This study is to investigate the binding capability of lidamycin apoprotein (LDP), an enediyne- associated apoprotein of the chromoprotein antitumor antibiotic family, to human breast cancer and normal   tissues, the correlation of LDP binding capability to human breast cancer tissues and the expression of tumor therapeutic targets such as VEGF and HER2.  In this study, the binding capability of LDP to human breast  cancer tissues was detected with tissue microarray.  The correlation study of LDP binding capability to human breast tumor tissues and relevant therapeutic targets was performed on breast cancer tissue microarrays.      Immunocytochemical examination was used to detect the binding capability of LDP to human breast carcinoma MCF-7 cells.  As a result, tissue microarray showed that LDP staining of 73.2% (30/41) of breast cancer tissues was positive, whereas that of 48.3% (15/31) of the adjacent normal breast specimens was positive.  The     difference between the tumor and normal samples was significant (χ² = 4.63, P < 0.05).  LDP immunoreactivity in breast cancer correlated significantly with the overexpression of VEGF and HER2 (P < 0.001 and < 0.01,    r = 0.389 and 0.287, respectively).  Determined with confocal immunofluorescent analysis, LDP showed the binding capability to mammary carcinoma MCF-7 cells.  It is demonstrated that LDP can bind to human breast cancer tissues and there is significant difference between the breast cancer tissues and the corresponding normal tissues.  Notably, the binding reactivity shows positive correlation with the expression of VEGF and HER2   in breast carcinoma tissues.  The results imply that LDP may have a potential use as targeting drug carrier in  the research and developmont of new anticancer therapeutics.  This study may provide reference for drug  combination of LDM and other therapeutic agents.