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1. Full Text Synergistic Multiresidue Substitutions of a Macrocyclic c[Pro-Arg-Phe-Phe-Asn-Ala-Phe‑dPro] Agouti-Related Protein (AGRP) Scaffold Yield Potent and >600-Fold MC4R versus MC3R Selective Melanocortin Receptor Antagonists
by Fleming, Katlyn A and Freeman, Katie T and Ericson, Mark D and Haskell-Luevano, Carrie
Journal of Medicinal Chemistry, ISSN 0022-2623, 09/2018, Volume 61, Issue 17, pp. 7729 - 7740
Antagonist ligands of the melanocortin-3 and -4 receptors (MC3R, MC4R), including agouti-related protein (AGRP), are postulated to be targets for the treatment... 
OBESITY | CHEMISTRY, MEDICINAL | LIMBIC SYSTEM | SOLID-PHASE SYNTHESIS | IN-VIVO | MOUSE MODEL | INVERSE AGONIST | NMR STRUCTURE | MOLECULAR-CLONING | AMINO-PROTECTING GROUP | CYCLIC-PEPTIDES
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2. Full Text Arg-Phe-Phe d‑Amino Acid Stereochemistry Scan in the Macrocyclic Agouti-Related Protein Antagonist Scaffold c[Pro-Arg-Phe-Phe-Xxx-Ala-Phe-DPro] Results in Unanticipated Melanocortin‑1 Receptor Agonist Profiles
by Ericson, Mark D and Koerperich, Zoe M and Freeman, Katie T and Fleming, Katlyn A and Haskell-Luevano, Carrie
ACS Chemical Neuroscience, ISSN 1948-7193, 12/2018, Volume 9, Issue 12, pp. 3015 - 3023
The melanocortin-3 and melanocortin-4 receptors (MC3R and MC4R), endogenous agonists derived from the proopiomelanocortin gene transcript, and naturally... 
d -amino acids | AGRP | macrocycles | melanocortin receptors | CHEMISTRY, MEDICINAL | ALPHA-MELANOTROPIN | BIOCHEMISTRY & MOLECULAR BIOLOGY | DECAPEPTIDE | NEUROSCIENCES | D-amino acids | IN-VITRO | OBESITY | POTENT | HORMONE | PHARMACOLOGY | INVERSE AGONIST | MOLECULAR-CLONING | EXPRESSION
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3. Full Text Synergistic Multi-Residue Substitutions of a Macrocyclic c[Pro-Arg-Phe-Phe-Asn-Ala-Phe-DPro] Agouti-Related Protein (AGRP) Scaffold Yield Potent and >600-Fold MC4R versus MC3R Selective Melanocortin Receptor Antagonists
by Fleming, Katlyn A and Freeman, Katie T and Ericson, Mark D and Haskell-Luevano, Carrie
Journal of medicinal chemistry, ISSN 0022-2623, 9/2018, Volume 61, Issue 17, pp. 7729 - 7740
Antagonist ligands of the melanocortin-3 and −4 receptors (MC3R, MC4R), including agouti-related protein (AGRP), are postulated to be targets for the treatment... 
structure-activity relationships | macrocycles | AGRP | melanocortin receptors
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4. Full Text A Macrocyclic Agouti-Related Protein/[Nle4,DPhe7]α-Melanocyte Stimulating Hormone Chimeric Scaffold Produces Subnanomolar Melanocortin Receptor Ligands
by Ericson, Mark D and Freeman, Katie T and Schnell, Sathya M and Haskell-Luevano, Carrie
Journal of Medicinal Chemistry, ISSN 0022-2623, 01/2017, Volume 60, Issue 2, pp. 805 - 813
The melanocortin system consists of five receptor subtypes, endogenous agonists, and naturally occurring antagonists. These receptors and ligands have been... 
