P. Marcotte

发表

Discovery of Potent Nonpeptide Inhibitors of Stromelysin Using SAR by NMR

Jean M. Severin, S. Davidsen, P. Hajduk, 1997 .

Thienopyrimidine ureas as novel and potent multitargeted receptor tyrosine kinase inhibitors.

K. Glaser, S. Davidsen, V. Stoll, 2005, Journal of medicinal chemistry.

Discovery of N-(4-(3-amino-1H-indazol-4-yl)phenyl)-N'-(2-fluoro-5-methylphenyl)urea (ABT-869), a 3-aminoindazole-based orally active multitargeted receptor tyrosine kinase inhibitor.

K. Glaser, S. Davidsen, V. Stoll, 2007, Journal of medicinal chemistry.

Inhibition of phosphorylation of the colony-stimulating factor-1 receptor (c-Fms) tyrosine kinase in transfected cells by ABT-869 and other tyrosine kinase inhibitors

Yujia Dai, K. Glaser, S. Davidsen, 2006, Molecular Cancer Therapeutics.

Preclinical Characterization of ABT-348, a Kinase Inhibitor Targeting the Aurora, Vascular Endothelial Growth Factor Receptor/Platelet-Derived Growth Factor Receptor, and Src Kinase Families

K. Glaser, S. Davidsen, C. Tse, 2012, Journal of Pharmacology and Experimental Therapeutics.

Inactivation of aromatase in vitro by 4-hydroxy-4-androstene-3,17-dione and 4-acetoxy-4-androstene-3,17-dione and sustained effects in vivo

C. Tsai-Morris, W. Garrett, P. Marcotte, 1981, Steroids.

Pure human inactive renin. Evidence that native inactive renin is prorenin.

D. Egan, C. Heusser, T. Inagami, 1989, The Journal of biological chemistry.

1,4-Dihydroindeno[1,2-c]pyrazoles with acetylenic side chains as novel and potent multitargeted receptor tyrosine kinase inhibitors with low affinity for the hERG ion channel.

S. Davidsen, G. Gintant, Eric F. Johnson, 2007, Journal of medicinal chemistry.

Human placental chorionic renin: production, purification and characterization.

D. Egan, P. Marcotte, W. Holleman, 1988, Biochimica et biophysica acta.

Identification of aminopyrazolopyridine ureas as potent VEGFR/PDGFR multitargeted kinase inhibitors.

K. Glaser, S. Davidsen, N. Soni, 2008, Bioorganic & medicinal chemistry letters.

Exploration of diverse hinge-binding scaffolds for selective Aurora kinase inhibitors.

K. Glaser, S. Davidsen, N. Soni, 2012, Bioorganic & medicinal chemistry letters.

Discovery of potent and selective thienopyrimidine inhibitors of Aurora kinases.

K. Glaser, S. Davidsen, C. Abad-Zapatero, 2011, Bioorganic & medicinal chemistry letters.

Sequence of reactions which follows enzymatic oxidation of propargylglycine.

C. Walsh, P. Marcotte, 1978, Biochemistry.

Modified peptides which display potent and specific inhibition of human renin.

P. Marcotte, J. Plattner, H. Kleinert, 1987, Biochemical and biophysical research communications.

Vinylglycine and proparglyglycine: complementary suicide substrates for L-amino acid oxidase and D-amino acid oxidase.

C. Walsh, P. Marcotte, 1976, Biochemistry.

Discovery and characterization of the potent, selective and orally bioavailable MMP inhibitor ABT-770.

S. Davidsen, M. Michaelides, P. Tapang, 2001, Bioorganic & Medicinal Chemistry Letters.

The matrix metalloproteinase pump-1 catalyzes formation of low molecular weight (pro)urokinase in cultures of normal human kidney cells.

