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Items: 1 to 20 of 101

1.

Identification of Diketopiperazine-Containing 2-Anilinobenzamides as Potent Sirtuin 2 (SIRT2)-Selective Inhibitors Targeting the "Selectivity Pocket", Substrate-Binding Site, and NAD+-Binding Site.

Mellini P, Itoh Y, Elboray EE, Tsumoto H, Li Y, Suzuki M, Takahashi Y, Tojo T, Kurohara T, Miyake Y, Miura Y, Kitao Y, Kotoku M, Iida T, Suzuki T.

J Med Chem. 2019 Jun 27;62(12):5844-5862. doi: 10.1021/acs.jmedchem.9b00255. Epub 2019 Jun 12.

PMID:
31144814
2.

Potent mechanism-based sirtuin-2-selective inhibition by an in situ-generated occupant of the substrate-binding site, "selectivity pocket" and NAD+-binding site.

Mellini P, Itoh Y, Tsumoto H, Li Y, Suzuki M, Tokuda N, Kakizawa T, Miura Y, Takeuchi J, Lahtela-Kakkonen M, Suzuki T.

Chem Sci. 2017 Sep 1;8(9):6400-6408. doi: 10.1039/c7sc02738a. Epub 2017 Jul 21.

3.

Design, synthesis, and biological activity of a novel series of human sirtuin-2-selective inhibitors.

Suzuki T, Khan MN, Sawada H, Imai E, Itoh Y, Yamatsuta K, Tokuda N, Takeuchi J, Seko T, Nakagawa H, Miyata N.

J Med Chem. 2012 Jun 28;55(12):5760-73. doi: 10.1021/jm3002108. Epub 2012 Jun 12.

PMID:
22642300
4.

Identification of a novel small molecule that inhibits deacetylase but not defatty-acylase reaction catalysed by SIRT2.

Kudo N, Ito A, Arata M, Nakata A, Yoshida M.

Philos Trans R Soc Lond B Biol Sci. 2018 Jun 5;373(1748). pii: 20170070. doi: 10.1098/rstb.2017.0070.

5.

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.

PMID:
28240897
6.

X-ray crystal structure guided discovery of new selective, substrate-mimicking sirtuin 2 inhibitors that exhibit activities against non-small cell lung cancer cells.

Yang LL, Wang HL, Zhong L, Yuan C, Liu SY, Yu ZJ, Liu S, Yan YH, Wu C, Wang Y, Wang Z, Yu Y, Chen Q, Li GB.

Eur J Med Chem. 2018 Jul 15;155:806-823. doi: 10.1016/j.ejmech.2018.06.041. Epub 2018 Jun 19.

PMID:
29957526
7.

Selective Sirt2 inhibition by ligand-induced rearrangement of the active site.

Rumpf T, Schiedel M, Karaman B, Roessler C, North BJ, Lehotzky A, Oláh J, Ladwein KI, Schmidtkunz K, Gajer M, Pannek M, Steegborn C, Sinclair DA, Gerhardt S, Ovádi J, Schutkowski M, Sippl W, Einsle O, Jung M.

Nat Commun. 2015 Feb 12;6:6263. doi: 10.1038/ncomms7263.

8.

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.

9.

Discovery of potent and selective sirtuin 2 (SIRT2) inhibitors using a fragment-based approach.

Cui H, Kamal Z, Ai T, Xu Y, More SS, Wilson DJ, Chen L.

J Med Chem. 2014 Oct 23;57(20):8340-57. doi: 10.1021/jm500777s. Epub 2014 Oct 2.

PMID:
25275824
10.

Discovery of 2-((4,6-dimethylpyrimidin-2-yl)thio)-N-phenylacetamide derivatives as new potent and selective human sirtuin 2 inhibitors.

Yang L, Ma X, Yuan C, He Y, Li L, Fang S, Xia W, He T, Qian S, Xu Z, Li G, Wang Z.

