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Delivery systems exploiting natural cell transport processes of macromolecules for intracellular targeting of Auger electron emitters.

Rosenkranz AA, Slastnikova TA, Georgiev GP, Zalutsky MR, Sobolev AS.

Nucl Med Biol. 2019 Nov 27. pii: S0969-8051(19)30466-4. doi: 10.1016/j.nucmedbio.2019.11.005. [Epub ahead of print] Review.


Observations on the Effects of Residualization and Dehalogenation on the Utility of N-Succinimidyl Ester Acylation Agents for Radioiodination of the Internalizing Antibody Trastuzumab.

Chitneni SK, Koumarianou E, Vaidyanathan G, Zalutsky MR.

Molecules. 2019 Oct 30;24(21). pii: E3907. doi: 10.3390/molecules24213907.


Pharmacodynamic study of radium-223 in men with bone metastatic castration resistant prostate cancer.

Armstrong AJ, Gupta S, Healy P, Kemeny G, Leith B, Zalutsky MR, Spritzer C, Davies C, Rothwell C, Ware K, Somarelli JA, Wood K, Ribar T, Giannakakou P, Zhang J, Gerber D, Anand M, Foo WC, Halabi S, Gregory SG, George DJ.

PLoS One. 2019 May 28;14(5):e0216934. doi: 10.1371/journal.pone.0216934. eCollection 2019.


Non-invasive sensitive brain tumor detection using dual-modality bioimaging nanoprobe.

Liu Y, Carpenter AB, Pirozzi CJ, Yuan H, Waitkus MS, Zhou Z, Hansen L, Seywald M, Odion R, Greer PK, Hawk T, Chin BB, Vaidyanathan G, Zalutsky MR, Yan H, Vo-Dinh T.

Nanotechnology. 2019 Jul 5;30(27):275101. doi: 10.1088/1361-6528/ab0e9c. Epub 2019 Mar 11.


Labeling Single Domain Antibody Fragments with Fluorine-18 Using 2,3,5,6-Tetrafluorophenyl 6-[18F]Fluoronicotinate Resulting in High Tumor-to-Kidney Ratios.

Zhou Z, McDougald D, Devoogdt N, Zalutsky MR, Vaidyanathan G.

Mol Pharm. 2019 Jan 7;16(1):214-226. doi: 10.1021/acs.molpharmaceut.8b00951. Epub 2018 Nov 28.


An Efficient Method for Labeling Single Domain Antibody Fragments with 18F Using Tetrazine- Trans-Cyclooctene Ligation and a Renal Brush Border Enzyme-Cleavable Linker.

Zhou Z, Devoogdt N, Zalutsky MR, Vaidyanathan G.

Bioconjug Chem. 2018 Dec 19;29(12):4090-4103. doi: 10.1021/acs.bioconjchem.8b00699. Epub 2018 Nov 14.


Synthesis and Evaluation of a 18F-Labeled Triazinediamine Analogue for Imaging Mutant IDH1 Expression in Gliomas by PET.

Chitneni SK, Yan H, Zalutsky MR.

ACS Med Chem Lett. 2018 May 1;9(7):606-611. doi: 10.1021/acsmedchemlett.7b00478. eCollection 2018 Jul 12.


Brush border enzyme-cleavable linkers: Evaluation for reducing renal uptake of radiolabeled prostate-specific membrane antigen inhibitors.

Vaidyanathan G, Kang CM, McDougald D, Minn I, Brummet M, Pomper MG, Zalutsky MR.

Nucl Med Biol. 2018 Jul - Aug;62-63:18-30. doi: 10.1016/j.nucmedbio.2018.05.002. Epub 2018 May 5.


d-Amino Acid Peptide Residualizing Agents for Protein Radioiodination: Effect of Aspartate for Glutamate Substitution.

Pruszynski M, Kang CM, Koumarianou E, Vaidyanathan G, Zalutsky MR.

Molecules. 2018 May 20;23(5). pii: E1223. doi: 10.3390/molecules23051223.


Fluorine-18 labeling of an anti-HER2 VHH using a residualizing prosthetic group via a strain-promoted click reaction: Chemistry and preliminary evaluation.

