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Items: 24


KEAP1-modifying small molecule reveals muted NRF2 signaling responses in neural stem cells from Huntington's disease patients.

Quinti L, Dayalan Naidu S, Träger U, Chen X, Kegel-Gleason K, Llères D, Connolly C, Chopra V, Low C, Moniot S, Sapp E, Tousley AR, Vodicka P, Van Kanegan MJ, Kaltenbach LS, Crawford LA, Fuszard M, Higgins M, Miller JRC, Farmer RE, Potluri V, Samajdar S, Meisel L, Zhang N, Snyder A, Stein R, Hersch SM, Ellerby LM, Weerapana E, Schwarzschild MA, Steegborn C, Leavitt BR, Degterev A, Tabrizi SJ, Lo DC, DiFiglia M, Thompson LM, Dinkova-Kostova AT, Kazantsev AG.

Proc Natl Acad Sci U S A. 2017 Jun 6;114(23):E4676-E4685. doi: 10.1073/pnas.1614943114. Epub 2017 May 22.


Correction: The mechanism of sirtuin 2-mediated exacerbation of alpha-synuclein toxicity in models of Parkinson disease.

de Oliveira RM, Vicente Miranda H, Francelle L, Pinho R, Szegö ÉM, Martinho R, Munari F, Lázaro DF, Moniot S, Guerreiro P, Fonseca-Ornelas L, Marijanovic Z, Antas P, Gerhardt E, Enguita FJ, Fauvet B, Penque D, Pais TF, Tong Q, Becker S, Kügler S, Lashuel HA, Steegborn C, Zweckstetter M, Outeiro TF.

PLoS Biol. 2017 Apr 5;15(4):e1002601. doi: 10.1371/journal.pbio.1002601. eCollection 2017 Apr.


A conserved NAD+ binding pocket that regulates protein-protein interactions during aging.

Li J, Bonkowski MS, Moniot S, Zhang D, Hubbard BP, Ling AJ, Rajman LA, Qin B, Lou Z, Gorbunova V, Aravind L, Steegborn C, Sinclair DA.

Science. 2017 Mar 24;355(6331):1312-1317. doi: 10.1126/science.aad8242.


The mechanism of sirtuin 2-mediated exacerbation of alpha-synuclein toxicity in models of Parkinson disease.

de Oliveira RM, Vicente Miranda H, Francelle L, Pinho R, Szegö ÉM, Martinho R, Munari F, Lázaro DF, Moniot S, Guerreiro P, Fonseca-Ornelas L, Marijanovic Z, Antas P, Gerhardt E, Enguita FJ, Fauvet B, Penque D, Pais TF, Tong Q, Becker S, Kügler S, Lashuel HA, Steegborn C, Zweckstetter M, Outeiro TF.

PLoS Biol. 2017 Mar 3;15(3):e2000374. doi: 10.1371/journal.pbio.2000374. eCollection 2017 Mar. Erratum in: PLoS Biol. 2017 Apr 5;15(4):e1002601.


Development of 1,2,4-Oxadiazoles as Potent and Selective Inhibitors of the Human Deacetylase Sirtuin 2: Structure-Activity Relationship, X-ray Crystal Structure, and Anticancer Activity.

Moniot S, Forgione M, Lucidi A, Hailu GS, Nebbioso A, Carafa V, Baratta F, Altucci L, Giacché N, Passeri D, Pellicciari R, Mai A, Steegborn C, Rotili D.

J Med Chem. 2017 Mar 23;60(6):2344-2360. doi: 10.1021/acs.jmedchem.6b01609. Epub 2017 Mar 14.


Thienopyrimidinone Based Sirtuin-2 (SIRT2)-Selective Inhibitors Bind in the Ligand Induced Selectivity Pocket.

Sundriyal S, Moniot S, Mahmud Z, Yao S, Di Fruscia P, Reynolds CR, Dexter DT, Sternberg MJ, Lam EW, Steegborn C, Fuchter MJ.

