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Theranostic approaches in nuclear oncology: From bench to bed.

Nock BA, Maina T.

J Labelled Comp Radiopharm. 2019 Aug;62(10):612-614. doi: 10.1002/jlcr.3787. No abstract available.


Instant kit preparation of 68Ga-radiopharmaceuticals via the hybrid chelator DATA: clinical translation of [68Ga]Ga-DATA-TOC.

Sinnes JP, Nagel J, Waldron BP, Maina T, Nock BA, Bergmann RK, Ullrich M, Pietzsch J, Bachmann M, Baum RP, Rösch F.

EJNMMI Res. 2019 May 23;9(1):48. doi: 10.1186/s13550-019-0516-7.


Trastuzumab cotreatment improves survival of mice with PC-3 prostate cancer xenografts treated with the GRPR antagonist 177 Lu-DOTAGA-PEG2 -RM26.

Mitran B, Rinne SS, Konijnenberg MW, Maina T, Nock BA, Altai M, Vorobyeva A, Larhed M, Tolmachev V, de Jong M, Rosenström U, Orlova A.

Int J Cancer. 2019 Dec 15;145(12):3347-3358. doi: 10.1002/ijc.32401. Epub 2019 May 23.


Comparative evaluation of the new GRPR-antagonist 111 In-SB9 and 111 In-AMBA in prostate cancer models: Implications of in vivo stability.

Lymperis E, Kaloudi A, Kanellopoulos P, Krenning EP, de Jong M, Maina T, Nock BA.

J Labelled Comp Radiopharm. 2019 Aug;62(10):646-655. doi: 10.1002/jlcr.3733. Epub 2019 Jun 13.


Localization of 99mTc-GRP Analogs in GRPR-Expressing Tumors: Effects of Peptide Length and Neprilysin Inhibition on Biological Responses.

Kaloudi A, Lymperis E, Kanellopoulos P, Waser B, de Jong M, Krenning EP, Reubi JC, Nock BA, Maina T.

Pharmaceuticals (Basel). 2019 Mar 20;12(1). pii: E42. doi: 10.3390/ph12010042.


Comparing Gly11/dAla11-Replacement vs. the in-Situ Neprilysin-Inhibition Approach on the Tumor-targeting Efficacy of the 111In-SB3/111In-SB4 Radiotracer Pair.

Lymperis E, Kaloudi A, Kanellopoulos P, de Jong M, Krenning EP, Nock BA, Maina T.

Molecules. 2019 Mar 13;24(6). pii: E1015. doi: 10.3390/molecules24061015.


A novel CCK2/gastrin receptor-localizing radiolabeled peptide probe for personalized diagnosis and therapy of patients with progressive or metastatic medullary thyroid carcinoma: a multicenter phase I GRAN-T-MTC study.

Erba PA, Maecke H, Mikolajczak R, Decristoforo C, Zaletel K, Maina-Nock T, Peitl PK, Garnuszek P, Froberg A, Goebel G, de Jong M, Jabrocka-Hybel A, Konijnenberg M, Virgolini I, Nock B, Lenda-Tracz W, Pawlak D, Rangger C, Trofimiuk-Müldner M, Sowa-Staszczak A, Tomaszuk M, von Guggenberg E, Scarpa L, Hubalewska-Dydejczyk A.

Pol Arch Intern Med. 2018 Dec 21;128(12):791-795. doi: 10.20452/pamw.4387. Epub 2018 Dec 5. No abstract available.


Radiometal-Dependent Biological Profile of the Radiolabeled Gastrin-Releasing Peptide Receptor Antagonist SB3 in Cancer Theranostics: Metabolic and Biodistribution Patterns Defined by Neprilysin.

Lymperis E, Kaloudi A, Sallegger W, Bakker IL, Krenning EP, de Jong M, Maina T, Nock BA.

Bioconjug Chem. 2018 May 16;29(5):1774-1784. doi: 10.1021/acs.bioconjchem.8b00225. Epub 2018 Apr 30.


In Vivo Stabilized SB3, an Attractive GRPR Antagonist, for Pre- and Intra-Operative Imaging for Prostate Cancer.

Bakker IL, van Tiel ST, Haeck J, Doeswijk GN, de Blois E, Segbers M, Maina T, Nock BA, de Jong M, Dalm SU.

