tg-003 and Neoplasms

The Cdc2-like kinases (CLKs 1-4) are involved in regulating the alternative splicing of a variety of genes. Their activity contributes to important cellular processes such as proliferation, differentiation, apoptosis, migration, and cell cycle regulation. Abnormal expression of CLKs can lead to cancers; therefore, pharmacological inhibition of CLKs may be a useful therapeutic strategy. This review summarises what is known about the roles of each of the CLKs in cancerous cells, as well as the effects of relevant small molecule CLK inhibitors.

Topics: Alternative Splicing; Humans; Neoplasms; Phosphorylation; Protein Serine-Threonine Kinases; Protein-Tyrosine Kinases

Alternative splicing is a key process required for the regulation of gene expression in normal development and physiology. It is regulated by splice factors whose activities are in turn regulated by splice factor kinases and phosphatases. The CDC-like protein kinases are a widespread family of splice factor kinases involved in normal physiology and in several diseases including cancer. In humans they include the CLK1, CLK2, CLK3 and CLK4 genes. The expression of CLK1 is regulated through alternative splicing producing both full-length catalytically active and truncated catalytically inactive isoforms, CLK

Topics: Alternative Splicing; Cell Line, Tumor; Exons; Gene Expression Regulation; Harmine; HL-60 Cells; Homeostasis; Hot Temperature; Humans; Introns; Neoplasms; Osmotic Pressure; Protein Serine-Threonine Kinases; Protein-Tyrosine Kinases; Stress, Physiological; Thiazoles