Quantitative Comparison of the Relative Cell Permeability of Cyclic and Linear Peptides

Yong Uk Kwon; Thomas Kodadek

doi:10.1016/j.chembiol.2007.05.006

Quantitative Comparison of the Relative Cell Permeability of Cyclic and Linear Peptides

Yong Uk Kwon, Thomas Kodadek

Department of Chemistry & Nanoscience

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

93 Scopus citations

Abstract

Cyclic peptides are of considerable interest as potential protein ligands. It has been postulated that cyclic molecules might be more cell permeable than their linear counterparts due to their reduced conformational flexibility. We report a study that tests this hypothesis by using a quantitative, reporter gene-based assay that measures the relative cell permeability of steroid conjugates of molecules of interest. We demonstrate that cyclic peptides are, in fact, not generally more permeable than their linear counterparts.

Original language	English
Pages (from-to)	671-677
Number of pages	7
Journal	Chemistry and Biology
Volume	14
Issue number	6
DOIs	https://doi.org/10.1016/j.chembiol.2007.05.006
State	Published - 25 Jun 2007

Bibliographical note

Funding Information:
This work was supported by a contract from the National Heart, Lung, and Blood Institute (NHLBI) (NO1-HV-28185). We thank Dr. Peng Yu, Mr. Jiyong Lee, and Mr. Chiang Tan for technical assistance and helpful discussions, and Dr. Kyung-Jong Lee for assistance with the fluorescence imaging experiment.

Keywords

CHEMBIOL

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10.1016/j.chembiol.2007.05.006

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title = "Quantitative Comparison of the Relative Cell Permeability of Cyclic and Linear Peptides",

abstract = "Cyclic peptides are of considerable interest as potential protein ligands. It has been postulated that cyclic molecules might be more cell permeable than their linear counterparts due to their reduced conformational flexibility. We report a study that tests this hypothesis by using a quantitative, reporter gene-based assay that measures the relative cell permeability of steroid conjugates of molecules of interest. We demonstrate that cyclic peptides are, in fact, not generally more permeable than their linear counterparts.",

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author = "Kwon, {Yong Uk} and Thomas Kodadek",

note = "Funding Information: This work was supported by a contract from the National Heart, Lung, and Blood Institute (NHLBI) (NO1-HV-28185). We thank Dr. Peng Yu, Mr. Jiyong Lee, and Mr. Chiang Tan for technical assistance and helpful discussions, and Dr. Kyung-Jong Lee for assistance with the fluorescence imaging experiment. ",

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AU - Kodadek, Thomas

N1 - Funding Information: This work was supported by a contract from the National Heart, Lung, and Blood Institute (NHLBI) (NO1-HV-28185). We thank Dr. Peng Yu, Mr. Jiyong Lee, and Mr. Chiang Tan for technical assistance and helpful discussions, and Dr. Kyung-Jong Lee for assistance with the fluorescence imaging experiment.

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N2 - Cyclic peptides are of considerable interest as potential protein ligands. It has been postulated that cyclic molecules might be more cell permeable than their linear counterparts due to their reduced conformational flexibility. We report a study that tests this hypothesis by using a quantitative, reporter gene-based assay that measures the relative cell permeability of steroid conjugates of molecules of interest. We demonstrate that cyclic peptides are, in fact, not generally more permeable than their linear counterparts.

AB - Cyclic peptides are of considerable interest as potential protein ligands. It has been postulated that cyclic molecules might be more cell permeable than their linear counterparts due to their reduced conformational flexibility. We report a study that tests this hypothesis by using a quantitative, reporter gene-based assay that measures the relative cell permeability of steroid conjugates of molecules of interest. We demonstrate that cyclic peptides are, in fact, not generally more permeable than their linear counterparts.

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ER -

Quantitative Comparison of the Relative Cell Permeability of Cyclic and Linear Peptides

Abstract

Bibliographical note

Keywords

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