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Crystal structure of human type II inosine monophosphate dehydrogenase: implications for ligand binding and drug design.
TLDR
The 2.9-A structure of a ternary complex of the human type II isoform of IMPDH is presented, suggesting strategies for the design of isoform-specific agents in antitumor and immunosuppressive drug design.
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Computational studies of nonbonded sulfur-oxygen and selenium-oxygen interactions in the thiazole and selenazole nucleosides
Computational studies have been performed to investigate the origin and magnitude of a biologically important nonbonded interaction: the sulfur-oxygen and selenium-oxygen interaction observed in the…
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Synthesis of 3-deazaneplanocin A, a powerful inhibitor of S-adenosylhomocysteine hydrolase with potent and selective in vitro and in vivo antiviral activities.
TLDR
3-deazaneplanocin A displayed excellent antiviral activity in cell culture against vesicular stomatitis, parainfluenza type 3, yellow fever, and vaccinia viruses, and in vivo against vaccinia virus by using a mouse tailpox assay.
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Crystal structure and amide H/D exchange of binary complexes of alcohol dehydrogenase from Bacillus stearothermophilus: insight into thermostability and cofactor binding.
TLDR
It was found that 9 of 21 peptides show some decrease in the level of deuteron incorporation upon NAD(+) binding, and another 4 peptides display slower exchange rates, which suggests that the transition from the open to the closed conformation caused by cofactor binding has some long-range effects on the protein structure and dynamics.
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Analogues of platelet activating factor. 4. Some modifications of the phosphocholine moiety.
TLDR
Racemic analogues of platelet activating factor (PAF) in which the methylene bridge separating the phosphate and trimethylammonium moieties is altered in length have been prepared and exhibited no detectable hypotensive or platelet aggregating activity.
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Cofactor mimics as selective inhibitors of NAD-dependent inosine monophosphate dehydrogenase (IMPDH)--the major therapeutic target.
TLDR
Recent progress in the development of new drugs based on inhibition of IMP dehydrogenase is described, with mizoribine and mycophenolic mofetil introduced as immunosuppressants.
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IMP dehydrogenase : structural aspects of inhibitor binding.
TLDR
A number of crystal structures of IMPDH reveal enzyme-ligand interactions which suggest strategies for the design of improved inhibitors, including structures of the human type II, hamster, Tritrichomonas foetus, Streptococcus pyogenes and Borrelia burgdorferi enzymes.
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A database study of nonbonded intramolecular sulfur-nucleophile contacts.
TLDR
A search of the Cambridge Structural Database was performed to investigate nonbonded intramolecular 1,4 S...O close contacts of the kind seen in the thiazole nucleoside tiazofurin and other classes of compounds, and findings indicate that 1, 4 S...
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Carboxamide group conformation in the nicotinamide and thiazole-4-carboxamide rings: implications for enzyme binding.
TLDR
Results indicate that the thiazole-4-carboxamide group is constrained in the conformation in which the amino group is cis-planar to the ring nitrogen, which confirms previous computational studies and is consistent with results from a survey of the Cambridge Structural Database.
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Chemical synthesis of benzamide adenine dinucleotide: inhibition of inosine monophosphate dehydrogenase (types I and II).
TLDR
Treatment of 3-(2,3-O-isopropylidene-beta-D-ribofuranosyl)benzamide with POCl3 in (EtO)3-PO afforded only little phosphorylation product, but the major product was 5'-chlorobenzamide riboside, which inhibits inosine monophosphate dehydrogenase type I and type II with same degree of potency.
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