RSC Medicinal Chemistry Blog

Audrey Odom, Raman Sharma and colleagues present a review examining the enzymes in the biosynthetic non-mevalonate (MEP) pathway from a detailed medicinal chemistry and structural biology perspective. The MEP pathway is utilised by plants but is absent in mammalian systems, making it a very attractive target for the development of potential next generation antimicrobial chemotherapeutics as well as novel herbicides.

Want to find out more about this pathway and its potential agents? You’re just a click away….

The MEP pathway and the development of inhibitors as potential anti-infective agents
Ian Hale, Paul M. O’Neill, Neil G. Berry, Audrey Odom and Raman Sharma
Med. Chem. Commun., DOI: 10.1039/C2MD00298A

Disruption of protein–protein or protein–DNA interactions involved in transcriptional machinery using small molecules poses a real challenge owing to several factors, including: the large interfacial areas involved, the lack of obvious binding sites, and the large free energy of association between the interfaces.

However, in recent years there has been considerable success in the dimeric transcription factor disruption using small molecules. Steven Fletcher and co-workers at University of Maryland School of Pharmacy, provide a review of the progress made in this area since 2008.

This review covers:

• Inhibitors of STAT3
• Inhibitors of c-Myc
• Inhibitors of AP-1
• Inhibitors of HIF-1

Small-molecule inhibitors of dimeric transcription factors: Antagonism of protein–protein and protein–DNA interactions
Jeremy L. Yap, Jay Chauhan, Kwan-Young Jung, Lijia Chen, Edward V. Prochownik and Steven Fletcher
Med. Chem. Commun., 2012,
DOI: 10.1039/C2MD00289B, Review