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Pretargeted radioimmunotherapy and SPECT imaging of peritoneal carcinomatosis using bioorthogonal click chemistry: probe selection and first proof-of-concept.

Rondon A, Schmitt S, Briat A, Ty N, Maigne L, Quintana M, Membreno R, Zeglis BM, Navarro-Teulon I, Pouget JP, Chezal JM, Miot-Noirault E, Moreau E, Degoul F.

Theranostics. 2019 Sep 19;9(22):6706-6718. doi: 10.7150/thno.35461. eCollection 2019.


Targeted Radionuclide Therapy Decreases Melanoma Lung Invasion by Modifying Epithelial-Mesenchymal Transition-Like Mechanisms.

Akil H, Rouanet J, Viallard C, Besse S, Auzeloux P, Chezal JM, Miot-Noirault E, Quintana M, Degoul F.

Transl Oncol. 2019 Nov;12(11):1442-1452. doi: 10.1016/j.tranon.2019.07.015. Epub 2019 Aug 14.


Targeting cyclic nucleotide phosphodiesterase 5 (PDE5) in brain: Toward the development of a PET radioligand labeled with fluorine-18.

Wenzel B, Liu J, Dukic-Stefanovic S, Deuther-Conrad W, Teodoro R, Ludwig FA, Chezal JM, Moreau E, Brust P, Maisonial-Besset A.

Bioorg Chem. 2019 May;86:346-362. doi: 10.1016/j.bioorg.2019.01.037. Epub 2019 Jan 28.


Structure-activity relationship study of hypoxia-activated prodrugs for proteoglycan-targeted chemotherapy in chondrosarcoma.

Ghedira D, Voissière A, Peyrode C, Kraiem J, Gerard Y, Maubert E, Vivier M, Miot-Noirault E, Chezal JM, Farhat F, Weber V.

Eur J Med Chem. 2018 Oct 5;158:51-67. doi: 10.1016/j.ejmech.2018.08.060. Epub 2018 Aug 23.


Radiation dosimetry of [131 I]ICF01012 in rabbits: Application to targeted radionuclide therapy for human melanoma treatment.

Jouberton E, Perrot Y, Dirat B, Billoux T, Auzeloux P, Cachin F, Chezal JM, Filaire M, Labarre P, Miot-Noirault E, Millardet C, Valla C, Vidal A, Degoul F, Maigne L.

Med Phys. 2018 Nov;45(11):5251-5262. doi: 10.1002/mp.13165. Epub 2018 Sep 24.


Evaluation of the Active Targeting of Melanin Granules after Intravenous Injection of Dendronized Nanoparticles.

Bordeianu C, Parat A, Piant S, Walter A, Zbaraszczuk-Affolter C, Meyer F, Begin-Colin S, Boutry S, Muller RN, Jouberton E, Chezal JM, Labeille B, Cinotti E, Perrot JL, Miot-Noirault E, Laurent S, Felder-Flesch D.

Mol Pharm. 2018 Feb 5;15(2):536-547. doi: 10.1021/acs.molpharmaceut.7b00904. Epub 2018 Jan 17.


Proteoglycan-targeting applied to hypoxia-activated prodrug therapy in chondrosarcoma: first proof-of-concept.

Voissiere A, Weber V, Gerard Y, Rédini F, Raes F, Chezal JM, Degoul F, Peyrode C, Miot-Noirault E.

Oncotarget. 2017 Sep 27;8(56):95824-95840. doi: 10.18632/oncotarget.21337. eCollection 2017 Nov 10.


Antibody PEGylation in bioorthogonal pretargeting with trans-cyclooctene/tetrazine cycloaddition: in vitro and in vivo evaluation in colorectal cancer models.

Rondon A, Ty N, Bequignat JB, Quintana M, Briat A, Witkowski T, Bouchon B, Boucheix C, Miot-Noirault E, Pouget JP, Chezal JM, Navarro-Teulon I, Moreau E, Degoul F.

Sci Rep. 2017 Nov 2;7(1):14918. doi: 10.1038/s41598-017-15051-y.


