Evidence map›Paper›PMID 20066263›Full record

ReviewOrganic & biomolecular chemistry2010

Glycosidase inhibition: assessing mimicry of the transition state.

Tracey M Gloster, Gideon J Davies

Abstract readReview
In one paragraph

Review in Organic & biomolecular chemistry, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 59 papers.

0numbers the graph read from it
0cells of the map it votes in
59citing papers in PubMed
–field-weighted citation impact
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

59 citing papers in PubMed.

  1. Article
  2. Article
  3. Review
  4. β-l-ACS chemical biology · 2023
    Article
  5. Chemical science · 2023
    Article
  6. Review
  7. Article
  8. Review
  9. Article
  10. Article
  11. Influence of Side Chain Conformation on the Activity of Glycosidase Inhibitors.Angewandte Chemie (International ed. in English) · 2023
    Article
  12. Article
  13. Article
  14. Review
  15. Tuning the activity of iminosugars: novelJournal of enzyme inhibition and medicinal chemistry · 2021
    Article
  16. Article
  17. Review
  18. Article
  19. Article
  20. Article
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

2 authors.

Tracey M GlosterYork Structural Biology Laboratory, Department of Chemistry, University of York, Heslington, York YO10 5YW, UK. gloster@ysbl.york.ac.uk
Gideon J Davies

Funding

Wellcome Trust 082572
6 · The paper itself

Abstract

Glycoside hydrolases, the enzymes responsible for hydrolysis of the glycosidic bond in di-, oligo- and polysaccharides, and glycoconjugates, are ubiquitous in Nature and fundamental to existence. The extreme stability of the glycosidic bond has meant these enzymes have evolved into highly proficient catalysts, with an estimated 10(17) fold rate enhancement over the uncatalysed reaction. Such rate enhancements mean that enzymes bind the substrate at the transition state with extraordinary affinity; the dissociation constant for the transition state is predicted to be 10(-22) M. Inhibition of glycoside hydrolases has widespread application in the treatment of viral infections, such as influenza and HIV, lysosomal storage disorders, cancer and diabetes. If inhibitors are designed to mimic the transition state, it should be possible to harness some of the transition state affinity, resulting in highly potent and specific drugs. Here we examine a number of glycosidase inhibitors which have been developed over the past half century, either by Nature or synthetically by man. A number of criteria have been proposed to ascertain which of these inhibitors are true transition state mimics, but these features have only be critically investigated in a very few cases.

Indexed as

Biomimetic MaterialsCarbohydrate MetabolismEnzyme InhibitorsGlycoside HydrolasesHumansHydrogen-Ion ConcentrationThermodynamicsEnzyme InhibitorsGlycoside Hydrolases

Identifiers

PMID20066263
PMCPMC2822703

What OpenQuestion holds

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Registered trials

None linked

Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.