Zobrazeno 1 - 10 of 20 pro vyhledávání: '"Siva Lavu"'
1
MIB-626, an Oral Formulation of a Microcrystalline Unique Polymorph of β-Nicotinamide Mononucleotide, Increases Circulating Nicotinamide Adenine Dinucleotide and its Metabolome in Middle-Aged and Older Adults
Autor: Karol M Pencina, Siva Lavu, Marcello dos Santos, Yusnie M Beleva, Ming Cheng, David Livingston, Shalender Bhasin
Publikováno v: The Journals of Gerontology: Series A. 78:90-96
Background Nicotinamide adenine dinucleotide (NAD) precursors, nicotinamide mononucleotide (NMN), or nicotinamide riboside (NR) extend healthspan and ameliorate some age-related conditions in model organisms. However, early-phase trials of NAD precur
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::be7312faaac801e347a38946d125d292
https://doi.org/10.1093/gerona/glac049
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4
Discovery of Thieno[3,2-d]pyrimidine-6-carboxamides as Potent Inhibitors of SIRT1, SIRT2, and SIRT3
Autor: Ghotas Evindar, Frank T. Coppo, George P. Vlasuk, Eli Schuman, Charles A. Blum, Cheney Mao, Lei Jin, Han Dai, Robert B. Perni, Jianghe Deng, Svetlana L. Belyanskaya, Todd L. Graybill, John W. Cuozzo, Leah Aquilani, Jeremy S. Disch, Cynthia H. Chiu, Siva Lavu, Kenneth E Lind
Publikováno v: Journal of Medicinal Chemistry. 56:3666-3679
The sirtuins SIRT1, SIRT2, and SIRT3 are NAD(+) dependent deacetylases that are considered potential targets for metabolic, inflammatory, oncologic, and neurodegenerative disorders. Encoded library technology (ELT) was used to affinity screen a 1.2 m
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a4d930b58d521e3aa0dbb27bc20c5fe4
https://doi.org/10.1021/jm400204k
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5
Pharmacokinetics and tolerability of SRT2104, a first-in-class small molecule activator of SIRT1, after single and repeated oral administration in man
Autor: Siva Lavu, Jeff Wald, Jon Haddad, Peter J. Elliott, Ethan Hoffmann, Eric W. Jacobson, Claire Beaumont, John Roberts, Christoph H. Westphal
Publikováno v: British Journal of Clinical Pharmacology. 75:186-196
Aim SRT2104 is a novel, first-in-class, highly selective small molecule activator of the NAD + dependent deacetylase SIRT1. SRT2104 was dosed to healthy male and female volunteers in a series of phase 1 clinical studies that were designed to elucidat
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::5c253b9d9d0c678296b2854d9fc529fd
https://doi.org/10.1111/j.1365-2125.2012.04340.x
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6
Acetylation of the C terminus of Ku70 by CBP and PCAF controls Bax-mediated apoptosis
Autor: David A. Sinclair, Haim Y. Cohen, Roy A. Frye, Benedikt M. Kessler, Brian G Hekking, Siva Lavu, Thomas A Imahiyerobo, Kevin J. Bitterman, Christine M. Miller, Hidde L. Ploegh
Apoptosis is a key tumor suppression mechanism that can be initiated by activation of the proapoptotic factor Bax. The Ku70 DNA end-joining protein has recently been shown to suppress apoptosis by sequestering Bax from mitochondria. The mechanism by
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f097c732baf02051db32f68fc2ce222d
https://ora.ox.ac.uk/objects/uuid:7988c853-6462-484a-b61a-ae22b0e0cd9b
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7
Discovery of oxazolo[4,5-b]pyridines and related heterocyclic analogs as novel SIRT1 activators
Autor: David P. Carney, Amy V. Lynch, Robert B. Perni, Pui Yee Ng, Jeremy S. Disch, Roger Xie, Michael R. Jirousek, Jill C. Milne, J. Joshua Smith, Lei Jin, Andre Iffland, Joseph J. Nunes, Jean Bemis, Siva Lavu, Chi B. Vu
Publikováno v: Bioorganic & Medicinal Chemistry Letters. 19:2350-2353
SIRT1 is an NAD+-dependent protein deacetylase that appears to produce beneficial effects on metabolic parameters such as glucose and insulin homeostasis. Activation of SIRT1 by resveratrol (1) has been shown to modulate insulin resistance, increase
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6f244e63f7cbed43f6d57bb08bab4ff2
https://doi.org/10.1016/j.bmcl.2008.11.106
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8
Discovery of Imidazo[1,2-b]thiazole Derivatives as Novel SIRT1 Activators
Autor: Philip D. Lambert, David J. Gagne, Joseph J. Nunes, Jerrold M. Olefsky, Jean Bemis, Chi B. Vu, Jill C. Milne, Amy V. Lynch, J. Joshua Smith, David P. Carney, Michael R. Jirousek, Robert B. Perni, Pui Yee Ng, Jeremy S. Disch, Simon Schenk, Siva Lavu
Publikováno v: Journal of Medicinal Chemistry. 52:1275-1283
A series of imidazo[1,2-b]thiazole derivatives is shown to activate the NAD(+)-dependent deacetylase SIRT1, a potential new therapeutic target to treat various metabolic disorders. This series of compounds was derived from a high throughput screening
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1f7c6857bfb9e2c4e77d9cfa1518e2e0
https://doi.org/10.1021/jm8012954
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9
Sirtuins — novel therapeutic targets to treat age-associated diseases
Autor: Olivier Boss, Peter J. Elliott, Siva Lavu, Philip D. Lambert
Publikováno v: Nature Reviews Drug Discovery. 7:841-853
Sirtuins post-translationally modulate the function of many cellular proteins that undergo reversible acetylation-deacetylation cycles, affecting physiological responses that have implications for treating diseases of ageing. Potent small-molecule mo
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bc49f615b21cf23ff33170ee01db6f15
https://doi.org/10.1038/nrd2665
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