G protein coupled receptors, or GPCRs, make up the largest family of transmembrane receptors, and transmit extracellular cues, such as hormones and neurotransmitters, into intracellular responses. Typically, GPCR activation engages broad networks of signaling pathways, which for most receptors are mediated by both G proteins and β-arrestins. Distinct biological responses are often linked to these different pathways. Standard agonists and antagonists activate or inactivate the entirety of a receptor's signaling network. However, "biased" ligands selectively engage some signals while avoiding, or even inactivating, other signals mediated by the same receptor. This enhanced functional specificity is the basis for Trevena's drug development programs. Trevena's approach represents a novel development in targeted therapies that we believe will provide the next generation of GPCR drugs.
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