The nuclear receptor family represents a plethora of therapeutic targets for many clinical conditions. While AstraZeneca's research will focus on respiratory and inflammation, broader application is possible across all of the company's research areas.
Nuclear receptors require co-activator binding in order to activate gene transcription. Ligand-induced nuclear receptor conformational changes facilitate the recruitment of certain co-activators through the recognition of a specific motif contained within the co-activator protein.
Prof. Malcolm Parker, who is director of research at the Institute of Reproductive and Developmental Biology at Imperial College, London, identified this motif within the co-activator protein known as the LXXLL motif (where L is Leucine and X is any amino acid).
A spokesman for Cancer Research Technology was unable to tell DrugResearcher.com any more, only confirming that the license to AstraZeneca was for the life of the patent.
Nuclear receptors are a family of proteins involved in key metabolic processes with great potential as targets for the treatment of significant diseases such as cancer, coronary heart disease, and diabetes. Collectively these diseases represent a large market for prescription drugs worldwide.
The nuclear receptor family contains a large group of transcription factors, with 49 members presently identified in the human genome. Nuclear receptors are attractive targets for drug discovery because those that have been discovered thus far have proved to be druggable, in other words, their activity can be modulated by small molecules.