Mol Imaging Biol. 2018 Dec;20(6):973-983. doi: 10.1007/s11307-018-1185-z.


New Gastrin Releasing Peptide Receptor-Directed [99mTc]Demobesin 1 Mimics: Synthesis and Comparative Evaluation.

Nock BA, Charalambidis D, Sallegger W, Waser B, Mansi R, Nicolas GP, Ketani E, Nikolopoulou A, Fani M, Reubi JC, Maina T.

J Med Chem. 2018 Apr 12;61(7):3138-3150. doi: 10.1021/acs.jmedchem.8b00177. Epub 2018 Mar 19.


NeoBOMB1, a GRPR-Antagonist for Breast Cancer Theragnostics: First Results of a Preclinical Study with [67Ga]NeoBOMB1 in T-47D Cells and Tumor-Bearing Mice.

Kaloudi A, Lymperis E, Giarika A, Dalm S, Orlandi F, Barbato D, Tedesco M, Maina T, de Jong M, Nock BA.

Molecules. 2017 Nov 11;22(11). pii: E1950. doi: 10.3390/molecules22111950.


Novel bifunctional DATA chelator for quick access to site-directed PET 68Ga-radiotracers: preclinical proof-of-principle with [Tyr3]octreotide.

Nock BA, Kaloudi A, Nagel J, Sinnes JP, Roesch F, Maina T.

Dalton Trans. 2017 Oct 31;46(42):14584-14590. doi: 10.1039/c7dt01684k.


Rhenium(I) Tricarbonyl Complexes with (2-Hydroxyphenyl)diphenylphosphine as PO Bidentate Ligand.

Shegani A, Triantis C, Nock BA, Maina T, Kiritsis C, Psycharis V, Raptopoulou C, Pirmettis I, Tisato F, Papadopoulos MS.

Inorg Chem. 2017 Jul 17;56(14):8175-8186. doi: 10.1021/acs.inorgchem.7b00894. Epub 2017 Jun 28.


Amide-to-triazole switch vs. in vivo NEP-inhibition approaches to promote radiopeptide targeting of GRPR-positive tumors.

Maina T, Kaloudi A, Valverde IE, Mindt TL, Nock BA.

Nucl Med Biol. 2017 Sep;52:57-62. doi: 10.1016/j.nucmedbio.2017.06.001. Epub 2017 Jun 10.


Theranostic Prospects of Gastrin-Releasing Peptide Receptor-Radioantagonists in Oncology.

Maina T, Nock BA, Kulkarni H, Singh A, Baum RP.

PET Clin. 2017 Jul;12(3):297-309. doi: 10.1016/j.cpet.2017.02.007. Epub 2017 Apr 3. Review.


From Bench to Bed: New Gastrin-Releasing Peptide Receptor-Directed Radioligands and Their Use in Prostate Cancer.

Maina T, Nock BA.

PET Clin. 2017 Apr;12(2):205-217. doi: 10.1016/j.cpet.2016.12.002. Epub 2017 Jan 31. Review.


68Ga/177Lu-NeoBOMB1, a Novel Radiolabeled GRPR Antagonist for Theranostic Use in Oncology.

Dalm SU, Bakker IL, de Blois E, Doeswijk GN, Konijnenberg MW, Orlandi F, Barbato D, Tedesco M, Maina T, Nock BA, de Jong M.

J Nucl Med. 2017 Feb;58(2):293-299. doi: 10.2967/jnumed.116.176636. Epub 2016 Sep 8. Erratum in: J Nucl Med. 2018 Jul;59(7):1164.


Improved Quantification of the Beta Cell Mass after Pancreas Visualization with 99mTc-demobesin-4 and Beta Cell Imaging with 111In-exendin-3 in Rodents.

van der Kroon I, Joosten L, Nock BA, Maina T, Boerman OC, Brom M, Gotthardt M.

Mol Pharm. 2016 Oct 3;13(10):3478-3483. Epub 2016 Aug 31.


Theranostic Perspectives in Prostate Cancer with the Gastrin-Releasing Peptide Receptor Antagonist NeoBOMB1: Preclinical and First Clinical Results.

