Molecular design of small organic molecules based on structural information for a conformationally constrained peptide that binds to G-CSF receptor

Radwan El-Haggar; Ken Kamikawa; Kazuya Machi; Zhengmao Ye; Yuko Ishino; Takeshi Tsumuraya; Ikuo Fujii

doi:10.1016/j.bmcl.2009.12.010

Molecular design of small organic molecules based on structural information for a conformationally constrained peptide that binds to G-CSF receptor

Bioorg Med Chem Lett. 2010 Feb 1;20(3):1169-72. doi: 10.1016/j.bmcl.2009.12.010. Epub 2009 Dec 4.

Authors

Radwan El-Haggar¹, Ken Kamikawa, Kazuya Machi, Zhengmao Ye, Yuko Ishino, Takeshi Tsumuraya, Ikuo Fujii

Affiliation

¹ Department of Biological Science, Graduate School of Science, Osaka Prefecture University, Sakai, Osaka 599-8531, Japan.

PMID: 20031402
DOI: 10.1016/j.bmcl.2009.12.010

Abstract

Based on structural information for a peptide (P8-2KAQ) that binds to granulocyte-colony stimulating factor receptor (G-CSFR), small ligands with a biaryl scaffold were designed and their binding affinities were evaluated.

Publication types

Comparative Study
Research Support, Non-U.S. Gov't

MeSH terms

Drug Design*
Helix-Loop-Helix Motifs / physiology
Molecular Conformation
Peptides / chemistry*
Peptides / metabolism*
Protein Binding / physiology
Protein Conformation*
Receptors, Granulocyte Colony-Stimulating Factor / metabolism*
Structure-Activity Relationship

Substances

Peptides
Receptors, Granulocyte Colony-Stimulating Factor