TY - JOUR
T1 - Targeting small-cell lung cancer with novel fluorescent analogs of somatostatin
AU - Kostenich, Genady
AU - Livnah, Nurit
AU - Bonasera, Thomas A.
AU - Yechezkel, Tamar
AU - Salitra, Yosef
AU - Litman, Pninit
AU - Kimel, Sol
AU - Orenstein, Arie
N1 - Funding Information:
This research was supported by the Israeli Ministry of Commerce and Industry, through the Izmel Consortium. S. Gazal and G. Gellerman developed and synthesized the S-building units (DeveloGen Israel, Ltd.). S. Salomon provided technical assistance (Sheba).
PY - 2005/12
Y1 - 2005/12
N2 - Early, accurate detection of small-cell lung cancer (SCLC), before it becomes systemic, is essential for successful treatment. Fluorescence-based imaging provides safe, sensitive detection of malignancies. Targeted delivery of fluorophores increases sensitivity of endoscopic imaging. We synthesized novel somatostatin analogs, based on backbone cyclic peptides, and conjugated them with fluorescent agents. Nineteen conjugates differing in core peptide, length of alkyl linker and fluorescence moiety (rhodamine and fluorescein) were tested in vitro, using a receptor binding assay, and nine of the more promising conjugates were tested in vivo by fiber-optic spectrofluorimetry and quantitative spectral imaging, on an H69 human SCLC tumor mouse xenograft model. The lead compound showed exceptional tumor/normal tissue ratios, ranging from 9 to 90, and has potential for targeting SCLC overexpressing somatostatin receptors.
AB - Early, accurate detection of small-cell lung cancer (SCLC), before it becomes systemic, is essential for successful treatment. Fluorescence-based imaging provides safe, sensitive detection of malignancies. Targeted delivery of fluorophores increases sensitivity of endoscopic imaging. We synthesized novel somatostatin analogs, based on backbone cyclic peptides, and conjugated them with fluorescent agents. Nineteen conjugates differing in core peptide, length of alkyl linker and fluorescence moiety (rhodamine and fluorescein) were tested in vitro, using a receptor binding assay, and nine of the more promising conjugates were tested in vivo by fiber-optic spectrofluorimetry and quantitative spectral imaging, on an H69 human SCLC tumor mouse xenograft model. The lead compound showed exceptional tumor/normal tissue ratios, ranging from 9 to 90, and has potential for targeting SCLC overexpressing somatostatin receptors.
KW - Fluorescence imaging
KW - Somatostatin conjugates
KW - Tumor targeting
UR - http://www.scopus.com/inward/record.url?scp=33344456606&partnerID=8YFLogxK
U2 - 10.1016/j.lungcan.2005.07.009
DO - 10.1016/j.lungcan.2005.07.009
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C2 - 16159681
AN - SCOPUS:33344456606
SN - 0169-5002
VL - 50
SP - 319
EP - 328
JO - Lung Cancer
JF - Lung Cancer
IS - 3
ER -