Animals | alpha-MSH - chemistry | Peptides, Cyclic - chemical synthesis | Agouti-Related Protein - chemistry | Humans | HEK293 Cells | Ligands | Peptides, Cyclic - pharmacology | Mice | Receptor, Melanocortin, Type 4 - agonists | Structure-Activity Relationship | alpha-MSH - analogs & derivatives
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5. Full Text Single Nucleotide Polymorphisms in the Melanocortin His-Phe-Arg-Trp Sequences Decrease Tetrapeptide Potency and Efficacy
by Winget, Marshall D and Ericson, Mark D and Freeman, Katie T and Haskell-Luevano, Carrie
ACS Medicinal Chemistry Letters, ISSN 1948-5875, 07/2019
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6. Full Text Capital as Will and Imagination: Schumpeter’s Guide to the Postwar Japanese Miracle by Mark Metzler (review)
by Ericson, Steven J
The Journal of Japanese Studies, ISSN 0095-6848, 2014, Volume 40, Issue 2, pp. 519 - 523
Metzler, Metzler, Mark, ‡d, Mark | Capital ‡z Japan ‡x History ‡y 20th century | Schumpeter, Joseph A | 1883-1950
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7. Full Text Structure⁻Activity Relationships of the Tetrapeptide Ac-His-Arg-( p I)DPhe-Tic-NH 2 at the Mouse Melanocortin Receptors: Modification at the ( p I)DPhe Position Leads to mMC3R Versus mMC4R Selective Ligands
by Schlasner, Katherine N and Ericson, Mark D and Doering, Skye R and Freeman, Katie T and Weinrich, Mary and Haskell-Luevano, Carrie
Molecules (Basel, Switzerland), 04/2019, Volume 24, Issue 8
The five melanocortin receptors (MC1R-MC5R) are involved in numerous biological pathways, including steroidogenesis, pigmentation, and food intake. In... 
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8. Full Text A Macrocyclic Agouti-Related Protein/[Nle4, DPhe7]α-Melanocyte Stimulating Hormone Chimeric Scaffold Produces Sub-nanomolar Melanocortin Receptor Ligands
by Ericson, Mark D and Freeman, Katie T and Schnell, Sathya M and Haskell-Luevano, Carrie
Journal of medicinal chemistry, ISSN 0022-2623, 1/2017, Volume 60, Issue 2, pp. 805 - 813
The melanocortin system consists of five receptor subtypes, endogenous agonists, and naturally occurring antagonists. These receptors and ligands have been... 
chimeric ligands | AGRP | NDP-MSH | macrocycles | obesity
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9. Full Text A Review of Single-Nucleotide Polymorphisms in Orexigenic Neuropeptides Targeting G Protein-Coupled Receptors
by Ericson, Mark D and Haskell-Luevano, Carrie
ACS Chemical Neuroscience, ISSN 1948-7193, 06/2018, Volume 9, Issue 6, pp. 1235 - 1246
Many physiological pathways are involved in appetite, food intake, and the maintenance of energy homeostasis. In particular, neuropeptides within the central... 
peptide | Single-nucleotide polymorphisms | galanin | melanocyte concentrating hormone | neuropeptide Y | agouti-related protein | hormone | orexin A | orexin B | pharmacogenomics | SNP | polypharmacology | GPCR | MELANOCYTE-STIMULATING HORMONE | FEEDING-BEHAVIOR | OREXIN-KNOCKOUT MICE | CHEMISTRY, MEDICINAL | BIOCHEMISTRY & MOLECULAR BIOLOGY | NEUROSCIENCES | PANCREATIC-POLYPEPTIDE | L-ALANINE SCAN | BODY-MASS INDEX | HUMAN OBESITY | MELANIN-CONCENTRATING HORMONE | Y GENE | Orexins - genetics | Orexins - metabolism | Receptors, G-Protein-Coupled - metabolism | Humans | Neuropeptides - metabolism | Intracellular Signaling Peptides and Proteins - metabolism | Melanins - genetics | Melanins - metabolism | Animals | Hypothalamic Hormones - metabolism | Pituitary Hormones - genetics | Pituitary Hormones - metabolism | Polymorphism, Single Nucleotide - genetics | Hypothalamic Hormones - genetics | Receptors, G-Protein-Coupled - genetics | Neuropeptides - genetics | Intracellular Signaling Peptides and Proteins - genetics
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10. Full Text A fragment of the Escherichia coli ClpB heat-shock protein is a micromolar melanocortin 1 receptor agonist
by Ericson, Mark D and Schnell, Sathya M and Freeman, Katie T and Haskell-Luevano, Carrie
Bioorganic & Medicinal Chemistry Letters, ISSN 0960-894X, 11/2015, Volume 25, Issue 22, pp. 5306 - 5308
The melanocortin system consists of five receptor subtypes (MC1–5R), endogenous agonists derived from the proopiomelanocortin gene transcript, and the... 