Zhou Z, Chitneni SK, Devoogdt N, Zalutsky MR, Vaidyanathan G.

Bioorg Med Chem. 2018 May 1;26(8):1939-1949. doi: 10.1016/j.bmc.2018.02.040. Epub 2018 Mar 15.


Synthesis and evaluation of radiolabeled AGI-5198 analogues as candidate radiotracers for imaging mutant IDH1 expression in tumors.

Chitneni SK, Reitman ZJ, Spicehandler R, Gooden DM, Yan H, Zalutsky MR.

Bioorg Med Chem Lett. 2018 Feb 15;28(4):694-699. doi: 10.1016/j.bmcl.2018.01.015. Epub 2018 Jan 12.


A model for optimizing delivery of targeted radionuclide therapies into resection cavity margins for the treatment of primary brain cancers.

Raghavan R, Howell RW, Zalutsky MR.

Biomed Phys Eng Express. 2017 Jun;3(3). pii: 035005. doi: 10.1088/2057-1976/aa6db9. Epub 2017 May 5.


Astatine-211 labeled anti-HER2 5F7 single domain antibody fragment conjugates: radiolabeling and preliminary evaluation.

Choi J, Vaidyanathan G, Koumarianou E, Kang CM, Zalutsky MR.

Nucl Med Biol. 2018 Jan;56:10-20. doi: 10.1016/j.nucmedbio.2017.09.003. Epub 2017 Sep 19.


131I-labeled Anti-HER2 Camelid sdAb as a Theranostic Tool in Cancer Treatment.

D'Huyvetter M, De Vos J, Xavier C, Pruszynski M, Sterckx YGJ, Massa S, Raes G, Caveliers V, Zalutsky MR, Lahoutte T, Devoogdt N.

Clin Cancer Res. 2017 Nov 1;23(21):6616-6628. doi: 10.1158/1078-0432.CCR-17-0310. Epub 2017 Jul 27.


Fluorine-18 Labeling of the HER2-Targeting Single-Domain Antibody 2Rs15d Using a Residualizing Label and Preclinical Evaluation.

Zhou Z, Vaidyanathan G, McDougald D, Kang CM, Balyasnikova I, Devoogdt N, Ta AN, McNaughton BR, Zalutsky MR.

Mol Imaging Biol. 2017 Dec;19(6):867-877. doi: 10.1007/s11307-017-1082-x.


Preparation, cytotoxicity, and in vivo antitumor efficacy of 111In-labeled modular nanotransporters.

Slastnikova TA, Rosenkranz AA, Morozova NB, Vorontsova MS, Petriev VM, Lupanova TN, Ulasov AV, Zalutsky MR, Yakubovskaya RI, Sobolev AS.

Int J Nanomedicine. 2017 Jan 10;12:395-410. doi: 10.2147/IJN.S125359. eCollection 2017.


Synthesis and Preliminary Evaluation of 5-[18F]fluoroleucine.

Chin BB, McDougald D, Weitzel DH, Hawk T, Reiman RE, Zalutsky MR, Vaidyanathan G.

Curr Radiopharm. 2017;10(1):41-50. doi: 10.2174/1874471009666161230114954.


Prostate-Specific Membrane Antigen-Targeted Radiohalogenated PET and Therapeutic Agents for Prostate Cancer.

Rowe SP, Drzezga A, Neumaier B, Dietlein M, Gorin MA, Zalutsky MR, Pomper MG.

J Nucl Med. 2016 Oct;57(Suppl 3):90S-96S. Review.


(2S)-2-(3-(1-Carboxy-5-(4-211At-Astatobenzamido)Pentyl)Ureido)-Pentanedioic Acid for PSMA-Targeted α-Particle Radiopharmaceutical Therapy.

Kiess AP, Minn I, Vaidyanathan G, Hobbs RF, Josefsson A, Shen C, Brummet M, Chen Y, Choi J, Koumarianou E, Baidoo K, Brechbiel MW, Mease RC, Sgouros G, Zalutsky MR, Pomper MG.

J Nucl Med. 2016 Oct;57(10):1569-1575. Epub 2016 May 26.


Radiolabeled inhibitors as probes for imaging mutant IDH1 expression in gliomas: Synthesis and preliminary evaluation of labeled butyl-phenyl sulfonamide analogs.

