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TitleNeurotensin Receptor Allosterism Revealed in Complex with a Biased Allosteric Modulator.
Journal, issue, pagesBiochemistry, Vol. 62, Issue 7, Page 1233-1248, Year 2023
Publish dateApr 4, 2023
AuthorsBrian E Krumm / Jeffrey F DiBerto / Reid H J Olsen / Hye Jin Kang / Samuel T Slocum / Shicheng Zhang / Ryan T Strachan / Xi-Ping Huang / Lauren M Slosky / Anthony B Pinkerton / Lawrence S Barak / Marc G Caron / Terry Kenakin / Jonathan F Fay / Bryan L Roth /
PubMed AbstractThe NTSR1 neurotensin receptor (NTSR1) is a G protein-coupled receptor (GPCR) found in the brain and peripheral tissues with neurotensin (NTS) being its endogenous peptide ligand. In the brain, NTS ...The NTSR1 neurotensin receptor (NTSR1) is a G protein-coupled receptor (GPCR) found in the brain and peripheral tissues with neurotensin (NTS) being its endogenous peptide ligand. In the brain, NTS modulates dopamine neuronal activity, induces opioid-independent analgesia, and regulates food intake. Recent studies indicate that biasing NTSR1 toward β-arrestin signaling can attenuate the actions of psychostimulants and other drugs of abuse. Here, we provide the cryoEM structures of NTSR1 ternary complexes with heterotrimeric Gq and GoA with and without the brain-penetrant small-molecule SBI-553. In functional studies, we discovered that SBI-553 displays complex allosteric actions exemplified by negative allosteric modulation for G proteins that are Gα subunit selective and positive allosteric modulation and agonism for β-arrestin translocation at NTSR1. Detailed structural analysis of the allosteric binding site illuminated the structural determinants for biased allosteric modulation of SBI-553 on NTSR1.
External linksBiochemistry / PubMed:36917754
MethodsEM (single particle)
Resolution2.59 - 2.89 Å
Structure data

29301

8fmz

EMDB-29301, PDB-8fmz:
Neurotensin receptor allosterism revealed in complex with a biased allosteric modulator
Method: EM (single particle) / Resolution: 2.59 Å

29302

8fn0

EMDB-29302, PDB-8fn0:
CryoEM structure of Go-coupled NTSR1 with a biased allosteric modulator
Method: EM (single particle) / Resolution: 2.89 Å

29303

8fn1

EMDB-29303, PDB-8fn1:
CryoEM structure of Go-coupled NTSR1
Method: EM (single particle) / Resolution: 2.88 Å

Chemicals

ChemComp-SRW:
2-[{2-(1-fluorocyclopropyl)-4-[4-(2-methoxyphenyl)piperidin-1-yl]quinazolin-6-yl}(methyl)amino]ethan-1-ol

Source
  • rattus norvegicus (Norway rat)
  • escherichia coli (E. coli)
  • homo sapiens (human)
  • lama glama (llama)
  • spodoptera frugiperda (fall armyworm)
KeywordsMEMBRANE PROTEIN / GPCR / neurotensin receptor / allosterism / SBI-553

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