NDP-MSH | AlphaScreen® cAMP assay | α-MSH | Melanocortin receptors | ClpB heat shock protein | CHEMISTRY, MEDICINAL | CHEMISTRY, ORGANIC | EATING-DISORDERS | MINIMAL ACTIVE SEQUENCE | PEPTIDES | alpha-MSH | MOLECULAR-CLONING | MELANOTROPIN | BETA-DEFENSIN 3 | EXPRESSION | SKIN BIOASSAY | AlphaScreen (R) cAMP assay | Amino Acid Sequence | Endopeptidase Clp | Escherichia coli | Humans | Peptide Fragments - pharmacology | Escherichia coli Proteins - chemical synthesis | Heat-Shock Proteins - pharmacology | Peptide Fragments - chemical synthesis | Animals | Heat-Shock Proteins - chemical synthesis | Escherichia coli Proteins - pharmacology | HEK293 Cells | Ligands | Mice | Receptor, Melanocortin, Type 1 - agonists | Melanocortin Receptors | ClpB Heat Shock Protein | AlphaScreen® cAMP Assay
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11. Full Text PEG length and chemical linkage controls polyacridine peptide DNA polyplex pharmacokinetics, biodistribution, metabolic stability and in vivo gene expression
by Khargharia, Sanjib and Kizzire, Koby and Ericson, Mark D and Baumhover, Nicholas J and Rice, Kevin G
Journal of Controlled Release, ISSN 0168-3659, 09/2013, Volume 170, Issue 3, pp. 325 - 333
The pharmacokinetics (PK), biodistribution and metabolism of non-viral gene delivery systems administered systemically are directly related to efficacy. The... 
Gene delivery | Polyethylene glycol | Hydrodynamic dosing | CIRCULATION | MECHANISM | COMPLEXES | TAIL VEIN INJECTION | CHEMISTRY, MULTIDISCIPLINARY | QUANTUM DOTS | DELIVERY | INTRAVENOUS-INJECTION | PLASMID DNA | LIVER | PHARMACOLOGY & PHARMACY | CHAIN-LENGTH | Acridines - chemistry | DNA - pharmacokinetics | Gene Transfer Techniques | Gene Expression | Peptides - chemistry | Peptides - pharmacokinetics | DNA - administration & dosage | Male | Polyethylene Glycols - chemistry | Mice, Inbred ICR | Peptides - administration & dosage | Luciferases - genetics | Tissue Distribution | DNA - chemistry | Animals | Polymers - chemistry | Mice | Thiols | Peptides | Analysis | Genes | DNA | Physiological aspects | Genetic research | Gene expression | Polyols | Hydrodynamic Dosing | Gene Delivery
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12. Full Text Structure-Activity Relationships of the Tetrapeptide Ac-His-Arg-(pI)DPhe-Tic-NH2 at the Mouse Melanocortin Receptors: Modification at the (pI)DPhe Position Leads to mMC3R Versus mMC4R Selective Ligands
by Schlasner, KN and Ericson, MD and Doering, SR and Freeman, KT and Weinrich, M and Haskell-Luevano, C
MOLECULES, ISSN 1420-3049, 04/2019, Volume 24, Issue 8, p. 1463
The five melanocortin receptors (MC1R-MC5R) are involved in numerous biological pathways, including steroidogenesis, pigmentation, and food intake. In... 
