Fluorescently Labeled Risedronate and Related Analogues: "Magic Linker" Synthesis

被引：47

作者：

Kashemirov, Boris A. ^{[1
]}

Bala, Joy Lynn F. ^{[1
]}

Chen, Xiaolan ^{[1
]}

Ebetino, F. H. ^{[2
]}

Xia, Zhidao ^{[3
]}

Russell, R. Graham G. ^{[3
]}

Coxon, Fraser P. ^{[4
]}

Roelofs, Anke J. ^{[4
]}

Rogers, Michael J. ^{[4
]}

McKenna, Charles E. ^{[1
]}

机构：

[1] Univ So Calif, Dept Chem, Los Angeles, CA 90089 USA

[2] Procter & Gamble Pharmaceut, Mason, OH 45040 USA

[3] Univ Oxford, Nuffield Dept Orthoped Surg, Nuffield Orthoped Ctr, Oxford OX3 7LD, England

[4] Univ Aberdeen, Inst Med Sci, Bone & Musculoskeletal Res Programme, Aberdeen AB25 2ZD, Scotland

来源：

BIOCONJUGATE CHEMISTRY | 2008年 / 19卷 / 12期

关键词：

D O I：

10.1021/bc800369c

中图分类号：

Q5 [生物化学];

学科分类号：

071010 ; 081704 ;

摘要：

We report synthesis of the first fluorescently labeled conjugates of risedronate (1), using an epoxide linker strategy enabling conjugation of 1 via its pyridyl nitrogen with the label (carboxyfluorescein). Unlike prior approaches to create fluorescent bisphosphonate probes, the new linking chemistry did not abolish the ability to inhibit protein prenylation in vitro, while significantly retaining hydroxyapatite affinity. The utility of a fluorescent 1 conjugate in visualizing osteoclast resorption in vitro was demonstrated.

引用

页码：2308 / 2310

页数：3

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