J. M. Ryan, S. Dorwin, P. Marcotte, 1992, The Journal of biological chemistry.

Discovery of selective hydroxamic acid inhibitors of tumor necrosis factor-α converting enzyme

K. Glaser, S. Davidsen, M. Michaelides, 2001 .

Active site-directed inactivation of cystathionine gamma-synthetase and glutamic pyruvic transaminase by propargylglycine.

C. Walsh, P. Marcotte, 1975, Biochemical and biophysical research communications.

Characterization of Matrix Metalloproteinase Inhibitors: Enzymatic Assays

S. Davidsen, P. Marcotte, 2001, Current protocols in pharmacology.

Synthesis of 2,2-dimethyl-4-hydroxy-4-androstene-3,17-dione as an inhibitor of aromatase.

P. Furth, P. Marcotte, C. Robinson, 1990, Journal of enzyme inhibition.

Pyrazole diaminopyrimidines as dual inhibitors of KDR and Aurora B kinases.

K. Glaser, C. Tse, M. Michaelides, 2012, Bioorganic & medicinal chemistry letters.

Thienopyridine ureas as dual inhibitors of the VEGF and Aurora kinase families.

K. Glaser, S. Davidsen, C. Tse, 2012, Bioorganic & medicinal chemistry letters.

Thienopyridine urea inhibitors of KDR kinase.

K. Glaser, S. Davidsen, N. Soni, 2007, Bioorganic & medicinal chemistry letters.

High-level bacterial expression and purification of human SirT2 protein for NMR studies.

P. Hajduk, D. Song, P. Richardson, 2006, Protein expression and purification.

Fluorescence assay of SIRT protein deacetylases using an acetylated peptide substrate and a secondary trypsin reaction.

K. Glaser, A. Gunasekera, P. Richardson, 2004, Analytical biochemistry.

Broad spectrum matrix metalloproteinase inhibitors: an examination of succinamide hydroxamate inhibitors with P1 C alpha gem-disubstitution.

S. Davidsen, D. Albert, M. Curtin, 1998, Bioorganic & medicinal chemistry letters.

Corrigendum to “Fluorescence assay of SIRT protein deacetylases using an acetylated peptide substrate and a secondary trypsin reaction” [Anal. Biochem. 332 (2004) 90–99]

K. Glaser, A. Gunasekera, P. Richardson, 2006 .

Biaryl ether retrohydroxamates as potent, long-lived, orally bioavailable MMP inhibitors.

S. Davidsen, M. Michaelides, D. Albert, 2001, Bioorganic & medicinal chemistry letters.

Domain structure and interactions of recombinant urokinase-type plasminogen activator.

A. Mazar, J. Henkin, P. Marcotte, 1992, The Journal of biological chemistry.

Suicide inactivation of bacterial cystathionine gamma-synthase and methionine gamma-lyase during processing of L-propargylglycine.

C. Walsh, H. Tanaka, K. Soda, 1979, Biochemistry.

Isothiazolopyrimidines and isoxazolopyrimidines as novel multi-targeted inhibitors of receptor tyrosine kinases.

K. Glaser, S. Davidsen, M. Michaelides, 2006, Bioorganic & medicinal chemistry letters.

Evaluation of the inhibition of other metalloproteinases by matrix metalloproteinase inhibitors.

S. Davidsen, D. Albert, M. Curtin, 1999, Journal of enzyme inhibition.

Inhibition and inactivation of estrogen synthetase (aromatase) by fluorinated substrate analogues.

P. Marcotte, C. Robinson, 1982, Biochemistry.

Synthesis and evaluation of 10β-substituted 4-estrene-3,17-diones as inhibitors of human placental microsomal aromatase

P. Marcotte, C. Robinson, 1982, Steroids.

ABT-869 a Multi-Targeted Receptor Tyrosine Kinase Inhibitor: Inhibition of FLT3 Phosphorylation and Signaling in Acute Myeloid Leukemia Running Title: ABT-869 Receptor Tyrosine Kinase Inhibitor in AML

K. Glaser, S. Davidsen, Eric F. Johnson, 2007 .

Trifluoromethyl ketones as inhibitors of histone deacetylase.

