Tubulin is a very important target for cancer-fighting therapies; therefore, the cancer research community continues to adopt new ways of developing the therapeutic potential of tubulin and tubulin-associated proteins. Two families of tubulin-associated kinases, Aurora and Polo-like, have received significant attention regarding how they contribute to tumorigenesis and can be targeted with selective small molecule inhibitors. Aurora and Polo-like kinases play essential roles in centrosome separation, chromosome alignment and segregation, and cytokinesis. Inhibition of any of these kinases results in abnormal mitotic events (which vary depending on the particular family member) and eventually leads to apoptosis. Because of the biological consequences of inhibiting these kinases, several Aurora or Polo-like selective inhibitors have advanced to various stages of preclinical and clinical development; the most advanced are currently in phase 2 clinical trials.
Download full-text PDF |
Source |
---|---|
http://dx.doi.org/10.1007/s11912-008-0020-0 | DOI Listing |
Cancer Sci
January 2025
Department of Orthopaedic Surgery, Osaka University Graduate School of Medicine, Osaka, Japan.
Effective therapeutic strategies for epithelioid sarcoma (EpS), a high-grade soft tissue sarcoma characterized by loss of integrase interactor 1 (INI1), have not yet been developed. The present study therefore investigated the association between INI1 loss and upregulation of the aurora kinase A (AURKA)/polo-like kinase 1 (PLK1)/cell division cycle 25C (CDC25C) axis, as well as the therapeutic relevance of this axis in EpS. Notably, our findings showed that the reintroduction of INI1 in VA-ES-BJ cells significantly reduced proliferation, mitigated tumorigenicity, and negatively regulated the expression of AURKA and its downstream effectors, as well as the activation of PLK1 and CDC25C.
View Article and Find Full Text PDFInt J Mol Sci
November 2024
Department of Medicine II, University Hospital Tuebingen, Eberhard Karls University, 72074 Tuebingen, Germany.
-rearranged (r) leukemia is characterized by a poor prognosis. Depending on the cell of origin, it differs in the aggressiveness and therapy response. For instance, in adults, volasertib blocking Polo-like kinase 1 (PLK-1) exhibited limited success.
View Article and Find Full Text PDFCell Death Dis
July 2024
The Second Affiliated Hospital, School of Medicine, The Chinese University of Hong Kong, Shenzhen & Longgang District People's Hospital of Shenzhen, Shenzhen, 518172, P.R. China.
Oncol Lett
July 2024
Laboratory of Chemical Carcinogenesis, Chulabhorn Research Institute, Bangkok 10210, Thailand.
Cholangiocarcinoma (CCA) is a lethal cancer originating from the epithelial cells within the bile duct and ranks as the second most prevalent form of liver cancer in Thailand. Polo-like kinase 1 (PLK1), a protein serine/threonine kinase, regulates a number of steps in cell mitosis and is upregulated in several types of cancer, including CCA. Our previous study identified PLK1 as a biomarker of the C1 subtype, correlating with poor prognosis in intrahepatic CCA.
View Article and Find Full Text PDFFront Oncol
March 2024
Department of Anatomy and Cell Biology, Schulich School of Medicine and Dentistry, Western University, London, ON, Canada.
Breast cancer is the most prevalent malignancy among women worldwide. Despite significant advances in treatment, it remains one of the leading causes of female mortality. The inability to effectively treat advanced and/or treatment-resistant breast cancer demonstrates the need to develop novel treatment strategies and targeted therapies.
View Article and Find Full Text PDFEnter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!