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In vivo and in vitro characterization of CCK8 bearing a histidine-based chelator labeled with Tc-99m-tricarbonyl (183 visite)

D'Andrea LD, Testa I, Panico M, Di Stasi R, Carac C, Tarallo L, Arra C, Barbieri A, Romanelli A, Aloj L

Biopolymers (ISSN: 0006-3525, 0006-6352, 0006-3525print), 2008; 90(5): 707-712.

Tipo di articolo: Journal Article, , Impact factor: 2.823, Impact factor a 5 anni: 2.631, Url: http://www.scopus.com/inward/record.url?eid=2-s2.0-58149179423&partnerID=40&md5=32c83bc7fb4e7699c311f2da5654da08

Parole chiave: Carbonyl, Cholecystokinin Receptors, Imaging, Organometallic Complexes, Radiopeptide, Technetium, Amines, Amino Acids, Animals, Binding Energy, Carbonylation, Nuclear Medicine, Oncology, Tumors, Chelating Agent, Cholecystokinin Octapeptide, Drug Derivative, Histidine, Peptide Fragment, Radiopharmaceutical Agent, Technetium Complex, Tricarbonylhistidinetechnetium(0), Unclassified Drug, Article, Cancer Transplantation, Chemistry, Comparative Study, Drug Design, Human, Isotope Labeling, Metabolism, Mouse, Nude Mouse, Synthesis, Tumor Cell Line, Xenograft, Neoplasm Transplantation, Organotechnetium Compounds, Heterologous, Tricarbonylhistidinetechnetium (0),

Affiliazioni: *** IBB - CNR ***
Istituto di Biostrutture e Bioimmagini, CNR, 80134 Napoli, Italy
Area Funzionale di Medicina Nucleare, Istituto Nazionale Tumori, Fondazione G. Pascale, Via M. Semmola, 80131 Napoli, Italy
UOS Sperimentazione Animale, Istituto Nazionale Tumori, Fondazione G. Pascale, 80131 Napoli, Italy
Dipartimento delle Scienze Biologiche, Università di Napoli Federico II, 80134 Napoli, Italy


