-
1
-
-
84861852370
-
Are sirtuins viable targets for improving healthspan and lifespan?
-
Bauer, J. A.; Ungvari, Z.; Minor, R. K.; Le Couteur, D. G.; de Cabo, R. Are sirtuins viable targets for improving healthspan and lifespan? Nat. Rev. Drug Disc., 2012, 11, 443-461.
-
(2012)
Nat. Rev. Drug Disc.
, vol.11
, pp. 443-461
-
-
Bauer, J.A.1
Ungvari, Z.2
Minor, R.K.3
Le Couteur, D.G.4
De Cabo, R.5
-
2
-
-
65549118773
-
Circadian control of the NAD+ salvage pathway by CLOCKSIRT1
-
Nakahata, Y.; Sahar, S.; Astarita, G.; Kaluzova, M.; Sassone-Corsi, P. Circadian control of the NAD+ salvage pathway by CLOCKSIRT1. Science, 2009, 324(5927), 654-657.
-
(2009)
Science
, vol.324
, Issue.5927
, pp. 654-657
-
-
Nakahata, Y.1
Sahar, S.2
Astarita, G.3
Kaluzova, M.4
Sassone-Corsi, P.5
-
3
-
-
56749156405
-
SIRT1 redistribution on chromatin promotes genomic stability but alters gene expression during aging
-
Oberdoerffer, P.; Michan, S.; McVay, M.; Mostoslavsky, R.; Vann, J.; Park, S. K.; Hartlerode, A.; Stegmuller, J.; Hafner, A.; Loerch, P.; Wright, S. M.; Mills, K. D.; Bonni, A.; Yankner, B. A.; Scully, R.; Prolla, T. A.; Alt, F. W.; Sinclair, D. A. SIRT1 redistribution on chromatin promotes genomic stability but alters gene expression during aging. Cell, 2008, 135(5), 907-918.
-
(2008)
Cell
, vol.135
, Issue.5
, pp. 907-918
-
-
Oberdoerffer, P.1
Michan, S.2
McVay, M.3
Mostoslavsky, R.4
Vann, J.5
Park, S.K.6
Hartlerode, A.7
Stegmuller, J.8
Hafner, A.9
Loerch, P.10
Wright, S.M.11
Mills, K.D.12
Bonni, A.13
Yankner, B.A.14
Scully, R.15
Prolla, T.A.16
Alt, F.W.17
Sinclair, D.A.18
-
4
-
-
52749091816
-
SirT1 gain of function increases energy efficiency and prevents diabetes in mice
-
Banks, A. S.; Kon, N.; Knight, C.; Matsumoto, M.; Gutierrez-Juarez, R.; Rossetti, L.; Gu, W.; Accili, D. SirT1 gain of function increases energy efficiency and prevents diabetes in mice. Cell Metab, 2008, 8(4), 333-341.
-
(2008)
Cell Metab
, vol.8
, Issue.4
, pp. 333-341
-
-
Banks, A.S.1
Kon, N.2
Knight, C.3
Matsumoto, M.4
Gutierrez-Juarez, R.5
Rossetti, L.6
Gu, W.7
Accili, D.8
-
5
-
-
61749095297
-
SIRT1 exerts anti-inflammatory effects and improves insulin sensitivity in adipocytes
-
Yoshizaki, T.; Milne, J. C.; Imamura, T.; Schenk, S.; Sonoda, N.; Babendure, J. L.; Lu, J. C.; Smith, J. J.; Jirousek, M. R.; Olefsky, J. M. SIRT1 exerts anti-inflammatory effects and improves insulin sensitivity in adipocytes. Mol Cell Biol, 2009, 29(5), 1363-1374.
