Synthesis and characterization of multiply-tyrosinated, multiply-iodinated somatostatin analogs.
Radio-labeled somatostatin analogs have recently gained popularity as agents useful in intraoperative tumor localization, external scintigraphy and in situ radiotherapy. We have synthesized and characterized a series of novel N-terminally extended multiply-tyrosinated somatostatin analogs that possess high binding affinity for somatostatin receptors, exhibit biological activity comparable to the native peptide and retain these characteristics after iodination. These analogs can be radio-iodinated to high specific activities. Following radioiodination, these analogs exhibit minimal radiolysis and may be clinically useful for tumor localization, scanning and therapy.
Woltering
E A
EA
Louisiana State University University Medical Center, Department of Surgery, Stanley S. Scott Cancer Center, New Orleans 70012-2822, USA. ewolte@lsumc.du
O'Dorisio
M S
MS
Murphy
W A
WA
Chen
F
F
Drouant
G J
GJ
Espenan
G D
GD
Fisher
D R
DR
Sharma
C
C
Diaco
D S
DS
Maloney
T M
TM
Fuselier
J A
JA
Nelson
J A
JA
O'Dorisio
T M
TM
Coy
D H
DH
D002282:Adenocarcinoma, Bronchiolo-Alveolar / Q000175:diagnosis / Q000473:pathology; D000067956:Adenylyl Cyclase Inhibitors; D000368:Aged; D000595:Amino Acid Sequence; D001932:Brain Neoplasms / Q000175:diagnosis / Q000556:secondary; D003952:Diagnostic Imaging; D013006:Growth Hormone / Q000037:antagonists & inhibitors; D006801:Humans; D007455:Iodine / Q000737:chemistry; D008175:Lung Neoplasms / Q000175:diagnosis / Q000473:pathology; D008297:Male; D009447:Neuroblastoma / Q000188:drug therapy / Q000378:metabolism; D010455:Peptides / Q000378:metabolism* / Q000493:pharmacokinetics; D011877:Radionuclide Imaging / Q000379:methods; D013004:Somatostatin / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology*; D014018:Tissue Distribution; D014407:Tumor Cells, Cultured; D014443:Tyrosine / Q000737:chemistry
D000067956:Adenylyl Cyclase Inhibitors; D010455:Peptides; D014443:Tyrosine; D013004:Somatostatin; D013006:Growth Hormone; D007455:Iodine