Allosteric modulation of G protein–coupled receptors

LT May, K Leach, PM Sexton… - Annu. Rev. Pharmacol …, 2007 - annualreviews.org
The past decade has witnessed a significant growth in the identification of allosteric
modulators of G protein–coupled receptors (GPCRs), ie, ligands that interact with binding …

Allosteric and biased g protein-coupled receptor signaling regulation: potentials for new therapeutics

E Khoury, S Clément, SA Laporte - Frontiers in endocrinology, 2014 - frontiersin.org
G protein-coupled receptors (GPCRs) are seven-transmembrane proteins that participate in
many aspects of the endocrine function and are important targets for drug development …

[HTML][HTML] Interactions of Oxytocin and Dopamine—Effects on Behavior in Health and Disease

M Petersson, K Uvnäs-Moberg - Biomedicines, 2024 - mdpi.com
The hypothalamic neuropeptide and hormone oxytocin are of fundamental importance for
maternal, social, and sexual behavior. Deviations in oxytocin levels have also been …

Stapling Amantadine to Melanostatin Neuropeptide: Discovery of Potent Positive Allosteric Modulators of the D2 Receptors

SC Silva-Reis, XC Correia… - ACS Medicinal …, 2023 - ACS Publications
This work describes the synthesis and pharmacological and toxicological evaluation of
melanostatin (MIF-1) bioconjugates with amantadine (Am) via a peptide linkage. The data …

Synthesis, pharmacological, and biological evaluation of 2-furoyl-based MIF-1 peptidomimetics and the development of a general-purpose model for allosteric …

IE Sampaio-Dias, JE Rodriguez-Borges… - ACS Chemical …, 2020 - ACS Publications
This work describes the synthesis and pharmacological evaluation of 2-furoyl-based
Melanostatin (MIF-1) peptidomimetics as dopamine D2 modulating agents. Eight novel …

Discovery of New Potent Positive Allosteric Modulators of Dopamine D2 Receptors: Insights into the Bioisosteric Replacement of Proline to 3-Furoic Acid in the …

IE Sampaio-Dias, A Reis-Mendes… - Journal of Medicinal …, 2021 - ACS Publications
The control of Parkinson's disease (PD) is challenged by the motor and non-motor
fluctuations as well as dyskinesias associated with levodopa long-term therapy. As such …

PAOPA, a potent dopamine D2 receptor allosteric modulator, prevents and reverses behavioral and biochemical abnormalities in an amphetamine-sensitized …

MGR Beyaert, RP Daya, BA Dyck, RL Johnson… - European …, 2013 - Elsevier
Allosteric modulators are emerging as new therapeutics for the treatment of psychiatric
illnesses, such as schizophrenia. Conventional antipsychotic drugs are typically dopamine …

Design and Synthesis of Photoaffinity-Labeling Ligands of the l-Prolyl-l-leucylglycinamide Binding Site Involved in the Allosteric Modulation of the Dopamine …

A Fisher, A Mann, V Verma, N Thomas… - Journal of medicinal …, 2006 - ACS Publications
Pro-Leu-Gly-NH2 (PLG), in addition to its endocrine effects, possesses the ability to
modulate dopamine D2 receptors within the central nervous system. However, the precise …

[CITATION][C] Endogenous allosteric modulators of G protein–coupled receptors

ET van der Westhuizen, C Valant, PM Sexton… - … of Pharmacology and …, 2015 - ASPET

Synthesis and Dopamine Receptor Modulating Activity of 3-Substituted γ-Lactam Peptidomimetics of l-Prolyl-l-leucyl-glycinamide

K Dolbeare, GF Pontoriero, SK Gupta… - Journal of medicinal …, 2003 - ACS Publications
γ-Lactam peptidomimetic 2 of Pro-Leu-Gly-NH2 (PLG) was substituted at the 3-position with
isobutyl, butyl, and benzyl moieties to give the PLG peptidomimetics 3− 5, respectively …