Indication

Target/marker/pathway

Summary

Licensing status

Publication and contact information

Cancer

Cancer

Heat shock protein 70 (Hsp70)

In vitro studies have identified an allosteric Hsp70 inhibitor that could help treat cancer. Homology modeling was used to identify a conformation-dependent allosteric site in the nucleotide-binding domain of Hsp70 and aided the design of a site-specific 2,5ʹ-thiodipyrimidine-derived inhibitor. In breast cancer cells, the compound increased degradation of the Hsp70-associated proteins HER2 (EGFR2; ErbB2; neu), CRAF (RAF1) and protein kinase B (PKB; PKBA; AKT; AKT1) and increased apoptosis compared with a nonspecific control compound. Next steps include improving the potency and drug-like properties of the inhibitor.
Minneamrita Therapeutics LLC has the small molecule Hsp70 inhibitor minnelide in Phase I trials to treat GI cancer.

SciBX 7(1); doi:10.1038/scibx.2014.8
Published online Jan. 9, 2014

Patent application filed; licensing negotiations ongoing with undisclosed partners

Rodina, A. et al. Chem. Biol.; published online Nov. 14, 2013;
doi:10.1016/j.chembiol.2013.10.008
Contact: Gabriela Chiosis, Memorial Sloan Kettering Cancer Center,
New York, N.Y.
e-mail:

chiosisg@mskcc.org
Contact: Jason C. Young, McGill University, Montreal, Quebec, Canada
e-mail:

jason.young2@mcgill.ca