Potential 18F-labeled biomarkers for epidermal growth factor receptor tyrosine kinase

被引：92

作者：

Bonasera, TA

Ortu, G

Rozen, Y

Krais, R

Freedman, NMT

Chisin, R

Gazit, A

Levitzki, A

Mishani, E ^{[1
]}

机构：

[1] Hebrew Univ Jerusalem, Hadassah Univ Hosp Campus, Dept Med Biophys & Nucl Med, IL-91120 Jerusalem, Israel

[2] Hebrew Univ Jerusalem, Inst Life Sci, Dept Biol Chem, IL-91904 Jerusalem, Israel

[3] Hebrew Univ Jerusalem, Dept Organ Chem, Inst Chem, IL-91904 Jerusalem, Israel

来源：

NUCLEAR MEDICINE AND BIOLOGY | 2001年 / 28卷 / 04期

基金：

美国国家科学基金会;

关键词：

EGFr; tyrosine kinase; quinazoline; biodistribution; fluorine-18; PET;

D O I：

10.1016/S0969-8051(01)00200-1

中图分类号：

R8 [特种医学]; R445 [影像诊断学];

学科分类号：

1002 ; 100207 ; 1009 ;

摘要：

As PET candidate tracers for EGFr-TK, five 4-(anilino)quinazoline derivatives, each fluorinated in the aniline moiety, were prepared. Each was tested in vitro for inhibition of EGFr autophosphorylation in A431 cell line. The leading compounds were then radiolabeled with F-18 and cell binding experiments, biodistribution and PET studies in A431 tumor-bearing mice were performed. Metabolic studies were carried out in a mice control group. From our results, we concluded that while in vitro experiments indicates efficacy of 4-(anilino)quinazoline compounds, kinetic factors and rapid blood clearance make them unsuitable as tracers for nuclear medicine imaging of EGFr-TK. (C) 2001 Elsevier Science Inc. All rights reserved.

引用

收藏

页码：359 / 374

页数：16

相关论文

共 26 条

[1] RECOVERY OF CELL SUBPOPULATIONS FROM HUMAN-TUMOR XENOGRAFTS FOLLOWING DISSOCIATION WITH DIFFERENT ENZYMES [J].

ALLALUNISTURNER, MJ ;

SIEMANN, DW .

BRITISH JOURNAL OF CANCER, 1986, 54 (04) :615-622

[2] Tyrosine kinase inhibitors .8. An unusually steep structure-activity relationship for analogues of 4-(3-bromoanilino)-6,7-dimethoxyquinazoline (PD 153035), a potent inhibitor of the epidermal growth factor receptor [J].

Bridges, AJ ;

Zhou, H ;

Cody, DR ;

Rewcastle, GW ;

McMichael, A ;

Showalter, HDH ;

Fry, DW ;

Kraker, AJ ;

Denny, WA .

JOURNAL OF MEDICINAL CHEMISTRY, 1996, 39 (01) :267-276

[3] Radiolabeling of epidermal growth factor with Tc-99m and in vivo localization following intracerebral injection into normal and glioma-bearing rats [J].

Capala, J ;

Barth, RF ;

Bailey, MQ ;

Fenstermaker, RA ;

Marek, MJ ;

Rhodes, BA .

BIOCONJUGATE CHEMISTRY, 1997, 8 (03) :289-295

[4]

DAVIS JM, BASIC CELL CULTURE P

[5] PHASE-I AND IMAGING TRIAL OF INDIUM-111-LABELED ANTIEPIDERMAL GROWTH-FACTOR RECEPTOR MONOCLONAL-ANTIBODY 225 IN PATIENTS WITH SQUAMOUS-CELL LUNG-CARCINOMA [J].

DIVGI, CR ;

WELT, S ;

KRIS, M ;

REAL, FX ;

YEH, SDJ ;

GRALLA, R ;

MERCHANT, B ;

SCHWEIGHART, S ;

UNGER, M ;

LARSON, SM ;

MENDELSOHN, J .

JOURNAL OF THE NATIONAL CANCER INSTITUTE, 1991, 83 (02) :97-104

[6] Sensitivity of new radiopharmaceuticals [J].

Eckelman, WC .

NUCLEAR MEDICINE AND BIOLOGY, 1998, 25 (03) :169-173

[7] In vivo evaluation of the biodistribution of 11C-labeled PD153035 in rats without and with neuroblastoma implants [J].

Fredriksson, A ;

Johnström, P ;

Thorell, JO ;

von Heijne, G ;

Hassan, M ;

Eksborg, S ;

Kogner, P ;

Borgström, P ;

Ingvar, M ;

Stone-Elander, S .

LIFE SCIENCES, 1999, 65 (02) :165-174

[8] A SPECIFIC INHIBITOR OF THE EPIDERMAL GROWTH-FACTOR RECEPTOR TYROSINE KINASE [J].

FRY, DW ;

KRAKER, AJ ;

MCMICHAEL, A ;

AMBROSO, LA ;

NELSON, JM ;

LEOPOLD, WR ;

CONNERS, RW ;

BRIDGES, AJ .

SCIENCE, 1994, 265 (5175) :1093-1095

[9] Tyrphostins .4. Highly potent inhibitors of EGF receptor kinase. Structure-activity relationship study of 4-anilidoquinazolines [J].

Gazit, A ;

Chen, J ;

App, H ;

McMahon, G ;

Hirth, P ;

Chen, I ;

Levitzki, A .

BIOORGANIC & MEDICINAL CHEMISTRY, 1996, 4 (08) :1203-1207

[10] IMAGING OF HUMAN-TUMOR XENOGRAFTS WITH AN INDIUM-111-LABELED ANTI-EPIDERMAL GROWTH-FACTOR RECEPTOR MONOCLONAL-ANTIBODY [J].

GOLDENBERG, A ;

MASUI, H ;

DIVGI, C ;

KAMRATH, H ;

PENTLOW, K ;

MENDELSOHN, J .

JOURNAL OF THE NATIONAL CANCER INSTITUTE, 1989, 81 (21) :1616-1625