MELK: a potential novel therapeutic target for TNBC and other aggressive malignancies

作者:Pitner Mary Kathryn; Taliaferro Juliana M; Dalby Kevin N*; Bartholomeusz Chandra*
来源:Expert Opinion on Therapeutic Targets, 2017, 21(9): 849-859.
DOI:10.1080/14728222.2017.1363183

摘要

Introduction: There is an unmet need in triple-negative breast cancer (TNBC) patients for targeted therapies. Maternal embryonic leucine zipper kinase (MELK) is a promising target for inhibition based on the abundance of correlative and functional data supporting its role in various cancer types. Areas covered: This review endeavors to outline the role of MELK in cancer. Studies covering a range of biological functions including proliferation, apoptosis, cancer stem cell phenotypes, epithelial-to-mesenchymal transition, metastasis, and therapy resistance are discussed here in order to understand the potential of MELK as a clinically significant target for TNBC patients. Expert opinion: Targeting MELK may offer a novel therapeutic opportunity in TNBC and other cancers. Despite the abundance of correlative data, there is still much we do not know. There are a lack of potent, specific inhibitors against MELK, as well as an insufficient understanding of MELK's downstream substrates. Addressing these issues is the first step toward identifying a patient population that could benefit from MELK inhibition in combination with other therapies.

  • 出版日期2017