Linker structure-activity relationships in fluorodeoxyglucose chlorambucil conjugates for tumor-targeted chemotherapy.

El Hilali M, Reux B, Debiton E, Leal F, Galmier MJ, Vivier M, Chezal JM, Miot-Noirault E, Coudert P, Weber V.

Bioorg Med Chem. 2017 Oct 15;25(20):5692-5708. doi: 10.1016/j.bmc.2017.08.043. Epub 2017 Aug 30.


Doxycycline and its quaternary ammonium derivative for adjuvant therapies of chondrosarcoma.

Miladi I, Vivier M, Dauplat MM, Chatard M, Besse S, Vidal A, Chassain K, Jean B, Forestier C, Chezal JM, Rédini F, Degoul F, Miot-Noirault E.

Cancer Chemother Pharmacol. 2017 Sep;80(3):517-526. doi: 10.1007/s00280-017-3377-7. Epub 2017 Jul 13.


Development and characterization of a human three-dimensional chondrosarcoma culture for in vitro drug testing.

Voissiere A, Jouberton E, Maubert E, Degoul F, Peyrode C, Chezal JM, Miot-Noirault É.

PLoS One. 2017 Jul 13;12(7):e0181340. doi: 10.1371/journal.pone.0181340. eCollection 2017.


Synthesis and in vitro evaluation of new fluorinated quinoline derivatives with high affinity for PDE5: Towards the development of new PET neuroimaging probes.

Liu J, Maisonial-Besset A, Wenzel B, Canitrot D, Baufond A, Chezal JM, Brust P, Moreau E.

Eur J Med Chem. 2017 Aug 18;136:548-560. doi: 10.1016/j.ejmech.2017.03.091. Epub 2017 Apr 19.


Tetraspanin 8 (TSPAN 8) as a potential target for radio-immunotherapy of colorectal cancer.

Maisonial-Besset A, Witkowski T, Navarro-Teulon I, Berthier-Vergnes O, Fois G, Zhu Y, Besse S, Bawa O, Briat A, Quintana M, Pichard A, Bonnet M, Rubinstein E, Pouget JP, Opolon P, Maigne L, Miot-Noirault E, Chezal JM, Boucheix C, Degoul F.

Oncotarget. 2017 Mar 28;8(13):22034-22047. doi: 10.18632/oncotarget.15787.


In vitro cytotoxic effects of DEHP-alternative plasticizers and their primary metabolites on a L929 cell line.

Eljezi T, Pinta P, Richard D, Pinguet J, Chezal JM, Chagnon MC, Sautou V, Grimandi G, Moreau E.

Chemosphere. 2017 Apr;173:452-459. doi: 10.1016/j.chemosphere.2017.01.026. Epub 2017 Jan 8.


Theranostic Approach for Metastatic Pigmented Melanoma Using ICF15002, a Multimodal Radiotracer for Both PET Imaging and Targeted Radionuclide Therapy.

Rbah-Vidal L, Vidal A, Billaud EM, Besse S, Ranchon-Cole I, Mishellany F, Perrot Y, Maigne L, Moins N, Guerquin-Kern JL, Degoul F, Chezal JM, Auzeloux P, Miot-Noirault E.

Neoplasia. 2017 Jan;19(1):17-27. doi: 10.1016/j.neo.2016.11.001. Epub 2016 Dec 14.


Proteoglycans as Target for an Innovative Therapeutic Approach in Chondrosarcoma: Preclinical Proof of Concept.

Peyrode C, Weber V, Voissière A, Maisonial-Besset A, Vidal A, Auzeloux P, Gaumet V, Borel M, Dauplat MM, Quintana M, Degoul F, Rédini F, Chezal JM, Miot-Noirault E.

Mol Cancer Ther. 2016 Nov;15(11):2575-2585. Epub 2016 Aug 29.


Preparation of core/shell NaYF4:Yb,Tm@dendrons nanoparticles with enhanced upconversion luminescence for in vivo imaging.