Nock BA, Kaloudi A, Lymperis E, Giarika A, Kulkarni HR, Klette I, Singh A, Krenning EP, de Jong M, Maina T, Baum RP.

J Nucl Med. 2017 Jan;58(1):75-80. doi: 10.2967/jnumed.116.178889. Epub 2016 Aug 4.


(99m)Tc-labeled gastrins of varying peptide chain length: Distinct impact of NEP/ACE-inhibition on stability and tumor uptake in mice.

Kaloudi A, Nock BA, Lymperis E, Krenning EP, de Jong M, Maina T.

Nucl Med Biol. 2016 Jun;43(6):347-54. doi: 10.1016/j.nucmedbio.2016.03.003. Epub 2016 Mar 19.


Preclinical pharmacokinetics, biodistribution, radiation dosimetry and toxicity studies required for regulatory approval of a phase I clinical trial with (111)In-CP04 in medullary thyroid carcinoma patients.

Maina T, Konijnenberg MW, KolencPeitl P, Garnuszek P, Nock BA, Kaloudi A, Kroselj M, Zaletel K, Maecke H, Mansi R, Erba P, von Guggenberg E, Hubalewska-Dydejczyk A, Mikolajczak R, Decristoforo C.

Eur J Pharm Sci. 2016 Aug 25;91:236-42. doi: 10.1016/j.ejps.2016.05.011. Epub 2016 May 14.


Impact of clinically tested NEP/ACE inhibitors on tumor uptake of [(111)In-DOTA]MG11-first estimates for clinical translation.

Kaloudi A, Nock BA, Lymperis E, Valkema R, Krenning EP, de Jong M, Maina T.

EJNMMI Res. 2016 Dec;6(1):15. doi: 10.1186/s13550-015-0158-3. Epub 2016 Feb 16.


Improving the In Vivo Profile of Minigastrin Radiotracers: A Comparative Study Involving the Neutral Endopeptidase Inhibitor Phosphoramidon.

Kaloudi A, Nock BA, Lymperis E, Krenning EP, de Jong M, Maina T.

Cancer Biother Radiopharm. 2016 Feb;31(1):20-8. doi: 10.1089/cbr.2015.1935.


In Vivo Stabilization of a Gastrin-Releasing Peptide Receptor Antagonist Enhances PET Imaging and Radionuclide Therapy of Prostate Cancer in Preclinical Studies.

Chatalic KL, Konijnenberg M, Nonnekens J, de Blois E, Hoeben S, de Ridder C, Brunel L, Fehrentz JA, Martinez J, van Gent DC, Nock BA, Maina T, van Weerden WM, de Jong M.

Theranostics. 2016 Jan 1;6(1):104-17. doi: 10.7150/thno.13580. eCollection 2016.


Preclinical and first clinical experience with the gastrin-releasing peptide receptor-antagonist [⁶⁸Ga]SB3 and PET/CT.

Maina T, Bergsma H, Kulkarni HR, Mueller D, Charalambidis D, Krenning EP, Nock BA, de Jong M, Baum RP.

Eur J Nucl Med Mol Imaging. 2016 May;43(5):964-973. doi: 10.1007/s00259-015-3232-1. Epub 2015 Dec 2.


In vivo inhibition of neutral endopeptidase enhances the diagnostic potential of truncated gastrin (111)In-radioligands.

Kaloudi A, Nock BA, Lymperis E, Sallegger W, Krenning EP, de Jong M, Maina T.

Nucl Med Biol. 2015 Nov;42(11):824-32. doi: 10.1016/j.nucmedbio.2015.07.009. Epub 2015 Jul 29.


Radiolabeled gastrin/CCK analogs in tumor diagnosis: towards higher stability and improved tumor targeting.

Kaloudi A, Nock BA, Krenning EP, Maina T, De Jong M.

Q J Nucl Med Mol Imaging. 2015 Sep;59(3):287-302. Epub 2015 Jul 9. Review.


In vitro and in vivo application of radiolabeled gastrin-releasing peptide receptor ligands in breast cancer.

Dalm SU, Martens JW, Sieuwerts AM, van Deurzen CH, Koelewijn SJ, de Blois E, Maina T, Nock BA, Brunel L, Fehrentz JA, Martinez J, de Jong M, Melis M.

