Anti-parasite drugs may treat cancer, immune diseases

Date: Nov-13-2013US researchers have discovered that by modifying a long-standing drug used to treat

serious parasitic diseases like malaria, they could get it to affect human proteins in a way that

looks promising for the treatment of cancer and immune-related diseases.

One of the researchers, Dr. Gregory Poon, a pharmaceutical scientist at Washington State

University (WSU), says of their discovery:

"This was rather unexpected, given how relatively simple the molecules are that we modified and

how difficult it has been to affect these proteins."

He and his colleagues write about their findings in a recent online issue of the journal

Nucleic Acids Research.

There they descibe how with simple modifications, they could get the drug furamidine to alter

human proteins that switch certain genes on and off.

Modified furamidine alters human transcription factors

The modified furamidine was able to alter a group of human proteins known as transcription

factors. These orchestrate the highly intricate sequences of gene expression that make cells

function, and they are attractive targets for therapeutic drugs for the treatment of cancer and immune-related diseases.

Until now, it has been very difficult to design drugs that target transcription factors, and for

this reason, says Dr. Poon, they have been called "undruggable." He adds:

"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's long history with humans an advantage

Furamidine, which belongs to a family of drugs known as heterocyclic dications, has long been

used to treat serious parasitic diseases, such as malaria, African sleeping sickness and PCP - a

serious infection that often affects people with HIV and AIDS.

Such a long history means we have gathered a lot of knowledge and experience about the use

furamidine and its relatives in humans, says Dr. Poon, "so these drugs have an important advantage

over other classes of drugs that are relatively behind in clinical experience."

Furamidine derivatives target PU.1

In their study, the team found that modified versions of furamidine can target a specific

transcription factor known as PU.1, which plays a key role in how the immune system develops and

functions. It also plays a major role in diseases, including certain leukemias, multiple sclerosis and

diabetes.

PU.1 is part of a large family of transcription factors known as ETS, which are involved in many

cancers and other diseases.

Dr. Poon says:

"The challenge now is to fine-tune this class of drugs to make them as specific as possible to

other ETS-family transcription factors as well."

Funds from the WSU College of Pharmacy and the National Institutes of Health at Georgia State

University helped finance the study.

In another recent study that found a new use for an old drug, researchers revealed how a common

high blood pressure drug could

enhance cancer treatment.

Written by Catharine Paddock PhD

Copyright: Medical News Today

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