Chitneni SK, Reitman ZJ, Gooden DM, Yan H, Zalutsky MR.

Eur J Med Chem. 2016 Aug 25;119:218-30. doi: 10.1016/j.ejmech.2016.04.066. Epub 2016 Apr 28.


Injectable polypeptide micelles that form radiation crosslinked hydrogels in situ for intratumoral radiotherapy.

Schaal JL, Li X, Mastria E, Bhattacharyya J, Zalutsky MR, Chilkoti A, Liu W.

J Control Release. 2016 Apr 28;228:58-66. doi: 10.1016/j.jconrel.2016.02.040. Epub 2016 Feb 27.


Preclinical Evaluation of 18F-Labeled Anti-HER2 Nanobody Conjugates for Imaging HER2 Receptor Expression by Immuno-PET.

Vaidyanathan G, McDougald D, Choi J, Koumarianou E, Weitzel D, Osada T, Lyerly HK, Zalutsky MR.

J Nucl Med. 2016 Jun;57(6):967-73. doi: 10.2967/jnumed.115.171306. Epub 2016 Feb 18.


Preclinical toxicity evaluation of a novel immunotoxin, D2C7-(scdsFv)-PE38KDEL, administered via intracerebral convection-enhanced delivery in rats.

Bao X, Chandramohan V, Reynolds RP, Norton JN, Wetsel WC, Rodriguiz RM, Aryal DK, McLendon RE, Levin ED, Petry NA, Zalutsky MR, Burnett BK, Kuan CT, Pastan IH, Bigner DD.

Invest New Drugs. 2016 Apr;34(2):149-58. doi: 10.1007/s10637-015-0318-3. Epub 2016 Jan 4.


Spatiotemporally photoradiation-controlled intratumoral depot for combination of brachytherapy and photodynamic therapy for solid tumor.

Mukerji R, Schaal J, Li X, Bhattacharyya J, Asai D, Zalutsky MR, Chilkoti A, Liu W.

Biomaterials. 2016 Feb;79:79-87. doi: 10.1016/j.biomaterials.2015.11.064. Epub 2015 Dec 2.


N-Succinimidyl 3-((4-(4-[(18)F]fluorobutyl)-1H-1,2,3-triazol-1-yl)methyl)-5-(guanidinomethyl)benzoate ([(18)F]SFBTMGMB): a residualizing label for (18)F-labeling of internalizing biomolecules.

Vaidyanathan G, McDougald D, Choi J, Pruszynski M, Koumarianou E, Zhou Z, Zalutsky MR.

Org Biomol Chem. 2016 Jan 28;14(4):1261-71. doi: 10.1039/c5ob02258d. Epub 2015 Dec 8.


A Plasmonic Gold Nanostar Theranostic Probe for In Vivo Tumor Imaging and Photothermal Therapy.

Liu Y, Ashton JR, Moding EJ, Yuan H, Register JK, Fales AM, Choi J, Whitley MJ, Zhao X, Qi Y, Ma Y, Vaidyanathan G, Zalutsky MR, Kirsch DG, Badea CT, Vo-Dinh T.

Theranostics. 2015 May 23;5(9):946-60. doi: 10.7150/thno.11974. eCollection 2015.


Synthesis and evaluation of 4-[18F]fluoropropoxy-3-iodobenzylguanidine ([18F]FPOIBG): A novel 18F-labeled analogue of MIBG.

Vaidyanathan G, McDougald D, Koumarianou E, Choi J, Hens M, Zalutsky MR.

Nucl Med Biol. 2015 Aug;42(8):673-84. doi: 10.1016/j.nucmedbio.2015.04.005. Epub 2015 Apr 20.


Reply: Pharmacokinetic and Pharmacodynamic Modifiers of EF5 Uptake and Binding.

Chitneni SK, Bida GT, Zalutsky MR, Dewhirst MW.

J Nucl Med. 2015 Apr;56(4):653-4. doi: 10.2967/jnumed.115.154054. Epub 2015 Mar 5. No abstract available.


Stability and in vivo behavior of Rh[16aneS4-diol]211 at complex: a potential precursor for astatine radiopharmaceuticals.

