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Discovery of N-(4-(2-amino-3-chloropyridin-4-yloxy)-3-fluorophenyl)-4-ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide (BMS-777607), a selective and orally efficacious inhibitor of…

• Gretchen M Schroeder, Yongmi An, +28 authors Robert M. Borzilleri
• Journal of medicinal chemistry
• 2009

Substituted N-(4-(2-aminopyridin-4-yloxy)-3-fluoro-phenyl)-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamides were identified as potent and selective Met kinase inhibitors. Substitution of… (More)

Oral administration of vanadate normalizes blood glucose levels in streptozotocin-treated rats. Characterization and mode of action.

• Joseph Meyerovitch, Zvi Farfel, John Sack, Yoram Shechter
• The Journal of biological chemistry
• 1987

The effect of oral administration of vanadate, in normalizing blood glucose levels of streptozotocin-treated rats (ST-rats), is further characterized and its mode of action is determined. We have… (More)

Periplasmic binding protein structure and function. Refined X-ray structures of the leucine/isoleucine/valine-binding protein and its complex with leucine.

• John Sack, March Saper, Florante A. Quiocho
• Journal of molecular biology
• 1989

The three-dimensional structure of the native unliganded form of the Leu/Ile/Val-binding protein (Mr = 36,700), an essential component of the high-affinity active transport system for the branched… (More)

Crystallographic structures of the ligand-binding domains of the androgen receptor and its T877A mutant complexed with the natural agonist dihydrotestosterone.

• John Sack, Kevin F Kish, +9 authors Howard M. Einspahr
• Proceedings of the National Academy of Sciences…
• 2001

The structures of the ligand-binding domains (LBD) of the wild-type androgen receptor (AR) and the T877A mutant corresponding to that in LNCaP cells, both bound to dihydrotestosterone, have been… (More)

CHAIN: a crystallographic modeling program.

• John Sack, Florante A. Quiocho
• Methods in enzymology
• 1997

Three-dimensional structure of calmodulin.

• Y. V. Suresh Babu, John Sack, T J Greenhough, Charles E. Bugg, Anthony R. Means, William J. Cook
• Nature
• 1985

The three-dimensional structure of calmodulin has been determined crystallographically at 3.0 A resolution. The molecule consists of two globular lobes connected by a long exposed alpha-helix. Each… (More)

N-(cycloalkylamino)acyl-2-aminothiazole inhibitors of cyclin-dependent kinase 2. N-[5-[[[5-(1,1-dimethylethyl)-2-oxazolyl]methyl]thio]-2-thiazolyl]-4- piperidinecarboxamide (BMS-387032), a highly…

• Raj N Misra, Hai-yun Xiao, +24 authors S David Kimball
• Journal of medicinal chemistry
• 2004

N-Acyl-2-aminothiazoles with nonaromatic acyl side chains containing a basic amine were found to be potent, selective inhibitors of CDK2/cycE which exhibit antitumor activity in mice. In particular,… (More)

Ontogenesis of hypothalamic--pituitary--thyroid function and metabolism in man, sheep, and rat.

• D. A. Fisher, Jerry Dussault, John Sack, Inderjit Chopra
• Recent progress in hormone research
• 1976

Identification of pyrrolo[2,1-f][1,2,4]triazine-based inhibitors of Met kinase.

• Gretchen M Schroeder, Xiao-Tao Chen, +19 authors Robert M. Borzilleri
• Bioorganic & medicinal chemistry letters
• 2008

An amide library derived from the pyrrolo[2,1-f][1,2,4]triazine scaffold led to the identification of modest inhibitors of Met kinase activity. Introduction of polar side chains at C-6 of the… (More)

Pharmacological and x-ray structural characterization of a novel selective androgen receptor modulator: potent hyperanabolic stimulation of skeletal muscle with hypostimulation of prostate in rats.

• Jacek Ostrowski, Joyce E Kuhns, +15 authors Lawrence G. Hamann
• Endocrinology
• 2007

A novel, highly potent, orally active, nonsteroidal tissue selective androgen receptor (AR) modulator (BMS-564929) has been identified, and this compound has been advanced to clinical trials for the… (More)

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