-
(2009)
Mol Cell Biol
, vol.29
, Issue.5
, pp. 1363-1374
-
-
Yoshizaki, T.1
Milne, J.C.2
Imamura, T.3
Schenk, S.4
Sonoda, N.5
Babendure, J.L.6
Lu, J.C.7
Smith, J.J.8
Jirousek, M.R.9
Olefsky, J.M.10
-
6
-
-
41549136422
-
Paths of convergence: Sirtuins in aging and neurodegeneration
-
Gan, L.; Mucke, L. Paths of convergence: sirtuins in aging and neurodegeneration. Neuron, 2008, 58(1), 10-14.
-
(2008)
Neuron
, vol.58
, Issue.1
, pp. 10-14
-
-
Gan, L.1
Mucke, L.2
-
7
-
-
44849096876
-
The SIRT1 deacetylase suppresses intestinal tumorigenesis and colon cancer growth
-
Firestein, R.; Blander, G.; Michan, S.; Oberdoerffer, P.; Ogino, S.; Campbell, J.; Bhimavarapu, A.; Luikenhuis, S.; de Cabo, R.; Fuchs, C.; Hahn, W. C.; Guarente, L. P.; Sinclair, D. A. The SIRT1 deacetylase suppresses intestinal tumorigenesis and colon cancer growth. PLoS One, 2008, 3(4), e2020.
-
(2008)
PLoS One
, vol.3
, Issue.4
-
-
Firestein, R.1
Blander, G.2
Michan, S.3
Oberdoerffer, P.4
Ogino, S.5
Campbell, J.6
Bhimavarapu, A.7
Luikenhuis, S.8
De Cabo, R.9
Fuchs, C.10
Hahn, W.C.11
Guarente, L.P.12
Sinclair, D.A.13
-
8
-
-
63149150180
-
Discovery of oxazolo[ 4,5-b]pyridines and related heterocyclic analogs as novel SIRT1 activators
-
Bemis, J. E.; Vu, C. B.; Xie, R.; Nunes, J. J.; Ng, P. Y.; Disch, J. S.; Milne, J. C.; Carney, D. P.; Lynch, A. V.; Jin, L.; Smith, J. J.; Lavu, S.; Iffland, A.; Jirousek, M. R.; Perni, R. B. Discovery of oxazolo[ 4,5-b]pyridines and related heterocyclic analogs as novel SIRT1 activators. Bioorg. Med. Chem. Lett., 2009, 19, 2350-2353.
-
(2009)
Bioorg. Med. Chem. Lett.
, vol.19
, pp. 2350-2353
-
-
Bemis, J.E.1
Vu, C.B.2
Xie, R.3
Nunes, J.J.4
Ng, P.Y.5
Disch, J.S.6
Milne, J.C.7
Carney, D.P.8
Lynch, A.V.9
Jin, L.10
Smith, J.J.11
Lavu, S.12
Iffland, A.13
Jirousek, M.R.14
Perni, R.B.15
-
9
-
-
64349118889
-
Discovery of imidazo[1,2-b]thiazole derivatives as novel SIRT1 activators
-
Vu, C. B.; Bemis, J. E.; Disch, J. S.; Ng, P. Y.; Nunes, J. J.; Milne, J. C.; Carney, D. P.; Lynch, A. V.; Smith, J. J.; Lavu, S.; Lambert, P. D.; Gagne, D. J.; Jirousek, M. R.; Schenk, S.; Olefsky, J. M.; Perni, R. B. Discovery of imidazo[1,2-b]thiazole derivatives as novel SIRT1 activators. J. Med. Chem., 2009, 52, 1275-1283.
-
(2009)
J. Med. Chem.
, vol.52
, pp. 1275-1283
-
-
Vu, C.B.1
Bemis, J.E.2
Disch, J.S.3
Ng, P.Y.4
Nunes, J.J.5
Milne, J.C.6
Carney, D.P.7
Lynch, A.V.8
Smith, J.J.9
Lavu, S.10
Lambert, P.D.11
Gagne, D.J.12
Jirousek, M.R.13
Schenk, S.14
Olefsky, J.M.15
Perni, R.B.16
-
10
-
-
84887964294
-
-
The methods for the preparation of each compound (4, 8-19) can be found in the Supplementary Material
-
The methods for the preparation of each compound (4, 8-19) can be found in the Supplementary Material.
