β-Turn secondary structure and melanocortin ligands

Erica M. Haslach; Jay W. Schaub; Carrie Haskell-Luevano

doi:10.1016/j.bmc.2008.02.090

β-Turn secondary structure and melanocortin ligands

Erica M. Haslach, Jay W. Schaub, Carrie Haskell-Luevano

Medicinal Chemistry

Research output: Contribution to journal › Article › peer-review

7 Scopus citations

Abstract

The melanocortin pathway has emerged during this past decade as an important target area for the discovery and development of therapeutic agents related to obesity and type 2 diabetes. This peptide-G-protein coupled receptor (GPCR) pathway has evolved from peptide-based ligands to small molecules possessing a variety of different molecular scaffolds. Herein, we summarize the originating hypothesis of the importance of the reverse β-turn secondary structure for agonist ligand potency at the melanocortin receptors and how that information was utilized for the discovery of small molecules based upon this type of turn structure.

Original language	English (US)
Pages (from-to)	952-958
Number of pages	7
Journal	Bioorganic and Medicinal Chemistry
Volume	17
Issue number	3
DOIs	https://doi.org/10.1016/j.bmc.2008.02.090
State	Published - Feb 1 2009

Bibliographical note

Funding Information:
We acknowledge financial support from NIH Grants RO1DK57080, RO1DK64250, RO1DK063974, and an American Diabetes Research Award. We thank Mic E. Mouse for his inspirational thoughts.

Keywords

Diabetes
MC4R
Melanocortin
Melanocortin receptors
Melanotropin
Obesity

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

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10.1016/j.bmc.2008.02.090

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title = "β-Turn secondary structure and melanocortin ligands",

abstract = "The melanocortin pathway has emerged during this past decade as an important target area for the discovery and development of therapeutic agents related to obesity and type 2 diabetes. This peptide-G-protein coupled receptor (GPCR) pathway has evolved from peptide-based ligands to small molecules possessing a variety of different molecular scaffolds. Herein, we summarize the originating hypothesis of the importance of the reverse β-turn secondary structure for agonist ligand potency at the melanocortin receptors and how that information was utilized for the discovery of small molecules based upon this type of turn structure.",

keywords = "Diabetes, MC4R, Melanocortin, Melanocortin receptors, Melanotropin, Obesity",

author = "Haslach, {Erica M.} and Schaub, {Jay W.} and Carrie Haskell-Luevano",

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AU - Haslach, Erica M.

AU - Schaub, Jay W.

AU - Haskell-Luevano, Carrie

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AB - The melanocortin pathway has emerged during this past decade as an important target area for the discovery and development of therapeutic agents related to obesity and type 2 diabetes. This peptide-G-protein coupled receptor (GPCR) pathway has evolved from peptide-based ligands to small molecules possessing a variety of different molecular scaffolds. Herein, we summarize the originating hypothesis of the importance of the reverse β-turn secondary structure for agonist ligand potency at the melanocortin receptors and how that information was utilized for the discovery of small molecules based upon this type of turn structure.

KW - Diabetes

KW - MC4R

KW - Melanocortin

KW - Melanocortin receptors

KW - Melanotropin

KW - Obesity

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β-Turn secondary structure and melanocortin ligands

Abstract

Bibliographical note

Keywords

UN SDGs

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