Bexarotene (Targretin®) is a synthetic retinoid analog used
to treat cutaneous T-cell lymphoma (as well as off label to treat other types of
cancer). It is especially effective because it has specific affinity for
retinoid X receptors (RXR), enabling up-regulation of RXR genes to slow or stop
cell proliferation of cancer cells. Despite these advantages, there are major
drawbacks to the use of bexarotene including hypothyroidism, hyperlipidemia, and
cutaneous toxicity.
To reduce these detrimental effects, researchers at Arizona
State University have developed bexarotene analogs that are specific only for
the RXR homodimer. By targeting the drug only to the homodimer, other pathways
that require RXR as a heterodimeric partner for other nuclear receptors are not
disrupted.
With this improved specificity of the new analogs discovered
here, the therapeutic effects of bexarotene are retained while the side effects
are minimized.
Potential Applications
- Anti-cancer treatment
- Drug discovery
Benefits and Advantages
