4.7 Article

Encounter Complexes Between the N-terminal of Neurotensin with the Extracellular Loop 2 of the Neurotensin Receptor 1 Steer Neurotensin to the Orthosteric Binding Pocket

Related references

Note: Only part of the references are listed.
Article Biochemistry & Molecular Biology

Neurotensin Receptor Allosterism Revealed in Complex with a Biased Allosteric Modulator

Brian E. Krumm et al.

Summary: The NTSR1 receptor is a GPCR found in the brain and peripheral tissues that binds with the endogenous peptide ligand NTS. Recent studies have shown that biasing NTSR1 towards beta-arrestin signaling can attenuate the effects of psychostimulants and drugs of abuse. This study provides cryoEM structures of NTSR1 complexes with Gq and GoA, and discusses the allosteric modulation of NTSR1 by the small-molecule SBI-553.

BIOCHEMISTRY (2023)

Article Multidisciplinary Sciences

Molecular mechanism of biased signaling at the kappa opioid receptor

Amal El Daibani et al.

Summary: Using structural determination, molecular dynamics simulations, and functional assays, the researchers identified molecular determinants of KOR signaling bias. They determined the crystal structure of KOR bound to the G protein-biased agonist nalfurafine and identified an arrestin-biased KOR agonist, WMS-X600. Through simulations and mutagenesis validation, they explained how agonists achieve biased signaling at KOR.

NATURE COMMUNICATIONS (2023)

Article Biochemistry & Molecular Biology

Structures of the entire human opioid receptor family

Yue Wang et al.

Summary: Opioids are powerful painkillers with serious side effects. The study examines the binding and selectivity mechanisms of endogenous opioid peptides with opioid receptors, revealing a structural framework for the design of safer pain relief drugs.
Article Multidisciplinary Sciences

The pocketome of G-protein-coupled receptors reveals previously untargeted allosteric sites

Janik B. Hedderich et al.

Summary: Researchers computationally describe alternative allosteric pockets in G-protein-coupled receptors, identifying nine previously untargeted sites for synthetic ligands. They further investigate the potential of modulating receptor function through ligand binding to these sites.

NATURE COMMUNICATIONS (2022)

Article Biochemistry & Molecular Biology

A lowly populated, transient β-sheet structure in monomeric Aβ1-42 identified by multinuclear NMR of chemical denaturation

Tayeb Kakeshpour et al.

Summary: Chemical denaturation is a useful method for detecting transiently folded structural elements in proteins that are considered to be intrinsically disordered. Analysis of chemical shift titrations can identify lowly populated structured elements in proteins.

BIOPHYSICAL CHEMISTRY (2021)

Article Chemistry, Medicinal

Design, Structural Optimization, and Characterization of the First Selective Macrocyclic Neurotensin Receptor Type 2 Non-opioid Analgesic

Magali Chartier et al.

Summary: The study presents the synthesis and functional in vivo characterization of the first NTS2-selective macrocyclic NT analog, demonstrating potent analgesic effects in rodent pain models without undesired effects associated with NTS1 activation. This highlights the strong therapeutic potential of NTS2-selective analogs for acute and chronic pain management.

JOURNAL OF MEDICINAL CHEMISTRY (2021)

Article Biochemistry & Molecular Biology

β-Arrestin-Biased Allosteric Modulator of NTSR1 Selectively Attenuates Addictive Behaviors

Lauren M. Slosky et al.

Review Chemistry, Multidisciplinary

Methods and Approaches for the Solid-Phase Synthesis of Peptide Alcohols

Fernando J. Ferrer-Gago et al.

CHEMPLUSCHEM (2020)

Review Cell Biology

Binding kinetics of ligands acting at GPCRs

David A. Sykes et al.

MOLECULAR AND CELLULAR ENDOCRINOLOGY (2019)

Article Multidisciplinary Sciences

Cryptic pocket formation underlies allosteric modulator selectivity at muscarinic GPCRs

Scott A. Hollingsworth et al.

