Number of the records: 1
Phosphatidylinositol 3-Kinase (PI3K) and phosphatidylinositol 3-kinase-related kinase (PIKK) inhibitors: importance of the morpholine ring
- 1.
SYSNO ASEP 0442570 Document Type J - Journal Article R&D Document Type Journal Article Subsidiary J Článek ve WOS Title Phosphatidylinositol 3-Kinase (PI3K) and phosphatidylinositol 3-kinase-related kinase (PIKK) inhibitors: importance of the morpholine ring Author(s) Andrs, M. (CZ)
Kobarecny, J. (CZ)
Jun, D. (CZ)
Hodný, Zdeněk (UMG-J) RID
Bártek, Jiří (UMG-J) RID
Kuca, K. (CZ)Source Title Journal of Medicinal Chemistry. - : American Chemical Society - ISSN 0022-2623
Roč. 58, č. 1 (2015), s. 41-71Number of pages 30 s. Language eng - English Country US - United States Keywords DEPENDENT PROTEIN-KINASE ; STRAND BREAK REPAIR ; SELECTIVE PI3K-BETA INHIBITORS ; TELANGIECTASIA MUTATED KINASE Subject RIV EB - Genetics ; Molecular Biology R&D Projects CZ.1.07/2.3.00/30.0044 GA MŠMT - Ministry of Education, Youth and Sports (MEYS) Institutional support UMG-J - RVO:68378050 UT WOS 000347743700004 DOI 10.1021/jm501026z Annotation Phosphatidylinositol 3-kinases (PI3Ks) and phosphatidylinositol 3-kinase-related protein kinases (PIKKs) are two related families of kinases that play key roles in regulation of cell proliferation, metabolism, migration, survival, and responses to diverse stresses including DNA damage. To design novel efficient strategies for treatment of cancer and other diseases, these kinases have been extensively studied. Despite their different nature, these two kinase families have related origin and share very similar kinase domains. Therefore, chemical inhibitors of these kinases usually carry analogous structural motifs. The most common feature of these inhibitors is a critical hydrogen bond to morpholine oxygen, initially present in the early nonspecific PI3K and PIKK inhibitor 3 (LY294002), which served as a valuable chemical tool for development of many additional PI3K and PIKK inhibitors. While several PI3K pathway inhibitors have recently shown promising clinical responses, inhibitors of the DNA damage-related PIKKs remain thus far largely in preclinical development. Workplace Institute of Molecular Genetics Contact Nikol Škňouřilová, nikol.sknourilova@img.cas.cz, Tel.: 241 063 217 Year of Publishing 2015
Number of the records: 1