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2 results on '"Moniot, Sébastien"'

1. SIRT2- and NRF2-Targeting Thiazole-Containing Compound with Therapeutic Activity in Huntington's Disease Models.

Author

Quinti, Luisa, Quinti, Luisa, Casale, Malcolm, Moniot, Sébastien, Pais, Teresa F, Van Kanegan, Michael J, Kaltenbach, Linda S, Pallos, Judit, Lim, Ryan G, Naidu, Sharadha Dayalan, Runne, Heike, Meisel, Lisa, Rauf, Nazifa Abdul, Leyfer, Dmitriy, Maxwell, Michele M, Saiah, Eddine, Landers, John E, Luthi-Carter, Ruth, Abagyan, Ruben, Dinkova-Kostova, Albena T, Steegborn, Clemens, Marsh, J Lawrence, Lo, Donald C, Thompson, Leslie M, Kazantsev, Aleksey G, Quinti, Luisa, Quinti, Luisa, Casale, Malcolm, Moniot, Sébastien, Pais, Teresa F, Van Kanegan, Michael J, Kaltenbach, Linda S, Pallos, Judit, Lim, Ryan G, Naidu, Sharadha Dayalan, Runne, Heike, Meisel, Lisa, Rauf, Nazifa Abdul, Leyfer, Dmitriy, Maxwell, Michele M, Saiah, Eddine, Landers, John E, Luthi-Carter, Ruth, Abagyan, Ruben, Dinkova-Kostova, Albena T, Steegborn, Clemens, Marsh, J Lawrence, Lo, Donald C, Thompson, Leslie M, and Kazantsev, Aleksey G

Abstract

There are currently no disease-modifying therapies for the neurodegenerative disorder Huntington's disease (HD). This study identified novel thiazole-containing inhibitors of the deacetylase sirtuin-2 (SIRT2) with neuroprotective activity in ex vivo brain slice and Drosophila models of HD. A systems biology approach revealed an additional SIRT2-independent property of the lead-compound, MIND4, as an inducer of cytoprotective NRF2 (nuclear factor-erythroid 2 p45-derived factor 2) activity. Structure-activity relationship studies further identified a potent NRF2 activator (MIND4-17) lacking SIRT2 inhibitory activity. MIND compounds induced NRF2 activation responses in neuronal and non-neuronal cells and reduced production of reactive oxygen species and nitrogen intermediates. These drug-like thiazole-containing compounds represent an exciting opportunity for development of multi-targeted agents with potentially synergistic therapeutic benefits in HD and related disorders.

Published
2016

2. SIRT2- and NRF2-Targeting Thiazole-Containing Compound with Therapeutic Activity in Huntington's Disease Models.

Author

Quinti, Luisa, Quinti, Luisa, Casale, Malcolm, Moniot, Sébastien, Pais, Teresa F, Van Kanegan, Michael J, Kaltenbach, Linda S, Pallos, Judit, Lim, Ryan G, Naidu, Sharadha Dayalan, Runne, Heike, Meisel, Lisa, Rauf, Nazifa Abdul, Leyfer, Dmitriy, Maxwell, Michele M, Saiah, Eddine, Landers, John E, Luthi-Carter, Ruth, Abagyan, Ruben, Dinkova-Kostova, Albena T, Steegborn, Clemens, Marsh, J Lawrence, Lo, Donald C, Thompson, Leslie M, Kazantsev, Aleksey G, Quinti, Luisa, Quinti, Luisa, Casale, Malcolm, Moniot, Sébastien, Pais, Teresa F, Van Kanegan, Michael J, Kaltenbach, Linda S, Pallos, Judit, Lim, Ryan G, Naidu, Sharadha Dayalan, Runne, Heike, Meisel, Lisa, Rauf, Nazifa Abdul, Leyfer, Dmitriy, Maxwell, Michele M, Saiah, Eddine, Landers, John E, Luthi-Carter, Ruth, Abagyan, Ruben, Dinkova-Kostova, Albena T, Steegborn, Clemens, Marsh, J Lawrence, Lo, Donald C, Thompson, Leslie M, and Kazantsev, Aleksey G

Abstract

There are currently no disease-modifying therapies for the neurodegenerative disorder Huntington's disease (HD). This study identified novel thiazole-containing inhibitors of the deacetylase sirtuin-2 (SIRT2) with neuroprotective activity in ex vivo brain slice and Drosophila models of HD. A systems biology approach revealed an additional SIRT2-independent property of the lead-compound, MIND4, as an inducer of cytoprotective NRF2 (nuclear factor-erythroid 2 p45-derived factor 2) activity. Structure-activity relationship studies further identified a potent NRF2 activator (MIND4-17) lacking SIRT2 inhibitory activity. MIND compounds induced NRF2 activation responses in neuronal and non-neuronal cells and reduced production of reactive oxygen species and nitrogen intermediates. These drug-like thiazole-containing compounds represent an exciting opportunity for development of multi-targeted agents with potentially synergistic therapeutic benefits in HD and related disorders.

Published
2016

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