NATURE COMMUNICATIONS (2019)

Article Multidisciplinary Sciences

Structure and dynamics of G protein-coupled receptor-bound ghrelin reveal the critical role of the octanoyl chain

Guillaume Ferre et al.

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2019)

Article Biochemistry & Molecular Biology

Optimization and 13CH3 methionine labeling of a signaling competent neurotensin receptor 1 variant for NMR studies

Fabian Bumbak et al.

BIOCHIMICA ET BIOPHYSICA ACTA-BIOMEMBRANES (2018)

Article Biochemistry & Molecular Biology

The molecular basis of subtype selectivity of human kinin G-protein-coupled receptors

Lisa Joedicke et al.

NATURE CHEMICAL BIOLOGY (2018)

Article Chemistry, Medicinal

Structural Optimization and Characterization of Potent Analgesic Macrocyclic Analogues of Neurotensin (8-13)

Marc Sousbie et al.

JOURNAL OF MEDICINAL CHEMISTRY (2018)

Article Multidisciplinary Sciences

A proline switch explains kinetic heterogeneity in a coupled folding and binding reaction

Franziska Zosel et al.

NATURE COMMUNICATIONS (2018)

Review Biochemistry & Molecular Biology

Drug-Target Kinetics in Drug Discovery

Peter J. Tonge

ACS CHEMICAL NEUROSCIENCE (2018)

Article Pharmacology & Pharmacy

The signaling signature of the neurotensin type 1 receptor with endogenous ligands

Elie Besserer-Offroy et al.

EUROPEAN JOURNAL OF PHARMACOLOGY (2017)

Article Chemistry, Medicinal

Use of Molecular Modeling to Design Selective NTS2 Neurotensin Analogues

Roberto Fanelli et al.

JOURNAL OF MEDICINAL CHEMISTRY (2017)

Review Biochemistry & Molecular Biology

Structure and Function of Peptide-Binding G Protein-Coupled Receptors

Fan Wu et al.

JOURNAL OF MOLECULAR BIOLOGY (2017)

Article Biochemistry & Molecular Biology

ML314: A Biased Neurotensin Receptor Ligand for Methamphetamine Abuse

Larry S. Barak et al.

ACS CHEMICAL BIOLOGY (2016)

Article Biochemistry & Molecular Biology

Coupled binding and folding of intrinsically disordered proteins: what can we learn from kinetics?

Stefano Gianni et al.

CURRENT OPINION IN STRUCTURAL BIOLOGY (2016)

Article Multidisciplinary Sciences

The role of kinetic context in apparent biased agonism at GPCRs

Carmen Klein Herenbrink et al.

NATURE COMMUNICATIONS (2016)

Article Biochemistry & Molecular Biology

A Molecular Mechanism for Sequential Activation of a G Protein-Coupled Receptor

Manuel Grundmann et al.

CELL CHEMICAL BIOLOGY (2016)

Article Chemistry, Multidisciplinary

Unwinding of the C-Terminal Residues of Neuropeptide Y is critical for Y2 Receptor Binding and Activation

Anette Kaiser et al.

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION (2015)

Article Multidisciplinary Sciences

NMR structure and dynamics of the agonist dynorphin peptide bound to the human kappa opioid receptor

Casey O'Connor et al.

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2015)

Article Multidisciplinary Sciences

Structural prerequisites for G-protein activation by the neurotensin receptor

Brian E. Krumm et al.

NATURE COMMUNICATIONS (2015)

Article Biochemistry & Molecular Biology

Improving the apo-state detergent stability of NTS1 with CHESS for pharmacological and structural studies

Daniel J. Scott et al.

BIOCHIMICA ET BIOPHYSICA ACTA-BIOMEMBRANES (2014)

Article Biochemistry & Molecular Biology

SnapShot: GPCR-Ligand Interactions

Eshan Ghosh et al.

Article Chemistry, Physical

The binding mechanisms of intrinsically disordered proteins

Jakob Dogan et al.

