Date: 2013-03-04
Type of information: R&D agreement
Compound: oral small molecule adenosine 2A receptor (A2AR) positive allosteric modulators (PAMs)
Company: Addex Therapeutics (Switzerland) Viva Biotech (China)
Therapeutic area: Rare diseases - Inflammatory diseases
Type agreement: R&D
Action mechanism: 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 a profound therapeutic effect in any number of inflammatory-based diseases including rare diseases such as sickle cell and Huntington\'s diseases.
Disease:
Details: Addex Therapeutics, a Swiss company pioneering allosteric modulation-based drug discovery and development, and Viva Biotech Ltd., a Chinese company in structure-based drug discovery based in Shanghai, have entered into a partnership to accelerate the advancement of oral small molecule adenosine 2A receptor (A2AR) positive allosteric modulators (PAMs) by leveraging the relative expertise of each company.
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.
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