Pruszyński M, Łyczko M, Bilewicz A, Zalutsky MR.

Nucl Med Biol. 2015 May;42(5):439-445. doi: 10.1016/j.nucmedbio.2014.12.011. Epub 2014 Dec 23.


Copper signaling axis as a target for prostate cancer therapeutics.

Safi R, Nelson ER, Chitneni SK, Franz KJ, George DJ, Zalutsky MR, McDonnell DP.

Cancer Res. 2014 Oct 15;74(20):5819-31. doi: 10.1158/0008-5472.CAN-13-3527.


Modular nanotransporters for targeted intracellular delivery of drugs: folate receptors as potential targets.

Slastnikova TA, Rosenkranz AA, Zalutsky MR, Sobolev AS.

Curr Pharm Des. 2015;21(9):1227-38. Review.


D-Amino acid peptide residualizing agents bearing N-hydroxysuccinimido- and maleimido-functional groups and their application for trastuzumab radioiodination.

Pruszynski M, Koumarianou E, Vaidyanathan G, Chitneni S, Zalutsky MR.

Nucl Med Biol. 2015 Jan;42(1):19-27. doi: 10.1016/j.nucmedbio.2014.08.007. Epub 2014 Aug 13.


N-Succinimidyl guanidinomethyl iodobenzoate protein radiohalogenation agents: influence of isomeric substitution on radiolabeling and target cell residualization.

Choi J, Vaidyanathan G, Koumarianou E, McDougald D, Pruszynski M, Osada T, Lahoutte T, Lyerly HK, Zalutsky MR.

Nucl Med Biol. 2014 Nov-Dec;41(10):802-12. doi: 10.1016/j.nucmedbio.2014.07.005. Epub 2014 Aug 1.


Comparison of the Hypoxia PET Tracer (18)F-EF5 to Immunohistochemical Marker EF5 in 3 Different Human Tumor Xenograft Models.

Chitneni SK, Bida GT, Zalutsky MR, Dewhirst MW.

J Nucl Med. 2014 Jul;55(7):1192-7. doi: 10.2967/jnumed.114.137448. Epub 2014 May 22.


Radiolabeling and in vitro evaluation of (67)Ga-NOTA-modular nanotransporter--a potential Auger electron emitting EGFR-targeted radiotherapeutic.

Koumarianou E, Slastnikova TA, Pruszynski M, Rosenkranz AA, Vaidyanathan G, Sobolev AS, Zalutsky MR.

Nucl Med Biol. 2014 Jul;41(6):441-9. doi: 10.1016/j.nucmedbio.2014.03.026. Epub 2014 Apr 2.


Improved tumor targeting of anti-HER2 nanobody through N-succinimidyl 4-guanidinomethyl-3-iodobenzoate radiolabeling.

Pruszynski M, Koumarianou E, Vaidyanathan G, Revets H, Devoogdt N, Lahoutte T, Lyerly HK, Zalutsky MR.

J Nucl Med. 2014 Apr;55(4):650-6. doi: 10.2967/jnumed.113.127100. Epub 2014 Feb 27.


Optical and radioiodinated tethered Hsp90 inhibitors reveal selective internalization of ectopic Hsp90 in malignant breast tumor cells.

Barrott JJ, Hughes PF, Osada T, Yang XY, Hartman ZC, Loiselle DR, Spector NL, Neckers L, Rajaram N, Hu F, Ramanujam N, Vaidyanathan G, Zalutsky MR, Lyerly HK, Haystead TA.

Chem Biol. 2013 Sep 19;20(9):1187-97. doi: 10.1016/j.chembiol.2013.08.004. Epub 2013 Sep 12.


18F-EF5 PET imaging as an early response biomarker for the hypoxia-activated prodrug SN30000 combined with radiation treatment in a non-small cell lung cancer xenograft model.

Chitneni SK, Bida GT, Yuan H, Palmer GM, Hay MP, Melcher T, Wilson WR, Zalutsky MR, Dewhirst MW.

J Nucl Med. 2013 Aug;54(8):1339-46. doi: 10.2967/jnumed.112.116293. Epub 2013 Jun 5.


