Discovery of Molecular Interactions of the Human Melanocortin-4 Receptor (hMC4R) Asp189 (D189) Amino Acid with the Endogenous G-Protein-Coupled Receptor (GPCR) Antagonist Agouti-Related Protein (AGRP) Provides Insights to AGRP’s Inverse Agonist Pharmacology at the hMC4R-Reference-Cited by-同舟云学术

Discovery of Molecular Interactions of the Human Melanocortin-4 Receptor (hMC4R) Asp189 (D189) Amino Acid with the Endogenous G-Protein-Coupled Receptor (GPCR) Antagonist Agouti-Related Protein (AGRP) Provides Insights to AGRP’s Inverse Agonist Pharmacology at the hMC4R

Published:2021-01-20 Issue:3 Volume:12 Page:542-556
ISSN:1948-7193
Container-title:ACS Chemical Neuroscience
language:en
Short-container-title:ACS Chem. Neurosci.

Author:

Ericson Mark D.¹,Haslach Erica M.²,Schnell Sathya M.¹,Freeman Katie T.¹,Xiang Zhimin M.²,Portillo Frederico P.²,Speth Robert³⁴,Litherland Sally A.⁵,Haskell-Luevano Carrie¹²^ORCID

Affiliation:

1. Department of Medicinal Chemistry and Institute for Translational Neuroscience, University of Minnesota, 308 Harvard Street SE, Minneapolis, Minnesota 55455, United States

2. Departments of Pharmacodynamics and Medicinal Chemistry, University of Florida, Gainesville, Florida 32610, United States

3. College of Pharmacy, Nova Southeastern University, Fort Lauderdale, Florida 33328, United States

4. College of Medicine, Georgetown University, Washington, D.C. 20057, United States

5. Translational Research, Florida Hospital Cancer Institute, Orlando, Florida 32804, United States

Funder

National Institute of Diabetes and Digestive and Kidney Diseases

Publisher

American Chemical Society (ACS)

Subject

Cell Biology,Cognitive Neuroscience,Physiology,Biochemistry,General Medicine

Link

https://pubs.acs.org/doi/pdf/10.1021/acschemneuro.0c00755

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1. Discovery of a Pan-Melanocortin Receptor Antagonist [Ac-DPhe(pI)-Arg-Nal(2′)-Orn-NH₂] at the MC1R, MC3R, MC4R, and MC5R that Mediates an Increased Feeding Response in Mice and a 40-Fold Selective MC1R Antagonist [Ac-DPhe(pI)-DArg-Nal(2′)-Arg-NH₂];Journal of Medicinal Chemistry;2023-06-12

2. Functional Mixture-Based Positional Scan Identifies a Library of Antagonist Tetrapeptide Sequences (LAtTeS) with Nanomolar Potency for the Melanocortin-4 Receptor and Equipotent with the Endogenous AGRP(86-132) Antagonist;Journal of Medicinal Chemistry;2021-09-30

3. Personalized Medicine Through GPCR Pharmacogenomics;Reference Module in Biomedical Sciences;2021