Allosteric modulation of G protein–coupled receptors
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 …
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 …
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 …
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 …
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 …
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 …
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 …
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 …
modulate dopamine D2 receptors within the central nervous system. However, the precise …
[CITATION][C] Endogenous allosteric modulators of G protein–coupled receptors
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 …
isobutyl, butyl, and benzyl moieties to give the PLG peptidomimetics 3− 5, respectively …