Structural diversity of G protein-coupled receptors and significance for drug discovery

By Malin C. Lagerström, Helgi B. Schiöth. 2008

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Improving homology modeling from low-sequence identity templates in Rosetta: A case study in GPCRs (2020, background): “They are a ubiquitous family of proteins evolved over time to respond to a variety of stimuli including ions, small molecules, larger peptides, and even light [2].”
Lifting the lid on GPCRs: the role of extracellular loops (2011, background): “They are central to cell signalling and are of great commercial value to the pharmaceutical industry worldwide, with ~50% of clinically marketed drugs and ~25% of top-selling drugs targeting this receptor family (Lagerström and Schiöth, 2008).”
The harmonizome: a collection of processed datasets gathered to serve and mine knowledge about genes and proteins (2016, background): “Predicting endogenous ligands for G protein-coupled receptors G-protein-coupled-receptors (GPCRs) are important biologically and pharmacologically due to their roles as sensors and signal transducers (144).”
Biophysical dissection of membrane proteins (2009, background): “GPCRs, which are categorized into six subclasses, form the largest single class of eukaryotic membrane proteins and are the targets of many of the drugs being developed by pharmaceutical companie”
Biased Signalling: From Simple Switches to Allosteric Microprocessors (2018, background): “For that reason, accepted approaches to Nature Reviews | Drug Discovery (1)= E max,1 × EC 50,ref RA i,ref pathA EC 50,1 × E max,ref Nature Reviews | Drug Discovery (2)= logβ RA i,ref pathA RA i,ref pathB Nature Reviews | Drug Discovery (3)= τ n[A]n τn[A]n + (K a + [A])n E E m Nature Reviews | Drug D”
Status of GPCR modeling and docking as reflected by community-wide GPCR Dock 2010 assessment (2011, unknown): “…G protein-coupled receptor (GPCR) superfamily has more than 800 members in the human genome (Fredriksson et al., 2003; Ono et al., 2005), detecting a variety of extracellular chemical, biological, or physical signals that are critical for human biology and disease (Lagerström and Schiöth, 2008).”
GPCRdb: the G protein‐coupled receptor database – an introduction (2016, background): “7TM, seven transmembrane; PDB, Protein Data Bank”
Multiple conformational states in retrospective virtual screening – homology models vs. crystal structures: beta-2 adrenergic receptor case study (2015, background): “For this reason, GPCRs are a very important target base for drugs [1-3].”
GPCRdb: an information system for G protein-coupled receptors (2015, background): “GPCRs have been systematized based on sequence homology into the classes A–”
Common activation mechanism of class A GPCRs (2019, background): “As the largest and most diverse group of membrane receptors in eukaryotes, GPCRs mediate a wide variety of physiological functions (Lagerström and Schiöth, 2008; Rosenbaum et al., 2009; Katritch et al., 2012; Venkatakrishnan et al., 2013; Katritch et al., 2013), including vision, olfac- tion,…”