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Structure-Activity Relationship Studies of a Macrocyclic AGRP-Mimetic Scaffold c[Pro-Arg-Phe-Phe-Asn-Ala-Phe-DPro] Yield Potent and Selective Melanocortin-4 Receptor Antagonists and Melanocortin-5 Receptor Inverse Agonists That Increase Food Intake in Mice.
Fleming KA, Ericson MD, Freeman KT, Adank DN, Lunzer MM, Wilber SL, Haskell-Luevano C. Fleming KA, et al. Among authors: lunzer mm. ACS Chem Neurosci. 2018 May 16;9(5):1141-1151. doi: 10.1021/acschemneuro.7b00495. Epub 2018 Feb 13. ACS Chem Neurosci. 2018. PMID: 29363944 Free PMC article.
Heteromer Induction: An Approach to Unique Pharmacology?
Portoghese PS, Akgün E, Lunzer MM. Portoghese PS, et al. Among authors: lunzer mm. ACS Chem Neurosci. 2017 Mar 15;8(3):426-428. doi: 10.1021/acschemneuro.7b00002. Epub 2017 Jan 31. ACS Chem Neurosci. 2017. PMID: 28139906
Comparative Intracerebroventricular and Intrathecal Administration of a Nanomolar Macrocyclic Melanocortin Receptor Agonist MDE6-5-2c (c[Pro-His-DPhe-Arg-Trp-Dap-Ala-DPro]) Decreases Food Intake in Mice.
Adank DN, Lunzer MM, Ericson MD, Koeperich ZM, Wilber SL, Fleming KA, Haskell-Luevano C. Adank DN, et al. Among authors: lunzer mm. ACS Chem Neurosci. 2020 Oct 7;11(19):3051-3063. doi: 10.1021/acschemneuro.0c00409. Epub 2020 Sep 10. ACS Chem Neurosci. 2020. PMID: 32822157 Free PMC article.
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].
Ericson MD, Tran LT, Mathre SS, Freeman KT, Holdaway K, John K, Lunzer MM, Bouchard JL, Haskell-Luevano C. Ericson MD, et al. Among authors: lunzer mm. J Med Chem. 2023 Jun 22;66(12):8103-8117. doi: 10.1021/acs.jmedchem.3c00432. Epub 2023 Jun 12. J Med Chem. 2023. PMID: 37307241 Free PMC article.
Incorporation of Three Extracyclic Arginine Residues into a Melanocortin Macrocyclic Agonist (c[Pro-His-DPhe-Arg-Trp-Dap-Lys(Arg-Arg-Arg-Ac)-DPro]) Decreases Food Intake When Administered Intrathecally or Subcutaneously Compared to a Macrocyclic Ligand Lacking Extracyclic Arginine Residues (c[Pro-His-DPhe-Arg-Trp-Dap-Ala-DPro)].
Ericson MD, Freeman KT, Larson CM, Bouchard JL, John K, Lunzer MM, Koerperich ZM, Haskell-Luevano C. Ericson MD, et al. Among authors: lunzer mm. ACS Pharmacol Transl Sci. 2024 Apr 2;7(4):1114-1125. doi: 10.1021/acsptsci.4c00011. eCollection 2024 Apr 12. ACS Pharmacol Transl Sci. 2024. PMID: 38633589
36 results