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Joseph J Nunes

Explore the profile of Joseph J Nunes including associated specialties, affiliations and a list of published articles. Areas
Snapshot
Articles 10
Citations 890
Followers 0
Related Specialties
Chemistry
Biochemistry
Science
Top 10 Co-Authors
Jean E Bemis
Xin Huang
Christina Boucher
Xiaotian Zhu
Susan M Turci
Matthew W Martin
Stephen Schneider
Faye Hsieh
Josie H Lee
John Newcomb
Published In
J Med Chem
Bioorg Med Chem Lett
Nature
Affiliations
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Recent Articles
1.
Discovery of oxazolo[4,5-b]pyridines and related heterocyclic analogs as novel SIRT1 activators
Bemis J, Vu C, Xie R, Nunes J, Ng P, Disch J, et al.
Bioorg Med Chem Lett . 2009 Mar; 19(8):2350-3. PMID: 19303289
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...
2.
Discovery of imidazo[1,2-b]thiazole derivatives as novel SIRT1 activators
Vu C, Bemis J, Disch J, Ng P, Nunes J, Milne J, et al.
J Med Chem . 2009 Feb; 52(5):1275-83. PMID: 19199480
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...
3.
Structure-guided design of aminopyrimidine amides as potent, selective inhibitors of lymphocyte specific kinase: synthesis, structure-activity relationships, and inhibition of in vivo T cell activation
DiMauro E, Newcomb J, Nunes J, Bemis J, Boucher C, Chai L, et al.
J Med Chem . 2008 Mar; 51(6):1681-94. PMID: 18321037
The lymphocyte-specific kinase (Lck), a member of the Src family of cytoplasmic tyrosine kinases, is expressed in T cells and natural killer (NK) cells. Genetic evidence, including knockout mice and...
4.
Structure-based design of novel 2-amino-6-phenyl-pyrimido[5',4':5,6]pyrimido[1,2-a]benzimidazol-5(6H)-ones as potent and orally active inhibitors of lymphocyte specific kinase (Lck): synthesis, SAR, and in vivo anti-inflammatory activity
Martin M, Newcomb J, Nunes J, Boucher C, Chai L, Epstein L, et al.
J Med Chem . 2008 Feb; 51(6):1637-48. PMID: 18278858
Lck, or lymphocyte specific kinase, is a cytoplasmic tyrosine kinase of the Src family expressed in T-cells and NK cells. Genetic evidence from knockout mice and human mutations demonstrates that...
5.
N-(3-(phenylcarbamoyl)arylpyrimidine)-5-carboxamides as potent and selective inhibitors of Lck: structure, synthesis and SAR
Deak H, Newcomb J, Nunes J, Boucher C, Cheng A, DiMauro E, et al.
Bioorg Med Chem Lett . 2007 Dec; 18(3):1172-6. PMID: 18083554
N-3-(Phenylcarbamoyl)arylpyrimidine-5-carboxamides are a novel class of selective Lck inhibitors. This series of compounds derives its selectivity from a hydrogen bond with the gatekeeper Thr316 of the enzyme. X-ray co-crystal structural...
6.
Small molecule activators of SIRT1 as therapeutics for the treatment of type 2 diabetes
Milne J, Lambert P, Schenk S, Carney D, Smith J, Gagne D, et al.
Nature . 2007 Nov; 450(7170):712-6. PMID: 18046409
Calorie restriction extends lifespan and produces a metabolic profile desirable for treating diseases of ageing such as type 2 diabetes. SIRT1, an NAD+-dependent deacetylase, is a principal modulator of pathways...
7.
Discovery of 4-amino-5,6-biaryl-furo[2,3-d]pyrimidines as inhibitors of Lck: development of an expedient and divergent synthetic route and preliminary SAR
DiMauro E, Newcomb J, Nunes J, Bemis J, Boucher C, Buchanan J, et al.
Bioorg Med Chem Lett . 2007 Feb; 17(8):2305-9. PMID: 17280833
4-Amino-5,6-biaryl-furo[2,3-d]pyrimidines were identified as potent non-selective inhibitors of Lck. A novel, divergent, and practical synthetic route was developed to access derivatives from bifunctional intermediates. Lead optimization was guided by X-ray...
8.
Discovery of novel 2,3-diarylfuro[2,3-b]pyridin-4-amines as potent and selective inhibitors of Lck: synthesis, SAR, and pharmacokinetic properties
Martin M, Newcomb J, Nunes J, Bemis J, McGowan D, White R, et al.
Bioorg Med Chem Lett . 2007 Feb; 17(8):2299-304. PMID: 17276681
2,3-Diarylfuro[2,3-b]pyridine-4-amines are a novel class of potent and selective inhibitors of Lck. The discovery, synthesis, and structure activity relationships of this series of inhibitors are reported. The most promising compounds...
9.
Discovery of aminoquinazolines as potent, orally bioavailable inhibitors of Lck: synthesis, SAR, and in vivo anti-inflammatory activity
DiMauro E, Newcomb J, Nunes J, Bemis J, Boucher C, Buchanan J, et al.
J Med Chem . 2006 Sep; 49(19):5671-86. PMID: 16970394
The lymphocyte-specific kinase (Lck) is a cytoplasmic tyrosine kinase of the Src family expressed in T cells and natural killer (NK) cells. Genetic evidence in both mice and humans demonstrates...
10.
Novel 2-aminopyrimidine carbamates as potent and orally active inhibitors of Lck: synthesis, SAR, and in vivo antiinflammatory activity
Martin M, Newcomb J, Nunes J, McGowan D, Armistead D, Boucher C, et al.
J Med Chem . 2006 Aug; 49(16):4981-91. PMID: 16884310
The lymphocyte-specific kinase (Lck) is a cytoplasmic tyrosine kinase of the Src family expressed in T cells and NK cells. Genetic evidence in both mice and humans demonstrates that Lck...