Publications by authors named "Lawrence K Chan"
Article Synopsis
- * The article introduces a new method called top-down drug discovery (TD), which involves searching through a large database of fungi to find genetic locations that produce molecules targeting specific human proteins, like cyclin-dependent kinases (CDKs).
- * Researchers successfully discovered two new molecules that inhibit CDKs and improved one of them to enhance its selectivity and effectiveness, showcasing the potential of TD for developing innovative medicines.
Split-and-pool synthesis of a 10,000-membered library of molecules resembling the natural product carpanone has been achieved. The synthesis features development of solid-phase multicomponent reactions between nitrogen nucleophiles, enones, and hydroxylamines, and a solid-phase application of the Huisgen cycloaddition affording substituted triazoles. The synthesis was performed in high-capacity (500 microm) polystyrene beads using a one bead-one stock solution strategy that enabled phenotypic screens of the resulting library.
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