Malaria drug could be used to treat cancer
The Washington State University research team determined that simple modifications to furamidine increase the drug's ability to affect certain human proteins involved in the on-off switches of certain genes. Transcription factors, proteins that regulate the expression of genes, are attractive targets for therapeutic drugs, but it has been difficult to design drugs to affect the proteins.
"For this reason, they have been called undruggable," Gregory Poon, a pharmaceutical scientist at Washington State, said. "Recently, however, scientists have been making headway in targeting these transcription factors with drugs, and now our results suggest this class of drugs can be a useful addition to the arsenal."
Furamidine is part of a family of drugs called heterocyclic dictations. The drug was used in serious parasitic infections like African sleeping sickness, PCP and malaria.
In a collaboration with researchers from Georgia State University, Poon found that derivatives of furamidine can target PU. 1, a transcription factor that plays important roles in diseases such as diabetes, multiple sclerosis and some leukemias.
"This was rather unexpected, given how relatively simple the molecules are that we modified and how difficult it has been to affect these proteins," Poon said.
PU. 1 is also a member of a family of related transcription factors called ETS. ETS transcription factors are involved in a broader range of cancers and other diseases.
Poon said the next challenge is to fine tune furamidine and other heterocyclic dictations to enable them to modify other ETS-family transcription factors.