The anti-mitotic program is evaluating CYC140, a
PLK1 inhibitor, in AML/MDS patients.
"The inhibition of the
PLK1 enzyme by onvansertib appears to enhance the efficacy of Zytiga by repressing the ARS pathway, which is consistent with preclinical data."
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.
The
Plk1 inhibitor BI 2536 temporarily arrests primary cardiac fibroblasts in mitosis and generates aneuploidy in vitro .
PLK1 (Polo-like kinase 1) is a member of the Polo-like kinase family [1], which plays an important role in cell cycle regulation [2].
Beasley et al., "Structure-Bioactivity Relationship for Benzimidazole Thiophene Inhibitors of Polo-Like Kinase 1 (
PLK1), a Potential Drug Target in Schistosoma mansoni," PLOS Neglected Tropical Diseases, vol.
Gao et al., "Comprehensive analysis of differentially expressed genes associated with
PLK1 in bladder cancer," BMC Cancer, vol.
Differential control of Eg5-dependent centrosome separation by
Plk1 and Cdk1.
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.
PLK1, a kinase, has been shown to be phosphorylated in response to TLR activation and results from RNA interference suggested that
PLK1 signaling was involved in the TLR-induced inflammatory response (Hu et al., 2013).
These modifications significantly improved the ability of the chimera to reduce tumor size and/or to decrease
PLK1 expression.