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DXS as a target for structure-based drug design.

Robin Matthias Gierse1, Eswar Redeem1, Eleonora Diamanti1

  • 1Stratingh Institute for Chemistry, University of Groningen, Nijenborgh 7, 9747 AG Groningen, The Netherlands.

Future Medicinal Chemistry
|June 22, 2017
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Summary

The enzyme 1-deoxy-xylulose-5-phosphate synthase (DXS) is crucial for isoprenoid biosynthesis and presents potential anti-infective drug targets for malaria and tuberculosis. This review analyzes DXS structure, conservation, and inhibitors for drug design.

Keywords:
DXSanti-infectivesantibioticsmalariamethylerythritol phosphate pathwayprotein crystallographystructure-based drug designtuberculosis

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Area of Science:

  • Biochemistry
  • Metabolic Pathways
  • Drug Discovery

Background:

  • The methylerythritol 4-phosphate (MEP) pathway, discovered in 1996, is essential for synthesizing isoprenoids, vital biological building blocks.
  • DXS (1-deoxy-xylulose-5-phosphate synthase) is the initial, rate-limiting enzyme in the MEP pathway.
  • The MEP pathway is a promising target for developing anti-infectives against pathogens like those causing malaria and tuberculosis.

Purpose of the Study:

  • To review the enzyme DXS, its role in the MEP pathway, and its potential as a drug target.
  • To analyze the sequence conservation of DXS on its protein structure.
  • To provide an overview of known DXS inhibitors and discuss future structure-based drug design.

Main Methods:

  • Sequence conservation mapping of DXS on its protein structure.
  • Analysis of DXS structure in relation to identified druggable pockets.
  • Literature review of known DXS inhibitors.

Main Results:

  • DXS is the rate-limiting enzyme in the MEP pathway, crucial for isoprenoid biosynthesis.
  • Sequence conservation analysis highlights key regions of the DXS protein.
  • A review of existing DXS inhibitors is presented, informing future drug development.

Conclusions:

  • DXS is a validated target for anti-infective drug development against malaria and tuberculosis.
  • Understanding DXS structure and inhibitor profiles is key for structure-based drug design.
  • Further research into DXS inhibitors can lead to novel therapeutic strategies.