Articoli

Purinome platform

The generation of novel chemotypes in support of our oncology research projects expanded in recent years from a canonical design of kinase targeted compound libraries to a broader interpretation of purinome targeted libraries addressing the specificity of cancer relevant targets. We added non-kinase oncology targets to our portfolio, thus expanding also into a wider purinome perspective, which includes target families such as ATPases and NAD-dependent enzymes, while maintaining a strong foothold in the kinase field. Successful screening of structurally diverse ATP-binding targets requires compound libraries covering multiple design elements, which may include phosphate surrogate moieties in ATPase inhibitors or far reaching lipophilic residues stabilizing inactive kinase conformations. Purinome targets are widely diversified in terms of their function, philogenetic origins and structural architecture. A common feature is their ability to bind ATP or other ligands possessing a purine substructure. (e.g. NAD), although the modes of binding and the sites of interaction may vary considerably. To this end the interaction with phosphate groups of ATP and ADP is dominant is certain ATPases, while it is often negligible or secondary in kinases. We therefore recognized the need for new, purinome targeted libraries (PTL), which were conceived with broadly diversified ATP-mimicking designs, taking into account the higher relevance of ATP and ADP phosphate groups in the binding complex of these targets.

 
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