BKT300 is a novel, first in class, potent and highly selective, small molecule PRC1 inhibitor developed as a targeted treatment for patients whose cancers are likely to be dependent on PRC1.
BKT300 binds PRC1 at high affinity and inhibits its function by arresting PRC1 in its phosphorylated non-active conformation.
PRC1 inhibition following BKT300 treatment leads to a dramatic reduction in CDC25c expression, up regulates p21 and inhibits PLK-1 activation leading to induction of tumor cell death. These molecular events drive cancer cells to mitotic catastrophe.
In addition to the induction of cancer cell death, BKT300 is a powerful inhibitor of cancer cells migration.
Protein Regulator of Cytokinesis 1(PRC1) is a scaffold protein that regulates essential metabolic pathways of cancer cells proliferation, survival, invasion and metastasis.
PRC1 was shown to be overexpressed in different cancer types, such as breast cancer, lung cancer, colorectal cancer, hepatocellular carcinoma, pancreatic cancer, ovarian cancer, bladder cancer well as hematological cancers. Clinical data analysis supports PRC1's key role in tumor resistance, recurrence and poor prognosis.