Synthesis and biological activity of conjugates between paclitaxel and the cell delivery vector penetratin

Shudong Wang; Nikolai Z. Zhelev; Susan Duff; Peter M. Fischer

doi:10.1016/j.bmcl.2006.02.035

Synthesis and biological activity of conjugates between paclitaxel and the cell delivery vector penetratin

Shudong Wang (Lead / Corresponding author), Nikolai Z. Zhelev, Susan Duff, Peter M. Fischer

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

18 Citations (Scopus)

Abstract

Synthesis of paclitaxel-penetratin (pAntp) constructs, in which the 2′- or 7-position of paclitaxel was used as the attachment site for linker connecting the drug and peptide moieties, is described. Paclitaxel-2′-pAntp[43-58]-NH₂ 3b and paclitaxel-2′-pAntp[52-58]-NH₂ 3c showed excellent antitumour activity against human lung and breast cancer cell lines. These conjugates were highly soluble and stable with a half-life of >8 h under cell culture conditions. The drug-peptide conjugates may be therapeutically useful due to improved pharmaceutical properties.

Original language	English
Pages (from-to)	2628-2631
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	16
Issue number	10
Early online date	2 Mar 2006
DOIs	https://doi.org/10.1016/j.bmcl.2006.02.035
Publication status	Published - 15 May 2006

Keywords

Antitumour activity
Cell delivery vector
Drug-peptide conjugate
Paclitaxel
Penetratin

ASJC Scopus subject areas

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

UN SDGs

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

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10.1016/j.bmcl.2006.02.035

Cite this

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abstract = "Synthesis of paclitaxel-penetratin (pAntp) constructs, in which the 2′- or 7-position of paclitaxel was used as the attachment site for linker connecting the drug and peptide moieties, is described. Paclitaxel-2′-pAntp[43-58]-NH2 3b and paclitaxel-2′-pAntp[52-58]-NH2 3c showed excellent antitumour activity against human lung and breast cancer cell lines. These conjugates were highly soluble and stable with a half-life of >8 h under cell culture conditions. The drug-peptide conjugates may be therapeutically useful due to improved pharmaceutical properties.",

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AU - Wang, Shudong

AU - Zhelev, Nikolai Z.

AU - Duff, Susan

AU - Fischer, Peter M.

PY - 2006/5/15

Y1 - 2006/5/15

N2 - Synthesis of paclitaxel-penetratin (pAntp) constructs, in which the 2′- or 7-position of paclitaxel was used as the attachment site for linker connecting the drug and peptide moieties, is described. Paclitaxel-2′-pAntp[43-58]-NH2 3b and paclitaxel-2′-pAntp[52-58]-NH2 3c showed excellent antitumour activity against human lung and breast cancer cell lines. These conjugates were highly soluble and stable with a half-life of >8 h under cell culture conditions. The drug-peptide conjugates may be therapeutically useful due to improved pharmaceutical properties.

AB - Synthesis of paclitaxel-penetratin (pAntp) constructs, in which the 2′- or 7-position of paclitaxel was used as the attachment site for linker connecting the drug and peptide moieties, is described. Paclitaxel-2′-pAntp[43-58]-NH2 3b and paclitaxel-2′-pAntp[52-58]-NH2 3c showed excellent antitumour activity against human lung and breast cancer cell lines. These conjugates were highly soluble and stable with a half-life of >8 h under cell culture conditions. The drug-peptide conjugates may be therapeutically useful due to improved pharmaceutical properties.

KW - Antitumour activity

KW - Cell delivery vector

KW - Drug-peptide conjugate

KW - Paclitaxel

KW - Penetratin

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M3 - Article

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AN - SCOPUS:33645868648

SN - 0960-894X

VL - 16

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EP - 2631

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 10

ER -

Synthesis and biological activity of conjugates between paclitaxel and the cell delivery vector penetratin

Abstract

Keywords

ASJC Scopus subject areas

UN SDGs

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