Discovery of Lead compounds targeting transcriptional regulation

Introduction

Transcriptional regulation plays key physiological functions in body growth and development. Transcriptional dysregulation is one of the important biomarkers of tumor genesis and progression, which is involved in regulating tumor cell processes such as cell proliferation, differentiation, and apoptosis. Additionally, it plays a pivotal role in angiogenesis and promotes tumor metastasis and drug resistance by regulating invasive metastasis and immune escape. The dysfunction of key proteins involved in transcriptional regulation mediates aberrant gene expressions that underlie the hallmarks of tumorigenesis. Although most of the key proteins involved in transcriptional regulation are historically recognized as undruggable targets, multiple targeting approaches at diverse levels of transcriptional regulation have been established in preclinical or clinical studies. Therefore, it is important to discover more novel chemical entities as antitumor lead compounds that target key tumor-associated proteins involved in transcriptional regulation.

Keywords

Lead compounds Discovery, transcriptional regulation, tumor growth and metastasis, structure activity relationship, transcription factor, anticancer drug discovery

Sub-topics

• Design and discovery of anticancer compounds targeting transcriptional key proteins.


• Summary of potential or real drug targets of transcriptional key proteins.


• Structural optimization based on active ingredients in plants