PHYSICAL CHEMISTRY CHEMICAL PHYSICS (2014)

Article Biochemistry & Molecular Biology

Revisiting the structure of the Vps10 domain of human sortilin and its interaction with neurotensin

Esben M. Quistgaard et al.

PROTEIN SCIENCE (2014)

Review Pharmacology & Pharmacy

Structure-Function of the G Protein-Coupled Receptor Superfamily

Vsevolod Katritch et al.

ANNUAL REVIEW OF PHARMACOLOGY AND TOXICOLOGY, VOL 53, 2013 (2013)

Article Biochemistry & Molecular Biology

Cooperative Unfolding of Compact Conformations of the Intrinsically Disordered Protein Osteopontin

Dennis Kurzbach et al.

BIOCHEMISTRY (2013)

Article Biochemistry & Molecular Biology

Intermolecular interactions between the neurotensin and the third extracellular loop of human neurotensin 1 receptor

Gregory Da Costa et al.

JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS (2013)

Article Multidisciplinary Sciences

Activation and allosteric modulation of a muscarinic acetylcholine receptor

Andrew C. Kruse et al.

NATURE (2013)

Article Endocrinology & Metabolism

Diverse Roles of Neurotensin Agonists in the Central Nervous System

Mona Boules et al.

Frontiers in Endocrinology (2013)

Article Biochemistry & Molecular Biology

Modulation of the neurotensin solution structure in the presence of ganglioside GM1 bicelle

Ummul Liha Khatun et al.

BIOPHYSICAL CHEMISTRY (2012)

Article Multidisciplinary Sciences

Structure of the agonist-bound neurotensin receptor

Jim F. White et al.

NATURE (2012)

Article Biochemistry & Molecular Biology

Kinetic Recognition of the Retinoblastoma Tumor Suppressor by a Specific Protein Target

Lucia B. Chemes et al.

JOURNAL OF MOLECULAR BIOLOGY (2011)

Article Multidisciplinary Sciences

Mapping backbone and side-chain interactions in the transition state of a coupled protein folding and binding reaction

Annett Bachmann et al.

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2011)

Article Biochemistry & Molecular Biology

19F NMR Studies of α-Synuclein Conformation and Fibrillation

Conggang Li et al.

BIOCHEMISTRY (2009)

Review Biochemistry & Molecular Biology

The courtship of proteins: Understanding the encounter complex

Marcellus Ubbink

FEBS LETTERS (2009)

Review Biotechnology & Applied Microbiology

Allosteric modulators of GPCRs: a novel approach for the treatment of CNS disorders

P. Jeffrey Conn et al.

NATURE REVIEWS DRUG DISCOVERY (2009)

Article Chemistry, Multidisciplinary

Interaction of urea with amino acids:: Implications for urea-induced protein denaturation

Martin C. Stumpe et al.

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY (2007)

Article Biochemistry & Molecular Biology

Critical role for the second extracellular loop in the binding of both orthosteric and allosteric g protein-coupled receptor Ligands

Vimesh A. Avlani et al.

JOURNAL OF BIOLOGICAL CHEMISTRY (2007)

Review Pharmacology & Pharmacy

Allosteric GPCR modulators: taking advantage of permissive receptor pharmacology

Katie Leach et al.

TRENDS IN PHARMACOLOGICAL SCIENCES (2007)

Article Biochemistry & Molecular Biology

An on-pathway intermediate in the folding of a PDZ domain

Ylva Ivarsson et al.

JOURNAL OF BIOLOGICAL CHEMISTRY (2007)

Article Biochemical Research Methods

Protein production by auto-induction in high-density shaking cultures

FW Studier

PROTEIN EXPRESSION AND PURIFICATION (2005)

Article Biochemistry & Molecular Biology

Conformation of a peptide ligand bound to its G-protein coupled receptor

H Inooka et al.

NATURE STRUCTURAL BIOLOGY (2001)