HIV Protease Inhibitors Act as Competitive Inhibitors of the Cytoplasmic Glucose Binding Site of GLUTs with Differing Affinities for GLUT1 and GLUT4
2011

HIV Protease Inhibitors and Their Effects on Glucose Transport

publication Evidence: moderate

Author Information

Author(s): Richard C. Hresko, Paul W. Hruz

Primary Institution: Washington University School of Medicine

Hypothesis

Do HIV protease inhibitors interfere with glucose transport by binding to GLUT1 and GLUT4?

Conclusion

The study found that different HIV protease inhibitors have varying effects on glucose transport, with indinavir acting as a competitive inhibitor of GLUT4.

Supporting Evidence

  • Indinavir selectively inhibits GLUT4 activity while ritonavir and atazanavir do not.
  • The binding affinity of indinavir for GLUT4 was determined to be 8.2 µM.
  • Different HIV protease inhibitors have varying effects on glucose transport.

Takeaway

Some medicines for HIV can make it harder for your body to use sugar, and different medicines affect this in different ways.

Methodology

The study used photolabeling assays and glucose uptake measurements in 3T3-L1 fibroblasts and primary rat adipocytes to assess the effects of HIV protease inhibitors on GLUT1 and GLUT4.

Limitations

The study primarily focused on in vitro models, which may not fully represent in vivo conditions.

Statistical Information

P-Value

8.2 µM

Statistical Significance

p<0.05

Digital Object Identifier (DOI)

10.1371/journal.pone.0025237

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