Search Results - "Kuyper, L F"

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 by Shewchuk, Lisa, Hassell, Anne, Wisely, Bruce, Rocque, Warren, Holmes, William, Veal, James, Kuyper, Lee F

“…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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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 by WHITLOW, Marc, HOWARD, Andrew J., STEWART, David, HARDMAN, Karl D., CHAN, Joseph H., BACCANARI, David P., TANSIK, Robert L., HONG, Jean S., KUYPER, Lee F.

“…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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Oxindole-Based Inhibitors of Cyclin-Dependent Kinase 2 (CDK2):  Design, Synthesis, Enzymatic Activities, and X-ray Crystallographic Analysis by Bramson, H. Neal, Corona, John, Davis, Stephen T, Dickerson, Scott H, Edelstein, Mark, Frye, Stephen V, Gampe, Robert T, Harris, Phil A, Hassell, Anne, Holmes, William D, Hunter, Robert N, Lackey, Karen E, Lovejoy, Brett, Luzzio, Michael J, Montana, Val, Rocque, Warren J, Rusnak, David, Shewchuk, Lisa, Veal, James M, Walker, Duncan H, Kuyper, Lee F

“…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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Basis of selectivity of antibacterial diaminopyrimidines by Baccanari, D P, Kuyper, L F

“…The basis for the high affinity and selectivity of trimethoprim [2,4-diamino-5-(3',4',5'-trimethoxybenzyl)pyrimidine, TMP] and several close structural…”
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Recent applications of protein crystallography and structure-guided drug design by Williams, Shawn P, Kuyper, Lee F, Pearce, Kenneth H

“…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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Selective Inhibitors of Candida albicans Dihydrofolate Reductase: Activity and Selectivity of 5-(Arylthio)-2,4-diaminoquinazolines by Chan, Joseph H, Hong, Jean S, Kuyper, Lee F, Baccanari, David P, Joyner, Suzanne S, Tansik, Robert L, Boytos, Christine M, Rudolph, Sharon K

“…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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X-ray crystallographic studies of Candida albicans dihydrofolate reductase. High resolution structures of the holoenzyme and an inhibited ternary complex by Whitlow, M, Howard, A J, Stewart, D, Hardman, K D, Kuyper, L F, Baccanari, D P, Fling, M E, Tansik, R L

“…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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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 by Kuyper, Lee F, Baccanari, David P, Jones, Michael L, Hunter, Robert N, Tansik, Robert L, Joyner, Suzanne S, Boytos, Christine M, Rudolph, Sharon K, Knick, Vince, Wilson, H. Robert, Caddell, J. Marc, Friedman, Henry S, Comley, John C. W, Stables, Jeremy N

“…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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Receptor-based design of dihydrofolate reductase inhibitors: comparison of crystallographically determined enzyme binding with enzyme affinity in a series of carboxy-substituted trimethoprim analogs by Kuyper, Lee F, Roth, Barbara, Baccanari, David P, Ferone, Robert, Beddell, Christopher R, Champness, John N, Stammers, David K, Dann, John G, Norrington, Frank E. A

“…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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Pyrrolo[2,3- d]pyrimidines and pyrido[2,3- d]pyrimidines as conformationally restricted analogues of the antibacterial agent trimethoprim by Kuyper, Lee F, Garvey, Janice M, Baccanari, David P, Champness, John N, Stammers, David K, Beddell, Christopher R

“…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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Synthesis of 1,3-diamino-7,8,9,10-tetrahydropyrido[3,2-f]-quinazolines. Inhibitors of Candida albicans dihydrofolate reductase as potential antifungal agents by Chan, Joseph H., Baccanari, David P., Tansik, Robert L., Boytos, Christine M., Rudolph, Sharon K., Brown, Andrew D., Hong, Jean S., Kuyper, Lee F., Jones, Michael L.

“…A series of novel 1,3‐diamino‐7,8,9,10‐tetrahydropyrido[3,2‐f]quinazolines were synthesized starting from 6‐amino‐5‐cyanoquinoline (4). These compounds…”
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The amino acid sequence and configuration of tentoxin by Meyer, W L, Kuyper, L F, Lewis, R B, Templeton, G E, Woodhead, S H

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Resolving crystal polymorphisms by finding “stationary points” from quantitative analysis of crystal growth response surfaces by Kuyper, Lee F., Carter, Charles W.

“…Quantitative analysis of statistically sampled experimental designs have shown that a functionally interesting crystal growth polymorphism for E. coli cytidine…”
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Prevention of Chemotherapy-Induced Alopecia in Rats by CDK Inhibitors by Davis, Stephen T., Benson, Bill G., Bramson, H. Neal, Chapman, Dennis E., Dickerson, Scott H., Dold, Karen M., Eberwein, Derek J., Edelstein, Mark, Frye, Stephen V., Gampe, Robert T., Griffin, Robert J., Harris, Philip A., Hassell, Anne M., Holmes, William D., Hunter, Robert N., Knick, Victoria B., Lackey, Karen, Lovejoy, Brett, Luzzio, Michael J., Murray, Doris, Parker, Patricia, Rocque, Warren J., Shewchuk, Lisa, Veal, James M., Walker, Duncan H., Kuyper, Lee F.

“…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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Free energy calculations on the relative solvation free energies of benzene, anisole, and 1,2,3-trimethoxybenzene: theoretical and experimental analysis of aromatic methoxy solvation by Kuyper, Lee F, Hunter, Robert N, Ashton, David

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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 by Kuyper, Lee F, Roth, Barbara, Baccanari, David P, Ferone, Robert, Beddell, Christopher R, Champness, John N, Stammers, David K, Dann, John G, Norrington, Frank E. A

“…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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Use of 1-H nuclear magnetic resonance spectroscopy for sequence and configuration analysis of cyclic tetrapeptides. The structure of Tentoxin-1,2a--d by Meyer, W L, Templeton, G E, Grable, C I, Jones, R, Kuyper, L F, Lewis, R B, Sigel, C W, Woodhead, S H

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Site-specific Conjugation on Serine arrow right Cysteine Variant Monoclonal Antibodies by Stimmel, J B, Merrill, B M, Kuyper, L F, Moxham, C P, Hutchins, J T, Fling, ME, Kull Jr, FC

“…We have engineered a cysteine residue at position 442 (EU/OU numbering) in the third constant domain (C sub(H)3) of the heavy chain of several IgGs with…”
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Site-specific conjugation on serine right-arrow cysteine variant monoclonal antibodies by Stimmel, J B, Merrill, B M, Kuyper, L F, Moxham, C P, Hutchins, J T, Fling, M E, Kull, Jr, F C

“…We have engineered a cysteine residue at position 442 (EU/OU numbering) in the third constant domain (C(H)3) of the heavy chain of several IgGs with different…”
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Site-specific Conjugation on Serine → Cysteine Variant Monoclonal Antibodies by Stimmel, Julie B., Merrill, Barbara M., Kuyper, Lee F., Moxham, Cary P., Hutchins, Jeff T., Fling, Mary E., Kull, Frederick C.

“…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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