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Keith L Constantine

Explore the profile of Keith L Constantine including associated specialties, affiliations and a list of published articles. Areas
Snapshot
Articles 8
Citations 63
Followers 0
Related Specialties
Chemistry
Biochemistry
Top 10 Co-Authors
Luciano Mueller
William J Metzler
Valentina Goldfarb
Patricia A McDonnell
John E Leet
Bennett T Farmer 2nd
Brian L Claus
Ning Yan
Margarita M Bastos
Michael A Poss
Published In
J Med Chem
J Am Chem Soc
Magn Reson Chem
Protein Sci
Bioorg Med Chem Lett
Affiliations
Soon will be listed here.
Recent Articles
1.
Design, synthesis, functional and structural characterization of an inhibitor of N-acetylneuraminate-9-phosphate phosphatase: observation of extensive dynamics in an enzyme/inhibitor complex
Kim S, Constantine K, Duke G, Goldfarb V, Hunt J, Johnson S, et al.
Bioorg Med Chem Lett . 2013 Jun; 23(14):4107-11. PMID: 23747226
The design, synthesis and characterization of a phosphonate inhibitor of N-acetylneuraminate-9-phosphate phosphatase (HDHD4) is described. Compound 3, where the substrate C-9 oxygen was replaced with a nonlabile CH2 group, inhibits...
2.
Eleven amino acid glucagon-like peptide-1 receptor agonists with antidiabetic activity
Mapelli C, Natarajan S, Meyer J, Bastos M, Bernatowicz M, Lee V, et al.
J Med Chem . 2009 Aug; 52(23):7788-99. PMID: 19702274
Glucagon-like peptide 1 (GLP-1) is a 30 or 31 amino acid peptide hormone that contributes to the physiological regulation of glucose homeostasis and food intake. Herein, we report the discovery...
3.
Multiple and single binding modes of fragment-like kinase inhibitors revealed by molecular modeling, residue type-selective protonation, and nuclear overhauser effects
Constantine K, Mueller L, Metzler W, McDonnell P, Todderud G, Goldfarb V, et al.
J Med Chem . 2008 Sep; 51(19):6225-9. PMID: 18771253
Fragment-like inhibitors of mitogen-activated protein kinase-activated protein kinase 2 (MK2) include 5-hydroxyisoquinoline (IC50 approximately 85 microM). Modeling studies identified four possible binding modes for this compound. Two-dimensional (1)H-(1)H NOESY data...
4.
Observation of O-H...N scalar coupling across a hydrogen bond in nocathiacin I
Huang X, Liu X, Constantine K, Leet J, Roongta V
Magn Reson Chem . 2007 Apr; 45(6):447-50. PMID: 17431856
We report here the observation of O-H...N hydrogen-bond (1h)J(N,OH) scalar coupling in a biologically active natural product. The intramolecular hydrogen bond between the threonine hydroxyl (Thr-OH) group and the thiazolyl...
5.
NMR structure of a potent small molecule inhibitor bound to human keratinocyte fatty acid-binding protein
McDonnell P, Constantine K, Goldfarb V, Johnson S, Sulsky R, Magnin D, et al.
J Med Chem . 2006 Aug; 49(16):5013-7. PMID: 16884313
The NMR structure is presented for compound 1 (BMS-480404) (Ki = 33 (+/-2) nM) bound to keratinocyte fatty acid-binding protein. This article describes interactions between a high affinity drug-like compound...
6.
Protein-ligand NOE matching: a high-throughput method for binding pose evaluation that does not require protein NMR resonance assignments
Constantine K, Davis M, Metzler W, Mueller L, Claus B
J Am Chem Soc . 2006 Jun; 128(22):7252-63. PMID: 16734479
Given the three-dimensional (3D) structure of a protein, the binding pose of a ligand can be determined using distance restraints derived from assigned intra-ligand and protein-ligand nuclear Overhauser effects (NOEs)....
7.
Structural and functional characterization of CFE88: evidence that a conserved and essential bacterial protein is a methyltransferase
Constantine K, Krystek S, Healy M, Doyle M, Siemers N, Thanassi J, et al.
Protein Sci . 2005 Jun; 14(6):1472-84. PMID: 15929997
CFE88 is a conserved essential gene product from Streptococcus pneumoniae. This 227-residue protein has minimal sequence similarity to proteins of known 3D structure. Sequence alignment models and computational protein threading...
8.
Conformation and absolute configuration of nocathiacin I determined by NMR spectroscopy and chiral capillary electrophoresis
Constantine K, Mueller L, Huang S, Abid S, Lam K, Li W, et al.
J Am Chem Soc . 2002 Jun; 124(25):7284-5. PMID: 12071733
Nocathiacin I (BMS-249524) is a highly cross-linked thiazolyl peptide that displays potent activity against Gram-positive bacteria, including a number of antibiotic-resistant strains. This natural product contains 10 chiral centers. NMR...