Abstract
By combining in the same molecule Ras-interacting aromatic moieties and a sugar, we prepared a water-soluble Ras ligand that binds Ras and inhibits guanine nucleotide exchange. With this compound it was possible to determine experimentally by a (15)N-edited HSQC NMR experiment the ligand-Ras binding interface.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Antineoplastic Agents / chemical synthesis*
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Antineoplastic Agents / pharmacology
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Chemistry, Pharmaceutical / methods*
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Drug Design
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Glucosides / chemical synthesis*
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Glucosides / pharmacology
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Guanine / chemistry
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Humans
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Ligands
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Magnetic Resonance Spectroscopy / methods
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Mice
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Models, Molecular
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Molecular Conformation
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NIH 3T3 Cells
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Protein Binding
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Sulfonamides / chemical synthesis*
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Sulfonamides / pharmacology
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ras Proteins / antagonists & inhibitors*
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ras Proteins / metabolism
Substances
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Antineoplastic Agents
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Glucosides
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Ligands
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SCH 54292
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Sulfonamides
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Guanine
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ras Proteins