Synthesis and evaluation of tripodal peptide analogues for cellular delivery of phosphopeptides.

Synthesis and evaluation of tripodal peptide analogues for cellular delivery of phosphopeptides. Research Abstract Details 

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Synthesis and evaluation of tripodal peptide analogues for cellular delivery of phosphopeptides. Abstract Text:

Guofeng Ye,Nguyen-Hai Nam,Anil Kumar,Ali Saleh,Dinesh B Shenoy,Mansoor M Amiji,Xiaofeng Lin,Gongqin Sun,Keykavous Parang,

Tripodal peptide analogues were designed on the basis of the phosphotyrosine binding pocket of the Src SH2 domain and assayed for their ability to bind to fluorescein-labeled phosphopeptides. Fluorescence polarization assays showed that a number of amphipathic linear peptide analogues (LPAs), such as LPA4, bind to fluorescein-labeled GpYEEI (F-GpYEEI). LPA4 was evaluated for potential application in cellular delivery of phosphopeptides. Fluorescence microimaging cellular uptake studies with fluorescein-attached LPA4 (F-LPA4) alone or with the mixture of LPA4 and F-GpYEEI in BT-20 cells showed dramatic increase of the fluorescence intensity in cytosol of cells, indicating that LPA4 can function as a delivery tool of F-GpYEEI across the cell membrane. Fluorescent flow cytometry studies showed the cellular uptake of F-LPA4 in an energy-independent pathway and confirmed the cellular uptake of F-GpYEEI in the presence of LPA4. These studies suggest that amphipathic tripodal peptide analogues, such as LPA4, can be used for cellular delivery of phosphopeptides.

Synthesis and evaluation of tripodal peptide analogues for cellular delivery of phosphopeptides. Publishing Authors By Initials

G Ye,NH Nam,A Kumar,A Saleh,DB Shenoy,MM Amiji,X Lin,G Sun,K Parang,

For similar biochemical phenomena, metabolism, and nutrition: biochemical phenomena: structure-activity relationship research abstracts see: biochemical phenomena, metabolism, and nutrition: biochemical phenomena: structure-activity relationship research

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Synthesis and evaluation of tripodal peptide analogues for cellular delivery of phosphopeptides. Journal Published:

PUBLICATION TYPE: Research Support, N.I.H., Extr

Journal: Journal of medicinal chemistry

VOLUME: 50

Page Numbers: 3604-17

Journal Abbreviation: J. Med. Chem.

ISSN: 0022-2623

DAY: 20

MONTH: 06

YEAR: 2007

Synthesis and evaluation of tripodal peptide analogues for cellular delivery of phosphopeptides. Information

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LANGUAGE: eng

NlmUniqueID: 9716531

Synthesis and evaluation of tripodal peptide analogues for cellular delivery of phosphopeptides. Keywords Mesh Terms:

KEYWORDS: Structure-Activity Relationship

MESH TERMS: metabolism

Chemical & Substance for Abstract: Synthesis and evaluation of tripodal peptide analogues for cellular delivery of phosphopeptides. Information

Substance Name: Phosphopeptides

Registry Number: 0

Grant and Affiliation Information for Synthesis and evaluation of tripodal peptide analogues for cellular delivery of phosphopeptides.

AFFILIATION: Department of Biomedical and Pharmaceutical Sciences, University of Rhode Island, Kingston, Rhode Island 02881, USA.

Country: United States

AGENCY: United States NCRR

GRANT: 1 P20 RR16457

ACRONYM: RR

MEDLINETA: J Med Chem

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