TOWARDS TUMOR TARGETING WITH COPPER-RADIOLABELED MACROCYCLE ANTIBODY CONJUGATES - SYNTHESIS, ANTIBODY LINKAGE, AND COMPLEXATION BEHAVIOR

被引：49

作者：

MORPHY, JR

PARKER, D

KATAKY, R

EATON, MAW

MILLICAN, AT

ALEXANDER, R

HARRISON, A

WALKER, C

机构：

[1] UNIV DURHAM,DEPT CHEM,S RD,DURHAM DH1 3LE,ENGLAND

[2] CELLTECH LTD,SLOUGH SL1 4EN,ENGLAND

[3] MRC,RADIOBIOL UNIT,DIDCOT OX11 0RD,OXON,ENGLAND

来源：

JOURNAL OF THE CHEMICAL SOCIETY-PERKIN TRANSACTIONS 2 | 1990年 / 04期

关键词：

D O I：

10.1039/p29900000573

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

A set of four tetra-azamacrocyclic ligands bearing aminomethylphenyl substituents have been prepared and may be attached to a monoclonal antibody via an intermediate thiol-specific vinyl-pyridine linker molecule. The resultant conjugates may be efficiently radiolabelled with 64Cu or 67Cu at pH 4 to minimise non-specific protein binding, and the copper labelled antibody-conjugate is stable with respect to copper loss in vivo. The forward rate of copper binding has been optimised through a kinetic analysis using stopped-flow spectrophotometry. In succinate buffer, anionic copper species Cu(succ)22- (log β = 4.35) and HCu(succ) 2- (log β = 9.64) are the kinetically significant copper species in the pH range 3.6-5.6.

引用

页码：573 / 585

页数：13

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