K. Glaser, S. Davidsen, M. Michaelides, 2002, Bioorganic & medicinal chemistry letters.

7-Aminopyrazolo[1,5-a]pyrimidines as potent multitargeted receptor tyrosine kinase inhibitors.

K. Glaser, S. Davidsen, N. Soni, 2008, Journal of medicinal chemistry.

Novel renin inhibitors containing analogues of statine retro-inverted at the C-termini: specificity at the P2 histidine site.

S. Rosenberg, P. Marcotte, J. Plattner, 1987, Journal of medicinal chemistry.

Renin inhibitors. Dipeptide analogues of angiotensinogen utilizing a dihydroxyethylene transition-state mimic at the scissile bond to impart greater inhibitory potency.

D. Egan, P. Marcotte, H. Kleinert, 1988, Journal of medicinal chemistry.

Succinimide hydroxamic acids as potent inhibitors of histone deacetylase (HDAC).

K. Glaser, S. Davidsen, M. Michaelides, 2002, Bioorganic & medicinal chemistry letters.

3-amino-benzo[d]isoxazoles as novel multitargeted inhibitors of receptor tyrosine kinases.

K. Glaser, S. Davidsen, N. Soni, 2008, Journal of medicinal chemistry.

Scaffold oriented synthesis. Part 2: Design, synthesis and biological evaluation of pyrimido-diazepines as receptor tyrosine kinase inhibitors.

Zhiqin Ji, Irini Akritopoulou-Zanze, K. Glaser, 2008, Bioorganic & medicinal chemistry letters.

Discovery of Selective Hydroxamic Acid Inhibitors of Tumor Necrosis Factor-α Converting Enzyme.

K. Glaser, S. Davidsen, M. Michaelides, 2010 .

Studies with mechanism-based inactivators of lysine epsilon-transaminase from Achromobacter liquidum.

C. Walsh, S. Coppersmith, P. Marcotte, 1979, Biochemistry.

[45] Suicide substrates for flavoprotein enzymes

C. Walsh, P. Marcotte, T. Cromartie, 1978 .

Indole amide hydroxamic acids as potent inhibitors of histone deacetylases.

Yan Guo, Jun Guo, Yujia Dai, 2003, Bioorganic & medicinal chemistry letters.

Inactivation of bacterial D-amino acid transaminases by the olefinic amino acid D-vinylglycine.

C. Walsh, P. Marcotte, J. Manning, 1977, The Journal of biological chemistry.

Characterization of the activation of pro-urokinase by thermolysin.

J. Henkin, P. Marcotte, 1993, Biochimica et biophysica acta.

A-chain isozymes of recombinant and natural urokinases: Preparation, characterization, and their biochemical and fibrinolytic properties

S. Badylak, R. B. Credo, J. Henkin, 1992 .

Characterization of a metalloprotease which cleaves with high site-specificity the Glu(143)-Leu(144) bond of urokinase

J. Henkin, P. Marcotte, M. Leski, 1992 .

Renin inhibitors. Design and synthesis of a new class of conformationally restricted analogues of angiotensinogen.

S. Fesik, J. Greer, H. Sham, 1988, Journal of medicinal chemistry.

Mechanistic studies with vinylglycine and beta-haloaminobutyrates as substrates for cystathionine gamma-synthetase from Salmonella typhimurium.

C. Walsh, P. Marcotte, J. Donovan, 1979, Biochemistry.

Aryl ketones as novel replacements for the C-terminal amide bond of succinyl hydroxamate MMP inhibitors.

S. Davidsen, D. Albert, J. Summers, 1998, Bioorganic & medicinal chemistry letters.

Abstract A239: Preclinical characterization of ABT-348, a kinase inhibitor targeting the Aurora, VEGFR/PDGFR, and SRC kinase families.

