|
Synonyms: BMS-875944 | CS-9803 | KAI-9803
Compound class:
Peptide or derivative
Comment: The synthesis of delcasertib is described in [1]. Delcasertib is a peptidic agent which is an isozyme-selective delta protein kinase C (PKCδ) inhibitor. It consists of a cargo peptide (CSFNSYELGSL) derived from the δV1-1 portion of PKCδ which acts to inhibit PKCδ translocation, conjugated to the cell-penetrating, arginine-rich peptide sequence of the HIV type 1 transactivator protein (TAT45-57 CYGRKKRRQRRR) which acts as a cellular delivery system.
|
| References |
|
1. Chen L, Hahn H, Wu G, Chen CH, Liron T, Schechtman D, Cavallaro G, Banci L, Guo Y, Bolli R et al.. (2001)
Opposing cardioprotective actions and parallel hypertrophic effects of delta PKC and epsilon PKC. Proc Natl Acad Sci USA, 98 (20): 11114-9. [PMID:11553773] |
|
2. Ikeno F, Inagaki K, Rezaee M, Mochly-Rosen D. (2007)
Impaired perfusion after myocardial infarction is due to reperfusion-induced deltaPKC-mediated myocardial damage. Cardiovasc Res, 73 (4): 699-709. [PMID:17234167] |
|
3. Inagaki K, Chen L, Ikeno F, Lee FH, Imahashi K, Bouley DM, Rezaee M, Yock PG, Murphy E, Mochly-Rosen D. (2003)
Inhibition of delta-protein kinase C protects against reperfusion injury of the ischemic heart in vivo. Circulation, 108 (19): 2304-7. [PMID:14597593] |
|
4. Tso-ping Li M. (2006)
Pharmaceutical formulation. Patent number: US7265092. Assignee: Kai Pharmaceuticals, Inc.. Priority date: 30/09/2005. Publication date: 04/09/2007. |
