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Selective targeting of 2'-deoxy-5-fluorouridine to urokinase positive malignant cells in vitro.

Abstract：

:A urokinase targeting conjugate of 2'-deoxy-5-fluorouridine (5-FUdr) was synthesized and tested for tumor-cell selective cytotoxicity in vitro. The 5-FUdr prodrug 2'-deoxy-5-fluoro-3'-O-(3-carboxypropanoyl)uridine (5-FUdrsuccOH) containing an ester-labile succinate linker was attached to the specific urokinase inhibitor plasminogen activator inhibitor type II (PAI-2) and was found to preferentially kill urokinase-over expressing cancer cells. Up to 7 molecules of 5-FUdr were incorporated per PAI-2 molecule without affecting protein activity. This is the first time a small organic cytotoxin has been conjugated to PAI-2.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Vine KL,Locke JM,Bremner JB,Pyne SG,Ranson M

doi

10.1016/j.bmcl.2010.03.029

subject

Has Abstract

pub_date

2010-05-01 00:00:00

pages

2908-11

issue

9

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(10)00350-1

journal_volume

20

pub_type

杂志文章

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