K. Glaser, S. Davidsen, C. Tse, 2011 .

ABT-869, a multitargeted receptor tyrosine kinase inhibitor: inhibition of FLT3 phosphorylation and signaling in acute myeloid leukemia.

Yujia Dai, K. Glaser, S. Davidsen, 2007, Blood.

Preclinical activity of ABT-869, a multitargeted receptor tyrosine kinase inhibitor

K. Glaser, S. Davidsen, Eric F. Johnson, 2005, Molecular Cancer Therapeutics.

Phenoxyphenyl sulfone N-formylhydroxylamines (retrohydroxamates) as potent, selective, orally bioavailable matrix metalloproteinase inhibitors.

Yan Guo, Yujia Dai, S. Davidsen, 2002, Journal of medicinal chemistry.

Synthesis and evaluation of a new generation of orally efficacious benzimidazole-based poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors as anticancer agents.

P. Ellis, Eric F. Johnson, N. Soni, 2009, Journal of medicinal chemistry.

Properties of D-amino acid oxidase covalently modified upon its oxidation of D-propargylglycine.

C. Walsh, P. Marcotte, 1978, Biochemistry.

Stromelysin Inhibitors Designed from Weakly Bound Fragments: Effects of Linking and Cooperativity

P. Hajduk, R. Meadows, E. Olejniczak, 1997 .

ChemInform Abstract: Discovery of Potent Nonpeptide Inhibitors of Stromelysin Using SAR by NMR.

Karl A. Walter, Jean M. Severin, Stephen W. Fesik, 1997 .

Alpha-keto amides as inhibitors of histone deacetylase.

K. Glaser, S. Davidsen, P. Richardson, 2003, Bioorganic & Medicinal Chemistry Letters.

Renin inhibitors. Dipeptide analogues of angiotensinogen incorporating transition-state, nonpeptidic replacements at the scissile bond.

J. Greer, P. Marcotte, G. Bolis, 1987, Journal of medicinal chemistry.

A novel series of histone deacetylase inhibitors incorporating hetero aromatic ring systems as connection units.

K. Glaser, S. Davidsen, M. Michaelides, 2003, Bioorganic & medicinal chemistry letters.

Mechanism-based inactivation of pig heart L-alanine transaminase by L-propargylglycine. Half-site reactivity.

C. Walsh, P. Marcotte, G. Burnett, 1980, Journal of Biological Chemistry.

Sequence of reactions which follows enzymatic oxidation of allylglycine.

C. Walsh, P. Marcotte, 1978, Biochemistry.

Heterocyclic ketones as inhibitors of histone deacetylase.

K. Glaser, S. Davidsen, A. Vasudevan, 2003, Bioorganic & medicinal chemistry letters.

α-Keto amides as inhibitors of histone deacetylase

Paul L. Richardson, Zhiqin Ji, Jun Guo, 2003 .

The design, synthesis, and structure-activity relationships of a series of macrocyclic MMP inhibitors.

S. Davidsen, D. Albert, M. Curtin, 1998, Bioorganic & medicinal chemistry letters.

Differential protein acetylation induced by novel histone deacetylase inhibitors.

K. Glaser, M. Staver, S. Davidsen, 2004, Biochemical and biophysical research communications.

Renin inhibitors. Dipeptide analogues of angiotensinogen utilizing a structurally modified phenylalanine residue to impart proteolytic stability.

J. Greer, H. Sham, P. Marcotte, 1988, Journal of Medicinal Chemistry.

Renin inhibitors Improvements in the stability and biological activity of small peptides containing novel Leu‐Val replacements

P. Marcotte, J. Plattner, H. Kleinert, 1988, FEBS Letters.

ABT-869, a multitargeted receptor tyrosine kinase inhibitor: inhibition of FLT3 phosphorylation and signaling in acute myeloid leukemia.

K. Glaser, S. Davidsen, Eric F. Johnson, 2007, Blood.

K. Glaser, S. Davidsen, Eric F. Johnson, 2007 .