mixed pharmacology | SOLID-PHASE SYNTHESIS | ALPHA-MELANOTROPIN | FOOD-INTAKE | SIDE-CHAIN | BIOCHEMISTRY & MOLECULAR BIOLOGY | CHEMISTRY, MULTIDISCIPLINARY | MC4R | tetrapeptides | MC3R | AGOUTI-RELATED PROTEIN | OBESITY | SEQUENCE | MOLECULAR-CLONING | melanocortins | AC-HIS-DPHE-ARG-TRP-NH2 | AGONIST
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13. Full Text Structure–Activity Relationship Studies on a Macrocyclic Agouti-Related Protein (AGRP) Scaffold Reveal Agouti Signaling Protein (ASP) Residue Substitutions Maintain Melanocortin‑4 Receptor Antagonist Potency and Result in Inverse Agonist Pharmacology at the Melanocortin‑5 Receptor
by Ericson, Mark D and Freeman, Katie T and Schnell, Sathya M and Fleming, Katlyn A and Haskell-Luevano, Carrie
Journal of Medicinal Chemistry, ISSN 0022-2623, 10/2017, Volume 60, Issue 19, pp. 8103 - 8114
The melanocortin system consists of five reported receptors, agonists from the proopio­melanocortin gene transcript, and two antagonists, agouti-signaling... 
IN-VITRO | CHEMISTRY, MEDICINAL | STIMULATING-HORMONE-RECEPTOR | GENE | CAUSES OBESITY | MOUSE | NMR STRUCTURE | MOLECULAR-CLONING | AMINO-PROTECTING GROUP | EXPRESSION | TRANSGENIC MICE | Receptor, Melanocortin, Type 4 - antagonists & inhibitors | Agouti-Related Protein - chemistry | Humans | Models, Molecular | Structure-Activity Relationship | Agouti Signaling Protein - chemistry | Animals | Receptors, Melanocortin - agonists | HEK293 Cells | Ligands | Mice | Cyclic AMP - metabolism | Energy Metabolism - drug effects | Amino Acid Substitution | AGRP | agouti | structure-activity relationships | inverse agonist | melanocortin receptors
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14. Full Text A convergent synthesis of homogeneous reducible polypeptides
by Ericson, Mark D and Rice, Kevin G
Tetrahedron Letters, ISSN 0040-4039, 08/2013, Volume 54, Issue 35, pp. 4746 - 4748
The convergent syntheses of homogeneous disulfide cross-linked polypeptides are reported. Reducible polypeptides were synthesized containing four and eight... 
Cysteine | Reducible polypeptides | Convergent synthesis | Acetamidomethyl | Thiazolidine | CHEMISTRY, ORGANIC | POTENT | MODELS | IN-VIVO | CONSTRUCTION | HETEROTRIMERIC COLLAGEN PEPTIDES | PROTEINS | EXPRESSION | DISULFIDE CROSS-LINKING | NONVIRAL GENE DELIVERY | Surgical implants | Silver | Polypeptides | Peptides | Genes | Disulfides | Crosslinking | Conjugation | thiazolidine | acetamidomethyl | convergent synthesis | cysteine
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15. Full Text Discovery of a β-Hairpin Octapeptide, c[Pro-Arg-Phe-Phe-Dap-Ala-Phe-DPro], Mimetic of Agouti-Related Protein(87-132) [AGRP(87-132)] with Equipotent Mouse Melanocortin-4 Receptor (mMC4R) Antagonist Pharmacology
by Ericson, Mark D and Wilczynski, Andrzej and Sorensen, Nicholas B and Xiang, Zhimin and Haskell-Luevano, Carrie
Journal of Medicinal Chemistry, ISSN 0022-2623, 06/2015, Volume 58, Issue 11, pp. 4638 - 4647
Agouti-related protein (AGRP) is a potent orexigenic peptide that antagonizes the melanocortin-3 and -4 receptors (MC3R and MC4R). While the C-terminal domain... 
