Drug intelligence / Profile preview

[(3R,4S)-4-hydroxy-3-methyl-2-oxohexyl]phosphonic acid

Development stage
Preclinical
Lead developer
University of Iowa
Modality
Small Molecules
01

Overview

[(3R,4S)-4-hydroxy-3-methyl-2-oxohexyl]phosphonic acid is a potent small-molecule inhibitor of **1-deoxy-D-xylulose 5-phosphate reductoisomerase (DXR)**, also known as **IspC**. DXR is a rate-limiting enzyme in the **non-mevalonate (MEP) pathway** for isoprenoid biosynthesis, which is essential in many human pathogens, including *Plasmodium falciparum* (the causative agent of malaria) and *Mycobacterium tuberculosis*, but absent in humans. This compound acts as a **transition-state analog**, mimicking the intermediate formed during the conversion of 1-deoxy-D-xylulose 5-phosphate (DXP) to 2-C-methyl-D-erythritol 4-phosphate (MEP). Due to its high specificity for the bacterial and protozoal enzyme over human metabolic pathways, it has been investigated as a potential lead for the development of novel **antimalarial** and **antibacterial** agents.

Other names
(3R,4S)-4-hydroxy-3-methyl-2-oxohexylphosphonic acidhexyl ketophosphonate DXR inhibitor
02

Targets

DXR (1-deoxy-D-xylulose-5-phosphate reductoisomerase)

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