Search Results - "Tomich, Paul K"
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Allosteric Inhibition of Staphylococcus aureus D-Alanine:D-Alanine Ligase Revealed by Crystallographic Studies
Published in Proceedings of the National Academy of Sciences - PNAS (10-10-2006)“…D-alanine:D-alanine ligase (DDI) is an essential enzyme in bacterial cell wall biosynthesis and an important target for developing new antibiotics. It…”
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Structure-Based Design of Novel HIV Protease Inhibitors: Sulfonamide-Containing 4-Hydroxycoumarins and 4-Hydroxy-2-pyrones as Potent Non-Peptidic Inhibitors
Published in Journal of medicinal chemistry (07-06-1996)“…The low oral bioavailability and rapid biliary excretion of peptide-derived HIV protease inhibitors have limited their utility as potential therapeutic agents…”
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Tipranavir (PNU-140690): A Potent, Orally Bioavailable Nonpeptidic HIV Protease Inhibitor of the 5,6-Dihydro-4-hydroxy-2-pyrone Sulfonamide Class
Published in Journal of medicinal chemistry (27-08-1998)“…A broad screening program previously identified phenprocoumon (1) as a small molecule template for inhibition of HIV protease. Subsequent modification of this…”
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4
The Ligand Affinity of Proteins Measured by Isothermal Denaturation Kinetics
Published in Analytical biochemistry (01-05-2001)“…An isothermal denaturation kinetic method was developed for identifying potential ligands of proteins and measuring their affinity. The method is suitable for…”
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3-arylpiperidines as potentiators of existing antibacterial agents
Published in Bioorganic & medicinal chemistry letters (23-07-2001)“…Important resistance patterns in Gram-negative pathogens include active efflux of antibiotics out of the cell via a cellular pump and decreased membrane…”
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A high-throughput resonance energy transfer assay for Staphylococcus aureus DNA ligase
Published in Analytical biochemistry (15-01-2004)Get full text
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7
Structure-Based Design of Novel HIV Protease Inhibitors: Carboxamide-Containing 4-Hydroxycoumarins and 4-Hydroxy-2-pyrones as Potent Nonpeptidic Inhibitors
Published in Journal of medicinal chemistry (01-09-1995)“…The low oral bioavailability and rapid biliary excretion of peptide-derived HIV protease inhibitors have limited their utility as potential therapeutic agents…”
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Structure-Based Design of HIV Protease Inhibitors: 5,6-Dihydro-4-hydroxy-2-pyrones as Effective, Nonpeptidic Inhibitors
Published in Journal of medicinal chemistry (08-11-1996)“…From a broad screening program, the 4-hydroxycoumarin phenprocoumon (I) was previously identified as a lead template with HIV protease inhibitory activity. The…”
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Identification of novel potent hydroxamic acid inhibitors of peptidyl deformylase and the importance of the hydroxamic acid functionality on inhibition
Published in Bioorganic & medicinal chemistry letters (04-06-2001)“…Peptidyl deformylase (PDF) is a metallo protease that catalyzes the removal of a formyl group from the N-termini of prokaryotic prepared polypeptides, an…”
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Non-peptidic HIV protease inhibitors : C2-SYMMETRY-BASED design of bis-sulfonamide dihydropyrones
Published in Bioorganic & medicinal chemistry letters (19-05-1998)“…Potent, non-peptidic, dihydropyrone sulfonamide HIV protease inhibitors have been previously described. Crystallographic analysis of dihydropyrone sulfonamide…”
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Use of Medium-Sized Cycloalkyl Rings To Enhance Secondary Binding: Discovery of a New Class of Human Immunodeficiency Virus (HIV) Protease Inhibitors
Published in Journal of medicinal chemistry (01-05-1995)“…A unique strategy for the enhancement of secondary binding of an inhibitor to an enzyme has been demonstrated in the design of new human immunodeficiency virus…”
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Structure-Based Design of Nonpeptidic HIV Protease Inhibitors from a Cyclooctylpyranone Lead Structure
Published in Journal of medicinal chemistry (01-10-1995)“…Recently, the novel cyclooctylpyranone HIV protease inhibitor 1 was identified in our labs, and an X-ray structure of this inhibitor complexed with HIV-2…”
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Cycloalkylpyranones and Cycloalkyldihydropyrones as HIV Protease Inhibitors: Exploring the Impact of Ring Size on Structure−Activity Relationships
Published in Journal of medicinal chemistry (27-09-1996)“…Previously, 3-substituted cycloalkylpyranones, such as 2d, have proven to be effective inhibitors of HIV protease. In an initial series of 3-(1-phenylpropyl)…”
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14
Evidence for a Complex Regulating the in Vivo Activities of Early Enzymes Induced by Bacteriophage T4
Published in The Journal of biological chemistry (10-12-1974)“…An in vivo assay of enzyme activity has been employed to investigate the mechanism of control of enzymes synthesizing deoxyribonucleotides after bacteriophage…”
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Structure-Based Design of HIV Protease Inhibitors: 4-Hydroxycoumarins and 4-Hydroxy-2-pyrones as Non-peptidic Inhibitors
Published in Journal of medicinal chemistry (01-09-1994)Get full text
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Direct Participation of dCMP Hydroxymethylase in Synthesis of Bacteriophage T4 DNA
Published in Proceedings of the National Academy of Sciences - PNAS (01-08-1973)“…In order to retain in an in situ system the control mechanisms involved in synthesis of bacteriophage T4 DNA, infected cells were made permeable to nucleotides…”
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Structure-Based Design of HIV Protease Inhibitors: Sulfonamide-Containing 5,6-Dihydro-4-hydroxy-2-pyrones as Non-Peptidic Inhibitors
Published in Journal of medicinal chemistry (25-10-1996)Get full text
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Non-peptidic HIV protease inhibitors: C 2-symmetry-based design of bis-sulfonamide dihydropyrones
Published in Bioorganic & medicinal chemistry letters (19-05-1998)“…Potent, non-peptidic, dihydropyrone sulfonamide HIV protease inhibitors have been previously described. Crystallographic analysis of dihydropyrone sulfonamide…”
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Structure-Based Design of Sulfonamide-Substituted Non-Peptidic HIV Protease Inhibitors
Published in Journal of medicinal chemistry (01-12-1995)Get full text
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Corrigendum to “Identification of novel potent hydroxamic acid inhibitors of peptidyl deformylase and the importance of the hydroxamic acid functionality on inhibition” [Bioorg. Med. Chem. Lett. 11 (2001) 1355]
Published in Bioorganic & medicinal chemistry letters (01-08-2001)Get full text
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