Výsledky vyhledávání - "Karl D. Hardman"

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

Autor: Lee F. Kuyper, Karl D. Hardman, Robert L. Tansik, Jean S. Hong, David Stewart, Marc Whitlow, Joseph H. Chan, Andrew J. Howard, David P. Baccanari

Publikováno v: Journal of Medicinal Chemistry. 44:2928-2932

X-ray crystallographic analysis of 5-(4'-substituted phenyl)sulfanyl-2,4-diaminoquinazoline inhibitors in ternary complex with Candida albicans dihydrofolate reductase (DHFR) and NADPH revealed two distinct modes of binding. The two compounds with sm

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b9280f132de00963466761d27b1ea5fc
https://doi.org/10.1021/jm0101444

Zobrazit plný text záznamu

X-ray Crystallographic Studies of Candida albicans Dihydrofolate Reductase

Autor: Mary E. Fling, Marc Whitlow, Karl D. Hardman, Lee F. Kuyper, David P. Baccanari, David H. Stewart, Robert L. Tansik, Andrew Howard

Publikováno v: Journal of Biological Chemistry. 272:30289-30298

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 effective inhibitors of fungal dihydrofolate reductase (DHFR), we have cloned, expressed, p

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::cd09531b1ded6179854d95f481b14dc4
https://doi.org/10.1074/jbc.272.48.30289

Zobrazit plný text záznamu

Potent carboxylate inhibitors of stromelysin containing P2′ piperazic acids and P1′ biaryl moeities

Autor: Carl P. Decicco, Li Wang, David J. Nelson, Dayton T. Meyer, Elizabeth C. Arner, Robert J. Cherney, Robert A. Copeland, Karl D. Hardman

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 7:1757-1762

Several carboxylate derivatives with variation at the P1′ residue were synthesized and evaluated as stromelysin (MMP-3) inhibitors. Compounds containing a biphenyl moiety at P1′ were found to be potent inhibitors of MMP-3. An X-ray crystal struct

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::c7d3bda6169c41b0a470236d40bf3502
https://doi.org/10.1016/s0960-894x(97)00308-9

Zobrazit plný text záznamu

Probing the P3′ pocket of stromelysin with piperazic acid analogs

Autor: David A. Nugiel, Karl D. Hardman, Robert A. Copeland, David J. Nelson, Carl P. Decicco, Kim Jacobs

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 5:3053-3056

The preparation and SAR of several piperazic acid-based stromelysin (MMP-3) inhibitors is presented. The standard P3′ methyl amide substituent can be replaced by other carboxy based substituents and maintain good binding affinity. Removal of a hydr

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::b5334bbe7536680ee17bc61e6335f25e
https://doi.org/10.1016/0960-894x(95)00536-1

Zobrazit plný text záznamu

1.85 Å structure of anti-fluorescein 4-4-20 Fab

Autor: Karl D. Hardman, Marc Whitlow, Jay F. Wood, Andrew Howard, Edward W. Voss

Publikováno v: "Protein Engineering, Design and Selection". 8:749-761

The crystal complex of fluorescein bound to the high-affinity anti-fluorescein 4-4-20 Fab (Ka = 10(10) M-1 at 2 degrees C) has been determined at 1.85 A. Isomorphous crystals of two isoelectric forms (pI = 7.5 and 7.9) of the anti-fluorescein 4-4-20

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::00427cbbbf5c15db16eae1a0908bb02d
https://doi.org/10.1093/protein/8.8.749

Zobrazit plný text záznamu

An improved linker for single-chain Fv with reduced aggregation and enhanced proteolytic stability

Autor: Brian A. Bell, Takashi Yokota, Karl D. Hardman, Diane E. Milenic, Mare Whitlow, James F. Wood, Margaret E. Schott, David Filpula, Steven L. Hubert, Sheau-Line Feng, Michele L. Rollence, Jeffrey Schlom

Publikováno v: "Protein Engineering, Design and Selection". 6:989-995

The effects of linker length on binding affinity and degree of aggregation have been examined in the antifluorescein 4-4-20 and anticarcinoma CC49 single-chain Fvs. Longer linkers in the antifluorescein sFvs have higher affinities for fluorescein and

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6319453d129059f78ba3b8b411e35a98
https://doi.org/10.1093/protein/6.8.989

Zobrazit plný text záznamu

ChemInform Abstract: Structure-Based Design and Synthesis of a Series of Hydroxamic Acids with a Quaternary-Hydroxy Group in P1 as Inhibitors of Matrix Metalloproteinases

Autor: Elizabeth C. Arner, Ronald L. Magolda, Carl P. Decicco, Irina Cipora Jacobson, Prabhakar G. Reddy, Zelda R. Wasserman, Karl D. Hardman, Robert A. Copeland, Maryanne B. Covington

Publikováno v: ChemInform. 29

Examination of the S1 area of the active site of pro-stromelysin has led us to the design of novel and potent inhibitors of matrix metalloproteinases containing constrained quaternary-hydroxy group at P1. The synthesis and biological activity of thes

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::5643733f37d9c8d172844838d0281a2d
https://doi.org/10.1002/chin.199830289

Zobrazit plný text záznamu

Vyhledávací nástroje:

Upřesnit hledání