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The development of receptor targeting radiolabeled ligands has gained much interest in recent years for diagnostic and therapeutic applications in nuclear medicine. Cholecystokinin (CCK) receptors have been shown to be overexpressed in a subset of neuroendocrine and other tumors. We are evaluating binding and biodistribution properties of a CCK8 peptide derivative labeled with Tc-99m(I)-tricarbonyl. The CCK8 peptide was modified at its N-terminus by adding to its N-terminus two lysine-histidine modules (KH), where histidine is coupled to the side chain of the lysine ((KH)(2)-CCK8). Tc-99m(I)-tricarbonyl was generated with the IsoLink (TM) kit. A431 cells stably transfected with a cDNA encoding for the human CCK2 receptor were utilized to determine binding affinity, internalization, and retention of the labeled peptide, in comparison with wild-type A431 cells. A nude mouse tumor model was obtained by generating A431-CCK2R and A431-control tumors in opposite flanks of the animals. High specific activity labeling with 99(m)Tc was achieved. In A431-CCK2R cells, specific saturable binding was observed as well as evident internalization of the radiolabeled peptide after binding. Biodistribution experiments showed rapid, specific localization of (KH)(2)-CCK8 on A431-CCK2R xenografts compared with control tun-tors, although absolute uptake values were not markedly higher compared with background activity. Clearance of unbound radioactivity was both urinary and hepatobiliary. In imaging experiments, while targeting to CCK2R positive tumors could be appreciated, there was poor contrast between target and nontarget areas. (KH)2-CCK8 shows adequate in vitro and in vivo properties for CCK2R targeting although improvement of biodistribution warrant further development. (C) 2008 Wiley Periodicals, Inc.
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Solid state and solution conformation of 6-{4-[N-tert-butoxycarbonyl-N- (N'-ethyl)propanamide]imidazolyl}-6-deoxycyclomaltoheptaose: Evidence of self-inclusion of the Boc group within the β-cyclodextrin cavity (101 visite)
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Cuocolo A, Acampa W, Nicolai E, Pace L, Petretta M, Salvatore M
Quantitative thallium-201 and technetium-99m sestamibi tomography at rest in detection of myocardial viability in patients with chronic ischemic left ventricular dysfunction (102 visite)
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Cuocolo A, Spinelli L, Petretta M, Nicolai E, Acampa W, Vicario L, Bonaduce D
Technetium-99m sestamibi cardiac tomography and low-dose dobutamine echocardiography in the prediction of recovery of left ventricular dysfunction after acute myocardial infarction (76 visite)
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Acampa W, Cuocolo A, Spinelli L, Petretta M, Nicolai E, Bonaduce D, Salvatore M
Prediction of recovery of left ventricular dysfunction after acute myocardial infarction: Comparison technetium-99m sestamibi tomography and low-dose dobutamine echocardiography (72 visite)
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Pace L, Catalano L, Pinto A, De Renzo A, Di Gennaro F, Califano C, Del Vecchio S, Rotoli B, Salvatore M
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Acampa W, Cuocolo A, Sullo P, Varrone A, Nicolai E, Pace L, Petretta M, Salvatore M
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Cuocolo A, Acampa W, Varrone A, Sullo P, Nicolai E, Pace L, Salvatore M
Direct comparison of technetium-99m labeled sestamibi and tetrofosmin cardiac tomography in patients with coronary artery disease (72 visite)
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Soricelli A, Cuocolo A, Varrone A, Discepolo A, Tedeschi E, Mainenti PP, Grivet-Fojaja MR, Covelli EM, Postiglione A, Salvatore M
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Ciarmiello A, Del Vecchio S, Silvestro P, Potena MI, Carriero MV, Thomas R, Botti G, D'Aiuto G, Salvatore M
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Del Vecchio S, Ciarmiello A, Pace L, Potena MI, Carriero MV, Mainolfi C, Thomas R, D'Aiuto G, Tsuruo T, Salvatore M
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Cuocolo A, Sullo P, Pace L, Nappi A, Gisonni P, Nicolai E, Trimarco B, Salvatore M
Adenosine coronary vasodilation in coronary artery disease: Technetium- 99m tetrofosmin myocardial tomography versus echocardiography (97 visite)
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Impact Factor: 3.491