J Nucl Med. 2015 May;56(5):752-7. doi: 10.2967/jnumed.114.153023. Epub 2015 Mar 19.


In vivo enzyme inhibition improves the targeting of [177Lu]DOTA-GRP(13-27) in GRPR-positive tumors in mice.

Marsouvanidis PJ, Melis M, de Blois E, Breeman WA, Krenning EP, Maina T, Nock BA, de Jong M.

Cancer Biother Radiopharm. 2014 Nov;29(9):359-67. doi: 10.1089/cbr.2014.1706. Epub 2014 Oct 6.


[111In-DOTA]LTT-SS28, a first pansomatostatin radioligand for in vivo targeting of somatostatin receptor-positive tumors.

Maina T, Cescato R, Waser B, Tatsi A, Kaloudi A, Krenning EP, de Jong M, Nock BA, Reubi JC.

J Med Chem. 2014 Aug 14;57(15):6564-71. doi: 10.1021/jm500581d. Epub 2014 Jul 23.


GRP receptor imaging of prostate cancer using [(99m)Tc]Demobesin 4: a first-in-man study.

Mather SJ, Nock BA, Maina T, Gibson V, Ellison D, Murray I, Sobnack R, Colebrook S, Wan S, Halberrt G, Szysko T, Powles T, Avril N.

Mol Imaging Biol. 2014 Dec;16(6):888-95. doi: 10.1007/s11307-014-0754-z.


[DOTA]Somatostatin-14 analogs and their (111)In-radioligands: effects of decreasing ring-size on sst1-5 profile, stability and tumor targeting.

Tatsi A, Maina T, Cescato R, Waser B, Krenning EP, de Jong M, Cordopatis P, Reubi JC, Nock BA.

Eur J Med Chem. 2014 Feb 12;73:30-7. doi: 10.1016/j.ejmech.2013.12.003. Epub 2013 Dec 16.


"To serve and protect": enzyme inhibitors as radiopeptide escorts promote tumor targeting.

Nock BA, Maina T, Krenning EP, de Jong M.

J Nucl Med. 2014 Jan;55(1):121-7. doi: 10.2967/jnumed.113.129411. Epub 2013 Nov 28.


Tumor diagnosis with new 111In-radioligands based on truncated human gastrin releasing peptide sequences: synthesis and preclinical comparison.

Marsouvanidis PJ, Maina T, Sallegger W, Krenning EP, de Jong M, Nock BA.

J Med Chem. 2013 Nov 14;56(21):8579-87. doi: 10.1021/jm4010237. Epub 2013 Oct 23.


99mTc radiotracers based on human GRP(18-27): synthesis and comparative evaluation.

Marsouvanidis PJ, Maina T, Sallegger W, Krenning EP, de Jong M, Nock BA.

J Nucl Med. 2013 Oct;54(10):1797-803. doi: 10.2967/jnumed.112.118695. Epub 2013 Sep 5.


Gastrin releasing peptide receptor-directed radioligands based on a bombesin antagonist: synthesis, (111)in-labeling, and preclinical profile.

Marsouvanidis PJ, Nock BA, Hajjaj B, Fehrentz JA, Brunel L, M'Kadmi C, van der Graaf L, Krenning EP, Maina T, Martinez J, de Jong M.

J Med Chem. 2013 Mar 28;56(6):2374-84. doi: 10.1021/jm301692p. Epub 2013 Mar 8.


[(99m)Tc]Demomedin C, a radioligand based on human gastrin releasing peptide(18-27): synthesis and preclinical evaluation in gastrin releasing peptide receptor-expressing models.

Nock BA, Cescato R, Ketani E, Waser B, Reubi JC, Maina T.

J Med Chem. 2012 Oct 11;55(19):8364-74. doi: 10.1021/jm300741f. Epub 2012 Sep 26.


[111In-DOTA]Somatostatin-14 analogs as potential pansomatostatin-like radiotracers - first results of a preclinical study.

Tatsi A, Maina T, Cescato R, Waser B, Krenning EP, de Jong M, Cordopatis P, Reubi JC, Nock BA.

EJNMMI Res. 2012 Jun 9;2(1):25. doi: 10.1186/2191-219X-2-25.


