title: Synthesis and characterization of multiply-tyrosinated, multiply-iodinated somatostatin analogs.
abstract: 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.
authors: Louisiana State University University Medical Center, Department of Surgery, Stanley S. Scott Cancer Center, New Orleans 70012-2822, USA. ewolte@lsumc.du
authors: E A
authors: EA
authors: Woltering
authors: M S
authors: MS
authors: O'Dorisio
authors: W A
authors: WA
authors: Murphy
authors: F
authors: F
authors: Chen
authors: G J
authors: GJ
authors: Drouant
authors: G D
authors: GD
authors: Espenan
authors: D R
authors: DR
authors: Fisher
authors: C
authors: C
authors: Sharma
authors: D S
authors: DS
authors: Diaco
authors: T M
authors: TM
authors: Maloney
authors: J A
authors: JA
authors: Fuselier
authors: J A
authors: JA
authors: Nelson
authors: T M
authors: TM
authors: O'Dorisio
authors: D H
authors: DH
authors: Coy
mesh_terms: 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
chemical_list: D000067956:Adenylyl Cyclase Inhibitors; D010455:Peptides; D014443:Tyrosine; D013004:Somatostatin; D013006:Growth Hormone; D007455:Iodine