Francolon N, Boyer D, Leccia F, Jouberton E, Walter A, Bordeianu C, Parat A, Felder-Flesch D, Begin-Colin S, Miot-Noirault E, Chezal JM, Mahiou R.

Nanomedicine. 2016 Oct;12(7):2107-2113. doi: 10.1016/j.nano.2016.05.020. Epub 2016 Jun 9.


Melanoma-targeted delivery system (part 2): Synthesis, radioiodination and biological evaluation in B16F0 bearing mice.

El Aissi R, Miladi I, Chezal JM, Chavignon O, Miot-Noirault E, Moreau E.

Eur J Med Chem. 2016 Sep 14;120:304-12. doi: 10.1016/j.ejmech.2016.05.019. Epub 2016 May 10.


Development of a New Radiofluorinated Quinoline Analog for PET Imaging of Phosphodiesterase 5 (PDE5) in Brain.

Liu J, Wenzel B, Dukic-Stefanovic S, Teodoro R, Ludwig FA, Deuther-Conrad W, Schröder S, Chezal JM, Moreau E, Brust P, Maisonial-Besset A.

Pharmaceuticals (Basel). 2016 Apr 21;9(2). pii: E22. doi: 10.3390/ph9020022.


3-(imidazo[1,2-a:5,4-b']dipyridin-2-yl)aniline inhibits pestivirus replication by targeting a hot spot drug binding pocket in the RNA-dependent RNA polymerase.

Musiu S, Leyssen P, Froeyen M, Chezal JM, Neyts J, Paeshuyse J.

Antiviral Res. 2016 May;129:99-103. doi: 10.1016/j.antiviral.2016.03.007. Epub 2016 Mar 9.


Targeting DNA repair by coDbait enhances melanoma targeted radionuclide therapy.

Viallard C, Chezal JM, Mishellany F, Ranchon-Cole I, Pereira B, Herbette A, Besse S, Boudhraa Z, Jacquemot N, Cayre A, Miot-Noirault E, Sun JS, Dutreix M, Degoul F.

Oncotarget. 2016 Mar 15;7(11):12927-36. doi: 10.18632/oncotarget.7340.


Melanoma-targeted delivery system (part 1): design, synthesis and evaluation of releasable disulfide drug by glutathione.

El Aissi R, Chezal JM, Tarrit S, Chavignon O, Moreau E.

Eur J Med Chem. 2015 Aug 28;101:668-80. doi: 10.1016/j.ejmech.2015.06.055. Epub 2015 Jul 13.


99mTc-NTP 15-5 Imaging for Cartilage Involvement in Experimental Rheumatoid Arthritis: Comparison with Routinely Used Molecular Imaging Methods and Sensitivity to Chronic Nonsteroidal Antiinflammatory Drug Treatment.

Khairnar A, Marchand F, Vidal A, Etienne M, Miladi I, Auzeloux P, Cachin F, Eschalier A, Chezal JM, Ardid D, Miot-Noirault E.

J Nucl Med. 2015 May;56(5):798-804. doi: 10.2967/jnumed.114.151415. Epub 2015 Apr 3.


Development of a freeze-dried kit formulation for the preparation of 99mTc-NTP 15-5, a radiotracer for scintigraphic imaging of proteoglycans.

Vidal A, Gaumet V, Galmier MJ, Besse S, Leal F, Gachon F, Viot G, Métin J, Chezal JM, Miot-Noirault E, Auzeloux P.

Appl Radiat Isot. 2015 Jul;101:1-9. doi: 10.1016/j.apradiso.2015.03.010. Epub 2015 Mar 11.


Development and Preliminary Evaluation of TFIB, a New Bimodal Prosthetic Group for Bioactive Molecule Labeling.

Billaud EM, Vidal A, Vincenot A, Besse S, Bouchon B, Debiton E, Miot-Noirault E, Miladi I, Rbah-Vidal L, Auzeloux P, Chezal JM.

ACS Med Chem Lett. 2014 Nov 24;6(2):168-72. doi: 10.1021/ml500423v. eCollection 2015 Feb 12.


