Small‐Molecule Probes to Target the Human Mediator Complex Journal Article uri icon



  • AbstractThe human Mediator complex is a central integrator for transcription that allows DNA‐binding transcription factors to communicate their regulatory signals to the RNA polymerase II enzyme. Because Mediator is dynamic both in terms of subunit composition and structure, it presents challenges as a target for small‐molecule probes. Moreover, little high‐resolution structural information exists for Mediator. Its global requirement for transcription, as well as its distinct, transcription factorspecific interaction surfaces, however, suggest that development of probes that bind specific Mediator subunits might enable gene‐ and pathway‐specific modulation of transcription. Here we provide a brief overview of the Mediator complex, highlighting biological and structural features that make it an attractive target for molecular probes. We then outline several chemical strategies that might be effective for targeting the complex.

publication date

  • August 1, 2013

has restriction

  • green

Date in CU Experts

  • November 11, 2015 10:55 AM

Full Author List

  • Phillips AJ; Taatjes DJ

author count

  • 2

Other Profiles

International Standard Serial Number (ISSN)

  • 0021-2148

Electronic International Standard Serial Number (EISSN)

  • 1869-5868

Additional Document Info

start page

  • 588

end page

  • 595


  • 53


  • 8