Novel inhibitors of Heat Shock Protein 70 (Hsp70)
Inducible Heat Shock Protein 70 (HSP-70) is overexpressed in a wide spectrum of human tumors and is a potent inhibitor of apoptosis. Its expression correlates with metastasis and poor outcomes in various cancers including breast, endometrial, oral, colorectal and prostate cancers, as well as certain types of leukemia. HSP-70 is also a drug target in several neurodegenerative diseases. Identification of small molecule inhibitors selective for HSP-70 could provide new therapeutic tools for cancer treatment, as well as a variety of other HSP-70 associated diseases.
The current technology encompasses the production of a pharmaceutical composition that inhibits HSP-70, acting as a novel therapeutic for a variety of diseases, including multiple forms of cancer and neurodegenerative diseases. Named HS-72, this novel compound allosterically and selectively inhibits HSP-70 by reducing ATP affinity. The inventors demonstrate in vivo and in vitro that HS-72 inhibits HSP-70 activity in a Huntington’s cell model and across multiple tumorigenic cell lines. For example, HS-72 reduces tumor growth in a spontaneous mouse mammary tumor model. Furthermore, the inventors demonstrate that HS-72 can inhibit tumor growth of multiple breast cancer cell lines (BT474, MCF7, and SkBr3) and high concentrations of HS-72 significantly induced apoptosis of human breast cancer cell proliferation:
Parasitic infection eradication – Inhibition of HSP-70 and HSP-90 has been shown to inhibit parasitic infections in vitro.
- S-72 could treat a large variety of HSP70 overexpressed cancers
- Combats resistance to radiation and chemotherapy in cancer patients
- Targets several neurodegenerative disorders, including Parkinson’s, Huntington’s, Alzheimer’s, and muscular atrophy
Duke File (IDF) Number
- Haystead, Timothy
- Bodoor, Khaldon
- Hughes, Philip
- Howe M., et al (2014). Identification of an allosteric small-molecule inhibitor selective for the inducible form of heat shock protein 70. Chem Biol. 21(12):1648-59.
For more information please contact
- Gopalakrishnan, Karthik
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