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Vecchio SD, Ciarmiello A, Potena MI, Carriero MV, Mainolfi C, Botti G, Thomas R, Cerra M, D'Aiuto G, Tsuruo T, Salvatore M
In vivo detection of multidrug-resistant (MDR1) phenotype by technetium-99m sestamibi scan in untreated breast cancer patients (96 visite)
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Impact Factor: 5.036
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Marcassa C, Galli M, Cuocolo A, Scappellato F, Maurea S, Salvatore M
Rest-redistribution thallium-201 and rest technetium-99m-sestamibi SPECT in patients with stable coronary artery disease and ventricular dysfunction (91 visite)
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Impact Factor: 3.491
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Lastoria S, Muto P, Acampa W, Caraco C, Vergara E, Varrella P, Pezzullo L, Ionna F, Mozzillo N, ListerJames J, Salvatore M
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Impact Factor: 3.491
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Di Blasio B, Galdiero S, Saviano M, De Simone G, Benedetti E, Pedone C, Gibbons WA, Deschenaux R, Rizzarelli E, Vecchio G
Functionalized cyclodextrins: Synthesis and structural characterization of 6-deoxy-6-{4-[N-tert-butoxycarbonyl-2-aminoethyl]-imidazolyl}-cyclomaltoheptaose (109 visite)
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Impact Factor: 3.19
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Maurea S, Cuocolo A, Soricelli A, Castelli L, Nappi A, Trimarco B, Salvatore M
Technetium-99m MIBI SPECT to identify viable myocardium in patients with chronic coronary artery disease and left ventricular dysfunction (102 visite)
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Impact Factor: 0.967
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Klain M, Maurea S, Cuocolo A, Colao A, Marzano L, Lombardi G, Salvatore M
Technetium-99m tetrofosmin imaging in thyroid diseases: Comparison with Tc-99m-pertechnetate, thallium-201 and Tc-99m-methioxyisobutylisonitrile scans (96 visite)
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Impact Factor: 2.692
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Klain M, Maurea S, Lastoria S, Cuocolo A, Colao A, Salvatore M
Technetium-99m-tetrofosmin imaging of differentiated mixed thyroid cancer (88 visite)
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Impact Factor: 3.491
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Lastoria S, Vergara E, Varrella P, Muto P, Acampa W, Caracò C, Salvatore M
[Imaging of thromboembolism by scintigraphy with the 99m-technetium-labelled synthetic peptide P280] (115 visite)
Radiol Med (ISSN: 0033-8362, 1826-6983, 1826-6983electronic), 1995 Dec; 90(6): 812-819.
Impact Factor: 0.967
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Maurea S, Cuocolo A, Soricelli A, Castelli L, Nappi A, Squame F, Imbriaco M, Trimarco B, Salvatore M
ENHANCED DETECTION OF VIABLE MYOCARDIUM BY TECHNETIUM-99M-MIBI IMAGING AFTER NITRATE ADMINISTRATION IN CHRONIC CORONARY-ARTERY DISEASE (104 visite)
J Nucl Med (ISSN: 0161-5505, 1535-5667, 1535-5667electronic), 1995 Nov; 36(11): 1945-1952.
Impact Factor: 3.491
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Maurea S, Cuocolo A, Soricelli A, Castelli L, Squame F, Imbriaco M, De Luca N, Trimarco B, Salvatore M
MYOCARDIAL VIABILITY INDEX IN CHRONIC CORONARY-ARTERY DISEASE - TECHNETIUM-99M-METHOXY ISOBUTYL ISONITRILE REDISTRIBUTION (90 visite)
J Nucl Med (ISSN: 0161-5505, 1535-5667, 1535-5667electronic), 1995 Nov; 36(11): 1953-1960.
Impact Factor: 3.491
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Nicolai E, Cuocolo A, Pace L, Maurea S, Nappi A, Imbriaco M, Morisco C, Argenziano L, Salvatore M
Assessment of systolic wall thickening using technetium-99m methoxyisobutylisonitrile in patients with coronary artery disease: relation to thallium-201 scintigraphy with re-injection (127 visite)
Eur J Nucl Med (ISSN: 0340-6997, 1619-7070, 1619-7089), 1995 Sep; 22(9): 1017-1022.
Impact Factor: 2.692
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CUOCOLO A, SORICELLI A, NICOLAI E, SQUAME F, NAPPI A, SULLO P, KLAIN M, CARDEI S, SALVATORE M
Technetium-99m-tetrofosmin regional myocardial uptake at rest: Relation to severity of coronary artery stenosis in previous myocardial infarction (98 visite)
J Nucl Med (ISSN: 0161-5505, 1535-5667, 1535-5667electronic), 1995 Jun; 36(6): 907-913.
Impact Factor: 3.491
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Cuocolo A, Soricelli A, Pace L, Nicolai E, Castelli L, Nappi A, Imbriaco M, Morisco C, Ell PJ, Salvatore M
