An innovative paper published in the Journal of Medicinal Chemistry has earned Dr Jonathan Baell a significant award from the Royal Australian Chemical Institute.
The amplification of some unusual qualities of a naturally-occurring substance, Khellinone, derived from a Chilean plant, raises the prospect of developing a compound to prevent the destructive autoimmune impact of the body's own T cells upon myelin proteins.
Myelin is the substance that, in effect, provides the insulation to the body's electrical wiring. The mistaken destruction of this insulation by the body's immune system is a major contributor to the development of multiple sclerosis (MS).
The natural anti-inflammatory effect of Khellinone is detectable but also quite weak – certainly far too weak in its natural state to prevent myelin destruction. Dr Baell and his collaborators in Australia and overseas have determined that it is possible to increase the potency of this substance, which acts to disrupt the potassium channels of the body's rogue T cells, thereby reducing their capacity to cause damage to the body.
Dr Baell, who heads the discovery team in the Medicinal Chemistry Group in WEHI's Structural Biology Division, says that the next step is to determine efficacy (or effectiveness) in the animal model. He adds, "Our ultimate objective is to reduce the incidence of MS in humans, certainly as far as rogue T cell action is concerned. Our way of doing this is not to repress the action of the entire immune system, which is what most current drugs tend to do. We have determined that the T cells causing the problems for MS patients are quite distinct in their chemical composition. Aiming new compounds at these distinct cells may well be a selective and productive way of tackling MS."
Reflecting on the award, Dr Baell added, "The Biota award will, I hope, raise the profile of early phase medicinal chemistry and emphasise its fundamental role in drug discovery – especially since this essential science is difficult to fund in Australia by conventional means. This is my first major award and I am deeply honoured to have been selected for it."
Source: Eurekalert & othersLast reviewed: By John M. Grohol, Psy.D. on 21 Feb 2009
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