Opportunities for tapping into three-dimensional chemical space through a quaternary carbon

TT Talele - Journal of Medicinal Chemistry, 2020 - ACS Publications
A quaternary carbon bears four other carbon substituents or combination of four non-
hydrogen substituents at four vertices of a tetrahedron. The spirocyclic quaternary carbon …

Biased allosteric modulators: new frontiers in GPCR drug discovery

LM Slosky, MG Caron, LS Barak - Trends in Pharmacological Sciences, 2021 - cell.com
G protein-coupled receptors (GPCRs) are the largest class of cell surface receptors in the
genome and the most successful family of targets of FDA-approved drugs. New frontiers in …

[HTML][HTML] β-arrestin-biased allosteric modulator of NTSR1 selectively attenuates addictive behaviors

LM Slosky, Y Bai, K Toth, C Ray, LK Rochelle, A Badea… - Cell, 2020 - cell.com
Small molecule neurotensin receptor 1 (NTSR1) agonists have been pursued for more than
40 years as potential therapeutics for psychiatric disorders, including drug addiction. Clinical …

Fluorinated cycloalkyl building blocks for drug discovery

OO Grygorenko, KP Melnykov, S Holovach… - …, 2022 - Wiley Online Library
The review covers various aspects of fluorinated cycloalkyl (C3− C7) building blocks for drug
discovery, including their synthesis, key physicochemical properties, and biological and …

Neurotensin receptor allosterism revealed in complex with a biased allosteric modulator

BE Krumm, JF DiBerto, RHJ Olsen, HJ Kang… - Biochemistry, 2023 - ACS Publications
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 …

Neurotensin and energy balance

GB Gereau, SKD Garrison… - Journal of …, 2023 - Wiley Online Library
The neurotensin system spans across the central nervous system, to the enteric nervous
system (gut), and the periphery to govern behaviors and physiological responses that tune …

Molecular glues as potential GPCR therapeutics

BL Roth, BE Krumm - Biochemical Pharmacology, 2024 - Elsevier
Abstract “Molecular Glues” are defined as small molecules that can either be endogenous or
synthetic which promote interactions between proteins at their interface. Allosteric …

The role of central neurotensin in regulating feeding and body weight

J Ramirez-Virella, GM Leinninger - Endocrinology, 2021 - academic.oup.com
The small peptide neurotensin (Nts) is implicated in myriad processes including analgesia,
thermoregulation, reward, arousal, blood pressure, and modulation of feeding and body …

Effect of ligands and transducers on the neurotensin receptor 1 conformational ensemble

AD Dixon, A Inoue, SA Robson… - Journal of the …, 2022 - ACS Publications
Using a discrete, intracellular 19F nuclear magnetic resonance (NMR) probe on
transmembrane helix 6 of the neurotensin receptor 1 (NTS1), we aim to understand how …

[HTML][HTML] Stabilization of pre-existing neurotensin receptor conformational states by β-arrestin-1 and the biased allosteric modulator ML314

F Bumbak, JB Bower, SC Zemmer, A Inoue… - Nature …, 2023 - nature.com
Abstract The neurotensin receptor 1 (NTS1) is a G protein-coupled receptor (GPCR) with
promise as a drug target for the treatment of pain, schizophrenia, obesity, addiction, and …