AsianScientist (Mar. 11, 2013) – US-based Addex Therapeutics and Viva Biotech Ltd., a company that focuses on structure-based drug discovery based in Shanghai, China, have entered into a partnership to accelerate the advancement of oral small molecule adenosine 2A receptor (A2AR) positive allosteric modulators (PAMs).
The A2AR natural ligand, extracellular adenosine, is locally produced at the sites of inflammation and has been characterized for decades as a “brake for inflammation.” An oral small molecule compound targeting A2AR activation, which selectively enhances the effect of high adenosine concentration only within inflamed tissues and not in other tissues, may have therapeutic applications in any number of inflammatory-based diseases including rare diseases such as sickle cell and Huntington’s disease.
Under the terms of the agreement, Viva Biotech will provide a fully-integrated structural biology discovery service to Addex to deliver high resolution crystal structures of A2AR in complex with positive allosteric modulators (PAMs) that were identified using Addex proprietary HTS technologies.
Based on this structural information, Addex scientists will then be able to rationally develop novel A2AR PAMs in a structure-guided lead optimization program. To date, Addex’ A2AR PAMs constitute the first examples of chemically tractable, selective, oral small molecule compounds with functional activity on this important GPCR target.
“With Addex, Viva brings unique structural biology expertise and capability to the partnership. We believe the combination of our capability with Addex’ state-of-the-art allosteric modulator platform will accelerate the delivery of a clinical candidate against this important GPCR drug target,” said Cheney Mao, Chief Executive Officer of Viva Biotech.
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Source: Addex Therapeutics.
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