In vitro study of the Polo‐like kinase 1 inhibitor volasertib in non‐small‐cell lung cancer reveals a role for the tumor suppressor p53
Sign Up to like & getrecommendations! Published in 2019 at "Molecular Oncology"
DOI: 10.1002/1878-0261.12477
Abstract: Polo‐like kinase 1 (Plk1), a master regulator of mitosis and the DNA damage response, is considered to be an intriguing target in the research field of mitotic intervention. The observation that Plk1 is overexpressed in… read more here.
Keywords: plk1; like kinase; volasertib; polo like ... See more keywords
The cell cycle‐related genes RHAMM, AURKA, TPX2, PLK1, and PLK4 are associated with the poor prognosis of breast cancer patients
Sign Up to like & getrecommendations! Published in 2022 at "Journal of Cellular Biochemistry"
DOI: 10.1002/jcb.30205
Abstract: Breast cancer is the third most common type of cancer diagnosed. Cell cycle is a complex but highly organized and controlled process, in which normal cells sense mitogenic growth signals that instruct them to enter… read more here.
Keywords: plk1; breast cancer; cell cycle; cancer ... See more keywords
Dual PLK1 and STAT3 inhibition promotes glioblastoma cells apoptosis through MYC.
Sign Up to like & getrecommendations! Published in 2020 at "Biochemical and biophysical research communications"
DOI: 10.1016/j.bbrc.2020.09.008
Abstract: Glioblastoma (GBM) is the deadliest primary brain tumor that is highly resistant to current treatments. Polo-like kinase 1 (PLK1) and signal transducer and activator of transcription 3 (STAT3) are highly expressed in gliomas, especially GBM.… read more here.
Keywords: plk1; apoptosis; dual plk1; inhibition ... See more keywords
Aflatoxin B1 induces S phase arrest by upregulating the expression of p21 via MYC, PLK1 and PLD1.
Sign Up to like & getrecommendations! Published in 2019 at "Biochemical pharmacology"
DOI: 10.1016/j.bcp.2019.05.008
Abstract: Aflatoxin B1 (AFB1), a member of the aflatoxin family, is a common contaminant in foods and feeds, and AFB1 exposure is associated with various clinical conditions. Thus far, research on the toxicity of AFB1 has… read more here.
Keywords: plk1; pld1; p21; phase arrest ... See more keywords
A Non-canonical BRCT-Phosphopeptide Recognition Mechanism Underlies RhoA Activation in Cytokinesis
Sign Up to like & getrecommendations! Published in 2020 at "Current Biology"
DOI: 10.1016/j.cub.2020.05.090
Abstract: Cytokinesis partitions the cell contents to complete mitosis. During cytokinesis, polo-like kinase 1 (PLK1) activates the small GTPase RhoA to assemble a contractile actomyosin ring. PLK1 is proposed to pattern RhoA activation by creating a… read more here.
Keywords: brct; plk1; cytokinesis; cyk4 ... See more keywords
A PLK1 kinase inhibitor enhances the chemosensitivity of cisplatin by inducing pyroptosis in oesophageal squamous cell carcinoma
Sign Up to like & getrecommendations! Published in 2019 at "EBioMedicine"
DOI: 10.1016/j.ebiom.2019.02.012
Abstract: Background Targeting PLK1 has recently been proven as a viable therapeutic strategy against oesophageal squamous cell carcinom (ESCC). Therefore, this study aimed to explore whether the PLK1 inhibitor BI2536 is able to sensitize ESCC cells… read more here.
Keywords: plk1; inhibitor; pyroptosis; escc cells ... See more keywords
Structure-based design and SAR development of novel selective polo-like kinase 1 inhibitors having the tetrahydropteridin scaffold.
Sign Up to like & getrecommendations! Published in 2019 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2019.111769
Abstract: Polo-like kinase 1 (Plk1) is a validated target for the treatment of cancer. In this report, by analyzing amino acid residue differences among the ATP-binding pockets of Plk1, Plk2 and Plk3, novel selective Plk1 inhibitors… read more here.
Keywords: plk1; like kinase; plk1 inhibitors; polo like ... See more keywords
Small-Molecule Dual PLK1 and BRD4 Inhibitors are Active Against Preclinical Models of Pediatric Solid Tumors
Sign Up to like & getrecommendations! Published in 2019 at "Translational Oncology"
DOI: 10.1016/j.tranon.2019.09.013
Abstract: Simultaneous inhibition of multiple molecular targets is an established strategy to improve the continuance of clinical response to therapy. Here, we screened 49 molecules with dual nanomolar inhibitory activity against BRD4 and PLK1, best classified… read more here.
Keywords: plk1; plk1 brd4; dual plk1; small molecule ... See more keywords
Novel Macrocyclic Peptidomimetics Targeting the Polo-Box Domain of Polo-Like Kinase 1.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.1c01359
Abstract: The polo-box domain (PBD) of Plk1 is a promising target for cancer therapeutics. We designed and synthesized novel phosphorylated macrocyclic peptidomimetics targeting PBD based on acyclic phosphopeptide PMQSpTPL. The inhibitory activities of 16e on Plk1-PBD… read more here.
Keywords: plk1; box domain; pbd; plk1 pbd ... See more keywords
Genome-wide CRISPR-cas9 knockout screening identifies GRB7 as a driver for MEK inhibitor resistance in KRAS mutant colon cancer
Sign Up to like & getrecommendations! Published in 2021 at "Oncogene"
DOI: 10.1038/s41388-021-02077-w
Abstract: Targeting the KRAS pathway is a promising but challenging approach for colorectal cancer therapy. Despite showing potent efficacy in BRAF-mutated melanoma, MEK inhibitors appeared to be tolerated by colorectal cancer cells due to their intrinsic… read more here.
Keywords: genome wide; plk1; mek inhibitor; mek inhibitors ... See more keywords
PLK1 promotes proliferation and suppresses apoptosis of renal cell carcinoma cells by phosphorylating MCM3
Sign Up to like & getrecommendations! Published in 2019 at "Cancer Gene Therapy"
DOI: 10.1038/s41417-019-0094-x
Abstract: Minichromosome maintenance 3 (MCM3) protein has been widely studied due to its essential role in DNA replication. In addition, it is overexpressed in several human tumor types. However, the role of this protein in renal… read more here.
Keywords: renal cell; plk1; cell carcinoma; proliferation ... See more keywords