This week in therapeutics

Indication

Target/marker/pathway

Summary

Licensing status

Publication and contact information

Infectious disease

HIV/AIDS

Protein kinase Cd (PRKCD)

In vitro studies suggest analogs of prostratin, a PRKCD inhibitor, could help treat HIV infection. Chemical synthesis and in vitro testing of prostratin analogs identified multiple compounds that inhibited PRKCD with 10- to 100-fold greater potency than prostratin. In a human cell-based assay, the compounds reactivated latent HIV at nanomolar EC50 values, whereas prostratin reactivated the virus at a micromolar EC50 value. In CD4+ T cells from patients infected with HIV who were on highly active antiretroviral therapy, a 50 nM dose of the lead compound increased HIV RNA production by >100-fold compared with the same dose of prostratin. Ongoing work includes testing the toxicity of the analogs in normal mice.
The AIDS Research Alliance has prostratin in preclinical testing to treat HIV infection.

SciBX 6(27); doi:10.1038/scibx.2013.687
Published online July 18, 2013

Patented by Stanford University; licensing status undisclosed

Beans, E.J. et al. Proc. Natl. Acad. Sci. USA; published online June 28, 2013;
doi:10.1073/pnas.1302634110
Contact: Paul A. Wender, Stanford University, Stanford, Calif.
e-mail:

wenderp@stanford.edu
Contact: Jerome A. Zack, University of California, Los Angeles, Calif.
e-mail:

jzack@ucla.edu
Contact: Tae-Wook Chun, National Institutes of Health, Bethesda, Md.
e-mail:

twchun@nih.gov