PLK1

PLK1

A gene on chromosome 16p12.2 that encodes a member of the CDC5/Polo subfamily of serine/threonine protein kinases, which performs several key functions during the M phase of the cell cycle—e.g., regulating centrosome maturation and spindle assembly, removing cohesins from chromosome arms, inactivating anaphase-promoting complex/cyclosome (APC/C) inhibitors, and regulating mitotic exit and cytokinesis.
 
Molecular pathology
Defects in PLK1 are associated with gastric, thyroid and B-cell malignancies, with increased expression linked to a worse prognosis.
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References in periodicals archive ?
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.