Results 141 to 150 of about 42,681 (176)

Bioorthogonal Probes for Polo‐like Kinase 1 Imaging and Quantification [PDF]

open access: yesAngewandte Chemie - International Edition, 2011
A nuclear protein target, polo-like kinase 1 (PLK1) was imaged using a biocompatible bioorthogonal ligation between a specific drug and a fluorescent dye in live cells. Colocalization of the dye and the protein target was confirmed by antibody staining and by expressing a GFP construct of PLK1.
Ghyslain Budin   +2 more
exaly   +5 more sources

Targeting polo-like kinase 1 for cancer therapy

Nature Reviews Cancer, 2006
Human polo-like kinase 1 (PLK1) is essential during mitosis and in the maintenance of genomic stability. PLK1 is overexpressed in human tumours and has prognostic potential in cancer, indicating its involvement in carcinogenesis and its potential as a therapeutic target.
Klaus Strebhardt   +2 more
exaly   +4 more sources

Structural basis for the inhibition of Polo-like kinase 1

Nature Structural & Molecular Biology, 2013
Polo-like kinase 1 (PLK1) is a master regulator of mitosis and is considered a potential drug target for cancer therapy. PLK1 is characterized by an N-terminal kinase domain (KD) and a C-terminal Polo-box domain (PBD). The KD and PBD are mutually inhibited, but the molecular mechanisms of the autoinhibition remain unclear.
Jun, Xu   +3 more
openaire   +2 more sources

Polo-Like Kinase 1 Pharmacological Inhibition as Monotherapy or in Combination: Comparative Effects of Polo-Like Kinase 1 Inhibition in Medulloblastoma Cells

Anti-Cancer Agents in Medicinal Chemistry, 2017
Medulloblastoma (MB) is one of most frequent malignant tumors that affect children. Despite the relatively good survival rate, long time sequels still represent a challenge for MB. Therefore, in an attempt to reduce treatment aftereffects, new therapeutic targets are constantly being explored.
Julia Alejandra, Pezuk   +4 more
openaire   +2 more sources

BI_2536 - Targeting the Mitotic Kinase Polo-Like Kinase 1 (Plk1)

2009
Human Polo-like kinase 1 (Plk1) is an essential regulator of mitotic progression. Targeted inhibition of this kinase was effective in killing tumor cells in vitro and in vivo. The Plk1 inhibitor BI_2536 was well tolerated and showed antitumor activity in the first clinical trials enrolling patients with advanced solid tumors and refractory or relapsed ...
Wäsch, Ralph   +3 more
openaire   +3 more sources

Polo-Like Kinase 1 and DNA Damage Response

DNA and Cell Biology
Polo-like kinase 1 (Plk1), an evolutionarily conserved serine/threonine protein kinase, is a key regulator involved in the mitotic process of the cell cycle. Mounting evidence suggests that Plk1 is also involved in a variety of nonmitotic events, including the DNA damage response, DNA replication, cytokinesis, embryonic development, apoptosis, and ...
Wei Li, Yongjian Hao
openaire   +2 more sources

Increased Human Polo-Like Kinase-1 Expression in Gliomas

Journal of Neuro-Oncology, 2001
PLK-1 (polo-like kinase) belongs to the family of serine/threonine kinases and is involved in spindle formation, centrosome cycles and chromosome segregation. Hence, the kinase is tightly linked to cell proliferation. We could detect immunohistochemically highly expressed PLK protein in astrocytic tumours depending on the grade of anaplasia, in ...
K, Dietzmann   +4 more
openaire   +2 more sources

Polo-Like Kinase 1 as a Potential Therapeutic Target for Osteosarcoma

Current Pharmaceutical Design, 2015
Osteosarcoma is the most common primary bone malignancy of adolescents and young adults. Existing treatment options and surgical intervention are unable to effectively manage this tumor. Therefore, novel mechanism-based targets and strategies need to be rationally established to strive for improvement in the survival of patients diagnosed with ...
Li, Cheng   +2 more
openaire   +2 more sources

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