Targeting breast carcinoma with radioiodinated anti-HER2 Nanobody.

Pruszynski M, Koumarianou E, Vaidyanathan G, Revets H, Devoogdt N, Lahoutte T, Zalutsky MR.

Nucl Med Biol. 2013 Jan;40(1):52-9. doi: 10.1016/j.nucmedbio.2012.08.008. Epub 2012 Nov 15.


SIB-DOTA: a trifunctional prosthetic group potentially amenable for multi-modal labeling that enhances tumor uptake of internalizing monoclonal antibodies.

Vaidyanathan G, White BJ, Affleck DJ, Zhao XG, Welsh PC, McDougald D, Choi J, Zalutsky MR.

Bioorg Med Chem. 2012 Dec 15;20(24):6929-39. doi: 10.1016/j.bmc.2012.10.025. Epub 2012 Oct 29.


Modular nanotransporters: a versatile approach for enhancing nuclear delivery and cytotoxicity of Auger electron-emitting 125I.

Slastnikova TA, Koumarianou E, Rosenkranz AA, Vaidyanathan G, Lupanova TN, Sobolev AS, Zalutsky MR.

EJNMMI Res. 2012 Oct 29;2(1):59. doi: 10.1186/2191-219X-2-59.


A simplified synthesis of the hypoxia imaging agent 2-(2-Nitro-1H-imidazol-1-yl)-N-(2,2,3,3,3-[(18)F]pentafluoropropyl)-acetamide ([18F]EF5).

Chitneni SK, Bida GT, Dewhirst MW, Zalutsky MR.

Nucl Med Biol. 2012 Oct;39(7):1012-8. doi: 10.1016/j.nucmedbio.2012.05.006. Epub 2012 Jun 22.


Protein polymer hydrogels by in situ, rapid and reversible self-gelation.

Asai D, Xu D, Liu W, Garcia Quiroz F, Callahan DJ, Zalutsky MR, Craig SL, Chilkoti A.

Biomaterials. 2012 Jul;33(21):5451-8. doi: 10.1016/j.biomaterials.2012.03.083. Epub 2012 Apr 25.


Modular nanotransporters: a multipurpose in vivo working platform for targeted drug delivery.

Slastnikova TA, Rosenkranz AA, Gulak PV, Schiffelers RM, Lupanova TN, Khramtsov YV, Zalutsky MR, Sobolev AS.

Int J Nanomedicine. 2012;7:467-82. doi: 10.2147/IJN.S28249. Epub 2012 Feb 2.


Applications of 211At and 223Ra in targeted alpha-particle radiotherapy.

Vaidyanathan G, Zalutsky MR.

Curr Radiopharm. 2011 Oct;4(4):283-94. Review.


Astatine-211: production and availability.

Zalutsky MR, Pruszynski M.

Curr Radiopharm. 2011 Jul;4(3):177-85. Review.


Radioimmunotargeting of malignant glioma by monoclonal antibody D2C7 reactive against both wild-type and variant III mutant epidermal growth factor receptors.

Zalutsky MR, Boskovitz A, Kuan CT, Pegram CN, Ayriss J, Wikstrand CJ, Buckley AF, Lipp ES, Herndon JE 2nd, McLendon RE, Bigner DD.

Nucl Med Biol. 2012 Jan;39(1):23-34. doi: 10.1016/j.nucmedbio.2011.06.005. Epub 2011 Sep 29.


An alternative and expedient synthesis of radioiodinated 4-iodophenylalanine.

Vaidyanathan G, McDougald D, Grasfeder L, Zalutsky MR, Chin B.

Appl Radiat Isot. 2011 Oct;69(10):1401-6. doi: 10.1016/j.apradiso.2011.05.004. Epub 2011 May 19.


Colocalization of gadolinium-diethylene triamine pentaacetic acid with high-molecular-weight molecules after intracerebral convection-enhanced delivery in humans.

Sampson JH, Brady M, Raghavan R, Mehta AI, Friedman AH, Reardon DA, Petry NA, Barboriak DP, Wong TZ, Zalutsky MR, Lally-Goss D, Bigner DD.

Neurosurgery. 2011 Sep;69(3):668-76. doi: 10.1227/NEU.0b013e3182181ba8.

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