Synthesis, radiolabeling and preliminary in vivo evaluation of multimodal radiotracers for PET imaging and targeted radionuclide therapy of pigmented melanoma.

Billaud EM, Maisonial-Besset A, Rbah-Vidal L, Vidal A, Besse S, Béquignat JB, Decombat C, Degoul F, Audin L, Deloye JB, Dollé F, Kuhnast B, Madelmont JC, Tarrit S, Galmier MJ, Borel M, Auzeloux P, Miot-Noirault E, Chezal JM.

Eur J Med Chem. 2015 Mar 6;92:818-38. doi: 10.1016/j.ejmech.2015.01.034. Epub 2015 Jan 21.


[¹²³I]ICF01012 melanoma imaging and [¹³¹I]ICF01012 dosimetry allow adapted internal targeted radiotherapy in preclinical melanoma models.

Viallard C, Perrot Y, Boudhraa Z, Jouberton E, Miot-Noirault E, Bonnet M, Besse S, Mishellany F, Cayre A, Maigne L, Rbah-Vidal L, D'Incan M, Cachin F, Chezal JM, Degoul F.

Eur J Dermatol. 2015 Jan-Feb;25(1):29-35. doi: 10.1684/ejd.2014.2481.


PEGylation enhances the tumor selectivity of melanoma-targeted conjugates.

André M, Besse S, Chezal JM, Mounetou E.

Org Biomol Chem. 2015 Jan 14;13(2):388-97. doi: 10.1039/c4ob01751j. Epub 2014 Nov 3.


Characterization of pro-invasive mechanisms and N-terminal cleavage of ANXA1 in melanoma.

Boudhraa Z, Merle C, Mazzocut D, Chezal JM, Chambon C, Miot-Noirault E, Theisen M, Bouchon B, Degoul F.

Arch Dermatol Res. 2014 Dec;306(10):903-14. doi: 10.1007/s00403-014-1517-z. Epub 2014 Nov 2.


Annexin A1 in primary tumors promotes melanoma dissemination.

Boudhraa Z, Rondepierre F, Ouchchane L, Kintossou R, Trzeciakiewicz A, Franck F, Kanitakis J, Labeille B, Joubert-Zakeyh J, Bouchon B, Perrot JL, Mansard S, Papon J, Dechelotte P, Chezal JM, Miot-Noirault E, Bonnet M, D'Incan M, Degoul F.

Clin Exp Metastasis. 2014 Oct;31(7):749-60. doi: 10.1007/s10585-014-9665-2. Epub 2014 Jul 6.


Small rigid platforms functionalization with quaternary ammonium: targeting extracellular matrix of chondrosarcoma.

Miot-Noirault E, Vidal A, Morlieras J, Bonazza P, Auzeloux P, Besse S, Dauplat MM, Peyrode C, Degoul F, Billotey C, Lux F, Rédini F, Tillement O, Chezal JM, Kryza D, Janier M.

Nanomedicine. 2014 Nov;10(8):1887-95. doi: 10.1016/j.nano.2014.06.011. Epub 2014 Jun 25.


Synthesis and Biological Evaluation of New Quinoxaline Derivatives of ICF01012 as Melanoma-Targeting Probes.

El Aissi R, Liu J, Besse S, Canitrot D, Chavignon O, Chezal JM, Miot-Noirault E, Moreau E.

ACS Med Chem Lett. 2014 Feb 20;5(5):468-73. doi: 10.1021/ml400468x. eCollection 2014 May 8.


Internal dosimetry through GATE simulations of preclinical radiotherapy using a melanin-targeting ligand.

Perrot Y, Degoul F, Auzeloux P, Bonnet M, Cachin F, Chezal JM, Donnarieix D, Labarre P, Moins N, Papon J, Rbah-Vidal L, Vidal A, Miot-Noirault E, Maigne L.

Phys Med Biol. 2014 May 7;59(9):2183-98. doi: 10.1088/0031-9155/59/9/2183. Epub 2014 Apr 8.


Evaluation of two (125)I-radiolabeled acridine derivatives for Auger-electron radionuclide therapy of melanoma.

