Synthesis and Characterization of a Selective Alpha(v)Beta(3) Receptor Cyclic Peptide Antagonist Functionalized with a Chelating Group for Metal Labelling
Synthesis and Characterization of a Selective Alpha(v)Beta(3) Receptor Cyclic Peptide Antagonist Functionalized with a Chelating Group for Metal Labelling(378 views) Monfregola L, Saviano M, De Luca S
Int J Pept Res Ther (ISSN: 1573-3149, 0929-5666), 2010 Mar; 16(1): 1-5.
Keywords: αvβ 3 Receptor, Selective Radioactive Probe, Solid Phase Synthesis, Diagnostic Agent, Indium Arginylglycylaspartic Acid Pentetic Acid Conjugate In 111, Lysine, Metal, Unclassified Drug, Vitronectin Receptor, Animal Experiment, Animal Tissue, Cell Adhesion, Conjugation, Controlled Study, Covalent Bond, Drug Structure, Drug Synthesis, In Vitro Study, In Vivo Study, Isotope Labeling, Isotope Tracing, Molecular Model, Mouse, Nonhuman, Protein Analysis, Protein Interaction, Protein Synthesis, Purification, V 3 Receptor,
Affiliations: *** IBB - CNR ***
Istituto di Biostrutture e Bioimmagini IBB, CNR, Naples 80134, Italy
References: Albelda, S.M., Mette, S.A., Elder, D.E., Integrin distribution in malignant melanoma: Association of the β3 subunit with tumor progression (1990) Cancer Res, 50, pp. 6757-676
Benneth, J.S., Structure and function of the platelet integrin α iIbβ3 (2005) J Clin Invest, 115, pp. 3363-3369
Del Gatto, A., Zaccaro, L., Grieco, P., Novel and selective α(v)β3 receptor peptide antagonist: Design, synthesis, and biological behavior (2006) J Med Chem, 49, pp. 3416-3420
Gasparini, G., Brooks, P.C., Bingazoli, E., Vascular integrin α(v)β3: A new prognostic indicator in breast cancer (1998) Clin Cancer Res, 4, pp. 2625-2634
Heppeler, A., Froidevaux, S., Eberle, A.N., Maecke, H.R., Receptor targeting for tumor localisation and therapy with radiopeptides (2000) Curr Med Chem, 7, pp. 971-994
Kaiser, E., Colescott, R.L., Bossinger, C.D., Cook, P.I., Colour test for detection of free terminal amino groups in the solid-phase synthesis of peptides (1970) Anal Biochem, 34, pp. 595-598
Liapis, H., Adler, L.M., Wick, M.R., Rader, J.S., Expression of integrin α(v)β3 integrin is less frequent in ovarian epithelial tumors of low malignant potential in contrast to avarian carcinomas (1997) Hum Pathol, 28, pp. 443-449
Schnell, O., Krebs, B., Wagner, E., Expression of integrin αvβ3 in gliomas correlates with tumor grade and is not restricted to tumor vasculature (2008) Brain Pathol, 18, pp. 378-386
Sheppard, R.C., Williams, B.J., Acid-Labile resin linkage agents for use in solid-phase peptide-synthesis (1982) Int J Pept Protein Res, 20, pp. 451-454
Zannetti, A., Del Vecchio, S., Iommelli, F., Imaging of αvβ3 expression by a bifunctional chimeric RGD peptide not cross-reacting with α vβ5 (2009) Clin Cancer Res, 15, pp. 5224-5233
Albelda, S. M., Mette, S. A., Elder, D. E., Integrin distribution in malignant melanoma: Association of the 3 subunit with tumor progression (1990) Cancer Res, 50, pp. 6757-676
Benneth, J. S., Structure and function of the platelet integrin iIb 3 (2005) J Clin Invest, 115, pp. 3363-3369
Sheppard, R. C., Williams, B. J., Acid-Labile resin linkage agents for use in solid-phase peptide-synthesis (1982) Int J Pept Protein Res, 20, pp. 451-454
Synthesis and Characterization of a Selective Alpha(v)Beta(3) Receptor Cyclic Peptide Antagonist Functionalized with a Chelating Group for Metal Labelling
Small radiolabelled compounds such as peptides are very attractive tools for the diagnosis of several different pathologies (Heppeler in Curr Med Chem 7:971-994, 2000). Among the possible biological targets for radiolabelled compounds, the alpha(v)beta(3) (alpha(v)beta(3)) integrin cell adhesion receptor has been extensively studied. It is expressed on proliferating but not quiescent endothelial cells and has been shown to be involved in tumour progression, angiogenesis and metastasis. The novel radioactive probe (111)In-DTPA-RGDechi has been successfully employed for selective alpha(v)beta(3) single-photon imaging studies. Herein we report the efficient synthetic protocol developed in order to obtain the conjugate diethylentriaminopentacetic acid (DTPA)-RGDechi in good yield and high purity.
Synthesis and Characterization of a Selective Alpha(v)Beta(3) Receptor Cyclic Peptide Antagonist Functionalized with a Chelating Group for Metal Labelling
Synthesis and Characterization of a Selective Alpha(v)Beta(3) Receptor Cyclic Peptide Antagonist Functionalized with a Chelating Group for Metal Labelling
Vitiello M, Finamore E, Falanga A, Raieta K, Cantisani M, Galdiero F, Pedone C, Galdiero M, Galdiero S * Fusion in Coq(479 views) Lecture Notes In Computer Science (ISSN: 0302-9743, 0302-974335404636319783540463634, 0302-974335402975459783540297543), 2001; 2178LNCS: 583-596. Impact Factor:0.415 ViewExport to BibTeXExport to EndNote