-
-
-
-
11
-
-
77950246109
-
SRT1720, SRT2183, SRT1460, and resveratrol are not direct activators of SIRT1
-
Pacholec, M.; Chrunyk, B. A.; Cunningham, D.; Flynn, D.; Griffith, D. A.; Griffor, M.; Loulakis, P.; Pabst, B.; Qiu, X.; Stockman, B.; Thanabal, V.; Varghese, A.; Ward, J.; Withka, J.; Ahn, K. SRT1720, SRT2183, SRT1460, and resveratrol are not direct activators of SIRT1. J. Biol. Chem., 2010, 285(11), 8340-8351.
-
(2010)
J. Biol. Chem.
, vol.285
, Issue.11
, pp. 8340-8351
-
-
Pacholec, M.1
Chrunyk, B.A.2
Cunningham, D.3
Flynn, D.4
Griffith, D.A.5
Griffor, M.6
Loulakis, P.7
Pabst, B.8
Qiu, X.9
Stockman, B.10
Thanabal, V.11
Varghese, A.12
Ward, J.13
Withka, J.14
Ahn, K.15
-
12
-
-
77958488312
-
SIRT1 activation by small molecules: Kinetic and biophysical evidence for direct interaction of enzyme and activator
-
Dai, H.; Kustigian, L.; Carney, D.; Case, A.; Considine, T.; Hubbard, B. P.; Perni, R. B.; Riera, T. V.; Szczepankiewicz, B.; Vlasuk, G. P.; Stein, R. L. SIRT1 activation by small molecules: kinetic and biophysical evidence for direct interaction of enzyme and activator. J. Biol. Chem., 2010, 285, 32695-32703.
-
(2010)
J. Biol. Chem.
, vol.285
, pp. 32695-32703
-
-
Dai, H.1
Kustigian, L.2
Carney, D.3
Case, A.4
Considine, T.5
Hubbard, B.P.6
Perni, R.B.7
Riera, T.V.8
Szczepankiewicz, B.9
Vlasuk, G.P.10
Stein, R.L.11
-
13
-
-
84874721105
-
Evidence for a common mechanism of SIRT1 regulation by allosteric activators
-
Hubbard, B. P.; Gomes, A. P.; Dai, H.; Li, J.; Case, A. W.; Considine, T.; Riera, T. V.; Lee, J. E.; Sook, Y. E.; Lamming, D. W.; Pentelute, B. L.; Schuman, E. R.; Stevens, L. A.; Ling, A. J. Y.; Armour, S. M.; Michan, S.; Zhao, H.; Jiang, Y.; Sweitzer, S. M.; Blum, C. A.; Disch, J. S.; Ng, P. Y.; Howitz, K. T.; Rolo, A. P.; Hamuro, Y.; Moss, J.; Perni, R. B.; Ellis, J. L.; Vlasuk, G. P.; Sinclair, D. A. Evidence for a common mechanism of SIRT1 regulation by allosteric activators. Science, 2013, 339, 1216-1219.
-
(2013)
Science
, vol.339
, pp. 1216-1219
-
-
Hubbard, B.P.1
Gomes, A.P.2
Dai, H.3
Li, J.4
Case, A.W.5
Considine, T.6
Riera, T.V.7
Lee, J.E.8
Sook, Y.E.9
Lamming, D.W.10
Pentelute, B.L.11
Schuman, E.R.12
Stevens, L.A.13
Ling, A.J.Y.14
Armour, S.M.15
Michan, S.16
Zhao, H.17
Jiang, Y.18
Sweitzer, S.M.19
Blum, C.A.20
Disch, J.S.21
Ng, P.Y.22
Howitz, K.T.23
Rolo, A.P.24
Hamuro, Y.25
Moss, J.26
Perni, R.B.27
Ellis, J.L.28
Vlasuk, G.P.29
Sinclair, D.A.30
more..