Gardette M, Viallard C, Paillas S, Guerquin-Kern JL, Papon J, Moins N, Labarre P, Desbois N, Wong-Wah-Chung P, Palle S, Wu TD, Pouget JP, Miot-Noirault E, Chezal JM, Degoul F.

Invest New Drugs. 2014 Aug;32(4):587-97. doi: 10.1007/s10637-014-0086-5. Epub 2014 Apr 2.


(123)I-BZA2 as a melanin-targeted radiotracer for the identification of melanoma metastases: results and perspectives of a multicenter phase III clinical trial.

Cachin F, Miot-Noirault E, Gillet B, Isnardi V, Labeille B, Payoux P, Meyer N, Cammilleri S, Gaudy C, Razzouk-Cadet M, Lacour JP, Granel-Brocard F, Tychyj C, Benbouzid F, Grange JD, Baulieu F, Kelly A, Merlin C, Mestas D, Gachon F, Chezal JM, Degoul F, D'Incan M.

J Nucl Med. 2014 Jan;55(1):15-22. doi: 10.2967/jnumed.113.123554. Epub 2013 Nov 21.


Synthesis, radiofluorination, and in vivo evaluation of novel fluorinated and iodinated radiotracers for PET imaging and targeted radionuclide therapy of melanoma.

Billaud EM, Rbah-Vidal L, Vidal A, Besse S, Tarrit S, Askienazy S, Maisonial A, Moins N, Madelmont JC, Miot-Noirault E, Chezal JM, Auzeloux P.

J Med Chem. 2013 Nov 14;56(21):8455-67. doi: 10.1021/jm400877v. Epub 2013 Oct 21.


Spacer optimization of new conjugates for a melanoma-selective delivery approach.

André M, Tarrit S, Couret MJ, Galmier MJ, Débiton E, Chezal JM, Mounetou E.

Org Biomol Chem. 2013 Oct 7;11(37):6372-84. doi: 10.1039/c3ob41428k.


99mTc-NTP 15-5 assessment of the early therapeutic response of chondrosarcoma to zoledronic acid in the Swarm rat orthotopic model.

Miot-Noirault E, David E, Vidal A, Peyrode C, Besse S, Dauplat MM, Heymann MF, Gouin F, Chezal JM, Heymann D, Rédini F.

EJNMMI Res. 2013 May 20;3(1):40. doi: 10.1186/2191-219X-3-40.


Synthesis, radioiodination and in vivo screening of novel potent iodinated and fluorinated radiotracers as melanoma imaging and therapeutic probes.

Maisonial A, Billaud EM, Besse S, Rbah-Vidal L, Papon J, Audin L, Bayle M, Galmier MJ, Tarrit S, Borel M, Askienazy S, Madelmont JC, Moins N, Auzeloux P, Miot-Noirault E, Chezal JM.

Eur J Med Chem. 2013 May;63:840-53. doi: 10.1016/j.ejmech.2012.11.047. Epub 2013 Mar 24.


In vivo evidence of the targeting of cartilaginous tissue by pyridinium functionalized nanoparticles.

Morlieras J, Chezal JM, Miot-Noirault E, Vidal A, Besse S, Kryza D, Truillet C, Mignot A, Antoine R, Dugourd P, Redini F, Sancey L, Lux F, Perriat P, Janier M, Tillement O.

Chem Commun (Camb). 2013 Apr 14;49(29):3046-8. doi: 10.1039/c3cc39106j.


In vivo efficacy of melanoma internal radionuclide therapy with a 131I-labelled melanin-targeting heteroarylcarboxamide molecule.

Degoul F, Borel M, Jacquemot N, Besse S, Communal Y, Mishellany F, Papon J, Penault-Llorca F, Donnarieix D, Doly M, Maigne L, Miot-Noirault E, Cayre A, Cluzel J, Moins N, Chezal JM, Bonnet M.

Int J Cancer. 2013 Sep 1;133(5):1042-53. doi: 10.1002/ijc.28103. Epub 2013 Mar 18.


Development of gadolinium based nanoparticles having an affinity towards melanin.

