Dimmer-switch Drugs

By Megan Scudellari Dimmer-switch Drugs A growing number of companies are exploring molecules that modulate targets, rather than just switching them on or off. It started with an obsession. In 2002, Vincent Mutel began to talk about allosteric modulators, think about allosteric modulators, even dream about them. Few drug companies were pursuing allosteric modulators—small molecules that regulate a receptor or enzyme by binding to a site disti

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It started with an obsession. In 2002, Vincent Mutel began to talk about allosteric modulators, think about allosteric modulators, even dream about them. Few drug companies were pursuing allosteric modulators—small molecules that regulate a receptor or enzyme by binding to a site distinct from the target's active (or orthosteric) site. Such ligands were widely recognized for their role in naturally regulating G protein–coupled receptors (GPCRs), many of which are known drug targets. But at the time, allosteric modulators and their signaling pathways had a reputation of being difficult to work with (they are), the molecules were believed to be insoluble (they are, in fact, soluble), and their efficacy was not proven (it soon would be). Still, Mutel had great hope.

His newly formed company, Addex Pharmaceuticals, was struggling under its original business plan as a specialty pharma focused on addiction therapies, and Mutel realized the company needed to make a ...

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