Structure-based design and characterization of novel platforms for ricin and shiga toxin inhibition.

No abstract is available for this paper.

• Publication year

  2002

• Venue

  Journal of Medicinal Chemistry

• Publication date

  2002-01-03

• Fields of study

  Medicine, Chemistry

• Identifiers
  DOI 10.1021/JM010186SPMID 11754581
• External record

  Open on Semantic Scholar

• Source metadata

  Semantic Scholar, PubMed

• No claims are published for this paper.

• No concepts are published for this paper.

• Shiga toxin attacks bacterial ribosomes as effectively as eucaryotic ribosomes.

  1998cited by this paper
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  1998cited by this paper
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  1997cited by this paper
• Structure-based identification of a ricin inhibitor.

  1997cited by this paper
• [21] Data collection strategy.

  1997cited by this paper
• Processing of X-ray diffraction data collected in oscillation mode.

  1997cited by this paper
• 2-Amino-4-oxo-5-substituted-pyrrolo[2,3-d]pyrimidines as Nonclassical Antifolate Inhibitors of Thymidylate Synthase.

  1997cited by this paper
• 2-amino-4-oxo-5-substituted-pyrrolo[2,3-d]pyrimidines as nonclassical antifolate inhibitors of thymidylate synthase.

  1996cited by this paper
• The Structure of Ribosome Inactivating Proteins from Plants

  1996cited by this paper
• X-ray structure of recombinant ricin A-chain at 1.8 A resolution.

  1994cited by this paper
• Ricin: structure, mode of action, and some current applications

  1994cited by this paper
• Purification of recombinant Shiga-like toxin type I A1 fragment from Escherichia coli.

  1994cited by this paper
• Crystal structure of the holotoxin from Shigella dysenteriae at 2.5 A resolution.

  1994cited by this paper
• THE STRUCTURE OF RECOMBINANT RICIN A CHAIN AT 2.3 ANGSTROMS

  1993cited by this paper
• The role of tyrosine-114 in the enzymatic activity of the Shiga-like toxin I A-chain

  1993cited by this paper
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  1993cited by this paper
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• X-ray analysis of substrate analogs in the ricin A-chain active site.

  1992cited by this paper
• Analysis of several key active site residues of ricin A chain by mutagenesis and X-ray crystallography.

  1992cited by this paper
• Shiga toxin: biochemistry, genetics, mode of action, and role in pathogenesis.

  1992cited by this paper
• X-PLOR Version 3.1: A System for X-ray Crystallography and NMR

  1992cited by this paper
• Structure of ricin A‐chain at 2.5 Å

  1991cited by this paper
• Improved methods for building protein models in electron density maps and the location of errors in these models.

  1991cited by this paper
• Site‐directed mutagenesis of ricin A‐chain and implications for the mechanism of action

  1991cited by this paper
• Role of arginine 180 and glutamic acid 177 of ricin toxin A chain in enzymatic inactivation of ribosomes

  1990cited by this paper
• The RNA N-glycosidase activity of ricin A-chain. The characteristics of the enzymatic activity of ricin A-chain with ribosomes and with rRNA.

  1988cited by this paper
• The RNA N-glycosidase activity of ricin A-chain.

  1988cited by this paper
• Synthesis of Queuine, the Base of Naturally Occurring Hypermodified Nucleoside (Queuosine), and Its Analogues.

  1988cited by this paper
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  1987cited by this paper
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  1987cited by this paper
• Crystallization of ricin A chain obtained from a cloned gene expressed in Escherichia coli.

  1987cited by this paper
• The three-dimensional structure of ricin at 2.8 A.

  1987cited by this paper
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  1986cited by this paper
• [Preparation of the disulfide of 3-mercaptopyridine-2-sulfonamide].

  1984cited by this paper
• A New Synthesis of Oxazolo[5,4-d]pyrimid-7-ones

  1983cited by this paper
• Toxic lectins and related proteins

  1982cited by this paper
• SYNTHESIS AND ANTIMICROBIAL TESTING OF 2-AMINO-6-HYDROXYMETHYL-4-(3H)PYRIDO(3,2-D)PYRIMIDINONE

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• STUDIES DIRECTED TOWARD A TOTAL SYNTHESIS OF NUCLEOSIDE Q. ANNULATION OF 2,6-DIAMINOPYRIMIDIN-4-ONE WITH α-HALO CARBONYLS TO FORM PYRROLO(2,3-D)PYRIMIDINES AND FURO(2,3-D)PYRIMIDINES

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  1978cited by this paper
• New synthesis of 5H-pyrrolo[3,2-d]pyrimidines via pyrimido[5,4-c]pyridazines

  1978cited by this paper
• PREPARATION OF 2,5‐DIAMINO‐4,6‐DICHLOROPYRIMIDINE

  1976cited by this paper
• 26. Pyrrolo[2,3-d]pyrimidines

  1960cited by this paper
• Potential Purine Antagonists. XIII. Synthesis of Some 8-Methylpurines1

  1958cited by this paper
• Potential Purine Antagonists. XI. Synthesis of Some 9-Aryl(alkyl)-2,6-disubstituted Purines

  1958cited by this paper
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  1949cited by this paper

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  2023cites this paper
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  2017cites this paper
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• Minisci reactions: Versatile CH-functionalizations for medicinal chemists

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  2010cites this paper
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  2010influential citation
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  2010cites this paper
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