Title:Targeting Kruppel-Like Factor 5 (KLF5) for Cancer Therapy
VOLUME: 15 ISSUE: 8
Author(s):Yu Gao, Ye Ding, Haiying Chen, Haijun Chen and Jia Zhou
Affiliation:College of Chemistry, Fuzhou University, Fuzhou, Fujian 350108, China., Department of Pharmacology and Toxicology, University of Texas Medical Branch, Galveston, Texas 77555, United States.
Keywords:Kruppel-like factor 5 (KLF5), Transcription factors, Signaling pathways, Cancer therapeutics, KLF5 ligands, Drug
discovery.
Abstract:Kruppel-like factor 5 (KLF5) belongs to a family of zinc-finger-containing
transcription factors which are involved in regulating expression of a wide range of
genes, thereby affecting diverse cellular functions. The activities of KLF5 are regulated
by multiple signaling pathways including Wnt, Ras, TGFβ, Hippo, Notch, retinoid
acid receptor, and hormone receptors. The expression of KLF5 is frequently abnormal
in human cancers and the functions of KLF5 are context dependent. Accumulating
evidence suggests that KLF5 represents a novel therapeutic target for cancer therapy. In this review, we discuss the
potential biological functions of KLF5 associated with several key signaling pathways that are relevant to cancer as well
as the involvement of KLF5 in various human cancers. We also describe the progress in the discovery and development of
small molecules targeting KLF5 as potential therapeutics that may benefit cancer patients. The challenges and future research
directions on the drug discovery of KLF5 ligands are also presented.