Description
MKT-077 is a cationic rhodacyanine dye that demonstrates antiproliferative activity against cancer cell lines (EC
50s = 1.4-2.2 μM
in vitro) through its ability to inhibit members of the heat shock protein 70 (Hsp70) family of molecular chaperones. It has been shown to bind to an allosteric site conserved in Hsp70 family members, interfering with ATP hydrolysis and abrogating the interaction of the chaperone with the tumor suppressor p53.
References
[1] XIAOKAI LI. Analogues of the Allosteric Heat Shock Protein 70 (Hsp70) Inhibitor, MKT-077, As Anti-Cancer Agents[J]. ACS Medicinal Chemistry Letters, 2013, 4 11: 1042-1047. DOI:
10.1021/ml400204n[2] AIKATERINI ROUSAKI . Allosteric Drugs: The Interaction of Antitumor Compound MKT-077 with Human Hsp70 Chaperones[J]. Journal of Molecular Biology, 2011, 411 3: Pages 614-632. DOI:
10.1016/j.jmb.2011.06.003[3] De Souza, F.I., Zumiotti, A.V., and Da Silva, C.F. Neuregulins 1-α and 1-β on the regeneration the peripheral nerves[J]. Acta Ortop Bras.