ADENOSINE TECHNETIUM-99M-METHOXY ISOBUTYL ISONITRILE MYOCARDIAL TOMOGRAPHY IN PATIENTS WITH CORONARY-ARTERY DISEASE - COMPARISON WITH EXERCISE (84 visite)
J Nucl Med (ISSN: 0161-5505, 1535-5667, 1535-5667electronic), 1994 Jul; 35(7): 1110-1115.
Impact Factor: 3.491
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Nicolai E, Cuocolo A, Pace L, Maurea S, Nappi A, Imbriaco M, Cardei S, Morisco C, Argenziano L, Salvatore M
Evaluation Of Systolic Parietal Thickening Of The Left Ventricle Using Technetium-99m Methoxy Isobutyl Isonitrile. Relationship With Coronary Anatomy (76 visite)
Radiol Med, 1994 Jul; 88(1-2): 100-106.
Impact Factor: 0
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Maurea S, Cuocolo A, Nicolai E, Salvatore M
Improved detection of viable myocardium with thallium-201 reinjection in chronic coronary artery disease: comparison with technetium-99m-MIBI imaging (98 visite)
J Nucl Med (ISSN: 0161-5505, 1535-5667, 1535-5667electronic), 1994 Apr; 35(4): 621-624.
Impact Factor: 3.491
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Maurea S, Cuocolo A, Pace L, Nicolai E, Nappi A, Imbriaco M, Trimarco B, Salvatore M
Left ventricular dysfunction in coronary artery disease: Comparison between rest-redistribution thallium 201 and resting technetium 99m methoxyisobutyl isonitrile cardiac imaging (111 visite)
J Nucl Cardiol (ISSN: 1071-3581, 1532-6551, 1532-6551electronic), 1994 Jan; 1(1): 65-71.
Impact Factor: 1.878
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Imbriaco M, Cuocolo A, Pace L, Nicolai E, Nappi A, Celentano L,  Palma G, Vosa C
Technetium-99m methoxy isobutyl isonitrile simultaneous evaluation of ventricular function and myocardial perfusion in patients with congenital heart disease (80 visite)
Clin Nucl Med (ISSN: 0363-9762, 1536-0229, 1536-0229electronic), 1994 Jan; 19(1): 28-32.
Impact Factor: 0.34
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Nicolai E, Cuocolo A, Pace L, Maurea S, Nappi A, Imbriaco M, Cardei S, Morisco C, Argenziano L, Salvatore M
Ventricular systolic wall thickening by Technetium-99m methoxy-isobutyl-isonitrile. Relationship with coronary anatomy (85 visite)
Radiol Med (ISSN: 0033-8362, 1826-6983, 1826-6983electronic), 1994; 88(1-2): 100-106.
Impact Factor: 0.967
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Cuocolo A, Maurea S, Pace L, Nicolai E, Nappi A, Imbriaco M, Trimarco B, Salvatore M
Resting technetium-99m methoxyisobutylisonitrile cardiac imaging in chronic coronary artery disease: comparison with rest-redistribution thallium-201 scintigraphy (103 visite)
Eur J Nucl Med (ISSN: 0340-6997, 1619-7070, 1619-7089), 1993 Dec; 20(12): 1186-1192.
Impact Factor: 2.692
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Maurea S, Cuocolo A, Pace L, Nicolai E, Nappi A, Imbriaco M, Morisco C, Chiariello M, Trimarco B, Salvatore M
Rest-injected thallium-201 redistribution and resting technetium-99m methoxyisobutylisonitrile uptake in coronary artery disease: relation to the severity of coronary artery stenosis (94 visite)
Eur J Nucl Med (ISSN: 0340-6997, 1619-7070, 1619-7089), 1993 Jun; 20(6): 502-510.
Impact Factor: 2.692
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Pace L, Cuocolo A, Nappi A, Nicolai E, Imbriaco M, Mangoni di Santo Stefano ML, Salvatore M
Myocardial scintigraphy with technetium 99m methoxyisobutylisonitrile. A comparison with coronary arteriography in patients with suspected ischemic cardiopathy (87 visite)
Radiol Med (ISSN: 1826-6983, 0033-8362, 1826-6983electronic), 1992; 83(1-2): 97-100.
Impact Factor: 0.967
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Capasso S, Mazzarella L, Sica F, Zagari A
Solid-state conformations of aminosuccinyl peptides: crystal structure of tert-butyloxycarbonyl-L-leucyl-L-aminosuccinyl-L-phenylalaninami de (109 visite)
Biopolymers (ISSN: 0006-3525, 0006-6352, 0006-3525print), 1989; 28(1): 139-147.
Impact Factor: 2.425
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Capasso S, Mazzarella L, Sica F, Zagari A
Type II' beta-bend conformation of tert. -butyloxycarbonyl-L-amino-succinyl-L-alanyl-glycine methyl ester in the solid state (98 visite)
Int J Pept Protein Res (ISSN: 0367-8377, 0367-8377print), 1984; 24(6): 588-596.
Impact Factor: 1.255
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48 Records (41 escludendo Abstract e Conferenze).
Impact factor totale: 130.396 (110.011 escludendo Abstract e Conferenze).
Impact factor a 5 anni totale: 181.711 (149.993 escludendo Abstract e Conferenze).







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