Linear Regression QSAR Models for Polo-Like Kinase-1 Inhibitors
A structurally diverse dataset of 530 polo-like kinase-1 (PLK1) inhibitors is compiled from the ChEMBL database and studied by means of a conformation-independent quantitative structure-activity relationship (QSAR) approach.
Pablo R. Duchowicz
doaj +1 more source
Modulating Polo-Like Kinase 1 as a Means for Cancer Chemoprevention [PDF]
Naturally occurring agents have always been appreciated for their medicinal value for both their chemopreventive and therapeutic effects against cancer. In fact, the majority of the drugs we use today, including the anti-cancer agents, were originally derived from natural compounds, either in their native form or modified to enhance their ...
Travis L, Schmit +2 more
openaire +2 more sources
PLK1 inhibitors as a new targeted treatment for adrenocortical carcinoma
Adrenocortical carcinoma (ACC) is an aggressive malignancy with limited treatment options. Polo-like kinase 1 (PLK1) is a promising drug target; PLK1 inhibitors (PLK1i) have been investigated in solid cancers and are more effective in TP53-mutated cases.
Emily Warmington +12 more
doaj +1 more source
Polo-like kinase 1 (PLK1) signaling in cancer and beyond
PLK1 is an evolutionary conserved Ser/Thr kinase that is best known for its role in cell cycle regulation and is expressed predominantly during the G2/S and M phase of the cell cycle. PLK1-mediated phosphorylation of specific substrates controls cell entry into mitosis, centrosome maturation, spindle assembly, sister chromatid cohesion and cytokinesis.
Styliani Iliaki +2 more
openaire +3 more sources
Toxicity modelling of Plk1-targeted therapies in genetically engineered mice and cultured primary mammalian cells [PDF]
High attrition rates of novel anti-cancer drugs highlight the need for improved models to predict toxicity. Although polo-like kinase 1 (Plk1) inhibitors are attractive candidates for drug development, the role of Plk1 in primary cells remains widely ...
Kappel, Sven +74 more
core +1 more source
The transforming parasite Theileria co-opts host cell mitotic and central spindles to persist in continuously dividing cells. [PDF]
The protozoan parasite Theileria inhabits the host cell cytoplasm and possesses the unique capacity to transform the cells it infects, inducing continuous proliferation and protection against apoptosis.
Conrad von Schubert +5 more
doaj +1 more source
STIL binding to Polo-box 3 of PLK4 regulates centriole duplication [PDF]
Polo-like kinases (PLK) are eukaryotic regulators of cell cycle progression, mitosis and cytokinesis; PLK4 is a master regulator of centriole duplication.
Timm Maier +15 more
core +1 more source
On the regulation of centriole duplication in human cells : exploring the interactions of polo-like kinase 4 with the centrosomal proteins Cep192 and STIL [PDF]
Centrioles duplicate once in each cell cycle to give rise to two centrosomes that form the spindle poles during mitosis. Aberrant centriole duplication can result in the formation of supernumerary centrosomes, leading to incorrect spindle assembly and ...
Gabryjonczyk, Anna-Maria
core +1 more source
Nearly one-third of patients with acute myeloid leukemia have FMS-like tyrosine kinase 3 mutations and thus have poor survival prospects. Receptor tyrosine kinase anexelekto is critical for FMS-like tyrosine kinase 3 signaling and participates in FMS ...
Peter P. Ruvolo +11 more
doaj +1 more source
Tumor inhibition by genomically integrated inducible RNAi-cassettes [PDF]
RNA interference (RNAi) has emerged as a powerful tool to induce loss-of-function phenotypes by post-transcriptional silencing of gene expression. In this study we wondered whether inducible RNAi-cassettes integrated into cellular DNA possess the power ...
Kappel, Sven +8 more
core +1 more source

