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Literature DB >> 30852058

Does Divergent Binding Pocket Closure Drive Ligand Bias for Class A GPCRs?

Abstract

GPCRs couple to intracellular transducer proteins, which reciprocally closes the extracellular ligand binding pocket, a process called allosteric coupling. Biased agonists preferentially stimulate receptor coupling to specific signaling pathways. Here, we postulate that agonists with extended binding modes selectively interfere with binding pocket closure, which results in divergent allosteric coupling, eventually leading to ligand bias.

Keywords: GPCR; allosteric coupling; biased signaling; drug design; extended binding mode; ligand bias

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Substances：

Year: 2019 PMID： 30852058 DOI： 10.1016/j.tips.2019.02.005

Source DB: PubMed Journal: Trends Pharmacol Sci ISSN： 0165-6147 Impact factor: 14.819

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Cited

8 in total

1. Angiotensin and biased analogs induce structurally distinct active conformations within a GPCR.

Authors: Laura M Wingler; Meredith A Skiba; Conor McMahon; Dean P Staus; Alissa L W Kleinhenz; Carl-Mikael Suomivuori; Naomi R Latorraca; Ron O Dror; Robert J Lefkowitz; Andrew C Kruse
Journal: Science Date: 2020-02-21 Impact factor: 47.728

2. PRECOG: PREdicting COupling probabilities of G-protein coupled receptors.

Authors: Gurdeep Singh; Asuka Inoue; J Silvio Gutkind; Robert B Russell; Francesco Raimondi
Journal: Nucleic Acids Res Date: 2019-07-02 Impact factor: 16.971

3. Phenylalanine 193 in Extracellular Loop 2 of the β ₂-Adrenergic Receptor Coordinates β-Arrestin Interaction.

Authors: Michael Ippolito; Francesco De Pascali; Asuka Inoue; Jeffrey L Benovic
Journal: Mol Pharmacol Date: 2021-12-01 Impact factor: 4.436

4. Encoding mu-opioid receptor biased agonism with interaction fingerprints.

Authors: R Bruno Hernández-Alvarado; Abraham Madariaga-Mazón; Fernando Cosme-Vela; Andrés F Marmolejo-Valencia; Adel Nefzi; Karina Martinez-Mayorga
Journal: J Comput Aided Mol Des Date: 2021-10-29 Impact factor: 3.686

5. Crystal structure of dopamine D1 receptor in complex with G protein and a non-catechol agonist.

Authors: Bingfa Sun; Dan Feng; Matthew Ling-Hon Chu; Inbar Fish; Silvia Lovera; Zara A Sands; Sebastian Kelm; Anne Valade; Martyn Wood; Tom Ceska; Tong Sun Kobilka; Florence Lebon; Brian K Kobilka
Journal: Nat Commun Date: 2021-06-03 Impact factor: 14.919

Does Divergent Binding Pocket Closure Drive Ligand Bias for Class A GPCRs?

1. Angiotensin and biased analogs induce structurally distinct active conformations within a GPCR.

2. PRECOG: PREdicting COupling probabilities of G-protein coupled receptors.

3. Phenylalanine 193 in Extracellular Loop 2 of the β ₂-Adrenergic Receptor Coordinates β-Arrestin Interaction.

4. Encoding mu-opioid receptor biased agonism with interaction fingerprints.

5. Crystal structure of dopamine D1 receptor in complex with G protein and a non-catechol agonist.

6. Biased Ligands Differentially Shape the Conformation of the Extracellular Loop Region in 5-HT_2B Receptors.

Review 7. The Impact of the Secondary Binding Pocket on the Pharmacology of Class A GPCRs.

Review 8. Biased agonism at β-adrenergic receptors.

Does Divergent Binding Pocket Closure Drive Ligand Bias for Class A GPCRs?

1. Angiotensin and biased analogs induce structurally distinct active conformations within a GPCR.

2. PRECOG: PREdicting COupling probabilities of G-protein coupled receptors.

3. Phenylalanine 193 in Extracellular Loop 2 of the β 2-Adrenergic Receptor Coordinates β-Arrestin Interaction.

4. Encoding mu-opioid receptor biased agonism with interaction fingerprints.

5. Crystal structure of dopamine D1 receptor in complex with G protein and a non-catechol agonist.

6. Biased Ligands Differentially Shape the Conformation of the Extracellular Loop Region in 5-HT2B Receptors.

Review 7. The Impact of the Secondary Binding Pocket on the Pharmacology of Class A GPCRs.

Review 8. Biased agonism at β-adrenergic receptors.

3. Phenylalanine 193 in Extracellular Loop 2 of the β ₂-Adrenergic Receptor Coordinates β-Arrestin Interaction.

6. Biased Ligands Differentially Shape the Conformation of the Extracellular Loop Region in 5-HT_2B Receptors.