Search Results - "SUDMEIER, James L"
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Chemical and Biological Evaluation of Dipeptidyl Boronic Acid Proteasome Inhibitors for Use in Prodrugs and Pro-Soft Drugs Targeting Solid Tumors
Published in Journal of medicinal chemistry (14-07-2011)“…Bortezomib, a dipeptidyl boronic acid and potent inhibitor of the 26S proteasome, is remarkably effective against multiple myeloma (MM) but not against solid…”
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Pro-Soft Val-boroPro: A Strategy for Enhancing in Vivo Performance of Boronic Acid Inhibitors of Serine Proteases
Published in Journal of medicinal chemistry (14-04-2011)“…Val-boroPro, 1, is a potent, but relatively nonspecific inhibitor of the prolyl peptidases. It has antihyperglycemic activity from inhibition of DPPIV but also…”
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A Low-Barrier Hydrogen Bond in the Catalytic Triad of Serine Proteases? Theory Versus Experiment
Published in Science (American Association for the Advancement of Science) (07-11-1997)“…Cleland and Kreevoy recently advanced the idea that a special type of hydrogen bond (H-bond), termed a low-barrier hydrogen bond (LBHB), may account for the…”
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Analyses of the Interaction between the Origin Binding Domain from Simian Virus 40 T Antigen and Single-Stranded DNA Provide Insights into DNA Unwinding and Initiation of DNA Replication
Published in Journal of Virology (01-12-2006)“…Article Usage Stats Services JVI Citing Articles Google Scholar PubMed Related Content Social Bookmarking CiteULike Delicious Digg Facebook Google+ Mendeley…”
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Identification of Selective and Potent Inhibitors of Fibroblast Activation Protein and Prolyl Oligopeptidase
Published in Journal of medicinal chemistry (09-05-2013)“…Fibroblast activation protein (FAP) is a serine protease selectively expressed on reactive stromal fibroblasts of epithelial carcinomas. It is widely believed…”
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α-Lytic protease can exist in two separately stable conformations with different His57 mobilities and catalytic activities
Published in Proceedings of the National Academy of Sciences - PNAS (25-01-2005)“…α-Lytic protease is a bacterial serine protease widely studied as a model system of enzyme catalysis. Here we report that lyophilization induces a structural…”
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A General Method for Making Peptide Therapeutics Resistant to Serine Protease Degradation: Application to Dipeptidyl Peptidase IV Substrates
Published in Journal of medicinal chemistry (14-11-2013)“…Bioactive peptides have evolved to optimally fulfill specific biological functions, a fact which has long attracted attention for their use as therapeutic…”
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Dipeptide Boronic Acid Inhibitors of Dipeptidyl Peptidase IV: Determinants of Potency and in Vivo Efficacy and Safety
Published in Journal of medicinal chemistry (09-10-2008)“…Dipeptidyl peptidase IV (DPP-IV; E.C. 3.4.14.5), a serine protease that degrades the incretin hormones GLP-1 and GIP, is now a validated target for the…”
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Identification of Histidine Tautomers in Proteins by 2D 1H/13Cδ2 One-Bond Correlated NMR
Published in Journal of the American Chemical Society (16-07-2003)“…If the 13Cδ2 chemical shift of neutral (“high pH”) histidine is >122 ppm, primarily Nδ1−H tautomer (2) is indicated; if it is <122 ppm, primarily Nε2−H…”
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4-Substituted boro-proline dipeptides: Synthesis, characterization, and dipeptidyl peptidase IV, 8, and 9 activities
Published in Bioorganic & medicinal chemistry letters (01-09-2012)“…The boroProline-based dipeptidyl boronic acids were among the first DPP-IV inhibitors identified, and remain the most potent known. We introduced various…”
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Synthesis and Characterization of Constrained Peptidomimetic Dipeptidyl Peptidase IV Inhibitors: Amino-Lactam boroAlanines
Published in Journal of medicinal chemistry (17-05-2007)“…We describe here the epimerization-free synthesis and characterization of a new class of conformationally constrained lactam aminoboronic acid inhibitors of…”
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Tautomerism, acid‐base equilibria, and H‐bonding of the six histidines in subtilisin BPN′ by NMR
Published in Protein science (01-04-2003)“…We have determined by 15N, 1H, and 13C NMR, the chemical behavior of the six histidines in subtilisin BPN′ and their PMSF and peptide boronic acid complexes in…”
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Autochelation in Dipeptide Boronic Acids: pH-Dependent Structures and Equilibria of Asp-boroPro and His-boroPro by NMR Spectroscopy
Published in Journal of the American Chemical Society (08-06-2005)“…Many dipeptide boronic acids of the type H2N-X − Y-B(OH)2 are potent protease inhibitors. Interest in these compounds as drugs for cancer, diabetes, and other…”
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T Antigen Origin-Binding Domain of Simian Virus 40: Determinants of Specific DNA Binding
Published in Biochemistry (Easton) (08-06-2004)“…To better understand origin recognition and initiation of DNA replication, we have examined by NMR complexes formed between the origin-binding domain of SV40 T…”
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Unusual 1H NMR chemical shifts support (His) Cɛ1—H⋅⋅⋅O⩵C H-bond: Proposal for reaction-driven ring flip mechanism in serine protease catalysis
Published in Proceedings of the National Academy of Sciences - PNAS (12-09-2000)“…13 C-selective NMR, combined with inhibitor perturbation experiments, shows that the C ɛ 1 —H proton of the catalytic histidine in resting α-lytic protease and…”
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Direct NMR Observation and p K a Determination of the Asp 102 Side Chain in a Serine Protease
Published in Journal of the American Chemical Society (01-02-2012)Get full text
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Nuclear Magnetic Resonance Study of Rate and Mechanism of Exchange Reactions Involving (Ethylenedinitrilo) tetraacetatocadmate(II)
Published in Inorganic chemistry (01-06-1966)Get full text
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