An image contrast agent selectively activated by prostate specific antigen

被引：15

作者：

Jones, GB ^{[1
]}

Crasto, CF

Mathews, JE

Xie, LF

Mitchell, MO

El-Shafey, A

D'Amico, AV

Bubley, GJ

机构：

[1] Northeastern Univ, Bioorgan & Med Chem Labs, Dept Chem & Chem Biol, Boston, MA 02115 USA

[2] Harvard Univ, Sch Med, Dana Farber Canc Inst, Boston, MA 02215 USA

[3] Harvard Univ, Sch Med, Brigham & Womens Hosp, Boston, MA 02215 USA

[4] Harvard Univ, Sch Med, Beth Israel Deaconess Med Ctr, Boston, MA 02215 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2006年 / 14卷 / 02期

关键词：

enzyme substrates; PSA; linker; imaging agents; chemical synthesis; prodrugs; coumarin; hexapeptides;

D O I：

10.1016/j.bmc.2005.08.015

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

A family of image contrast agent conjugates designed to undergo enzymatic activation has been synthesized. The agents underwent activation both with enzymatically active prostate specific antigen (PSA) and a-chymotrypsin, releasing free fluorophore via cleavage of a three-component system. A hexapeptide derivative showed exclusive activation by PSA and constitutes a method for tracking PSA activity in vitro. (c) 2005 Elsevier Ltd. All rights reserved.

引用

页码：418 / 425

页数：8

共 16 条

[1] CONTROL OF PROSTATE-CANCER WITH RADIOTHERAPY - LONG-TERM RESULTS [J].

BAGSHAW, MA ;

COX, RS ;

HANCOCK, SL .

JOURNAL OF UROLOGY, 1994, 152 (05) :1781-1785

[2] GLEASON GRADING OF PROSTATIC NEEDLE BIOPSIES - CORRELATION WITH GRADE IN 316 MATCHED PROSTATECTOMIES [J].

BOSTWICK, DG .

AMERICAN JOURNAL OF SURGICAL PATHOLOGY, 1994, 18 (08) :796-803

[3] A NOVEL CONNECTOR LINKAGE APPLICABLE IN PRODRUG DESIGN [J].

CARL, PL ;

CHAKRAVARTY, PK ;

KATZENELLENBOGEN, JA .

JOURNAL OF MEDICINAL CHEMISTRY, 1981, 24 (05) :479-480

[4]

D'Amico AV, 1999, PROSTATE, V41, P208, DOI 10.1002/(SICI)1097-0045(19991101)41:3<208::AID-PROS9>3.0.CO

[5]

2-B

[6] Elongated multiple electronic cascade and cyclization spacer systems in activatible anticancer prodrugs for enhanced drug release [J].

de Groot, FMH ;

Loos, WJ ;

Koekkoek, R ;

van Berkom, LWA ;

Busscher, GF ;

Seelen, AE ;

Albrecht, C ;

de Bruijn, P ;

Scheeren, HW .

JOURNAL OF ORGANIC CHEMISTRY, 2001, 66 (26) :8815-8830

[7]

Denmeade SR, 1998, CANCER RES, V58, P2537

[8] Towards enzyme activated antiprostatic agents [J].

Jones, GB ;

Mitchell, MO ;

Weinberg, JS ;

D'Amico, AV ;

Bubley, GJ .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2000, 10 (17) :1987-1989

[9]

LILJA H, 1989, J BIOL CHEM, V264, P1894

[10] CYANINE DYE LABELING REAGENTS - SULFOINDOCYANINE SUCCINIMIDYL ESTERS [J].

MUJUMDAR, RB ;

ERNST, LA ;

MUJUMDAR, SR ;

LEWIS, CJ ;

WAGGONER, AS .

BIOCONJUGATE CHEMISTRY, 1993, 4 (02) :105-111

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