STAT inhibitors for cancer therapy

JAK-STAT pathway and JAK inhibitors: a primer for dermatologists

Background: All cellular events depend upon the DNA synthesis and gene expression involving complex interplay between ligands such as interleukins and interferons, with various cell membrane receptors. These ligand-receptors interactions transmit signals within the cell via numerous signal transduction pathways to affect gene expression. Janus kinase/signal transducer and activator of transcrip...

STAT 3 Inhibitors for Cancer Therapy – the Rationale and Remained Problems

STAT3 regulates various cellular functions, which is diverted to malignant phenotypes of cancer cells. Aberrant activation of STAT3 in cancer cells has motivated researchers to develop STAT3 inhibitors as a novel line of anti-cancer drugs. The attempt has not been successful so far. There are some hurdles to be overcome. Basic concepts of STAT3 inhibitors and remained problems will be discussed.

Effect of valproic acid on JAK/STAT pathway, SOCS1, SOCS3, Bcl-xL, c-Myc, and Mcl-1 gene expression, cell growth inhibition and apoptosis induction in human colon cancer HT29 cell line.

Background and aim: Cytokines are a large family of protein messengers. These proteins induce various cellular responses. Janus kinases (JAKs) are mediators of cytokine, activated JAKs phosphorylate signal transducers, and activators of transcription (STAT) proteins that regulate cell differentiation, proliferation, and apoptosis. Aberrant JAK/STAT signaling is involved in the oncogenesis of se...

Screening approaches to generating STAT inhibitors

STAT transcription factors are regulators of critical cellular processes such as proliferation, survival, and self-renewal. While the activity of these proteins is tightly regulated under physiological conditions, they can become constitutively activated in a broad range of human cancers. This inappropriate STAT activation leads to enhanced transcription of genes that can directly lead to the m...

Screening approaches to generating STAT inhibitors: Allowing the hits to identify the targets