Structure-Based Design of Melanocortin 4 Receptor Ligands Based on the SHU-9119-hMC4R Cocrystal Structure†.

Crystallography, X-Ray Humans Ligands Molecular Structure Receptor, Melanocortin, Type 4 / chemistry

Journal

Journal of medicinal chemistry
ISSN: 1520-4804
Titre abrégé: J Med Chem
Pays: United States
ID NLM: 9716531

Informations de publication

Date de publication:
14 01 2021
Historique:
pubmed: 17 11 2020
medline: 9 3 2021
entrez: 16 11 2020
Statut: ppublish

Résumé

The melanocortin receptors (MC1R-MC5R) belong to class A G-protein-coupled receptors (GPCRs) and are known to have receptor-specific roles in normal and diseased states. Selectivity for MC4R is of particular interest due to its involvement in various metabolic disorders, including obesity, feeding regulation, and sexual dysfunctions. To further improve the potency and selectivity of MC4R (ant)agonist peptide ligands, we designed and synthesized a series of cyclic peptides based on the recent crystal structure of MC4R in complex with the well-characterized antagonist

Identifiants

DOI: 10.1021/acs.jmedchem.0c01620 PMID: 33190475
pubmed: 33190475
doi: 10.1021/acs.jmedchem.0c01620
doi:

Substances chimiques

Ligands 0
MC4R protein, human 0
Receptor, Melanocortin, Type 4 0

Types de publication

Journal Article Research Support, N.I.H., Extramural Research Support, Non-U.S. Gov't

Langues

eng

Sous-ensembles de citation

IM

Pagination

357-369

Subventions

Organisme : NIDDK NIH HHS
ID : R01 DK070332
Pays : United States

Auteurs

Charlotte Martin (C)

Research Group of Organic Chemistry, Vrije Universiteit Brussel, Pleinlaan 2, B-1050 Brussels, Belgium.

Luis E Gimenez (LE)

Life Sciences Institute, University of Michigan, Ann Arbor, Michigan 48109, United States.

Savannah Y Williams (SY)

Life Sciences Institute, University of Michigan, Ann Arbor, Michigan 48109, United States.

Yu Jing (Y)

iHuman Institute, ShanghaiTech University, Ren Building, 393 Middle Huaxia Road, Pudong, Shanghai 201210, China.

Yiran Wu (Y)

iHuman Institute, ShanghaiTech University, Ren Building, 393 Middle Huaxia Road, Pudong, Shanghai 201210, China.

Charlie Hollanders (C)

Research Group of Organic Chemistry, Vrije Universiteit Brussel, Pleinlaan 2, B-1050 Brussels, Belgium.

Olivier Van der Poorten (O)

Research Group of Organic Chemistry, Vrije Universiteit Brussel, Pleinlaan 2, B-1050 Brussels, Belgium.

Simon Gonzalez (S)

Research Group of Organic Chemistry, Vrije Universiteit Brussel, Pleinlaan 2, B-1050 Brussels, Belgium.

Kevin Van Holsbeeck (K)

Research Group of Organic Chemistry, Vrije Universiteit Brussel, Pleinlaan 2, B-1050 Brussels, Belgium.

Santo Previti (S)

Research Group of Organic Chemistry, Vrije Universiteit Brussel, Pleinlaan 2, B-1050 Brussels, Belgium.

Arthur Lamouroux (A)

Research Group of Organic Chemistry, Vrije Universiteit Brussel, Pleinlaan 2, B-1050 Brussels, Belgium.

Suwen Zhao (S)

iHuman Institute, ShanghaiTech University, Ren Building, 393 Middle Huaxia Road, Pudong, Shanghai 201210, China.
School of Life Science and Technology, ShanghaiTech University, 393 Middle Huaxia Road, Pudong, Shanghai 201210, China.
ORCID: 0000-0001-5609-434X

Dirk Tourwé (D)

Research Group of Organic Chemistry, Vrije Universiteit Brussel, Pleinlaan 2, B-1050 Brussels, Belgium.

Raymond C Stevens (RC)

iHuman Institute, ShanghaiTech University, Ren Building, 393 Middle Huaxia Road, Pudong, Shanghai 201210, China.
School of Life Science and Technology, ShanghaiTech University, 393 Middle Huaxia Road, Pudong, Shanghai 201210, China.

Roger D Cone (RD)

Life Sciences Institute, University of Michigan, Ann Arbor, Michigan 48109, United States.
Department of Molecular and Integrative Physiology, University of Michigan, Ann Arbor, Michigan 48109, United States.

Steven Ballet (S)

Research Group of Organic Chemistry, Vrije Universiteit Brussel, Pleinlaan 2, B-1050 Brussels, Belgium.
ORCID: 0000-0003-4123-1641

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Classifications MeSH

questionsmedicales.fr › Techniques d'investigation › Techniques de chimie analytique › Cristallographie aux rayons X › Structure-Based Design of Melanocortin 4...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Primates › Haplorhini › Catarrhini › Hominidae › Humains › Structure-Based Design of Melanocortin 4...
questionsmedicales.fr › Actions chimiques et utilisations › Utilisations spécialisées de produits chimiques › Produits chimiques de laboratoire › Ligands › Structure-Based Design of Melanocortin 4...
questionsmedicales.fr › Phénomènes chimiques › Structure moléculaire › Structure-Based Design of Melanocortin 4...
questionsmedicales.fr › Acides aminés, peptides et protéines › Protéines › Protéines membranaires › Récepteurs de surface cellulaire › Récepteurs peptidiques › Récepteur hormone hypophysaire › Récepteur corticotrophine › Récepteurs à la mélanocortine › Récepteur de la mélanocortine de type 4 › Structure-Based Design of Melanocortin 4...