Search Results - "Kuyper, Lee F."
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Binding Mode of the 4-Anilinoquinazoline Class of Protein Kinase Inhibitor: X-ray Crystallographic Studies of 4-Anilinoquinazolines Bound to Cyclin-Dependent Kinase 2 and p38 Kinase
Published in Journal of medicinal chemistry (13-01-2000)“…4-Anilinoquinazolines represent an important class of protein kinase inhibitor. Modes of binding for two members of this inhibitor class were determined by…”
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Prevention of Chemotherapy-Induced Alopecia in Rats by CDK Inhibitors
Published in Science (American Association for the Advancement of Science) (05-01-2001)“…Most traditional cytotoxic anticancer agents ablate the rapidly dividing epithelium of the hair follicle and induce alopecia (hair loss). Inhibition of…”
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Recent applications of protein crystallography and structure-guided drug design
Published in Current opinion in chemical biology (01-08-2005)“…Technological advances to increase the throughput of purified protein production and co-crystallization of target proteins with small molecules have helped to…”
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Chemical genomic profiling to identify intracellular targets of a multiplex kinase inhibitor
Published in Proceedings of the National Academy of Sciences - PNAS (08-03-2005)“…The identification of the kinase or kinases targeted by protein kinase inhibitors is a critical challenge in validating their use as therapeutic agents or…”
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Oxindole-Based Inhibitors of Cyclin-Dependent Kinase 2 (CDK2): Design, Synthesis, Enzymatic Activities, and X-ray Crystallographic Analysis
Published in Journal of medicinal chemistry (06-12-2001)“…Two closely related classes of oxindole-based compounds, 1H-indole-2,3-dione 3-phenylhydrazones and 3-(anilinomethylene)-1,3-dihydro-2H-indol-2-ones, were…”
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Site-specific Conjugation on Serine → Cysteine Variant Monoclonal Antibodies
Published in The Journal of biological chemistry (29-09-2000)“…We have engineered a cysteine residue at position 442 (EU/OU numbering) in the third constant domain (CH3) of the heavy chain of several IgGs with different…”
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X-ray Crystal Structures of Candida albicans Dihydrofolate Reductase: High Resolution Ternary Complexes in Which the Dihydronicotinamide Moiety of NADPH Is Displaced by an Inhibitor
Published in Journal of medicinal chemistry (30-08-2001)“…X-ray crystallographic analysis of 5-(4'-substituted phenyl)sulfanyl-2,4-diaminoquinazoline inhibitors in ternary complex with Candida albicans dihydrofolate…”
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Theoretical investigations of the rotational barrier in anisole: an ab initio and molecular dynamics study
Published in Journal of physical chemistry (1952) (01-05-1990)Get full text
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High-Affinity Inhibitors of Dihydrofolate Reductase: Antimicrobial and Anticancer Activities of 7,8-Dialkyl-1,3-diaminopyrrolo[3,2-f]quinazolines with Small Molecular Size
Published in Journal of medicinal chemistry (16-02-1996)“…A series of 7,8-dialkylpyrrolo[3,2-f]quinazolines were prepared as inhibitors of dihydrofolate reductase (DHFR). On the basis of an apparent inverse…”
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Selective Inhibitors of Candida albicans Dihydrofolate Reductase: Activity and Selectivity of 5-(Arylthio)-2,4-diaminoquinazolines
Published in Journal of medicinal chemistry (01-09-1995)“…The recent increase in fungal infections, especially among AIDS patients, has resulted in the need for more effective antifungal agents. In our search for such…”
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Pyrrolo[2,3- d]pyrimidines and pyrido[2,3- d]pyrimidines as conformationally restricted analogues of the antibacterial agent trimethoprim
Published in Bioorganic & medicinal chemistry (01-04-1996)“…Conformationally restricted analogues of the antibacterial agent trimethoprim (TMP) were designed to mimic the conformation of drug observed in its complex…”
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X-ray Crystal Structures of Candida a lbicans Dihydrofolate Reductase: High Resolution Ternary Complexes in Which the Dihydronicotinamide Moiety of NADPH Is Displaced by an Inhibitor
Published in Journal of medicinal chemistry (30-08-2001)“…X-ray crystallographic analysis of 5-(4‘-substituted phenyl)sulfanyl-2,4-diaminoquinazoline inhibitors in ternary complex with Candida albicans dihydrofolate…”
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Resolving crystal polymorphisms by finding “stationary points” from quantitative analysis of crystal growth response surfaces
Published in Journal of crystal growth (1996)“…Quantitative analysis of statistically sampled experimental designs have shown that a functionally interesting crystal growth polymorphism for E. coli cytidine…”
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Journal Article Conference Proceeding -
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X-ray Crystallographic Studies of Candida albicans Dihydrofolate Reductase
Published in The Journal of biological chemistry (28-11-1997)“…The recent rise in systemic fungal infections has created a need for the development of new antifungal agents. As part of an effort to provide therapeutically…”
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Receptor-based design of dihydrofolate reductase inhibitors: comparison of crystallographically determined enzyme binding with enzyme affinity in a series of carboxy-substituted trimethoprim analogs
Published in Journal of medicinal chemistry (01-03-1985)“…By the use of molecular models of Escherichia coli dihydrofolate reductase (DHFR), analogues of trimethoprim (TMP) were designed which incorporated various…”
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Receptor-based design of dihydrofolate reductase inhibitors: comparison of crystallographically determined enzyme binding with enzyme affinity in a series of carboxy-substituted trimethoprim analogs
Published in Journal of medicinal chemistry (01-10-1982)“…The author report here the design, synthesis, DHFR affinity, and X-ray crystallographic binding analysis of a series of 3'-carboxyalkoxy analogues of TMP. At…”
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X-ray crystallographic studies of Candida albicans dihydrofolate reductase. High resolution structures of the holoenzyme and an inhibited ternary complex
Published in The Journal of biological chemistry (28-11-1997)“…The recent rise in systemic fungal infections has created a need for the development of new antifungal agents. As part of an effort to provide therapeutically…”
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