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Development of a series of aryl pyrimidine kynurenine monooxygenase inhibitors as potential therapeutic agents for the treatment of Huntington's disease.
Toledo-Sherman LM, Prime ME, Mrzljak L, Beconi MG, Beresford A, Brookfield FA, Brown CJ, Cardaun I, Courtney SM, Dijkman U, Hamelin-Flegg E, Johnson PD, Kempf V, Lyons K, Matthews K, Mitchell WL, O'Connell C, Pena P, Powell K, Rassoulpour A, Reed L, Reindl W, Selvaratnam S, Friley WW, Weddell DA, Went NE, Wheelan P, Winkler C, Winkler D, Wityak J, Yarnold CJ, Yates D, Munoz-Sanjuan I, Dominguez C. Toledo-Sherman LM, et al. Among authors: mrzljak l. J Med Chem. 2015 Feb 12;58(3):1159-83. doi: 10.1021/jm501350y. Epub 2015 Jan 23. J Med Chem. 2015. PMID: 25590515
Imaging Mutant Huntingtin Aggregates: Development of a Potential PET Ligand.
Liu L, Prime ME, Lee MR, Khetarpal V, Brown CJ, Johnson PD, Miranda-Azpiazu P, Chen X, Clark-Frew D, Coe S, Davis R, Dickie A, Ebneth A, Esposito S, Gadouleau E, Gai X, Galan S, Green S, Greenaway C, Giles P, Halldin C, Hayes S, Herbst T, Herrmann F, Heßmann M, Jia Z, Kiselyov A, Kotey A, Krulle T, Mangette JE, Marston RW, Menta S, Mills MR, Monteagudo E, Nag S, Nibbio M, Orsatti L, Schaertl S, Scheich C, Sproston J, Stepanov V, Svedberg M, Takano A, Taylor M, Thomas W, Toth M, Vaidya D, Vanräs K, Weddell D, Wigginton I, Wityak J, Mrzljak L, Munoz-Sanjuan I, Bard JA, Dominguez C. Liu L, et al. Among authors: mrzljak l. J Med Chem. 2020 Aug 13;63(15):8608-8633. doi: 10.1021/acs.jmedchem.0c00955. Epub 2020 Jul 30. J Med Chem. 2020. PMID: 32662649
[11C]CHDI-626, a PET Tracer Candidate for Imaging Mutant Huntingtin Aggregates with Reduced Binding to AD Pathological Proteins.
Liu L, Johnson PD, Prime ME, Khetarpal V, Lee MR, Brown CJ, Chen X, Clark-Frew D, Coe S, Conlon M, Davis R, Ensor S, Esposito S, Moren AF, Gai X, Green S, Greenaway C, Haber J, Halldin C, Hayes S, Herbst T, Herrmann F, Heßmann M, Hsai MM, Kotey A, Mangette JE, Mills MR, Monteagudo E, Nag S, Nibbio M, Orsatti L, Schaertl S, Scheich C, Sproston J, Stepanov V, Varnäs K, Varrone A, Wityak J, Mrzljak L, Munoz-Sanjuan I, Bard JA, Dominguez C. Liu L, et al. Among authors: mrzljak l. J Med Chem. 2021 Aug 26;64(16):12003-12021. doi: 10.1021/acs.jmedchem.1c00667. Epub 2021 Aug 5. J Med Chem. 2021. PMID: 34351166
Therapeutic Strategies for Huntington's Disease.
Mrzljak L, Munoz-Sanjuan I. Mrzljak L, et al. Curr Top Behav Neurosci. 2015;22:161-201. doi: 10.1007/7854_2013_250. Curr Top Behav Neurosci. 2015. PMID: 24277342 Review.
The novel KMO inhibitor CHDI-340246 leads to a restoration of electrophysiological alterations in mouse models of Huntington's disease.
Beaumont V, Mrzljak L, Dijkman U, Freije R, Heins M, Rassoulpour A, Tombaugh G, Gelman S, Bradaia A, Steidl E, Gleyzes M, Heikkinen T, Lehtimäki K, Puoliväli J, Kontkanen O, Javier RM, Neagoe I, Deisemann H, Winkler D, Ebneth A, Khetarpal V, Toledo-Sherman L, Dominguez C, Park LC, Munoz-Sanjuan I. Beaumont V, et al. Among authors: mrzljak l. Exp Neurol. 2016 Aug;282:99-118. doi: 10.1016/j.expneurol.2016.05.005. Epub 2016 May 6. Exp Neurol. 2016. PMID: 27163548
Development of a ligand for in vivo imaging of mutant huntingtin in Huntington's disease.
Bertoglio D, Bard J, Hessmann M, Liu L, Gärtner A, De Lombaerde S, Huscher B, Zajicek F, Miranda A, Peters F, Herrmann F, Schaertl S, Vasilkovska T, Brown CJ, Johnson PD, Prime ME, Mills MR, Van der Linden A, Mrzljak L, Khetarpal V, Wang Y, Marchionini DM, Skinbjerg M, Verhaeghe J, Dominguez C, Staelens S, Munoz-Sanjuan I. Bertoglio D, et al. Among authors: mrzljak l. Sci Transl Med. 2022 Feb 2;14(630):eabm3682. doi: 10.1126/scitranslmed.abm3682. Epub 2022 Feb 2. Sci Transl Med. 2022. PMID: 35108063
Longitudinal Small-Animal PET Imaging of the zQ175 Mouse Model of Huntington Disease Shows In Vivo Changes of Molecular Targets in the Striatum and Cerebral Cortex.
Häggkvist J, Tóth M, Tari L, Varnäs K, Svedberg M, Forsberg A, Nag S, Dominguez C, Munoz-Sanjuan I, Bard J, Wityak J, Varrone A, Halldin C, Mrzljak L. Häggkvist J, et al. Among authors: mrzljak l. J Nucl Med. 2017 Apr;58(4):617-622. doi: 10.2967/jnumed.116.180497. Epub 2016 Nov 10. J Nucl Med. 2017. PMID: 27856625 Free article.
Synaptic Vesicle Glycoprotein 2A Is Affected in the Central Nervous System of Mice with Huntington Disease and in the Brain of a Human with Huntington Disease Postmortem.
Bertoglio D, Verhaeghe J, Wyffels L, Miranda A, Stroobants S, Mrzljak L, Dominguez C, Skinbjerg M, Bard J, Liu L, Munoz-Sanjuan I, Staelens S. Bertoglio D, et al. Among authors: mrzljak l. J Nucl Med. 2022 Jun;63(6):942-947. doi: 10.2967/jnumed.121.262709. Epub 2021 Sep 16. J Nucl Med. 2022. PMID: 34531262 Free PMC article.
Longitudinal preclinical evaluation of the novel radioligand [11C]CHDI-626 for PET imaging of mutant huntingtin aggregates in Huntington's disease.
Bertoglio D, Verhaeghe J, Miranda A, Wyffels L, Stroobants S, Mrzljak L, Khetarpal V, Skinbjerg M, Liu L, Dominguez C, Munoz-Sanjuan I, Bard J, Staelens S. Bertoglio D, et al. Among authors: mrzljak l. Eur J Nucl Med Mol Imaging. 2022 Mar;49(4):1166-1175. doi: 10.1007/s00259-021-05578-8. Epub 2021 Oct 15. Eur J Nucl Med Mol Imaging. 2022. PMID: 34651228 Free PMC article.
57 results