Signalling bias in new drug discovery: detection, quantification and therapeutic impact

By Terry Kenakin, Arthur Christopoulos. Nature reviews. Drug discovery, 2012

726 citations recorded by the source corpus.

Subfields: Cellular and Molecular Neuroscience, Molecular Biology

View Paper: https://www.semanticscholar.org/paper/9025a069336932d711eb888ad6fb4e149ca3ec6f

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Citations in the corpus

• Exploring the free-energy landscape of GPCR activation (2018, background): “Although studies showed that the receptor can assume several distinct active conformational states (38, 39), we focus here on only one active conformation of the receptor, because this work deals only with the canonical G-protein activation pathway.”
• Molecular dynamics simulation for all (2018, neutral): “An area of great current interest in GPCR drug discovery is the design of biased ligands that selectively stimulate certain signaling pathways but not others controlled by the same receptor (Kenakin and Christopoulos, 2013; Violin et al., 2014; Wacker et al., 2017a).”