J Med Chem. 2017 Mar 9;60(5):1928-1945. doi: 10.1021/acs.jmedchem.6b01690. Epub 2017 Feb 15.


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

Quinti L, Casale M, Moniot S, Pais TF, Van Kanegan MJ, Kaltenbach LS, Pallos J, Lim RG, Naidu SD, Runne H, Meisel L, Rauf NA, Leyfer D, Maxwell MM, Saiah E, Landers JE, Luthi-Carter R, Abagyan R, Dinkova-Kostova AT, Steegborn C, Marsh JL, Lo DC, Thompson LM, Kazantsev AG.

Cell Chem Biol. 2016 Jul 21;23(7):849-861. doi: 10.1016/j.chembiol.2016.05.015. Epub 2016 Jul 14.


1,4-Dihydropyridines Active on the SIRT1/AMPK Pathway Ameliorate Skin Repair and Mitochondrial Function and Exhibit Inhibition of Proliferation in Cancer Cells.

Valente S, Mellini P, Spallotta F, Carafa V, Nebbioso A, Polletta L, Carnevale I, Saladini S, Trisciuoglio D, Gabellini C, Tardugno M, Zwergel C, Cencioni C, Atlante S, Moniot S, Steegborn C, Budriesi R, Tafani M, Del Bufalo D, Altucci L, Gaetano C, Mai A.

J Med Chem. 2016 Feb 25;59(4):1471-91. doi: 10.1021/acs.jmedchem.5b01117. Epub 2016 Jan 5.


The sirtuin-2 inhibitor AK7 is neuroprotective in models of Parkinson's disease but not amyotrophic lateral sclerosis and cerebral ischemia.

Chen X, Wales P, Quinti L, Zuo F, Moniot S, Herisson F, Rauf NA, Wang H, Silverman RB, Ayata C, Maxwell MM, Steegborn C, Schwarzschild MA, Outeiro TF, Kazantsev AG.

PLoS One. 2015 Jan 21;10(1):e0116919. doi: 10.1371/journal.pone.0116919. eCollection 2015.


The discovery of a highly selective 5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidin-4(3H)-one SIRT2 inhibitor that is neuroprotective in an in vitro Parkinson's disease model.

Di Fruscia P, Zacharioudakis E, Liu C, Moniot S, Laohasinnarong S, Khongkow M, Harrison IF, Koltsida K, Reynolds CR, Schmidtkunz K, Jung M, Chapman KL, Steegborn C, Dexter DT, Sternberg MJ, Lam EW, Fuchter MJ.

ChemMedChem. 2015 Jan;10(1):69-82. doi: 10.1002/cmdc.201402431. Epub 2014 Nov 13.


Crystal structures of human soluble adenylyl cyclase reveal mechanisms of catalysis and of its activation through bicarbonate.

Kleinboelting S, Diaz A, Moniot S, van den Heuvel J, Weyand M, Levin LR, Buck J, Steegborn C.

Proc Natl Acad Sci U S A. 2014 Mar 11;111(10):3727-32. doi: 10.1073/pnas.1322778111. Epub 2014 Feb 24.


Molecular architecture of the human protein deacetylase Sirt1 and its regulation by AROS and resveratrol.

Lakshminarasimhan M, Curth U, Moniot S, Mosalaganti S, Raunser S, Steegborn C.

Biosci Rep. 2013 May 15;33(3). pii: e00037. doi: 10.1042/BSR20120121.


Crystal structure analysis of human Sirt2 and its ADP-ribose complex.

Moniot S, Schutkowski M, Steegborn C.

J Struct Biol. 2013 May;182(2):136-43. doi: 10.1016/j.jsb.2013.02.012. Epub 2013 Feb 26.


Crystallization and preliminary crystal structure analysis of the ligand-binding domain of PqsR (MvfR), the Pseudomonas quinolone signal (PQS) responsive quorum-sensing transcription factor of Pseudomonas aeruginosa.