-
14
-
-
84887944536
-
-
Cell viability was assessed in primary human skeletal muscle myoblast cells (hSkMM) using Alamar Blue staining, which measures metabolic activity in the cell. LC50 was determined after a 24 h compound treatment
-
Cell viability was assessed in primary human skeletal muscle myoblast cells (hSkMM) using Alamar Blue staining, which measures metabolic activity in the cell. LC50 was determined after a 24 h compound treatment.
-
-
-
-
15
-
-
84866986715
-
SIRT1 activators suppress inflammatory responses through promotion of p65 deacetylation and inhibition of NF-kB activity
-
Yang, H.; Zhang, W.; Pan, H.; Feldser, H. G.; Lainez, E.; Miller, C.; Leung, S.; Zhong, Z.; Zhao, H.; Sweitzer, S.; Considine, T.; Riera, T.; Suri, V.; White, B.; Ellis, J. L.; Vlasuk, G. P.; Loh, C. SIRT1 activators suppress inflammatory responses through promotion of p65 deacetylation and inhibition of NF-kB activity. PLoS ONE, 2012, 7(9), e46364.
-
(2012)
PLoS ONE
, vol.7
, Issue.9
-
-
Yang, H.1
Zhang, W.2
Pan, H.3
Feldser, H.G.4
Lainez, E.5
Miller, C.6
Leung, S.7
Zhong, Z.8
Zhao, H.9
Sweitzer, S.10
Considine, T.11
Riera, T.12
Suri, V.13
White, B.14
Ellis, J.L.15
Vlasuk, G.P.16
Loh, C.17
-
16
-
-
84887907026
-
-
The results of the selectivity panel for SRT2104 can be found in the Supplementary Material
-
The results of the selectivity panel for SRT2104 can be found in the Supplementary Material.
-
-
-
-
17
-
-
84871118476
-
Pharmacokinetics and tolerability of SRT2104, a first-in-class small molecule activator of SIRT1, after single and repeated oral administration in man
-
Hoffmann, E.; Wald, J.; Lavu, S.; Roberts, J.; Beaumont, C.; Haddad, J.; Elliott, P.; Westphal, C.; Jacobson, E. Pharmacokinetics and tolerability of SRT2104, a first-in-class small molecule activator of SIRT1, after single and repeated oral administration in man. Br. J. Clin. Pharmacol., 2013, 75(1), 186-196.
-
(2013)
Br. J. Clin. Pharmacol.
, vol.75
, Issue.1
, pp. 186-196
-
-
Hoffmann, E.1
Wald, J.2
Lavu, S.3
Roberts, J.4
Beaumont, C.5
Haddad, J.6
Elliott, P.7
Westphal, C.8
Jacobson, E.9
-
18
-
-
84871431259
-
A pilot randomized, placebo controlled, double blind Phase i trial of the novel SIRT1 activator SRT2104 in elderly volunteers
-
Libri, V.; Brown, A. P.; Gambarota, G.; Haddad, J.; Shields, G. S.; Dawes, H.; Pinato, D. J.; Hoffman, E.; Elliot, P. J.; Vlasuk, G. P.; Jacobson, E.; Wilkins, M. R.; Matthews, P. M. A pilot randomized, placebo controlled, double blind Phase I trial of the novel SIRT1 activator SRT2104 in elderly volunteers. PLoS ONE, 2012, 7(12), e51395.
-
(2012)
PLoS ONE
, vol.7
, Issue.12
-
-
Libri, V.1
Brown, A.P.2
Gambarota, G.3
Haddad, J.4
Shields, G.S.5
Dawes, H.6
Pinato, D.J.7
Hoffman, E.8
Elliot, P.J.9
Vlasuk, G.P.10
Jacobson, E.11
Wilkins, M.R.12
Matthews, P.M.13
|