Search Results - "Howe, W. Jeffrey"
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Epilogue to the Gerald Maggiora Festschrift: a tribute to an exemplary mentor, colleague, collaborator, and innovator
Published in Journal of computer-aided molecular design (01-09-2022)“…In May 2022, JCAMD published a Special Issue in honor of Gerald (Gerry) Maggiora, whose scientific leadership over many decades advanced the fields of…”
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Prediction of the Tertiary Structure of the β-Secretase Zymogen
Published in Biochemical and biophysical research communications (05-04-2002)“…β-Secretase, also known as BACE, is a transmembrane aspartyl protease, which generates the N terminus of Alzheimer's disease amyloid β-peptide. The activity of…”
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Protein Binding Chiral Discrimination of HPLC Stationary Phases Made with Whole, Fragmented, and Third Domain Turkey Ovomucoid
Published in Analytical chemistry (Washington) (15-07-1995)“…Individual protein domains and two domains in combination were prepared by enzymatic and chemical cleavage of turkey ovomucoid followed by isolation and…”
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Computer design of bioactive molecules: a method for receptor-based de novo ligand design
Published in Proteins, structure, function, and bioinformatics (01-12-1991)“…The design of molecules to bind specifically to protein receptors has long been a goal of computer-assisted molecular design. Given detailed structural…”
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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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CXC Chemokines Connective Tissue Activating Peptide-III and Neutrophil Activating Peptide-2 are Heparin/Heparan Sulfate-degrading Enzymes (∗)
Published in The Journal of biological chemistry (17-02-1995)“…Heparan sulfate proteoglycans at cell surfaces or in extracellular matrices bind diverse molecules, including growth factors and cytokines, and it is believed…”
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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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General methods of synthetic analysis. Strategic bond disconnections for bridged polycyclic structures
Published in Journal of the American Chemical Society (01-10-1975)Get full text
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Structure-Based Design of Nonpeptidic HIV Protease Inhibitors: The Sulfonamide-Substituted Cyclooctylpyranones
Published in Journal of medicinal chemistry (28-03-1997)“…Recently, cyclooctylpyranone derivatives with m-carboxamide substituents (e.g. 2c) were identified as potent, nonpeptidic HIV protease inhibitors, but these…”
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The HIV-1 Protease as Enzyme and Substrate: Mutagenesis of Autolysis Sites and Generation of a Stable Mutant with Retained Kinetic Properties
Published in Biochemistry (Easton) (16-08-1994)“…Site-directed mutagenesis of autolysis sites in the human immunodeficiency virus type 1 (HIV-1) protease was applied in an analysis of enzyme specificity; the…”
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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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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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Crystal structure of a complex of HIV‐1 protease with a dihydroxyethylene‐containing inhibitor: Comparisons with molecular modeling
Published in Protein science (01-08-1992)“…The structure of a crystal complex of recombinant human immunodeficiency virus type 1 (HIV‐1) protease with a peptide‐mimetic inhibitor containing a…”
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Specificity and inhibition of proteases from human immunodeficiency viruses 1 and 2
Published in The Journal of biological chemistry (25-08-1990)“…Highly purified, recombinant preparations of the virally encoded proteases from human immunodeficiency viruses (HIV) 1 and 2 have been compared relative to 1)…”
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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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Human immunodeficiency virus type‐1 reverse transcriptase and ribonuclease h as substrates of the viral protease
Published in Protein science (01-12-1993)“…A study has been made of the susceptibility of recombinant constructs of reverse transcriptase (RT) and ribonuclease H (RNase H) from human immunodeficiency…”
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