Eur J Med Chem. 2017 Jul 7;134:230-241. doi: 10.1016/j.ejmech.2017.04.010. Epub 2017 Apr 12.

PMID:
28415012
11.

Insight into the Mechanism of Intramolecular Inhibition of the Catalytic Activity of Sirtuin 2 (SIRT2).

Li J, Flick F, Verheugd P, Carloni P, Lüscher B, Rossetti G.

PLoS One. 2015 Sep 25;10(9):e0139095. doi: 10.1371/journal.pone.0139095. eCollection 2015.

12.

Design, synthesis and structure-activity relationship studies of novel sirtuin 2 (SIRT2) inhibitors with a benzamide skeleton.

Sakai T, Matsumoto Y, Ishikawa M, Sugita K, Hashimoto Y, Wakai N, Kitao A, Morishita E, Toyoshima C, Hayashi T, Akiyama T.

Bioorg Med Chem. 2015 Jan 15;23(2):328-39. doi: 10.1016/j.bmc.2014.11.027. Epub 2014 Dec 2.

PMID:
25515955
13.

Identification of a Selective SIRT2 Inhibitor and Its Anti-breast Cancer Activity.

Shah AA, Ito A, Nakata A, Yoshida M.

Biol Pharm Bull. 2016;39(10):1739-1742.

14.

Molecular modeling study for conformational changes of Sirtuin 2 due to substrate and inhibitor binding.

Sakkiah S, Chandrasekaran M, Lee Y, Kim S, Lee KW.

J Biomol Struct Dyn. 2012;30(3):235-54. doi: 10.1080/07391102.2012.680026. Epub 2012 Jun 12.

PMID:
22694102
15.

Opening the Selectivity Pocket in the Human Lysine Deacetylase Sirtuin2 - New Opportunities, New Questions.

Robaa D, Monaldi D, Wössner N, Kudo N, Rumpf T, Schiedel M, Yoshida M, Jung M.

Chem Rec. 2018 Dec;18(12):1701-1707. doi: 10.1002/tcr.201800044. Epub 2018 Jun 21. Review.

PMID:
29931800
16.

Chroman-4-one- and chromone-based sirtuin 2 inhibitors with antiproliferative properties in cancer cells.

Seifert T, Malo M, Kokkola T, Engen K, Fridén-Saxin M, Wallén EA, Lahtela-Kakkonen M, Jarho EM, Luthman K.

J Med Chem. 2014 Dec 11;57(23):9870-88. doi: 10.1021/jm500930h. Epub 2014 Dec 2.

PMID:
25383691
17.

Identification of inhibitor binding site in human sirtuin 2 using molecular docking and dynamics simulations.

Sakkiah S, Arooj M, Kumar MR, Eom SH, Lee KW.

PLoS One. 2013;8(1):e51429. doi: 10.1371/journal.pone.0051429. Epub 2013 Jan 28.

18.

Discovery of New SIRT2 Inhibitors by Utilizing a Consensus Docking/Scoring Strategy and Structure-Activity Relationship Analysis.

Huang S, Song C, Wang X, Zhang G, Wang Y, Jiang X, Sun Q, Huang L, Xiang R, Hu Y, Li L, Yang S.

J Chem Inf Model. 2017 Apr 24;57(4):669-679. doi: 10.1021/acs.jcim.6b00714. Epub 2017 Mar 28.

PMID:
28301150
19.

Identification of novel SIRT2-selective inhibitors using a click chemistry approach.

Tatum PR, Sawada H, Ota Y, Itoh Y, Zhan P, Ieda N, Nakagawa H, Miyata N, Suzuki T.

Bioorg Med Chem Lett. 2014 Apr 15;24(8):1871-4. doi: 10.1016/j.bmcl.2014.03.026. Epub 2014 Mar 20.

PMID:
24675380
20.

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.

PMID:
25395356

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