GPCRs as Pharmaceutical Targets Sample Clauses

GPCRs as Pharmaceutical Targets. GPCRs are essential for most physiological processes and their dysfunction has been shown to contribute to the etiology of many disease states and disorders. GPCRs have been implicated in endocrine and metabolic disorders, immune dysfunction, cancer and vascular disease, among others (Vassart and Xxxxxxxxxxx 2011; Heng, Aubel, and Fussenegger 2013; Rockman, Koch, and Xxxxxxxxx 2002; Xxxxx and Xxxxxxxx 2006). In the brain, GPCRs serve as the molecular targets for many neurotransmitters, neuropeptides, and neuromodulators. With over 90% of non-sensory GPCRs expressed in the brain, it is not surprising that GPCRs can contribute to addiction, neurodegeneration, neuropathic pain, and movement disorders, as well as psychiatric and neuroinflammatory diseases (Gainetdinov et al. 2004; Xxxxxxx and Conn 2014). GPCRs make excellent drug targets, with ~30% of drugs on the market targeting GPCRs (Xxxxxx et al. 2017). The success of drugs targeting GPCRs is a result of the unique features of GPCRs, they are involved in nearly all physiological processes and disease states, capable of producing diverse effects, have multiple mechanisms for modulation, frequently respond to small molecules, are relatively easy to screen, often have restricted cellular expression, and they are ideally localized to the cell surface. While drugs targeting GPCRs represent a large portion of the market, current drugs only target 10% of human GPCRs, underscoring why they are among the most pursued targets for drug development (Xxxx-Xxxxxxxx, Masuram, and Schioth 2014).
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