75914-62-4Relevant academic research and scientific papers
Preparation of targeted eEF2K degradation agent and application of targeted eEF2K degradation agent in breast cancer prevention
-
Paragraph 0032-0033, (2020/06/17)
The invention relates to preparation of a degradation agent targeting eEF2K and application of the degradation agent in breast cancer prevention, and belongs to the technical field of antitumor pharmacy. The technical problem to be solved by the invention is to provide a compound used as an eEF2K degradation agent. The compound comprises a compound product as shown in a specification in the invention or a pharmaceutically acceptable salt thereof. The compound product or the pharmaceutically acceptable salt thereof has activity of degrading eEF2K protein, can be used as a degradation agent of eEF2K, and can induce apoptosis of tumor cells so as to play a role in resisting breast cancer. The compound is preferably an anti-breast cancer compound, and is characterized by being a compound capable of degrading eEF2K protein.
Designing an eEF2K-Targeting PROTAC small molecule that induces apoptosis in MDA-MB-231 cells
Liu, Yao,Zhen, Yongqi,Wang, Guan,Yang, Gaoxia,Fu, Leilei,Liu, Bo,Ouyang, Liang
, (2020/07/27)
Eukaryotic elongation factor 2 kinase (eEF2K) is a key α-kinase that negatively regulates the extension step of protein synthesis, which consumes most of the energy and amino acids required for protein synthesis. Studies have found that eEF2K protein is related to the breast cancer. However, existing inhibitor effect has not achieved the desired effect in cancer therapy. Proteolysis target chimeric (PROTAC) technology is uses proteasome to degrade target protein to achieve the purpose of inhibiting tumour cell growth. Here, we reported that the use of PROTAC strategy in combining with star eEF2K inhibitor A484954 and its potential derivatives. Consequently, candidate compound 11l was found to degrade eEF2K and induce apoptosis in human breast carcinoma MDA-MB-231 cells. Together, these findings demonstrate that our eEF2K-targeting PROTAC small molecule would be a potential new strategy for future breast cancer therapy.
Alkylxanthine phosphonates and alkylxanthine phosphine oxides and their use as pharmaceuticals
-
, (2008/06/13)
Alkylxanthine phosphonates and alkylxanthine phosphine oxides and their use as pharmaceuticals A compound of the formula STR1 where R1 and R3 are identical or different and at least one of the radicals R1 and R3 is a radical of the formula XI STR2 in which E is a covalent bond or a (C1 -C5)-alkyl, are suitable for the production of pharmaceuticals for the treatment of muscular atrophy, cachexia, muscular dystrophy, sepsis, septic shock, endotoxic shock, systemic inflammation response syndrome, adult respiratory distress syndrome, cerebral malaria, chronic pneumonia, pulmonary sarcoidosis, reperfusion damage, scar formation, inflammation of the bowel and ulcerative colitis, as a result of infections, acquired immune deficiency syndrome, cancer, trauma and other disorders having increased protein loss, peripheral circulatory disorders, disorders having altered leucocyte adhesion, and also disorders which are accompanied by an increased or unregulated tumor necrosis factor production such as rheumatoid arthritis, rheumatoid spondylitis, osteoarthritis and other arthritic disorders.
Composition and methods for the treatment of chronic obstructive airway disease and cardiac disease using 3-alkylxanthines
-
, (2008/06/13)
Compounds having activity against chronic obstructive airway disease or cardiac disease, characterized by the formula STR1 wherein R1 is n-propyl, n-butyl, isobutyl, n-pentyl, 2-methylbutyl, 3-methylbutyl, 2,2-dimethylpropyl, cyclopropyl, cyclo
