MPK-09, a small molecule inspired from bioactive styryllactone restores the wild-type function of mutant p53
Data(s) |
01/07/2013
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Resumo |
In the search for more efficacious and less toxic cancer drugs, the tumor suppressor p53 protein has long been a desirable therapeutic target. In the recent past, few independent studies have demonstrated that the antitumor activity of wild-type p53 can be restored in cancer cells harboring mutant form of p53 using small molecule activators. In this study, we describe a novel small molecule MPK-09, which is selective and highly potent against allele specific p53 mutations mainly, R175H, R249S, R273H, R273C, and E285K. Except E285K, all other mutations tested are among the six ``hot spot'' p53 mutations reported in majority of human cancer. Furthermore, our study conclusively demonstrates that the apoptotic activity of the small molecule MPK-09 against cancer cells harboring R273C and E285K mutations is due to restoration of the wild-type conformation to the corresponding mutant form of p53. |
Formato |
application/pdf application/pdf |
Identificador |
http://eprints.iisc.ernet.in/47443/1/ACS_Chem_Biol_8-7_1429_2013.pdf http://eprints.iisc.ernet.in/47443/2/ACS_Chem_Bio_8-7_1_2013.pdf Metri, Prashant K and Naz, Sarwat and Kondaiah, Paturu and Prasad, Kavirayani R (2013) MPK-09, a small molecule inspired from bioactive styryllactone restores the wild-type function of mutant p53. In: ACS Chemical Biology, 8 (7). pp. 1429-1434. |
Publicador |
American Chemical Society |
Relação |
http://dx.doi.org/10.1021/cb3005929 http://eprints.iisc.ernet.in/47443/ |
Palavras-Chave | #Molecular Reproduction, Development & Genetics (formed by the merger of DBGL and CRBME) #Organic Chemistry |
Tipo |
Journal Article PeerReviewed |