Back to Search
Start Over
Identification of TRD‐35 as Potent and Selective DRAK2 Inhibitor.
- Source :
-
Bulletin of the Korean Chemical Society . May2020, Vol. 41 Issue 5, p567-569. 3p. - Publication Year :
- 2020
-
Abstract
- DAP kinase-related apoptosis-inducing protein kinase 2 (DRAK2) is a member of the death-associated protein kinase (DAPK) family[1] and originally identified as a proapoptotic protein with the ability to induce apoptosis when overexpressed in various cell types.[2] However, the apoptosis-inducing ability of DRAK2 seems to be controversial and influenced by cellular factors within a specific cell types.[[3]] Recently, it has been suggested that DRAK2 is closely involved in tumorigenesis; DRAK2 expression was found to be highly elevated in multiple tumor types such as basal-like and HER2-enriched breast cancers. B Vertex-3 b is a pyrimidine C5-methylated analog of B UC-3 b .[9] When B UC-3 b was assessed to ATP-binding site of 359 diverse kinases at 10 micromolar concentration, it bound to 337 kinases including CDK2, CDK5, JNK3, and others. We believe the nitrile of the B UC-3 b has hydrogen-bonding interaction to DRAK2 Lys62 and plays a key role for its kinase promiscuous activities. [Extracted from the article]
- Subjects :
- *INDUSTRIAL chemistry
*PROTEIN kinases
*IMIDAZOPYRIDINES
Subjects
Details
- Language :
- English
- ISSN :
- 02532964
- Volume :
- 41
- Issue :
- 5
- Database :
- Academic Search Index
- Journal :
- Bulletin of the Korean Chemical Society
- Publication Type :
- Academic Journal
- Accession number :
- 143380937
- Full Text :
- https://doi.org/10.1002/bkcs.12005