A suite of bioassays to evaluate CREB inhibitors

Methods Enzymol. 2020:633:169-184. doi: 10.1016/bs.mie.2019.11.002. Epub 2019 Nov 22.

Abstract

The cyclic-AMP response element binding protein (CREB) is an important nuclear transcription factor and has been shown to be overexpressed and/or over-activated in many different cancer types, suggesting that targeting CREB is a novel approach for developing cancer therapies. Our lab discovered the first cell-permeable small molecule inhibitor of CREB, from which we further developed a potent CREB inhibitor with in vivo anti-cancer activity. In this article, we detailed our biochemical and cell-based bioassays to assess different small molecule CREB inhibitors.

Keywords: CREB; Inhibitor; Luciferase; Protein-protein interaction; Reporter; Transcription.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Biological Assay*
  • Cyclic AMP Response Element-Binding Protein* / antagonists & inhibitors
  • Cyclic AMP Response Element-Binding Protein* / genetics
  • Cyclic AMP Response Element-Binding Protein* / metabolism
  • Phosphorylation
  • Transcription, Genetic

Substances

  • Cyclic AMP Response Element-Binding Protein