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

Abstract

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.

• Authors: Mary Kathryn Pitner, Juliana M Taliaferro, Kevin N Dalby, Chandra Bartholomeusz
• Journal: Expert opinion on therapeutic targets (Expert Opin Ther Targets) Vol. 21 Issue 9 Pg. 849-859 (09 2017) ISSN: 1744-7631 [Electronic] England
• PMID: 28764577 (Publication Type: Journal Article, Review)

Chemical References

• Antineoplastic Agents
• Protein Kinase Inhibitors
• MELK protein, human
• Protein Serine-Threonine Kinases

Topics

• Animals
• Antineoplastic Agents (pharmacology)
• Apoptosis (drug effects)
• Cell Proliferation (drug effects)
• Drug Design
• Female
• Humans
• Molecular Targeted Therapy
• Neoplasms (drug therapy, pathology)
• Neoplastic Stem Cells (metabolism)
• Protein Kinase Inhibitors (pharmacology)
• Protein Serine-Threonine Kinases (antagonists & inhibitors, metabolism)
• Triple Negative Breast Neoplasms (drug therapy, pathology)