (Euphractus sexcinctus) skin-derived fibroblast lines.
Tissue Cell
December 2024
Laboratory of Animal Biotechnology, Federal Rural University of Semi-Arid (UFERSA), Mossoró, RN, Brazil. Electronic address:
Background: Several studies have evaluated different cell cycle synchronization methods to improve reprogramming efficiency aimed at wild species conservation. The six-banded armadillo is one of the wild mammals with significant ecological and biomedical interests but has not yet been evaluated for reprogramming purposes.
Objective: We investigated the effects in a time-dependent manner of serum starvation (SS; 0.
Roscovitine, a CDK Inhibitor, Reduced Neuronal Toxicity of mHTT by Targeting HTT Phosphorylation at S1181 and S1201 In Vitro.
Int J Mol Sci
November 2024
Division of Neurobiology, Department of Psychiatry, Johns Hopkins University School of Medicine, Baltimore, MD 21287, USA.
Article Synopsis
- * Research has focused on post-translational modifications of the HTT protein, with findings showing that certain modifications can reduce the toxicity of the mutant protein in cell and animal models.
- * A study identified cyclin-dependent kinases (CDKs) that influence the phosphorylation of specific serine sites on HTT, and the CDK inhibitor roscovitine demonstrated protective effects against mutant HTT toxicity in HD mice, highlighting its potential as a pre-clinical therapeutic.
Exploring the role of Cdk5 on striatal synaptic plasticity in a 3-NP-induced model of early stages of Huntington's disease.
Front Mol Neurosci
November 2024
Laboratorio de Neurofisiología del Desarrollo y la Neurodegeneración, Unidad de Biomedicina, FES-I, Universidad Nacional Autónoma de México, Mexico City, Mexico.
Article Synopsis
- Impaired mitochondrial function is linked to neurodegenerative diseases like Huntington's disease (HD), with 3-NP as a toxin that induces relevant cellular changes in the striatum.
- Cyclin-dependent kinase 5 (Cdk5) is a key signaling molecule involved in both cellular pathology and synaptic plasticity, prompting investigations into its role in corticostriatal changes under 3-NP treatment.
- The study reveals that while Cdk5 levels increase with 3-NP treatment, it affects long-term depression (LTD) and long-term potentiation (LTP) differently, suggesting that Cdk5 may alter signaling pathways that affect neuronal activity during the early phases of neurodegeneration.
Novel Fused Pyrimidines as Potent Cyclin-Dependent Kinases Inhibitor for Gastric Adenocarcinoma: Combined In Vitro, In Silico Anticancer Studies.
Chem Biol Drug Des
November 2024
Supramolecular and Catalysis Lab, Department of Natural Products Chemistry, School of Chemistry, Madurai Kamaraj University, Madurai, India.
Our research aims to design novel pyrimidine derivatives inspired by the common pyrimidine core found in many FDA-approved drugs. However, extensive prior research on the pyrimidine scaffold has made discovering new molecules more challenging. To overcome this obstacle, we employed a molecular hybridisation strategy, opting to hybridise tetralin and pyrimidine, recognising their potential in cancer therapeutics.
View Article and Find Full Text PDFWant 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!