Trovagene is developing onvansertib, a first-in-class, third-generation, oral and highly-selective Polo-like Kinase
1 inhibitor that targets the key master regulator of tumor cell division, for the treatment of leukemias, lymphomas and solid tumor cancers.
According to the company's CEO and chair Thomas Adams, more investors are becoming aware of its multi-faceted clinical development programme of Onvansertib, a first-in-class, third generation, oral and highly-selective Polo-like Kinase
1 (PLK1) inhibitor.
As part of the agreement, PoC Capital LLC will fund the clinical development of Onvansertib, Trovagene's first-in-class, 3rd generation oral and highly selective Polo-like Kinase
1 (PLK1) inhibitor in a Phase 1b/2 clinical trial in patients with metastatic Colorectal Cancer (mCRC), the second leading cause of cancer mortality in the US.
PCM-075 is an oral, highly-selective adenosine triphosphate (ATP) competitive inhibitor of the serine/threonine Polo-like Kinase
1 (PLK1) enzyme, which appears to be over expressed in several different hematologic malignancies and solid tumor cancers.
Lurie Children's Hospital of Chicago found that these tumours' growth and tendency to metastasize are regulated by a protein kinase called Polo-like kinase
4 (PLK4), which is increased in AT/RT.
Acting on the knowledge that the gene polo-like kinase
1 (PLK1) can become overexpressed during ADT and that its overexpression can also stimulate androgen synthesis, Xiaoqui Liu and colleagues tested the effects of administering the PLK1-inhibitor B12536 with low-dose metformin in prostate cancer cells.
The target of the new drug is an enzyme in cancer stem cells and tumor cells called Polo-like kinase
4, which was selected because blocking it negatively affects cell fate decisions associated with cancer stem cell renewal and tumor cell growth, thus stopping tumor growth.
It is worth mentioning that, in addition to AuroraA, the G2/M specific transcription of different genes such as cyclin A, cdc25C, cdc2, polo-like kinase
, and others is regulated by similar tandem repression elements [6-9].
MAP9 is phosphorylated by the mitotic kinases Aurora A (AURKA)  and Polo-like kinase
1 (PLK1)  to ensure bipolar spindle assembly and centrosome integrity.
Ullrich, "Targeting polo-like kinase
1 for cancer therapy," Nature Reviews Cancer, vol.
Sidhu et al., "Expression, adverse prognostic significance and therapeutic small molecule inhibition of Polo-like kinase
1 in multiple myeloma," Leukemia Research, vol.