Morlieras J, Chezal JM, Miot-Noirault E, Roux A, Heinrich-Balard L, Cohen R, Tarrit S, Truillet C, Mignot A, Hachani R, Kryza D, Antoine R, Dugourd P, Perriat P, Janier M, Sancey L, Lux F, Tillement O.

Nanoscale. 2013 Feb 21;5(4):1603-15. doi: 10.1039/c2nr33457g.


Early detection and longitudinal monitoring of experimental primary and disseminated melanoma using [¹⁰F]ICF01006, a highly promising melanoma PET tracer.

Rbah-Vidal L, Vidal A, Besse S, Cachin F, Bonnet M, Audin L, Askienazy S, Dollé F, Degoul F, Miot-Noirault E, Moins N, Auzeloux P, Chezal JM.

Eur J Nucl Med Mol Imaging. 2012 Sep;39(9):1449-61. doi: 10.1007/s00259-012-2168-y. Epub 2012 Jun 16.


Imidazonaphthyridine systems (part 2): Functionalization of the phenyl ring linked to the pyridine pharmacophore and its replacement by a pyridinone ring produces intriguing differences in cytocidal activity.

Masurier N, Debiton E, Jacquemet A, Bussière A, Chezal JM, Ollivier A, Tétégan D, Andaloussi M, Galmier MJ, Lacroix J, Canitrot D, Teulade JC, Gaudreault RC, Chavignon O, Moreau E.

Eur J Med Chem. 2012 Jun;52:137-50. doi: 10.1016/j.ejmech.2012.03.011. Epub 2012 Mar 20.


In vivo experimental imaging of osteochondral defects and their healing using (99m)Tc-NTP 15-5 radiotracer.

Miot-Noirault E, Guicheux J, Vidal A, Gauthier O, Auzeloux P, Lesoeur J, Cachin F, Askienazy S, Chezal JM, Vinatier C.

Eur J Nucl Med Mol Imaging. 2012 Jul;39(7):1169-72. doi: 10.1007/s00259-012-2081-4. Epub 2012 Mar 8.


In vivo scintigraphic imaging of proteoglycans.

Miot-Noirault E, Vidal A, Auzeloux P, Peyrode C, Madelmont JC, Chezal JM.

Methods Mol Biol. 2012;836:183-98. doi: 10.1007/978-1-61779-498-8_13.


Relevance of the POS-1 orthotopic model as an "imaging model" for in vivo and simultaneous monitoring of tumor proliferation and bone remodeling in osteosarcoma.

Miot-Noirault E, Gouin F, Dauplat MM, Heymann D, Chezal JM, Redini F.

Cancer Biother Radiopharm. 2012 Feb;27(1):96-103. doi: 10.1089/cbr.2011.1059. Epub 2012 Jan 4.


New aldehyde and vinylsulfone proteasome inhibitors for targeted melanoma therapy.

Vivier M, Rapp M, Galmier MJ, Jarrousse AS, Miot-Noirault E, Leal F, Weber V, Métin J, Sauzière J, Chezal JM, Madelmont JC.

Eur J Med Chem. 2011 Nov;46(11):5705-10. doi: 10.1016/j.ejmech.2011.07.037. Epub 2011 Jul 27.


First ex vivo study demonstrating that 99mTc-NTP 15-5 radiotracer binds to human articular cartilage.

Cachin F, Boisgard S, Vidal A, Filaire M, Auzeloux P, Culot D, Askienazy S, Madelmont JC, Chezal JM, Miot-Noirault E.

Eur J Nucl Med Mol Imaging. 2011 Nov;38(11):2077-82. doi: 10.1007/s00259-011-1890-1. Epub 2011 Aug 4.


Design, synthesis and in vitro drug release investigation of new potential 5-FU prodrugs.

Daumar P, Decombat C, Chezal JM, Debiton E, Madesclaire M, Coudert P, Galmier MJ.

Eur J Med Chem. 2011 Jul;46(7):2867-79. doi: 10.1016/j.ejmech.2011.04.010. Epub 2011 Apr 14.


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