CHEMISTRY, MEDICINAL | MELANOCYTE-STIMULATING HORMONE | PROTEIN AGRP | INVERSE AGONIST | NMR STRUCTURE | MOLECULAR-CLONING | TETRAPEPTIDE AC-HIS-DPHE-ARG-TRP-NH2 | AMINO-PROTECTING GROUP | AGONIST ACTIVITY | EVALUATION IN-VITRO | PEPTIDE | Receptor, Melanocortin, Type 4 - antagonists & inhibitors | Agouti-Related Protein - chemistry | Humans | Models, Molecular | Peptide Fragments - pharmacology | Structure-Activity Relationship | Drug Discovery | Peptide Fragments - chemistry | Animals | Biomimetics | Receptor, Melanocortin, Type 3 - antagonists & inhibitors | HEK293 Cells | Ligands | Mice | Molecular Structure | Cyclic AMP - metabolism | GPCR | AGRP | β-hairpin mimetics | structure-activity relationship | melanocortin receptors
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16. Full Text Bench-top to clinical therapies: A review of melanocortin ligands from 1954 to 2016
by Ericson, Mark D and Lensing, Cody J and Fleming, Katlyn A and Schlasner, Katherine N and Doering, Skye R and Haskell-Luevano, Carrie
BBA - Molecular Basis of Disease, ISSN 0925-4439, 10/2017, Volume 1863, Issue 10, pp. 2414 - 2435
The discovery of the endogenous melanocortin agonists in the 1950s have resulted in sixty years of melanocortin ligand research. Early efforts involved... 
Clinical trials | Small molecules | Sexual dimorphism | Selective ligands | Bivalent/multivalent ligands | BIOCHEMISTRY & MOLECULAR BIOLOGY | MELANOCYTE-STIMULATING-HORMONE | EARLY-ONSET OBESITY | SMALL-MOLECULE LIGANDS | TOBACCO MOSAIC-VIRUS | AGOUTI-RELATED PROTEIN | ALPHA-MSH ANALOGS | ANTAGONIST BIVALENT LIGANDS | AMINO-ACID-SEQUENCE | BIOPHYSICS | FEMALE SEXUAL DYSFUNCTIONS | RECEPTOR AGONIST
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17. Full Text Iterative reducible ligation to form homogeneous penicillamine cross-linked polypeptides
by Ericson, Mark D and Rice, Kevin G
Tetrahedron Letters, ISSN 0040-4039, 06/2013, Volume 54, Issue 26, pp. 3440 - 3443
The syntheses of homogeneous penicillamine disulfide cross-linked polypeptides are reported. Dodecapeptides containing N-terminal, C-terminal, or N- and... 
Gene delivery | Reducible polypeptides | Penicillamine | Thiazolidine | STABILITY | CHEMISTRY, ORGANIC | DISULFIDE | CARRIERS | NUCLEIC-ACIDS | LINKING | STERIC HINDRANCE | CONSTRUCTION | HETEROTRIMERIC COLLAGEN PEPTIDES | LINKAGE | Biopolymers | Hydrolysis | Residues | Polypeptides | Genes | Disulfides | Tetrahedrons | Crosslinking | Amino acids | thiazolidine | gene delivery | penicillamine
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18. Full Text 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
by Fleming, Katlyn A and Ericson, Mark D and Freeman, Katie T and Adank, Danielle N and Lunzer, Mary M and Wilber, Stacey L and Haskell-Luevano, Carrie
ACS Chemical Neuroscience, ISSN 1948-7193, 05/2018, Volume 9, Issue 5, pp. 1141 - 1151
The melanocortin system has five receptors, and antagonists of the central melanocortin receptors (MC3R, MC4R) are postulated to be viable therapeutics for... 
AGRP | structure-activity relationships | melanocortin receptors | food intake
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