Hec 1 Inhibitor For Cancer Treatment

Brief Description

Hec1 is a novel target for cancer therapy. Researchers at UC Irvine developed Hec1 inhibitors that could potentially be new anti-cancer drugs.

Full Description

Hec1 overexpression has been observed in a variety of human cancers and is associated with adverse clinical outcomes in primary breast cancers. The phosphorylation of Hec1 by Nek2 is critical for proper mitotic progress and chromosome segregation. Perturbation of Hec1 or Nek2 function by antagonists leads to mitotic abnormalities, which lead to cell death. Therefore, Hec1 could be an important target for developing novel cancer therapies.

Researchers at UC Irvine developed small compounds, INH41, INH78, INH81, INH154, INH168, and INH174, that directly bound to Hec1. They were identified as potent, sub-micromolar IC50 inhibitors of cancer cell growth. In addition, both INH41 and INH154, suppressed leukemia, osteosarcoma, and glioblastoma cancer cell growth (see the attached table). Neither INH41 nor INH154 had significant growth inhibitory effects on non-tumorgenic fibroblast and epithelial cells, which makes those compounds potentially ideal treatments for a variety of cancers.

Table. INH41 and INH154 suppressed leukemia, osteosarcoma, and glioblastoma cancer cell growth.

Suggested uses

The invention can be used for cancer therapy.

Advantages

The invented Hec1 inhibitory compounds have specific adverse effects to the cancer cells. No significant growth inhibitory effects to normal tissue were caused by the Hec1 inhibitors treatments.

Patent Status