We used RNAase protection and restriction fragment length polymorphism assays to detect activating mutations of c-src in a spectrum of human tumours. No mutations were detected at codons 98, 381, 444, and 530. We conclude that mutational activation is not the mechanism of enhancement of pp60c-src-specific kinase activity found in a number of human cancer types.

Download full-text PDF

Source
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC1977675PMC
http://dx.doi.org/10.1038/bjc.1991.344DOI Listing

Publication Analysis

Top Keywords

c-src structure
4
structure human
4
human cancers
4
cancers elevated
4
elevated pp60c-src
4
pp60c-src activity
4
activity rnaase
4
rnaase protection
4
protection restriction
4
restriction fragment
4

Similar Publications

Discovery of anti-tumor small molecule lead compounds targeting the SH3 domain of c-Src protein through virtual screening and biological evaluation.

Arch Biochem Biophys

December 2024

Advanced Medical Research Institute, Cheeloo College of Medicine, Shandong University, Jinan, Shandong, 250012, China; The Second Hospital of Shandong University, Cheeloo College of Medicine, Shandong University, Jinan, 250012, China. Electronic address:

Article Synopsis
  • c-Src is a non-receptor tyrosine kinase involved in important cellular functions like growth and movement, and its dysfunction is linked to cancer progression.
  • Current treatments mainly target its kinase domain, but drug resistance limits their effectiveness.
  • This study discovered three compounds that effectively bind to the SH3 domain of c-Src and inhibit its activity, suggesting new potential anti-cancer drugs that could overcome resistance issues.
View Article and Find Full Text PDF

Structural Basis for Long Residence Time c-Src Antagonist: Insights from Molecular Dynamics Simulations.

Int J Mol Sci

September 2024

Jiangsu Key Laboratory of New Drug Research and Clinical Pharmacy, Xuzhou Medical University, 209 Tongshan Road, Xuzhou 221004, China.

Article Synopsis
  • c-Src plays a crucial role in various cancer signaling pathways and is a key target for cancer treatment.
  • Research indicates that extending the residence time of drugs can improve their effectiveness, leading to the development of c-Src antagonists with longer residence times.
  • The study utilized molecular dynamics simulations to analyze the binding behavior of different antagonists, identifying a new compound, DFOGS, that enhances binding stability by replacing an unstable amide group, which could lead to better therapeutic outcomes.
View Article and Find Full Text PDF

Applying molecular hybridization to design a new class of pyrazolo[3,4-d]pyrimidines as Src inhibitors active in hepatocellular carcinoma.

Eur J Med Chem

December 2024

Department of Pharmacy, University of Genoa, Viale Benedetto XV 3, 16132, Genoa, Italy; IRCCS Ospedale Policlinico San Martino, Genova, Largo Rosanna Benzi 10, 16132, Genoa, Italy.

Hepatocellular carcinoma (HCC) is the most common type of liver solid tumor and the second leading cause of cancer-related deaths worldwide. Although new treatment options have been recently approved, the development of tumor resistance and the poor prognosis for advanced HCC make the current standard of care unsatisfying. In this scenario, the non-receptor tyrosine kinase (TK) c-Src emerged as a promising target for developing new anti-HCC agents.

View Article and Find Full Text PDF

Endothelial c-Src Mediates Neovascular Tuft Formation in Oxygen-Induced Retinopathy.

Am J Pathol

December 2024

Centre for Cell Biology of Chronic Disease, Institute for Molecular Bioscience, The University of Queensland, St Lucia, Brisbane, Queensland, Australia. Electronic address:

Vascular retinopathy, characterized by abnormal blood vessel growth in the retina, frequently results in vision impairment or loss. Neovascular tufts, a distinctive pathologic feature of this condition, are highly leaky blood vessel structures, exacerbating secondary complications. Despite their clinical significance, the mechanisms underlying tuft development are not fully elucidated, posing challenges for effective management and treatment of vascular retinopathy.

View Article and Find Full Text PDF

Acacetin (ACA) and biochanin A (BCA) are isomeric monomethoxyflavones with different structural positions of the 4'-methoxy-phenyl group. Both of them are present in many commonly consumed foods, such as citrus fruits and vegetables, and have been discovered with anti-inflammatory activities, but their mechanisms of action are not clearly elucidated at the molecular level. Herein, we reported the structure-activity relationship of ACA and BCA regarding their potency in inhibiting nitric oxide (NO) production, proinflammatory enzyme expression, and mRNA expression of proinflammatory cytokines in the lipopolysaccharide (LPS)-induced RAW 264.

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!