Distribution, elimination, and renal handling of (99m)technetium-Demogastrin 1.

Trejtnar F, Laznickova A, Laznicek M, Novy Z, Maina T, Nock BA, Behe M.

Cancer Biother Radiopharm. 2012 Mar;27(2):169-74. doi: 10.1089/cbr.2011.1008.


[99mTc]demotensin VI: biodistribution and initial clinical results in tumor patients of a pilot/phase I study.

Gabriel M, Decristoforo C, Wöll E, Eisterer W, Nock B, Maina T, Moncayo R, Virgolini I.

Cancer Biother Radiopharm. 2011 Oct;26(5):557-63. doi: 10.1089/cbr.2010.0952. Epub 2011 Sep 1.


Comparison of biological stability and metabolism of CCK2 receptor targeting peptides, a collaborative project under COST BM0607.

Ocak M, Helbok A, Rangger C, Peitl PK, Nock BA, Morelli G, Eek A, Sosabowski JK, Breeman WA, Reubi JC, Decristoforo C.

Eur J Nucl Med Mol Imaging. 2011 Aug;38(8):1426-35. doi: 10.1007/s00259-011-1818-9. Epub 2011 Apr 29.


Intramolecular azo-bridge as a cystine disulfide bond surrogate: Somatostatin-14 and brain natriuretic peptide (BNP) analogs.

Fridkin G, Maina T, Nock BA, Blat D, Lev-Goldman V, Scolnik Y, Kapitkovski A, Vachutinsky Y, Shechter Y, Levy Y.

Bioorg Med Chem. 2011 Jan 15;19(2):798-806. doi: 10.1016/j.bmc.2010.12.014. Epub 2010 Dec 13.


Comparison of three radiolabelled peptide analogues for CCK-2 receptor scintigraphy in medullary thyroid carcinoma.

Fröberg AC, de Jong M, Nock BA, Breeman WA, Erion JL, Maina T, Verdijsseldonck M, de Herder WW, van der Lugt A, Kooij PP, Krenning EP.

Eur J Nucl Med Mol Imaging. 2009 Aug;36(8):1265-72. doi: 10.1007/s00259-009-1098-9. Epub 2009 Mar 6.


Optimised labeling, preclinical and initial clinical aspects of CCK-2 receptor-targeting with 3 radiolabeled peptides.

Breeman WA, Fröberg AC, de Blois E, van Gameren A, Melis M, de Jong M, Maina T, Nock BA, Erion JL, Mäcke HR, Krenning EP.

Nucl Med Biol. 2008 Nov;35(8):839-49. doi: 10.1016/j.nucmedbio.2008.09.006.


Synthesis and sst(2) binding profiles of new [Tyr(3)]octreotate analogs.

Petrou C, Magafa V, Nikolopoulou A, Pairas G, Nock B, Maina T, Cordopatis P.

J Pept Sci. 2008 Jun;14(6):725-30. doi: 10.1002/psc.989.


Bombesin receptor antagonists may be preferable to agonists for tumor targeting.

Cescato R, Maina T, Nock B, Nikolopoulou A, Charalambidis D, Piccand V, Reubi JC.

J Nucl Med. 2008 Feb;49(2):318-26. doi: 10.2967/jnumed.107.045054. Epub 2008 Jan 16.


[99mTc]Demotensin 5 and 6 in the NTS1-R-targeted imaging of tumours: synthesis and preclinical results.

Maina T, Nikolopoulou A, Stathopoulou E, Galanis AS, Cordopatis P, Nock BA.

Eur J Nucl Med Mol Imaging. 2007 Nov;34(11):1804-14. Epub 2007 Jun 27.


Biodistribution and elimination characteristics of two 111In-labeled CCK-2/gastrin receptor-specific peptides in rats.

Trejtnar F, Laznicek M, Laznickova A, Kopecky M, Petrik M, Béhé M, Schmidt J, Maecke H, Maina T, Nock B.

Anticancer Res. 2007 Mar-Apr;27(2):907-12.


Targeting prostate cancer with radiolabelled bombesins.

Maina T, Nock B, Mather S.

Cancer Imaging. 2006 Nov 8;6:153-7. Review.

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