Xu N, Yu S, Moniot S, Weyand M, Blankenfeldt W.

Acta Crystallogr Sect F Struct Biol Cryst Commun. 2012 Sep 1;68(Pt 9):1034-9. doi: 10.1107/S1744309112032538. Epub 2012 Aug 30.


Structures, substrates, and regulators of Mammalian sirtuins - opportunities and challenges for drug development.

Moniot S, Weyand M, Steegborn C.

Front Pharmacol. 2012 Feb 9;3:16. doi: 10.3389/fphar.2012.00016. eCollection 2012.


Crystal structures of N-acetylmannosamine kinase provide insights into enzyme activity and inhibition.

Martinez J, Nguyen LD, Hinderlich S, Zimmer R, Tauberger E, Reutter W, Saenger W, Fan H, Moniot S.

J Biol Chem. 2012 Apr 20;287(17):13656-65. doi: 10.1074/jbc.M111.318170. Epub 2012 Feb 16.


Crystal structures of receptors involved in small molecule transport across membranes.

Bulut H, Ma Q, Moniot S, Saenger W, Schneider E, Vahedi-Faridi A.

Eur J Cell Biol. 2012 Apr;91(4):318-25. doi: 10.1016/j.ejcb.2011.12.004. Epub 2012 Feb 16. Review.


Crystal structures of two solute receptors for L-cystine and L-cysteine, respectively, of the human pathogen Neisseria gonorrhoeae.

Bulut H, Moniot S, Licht A, Scheffel F, Gathmann S, Saenger W, Schneider E.

J Mol Biol. 2012 Jan 20;415(3):560-72. doi: 10.1016/j.jmb.2011.11.030. Epub 2011 Nov 23.


Elucidation of the phosphate binding mode of DING proteins revealed by subangstrom X-ray crystallography.

Liebschner D, Elias M, Moniot S, Fournier B, Scott K, Jelsch C, Guillot B, Lecomte C, Chabrière E.

J Am Chem Soc. 2009 Jun 10;131(22):7879-86. doi: 10.1021/ja901900y.


Structural basis for natural lactonase and promiscuous phosphotriesterase activities.

Elias M, Dupuy J, Merone L, Mandrich L, Porzio E, Moniot S, Rochu D, Lecomte C, Rossi M, Masson P, Manco G, Chabriere E.

J Mol Biol. 2008 Jun 20;379(5):1017-28. doi: 10.1016/j.jmb.2008.04.022. Epub 2008 Apr 16.


Trapping of the thioacylglyceraldehyde-3-phosphate dehydrogenase intermediate from Bacillus stearothermophilus. Direct evidence for a flip-flop mechanism.

Moniot S, Bruno S, Vonrhein C, Didierjean C, Boschi-Muller S, Vas M, Bricogne G, Branlant G, Mozzarelli A, Corbier C.

J Biol Chem. 2008 Aug 1;283(31):21693-702. doi: 10.1074/jbc.M802286200. Epub 2008 May 14.


Crystallization, diffraction data collection and preliminary crystallographic analysis of DING protein from Pseudomonas fluorescens.

Moniot S, Elias M, Kim D, Scott K, Chabriere E.

Acta Crystallogr Sect F Struct Biol Cryst Commun. 2007 Jul 1;63(Pt 7):590-2. Epub 2007 Jun 15.


Structure-function relationships in a bacterial DING protein.

Ahn S, Moniot S, Elias M, Chabriere E, Kim D, Scott K.

FEBS Lett. 2007 Jul 24;581(18):3455-60. Epub 2007 Jun 27.


The topical anti-inflammatory effects of a topical preparation of meclofenamic acid on carrageenan-induced footpad swelling in mice.

Schrier DJ, Moniot S, Gluckman MI, Gilbertsen RB.

J Pharm Pharmacol. 1987 Jan;39(1):57-9.


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