The pharmacophore of a peptoid VEGF receptor 2 antagonist includes both side chain and main chain residues

D. Gomika Udugamasooriya; Geoff Dunham; Caroline Ritchie; Rolf A. Brekken; Thomas Kodadek

doi:10.1016/j.bmcl.2008.07.023

The pharmacophore of a peptoid VEGF receptor 2 antagonist includes both side chain and main chain residues

D. Gomika Udugamasooriya, Geoff Dunham, Caroline Ritchie, Rolf A. Brekken, Thomas Kodadek

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

29 Scopus citations

Abstract

Here we identify the pharmacophore in a peptoid that antagonizes Vascular Endothelial Growth Factor Receptor-2 (VEGFR2) in vitro and in vivo. Only three of the side chains in the peptoid are required for activity. Surprisingly, however, main chain atoms also form critical interactions with the receptor.

Original language	English (US)
Pages (from-to)	5892-5894
Number of pages	3
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	18
Issue number	22
DOIs	https://doi.org/10.1016/j.bmcl.2008.07.023
State	Published - Nov 15 2008

Keywords

Glycine scan
Minimum pharmacophore
Peptoid
Sarcosine scan

ASJC Scopus subject areas

Biochemistry
Molecular Medicine
Molecular Biology
Pharmaceutical Science
Drug Discovery
Clinical Biochemistry
Organic Chemistry

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10.1016/j.bmcl.2008.07.023

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title = "The pharmacophore of a peptoid VEGF receptor 2 antagonist includes both side chain and main chain residues",

abstract = "Here we identify the pharmacophore in a peptoid that antagonizes Vascular Endothelial Growth Factor Receptor-2 (VEGFR2) in vitro and in vivo. Only three of the side chains in the peptoid are required for activity. Surprisingly, however, main chain atoms also form critical interactions with the receptor.",

keywords = "Glycine scan, Minimum pharmacophore, Peptoid, Sarcosine scan",

author = "Udugamasooriya, {D. Gomika} and Geoff Dunham and Caroline Ritchie and Brekken, {Rolf A.} and Thomas Kodadek",

note = "Funding Information: This work was supported by a contract from the National Heart, Lung, and Blood Institute (NO1-HV-28185) for the UT Southwestern Center for Proteomics Research, a grant from the Welch Foundation (I-1299), and the Effie Marie Cain Scholarship for Angiogenesis Research. ",

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T1 - The pharmacophore of a peptoid VEGF receptor 2 antagonist includes both side chain and main chain residues

AU - Udugamasooriya, D. Gomika

AU - Dunham, Geoff

AU - Ritchie, Caroline

AU - Brekken, Rolf A.

AU - Kodadek, Thomas

N1 - Funding Information: This work was supported by a contract from the National Heart, Lung, and Blood Institute (NO1-HV-28185) for the UT Southwestern Center for Proteomics Research, a grant from the Welch Foundation (I-1299), and the Effie Marie Cain Scholarship for Angiogenesis Research.

PY - 2008/11/15

Y1 - 2008/11/15

N2 - Here we identify the pharmacophore in a peptoid that antagonizes Vascular Endothelial Growth Factor Receptor-2 (VEGFR2) in vitro and in vivo. Only three of the side chains in the peptoid are required for activity. Surprisingly, however, main chain atoms also form critical interactions with the receptor.

AB - Here we identify the pharmacophore in a peptoid that antagonizes Vascular Endothelial Growth Factor Receptor-2 (VEGFR2) in vitro and in vivo. Only three of the side chains in the peptoid are required for activity. Surprisingly, however, main chain atoms also form critical interactions with the receptor.

KW - Glycine scan

KW - Minimum pharmacophore

KW - Peptoid

KW - Sarcosine scan

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JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 22

ER -

The pharmacophore of a peptoid VEGF receptor 2 antagonist includes both side chain and main chain residues

Abstract

Keywords

ASJC Scopus subject areas

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