ArticleChembiochem : a European journal of chemical biology2009
The molecular basis of inhibition of Golgi alpha-mannosidase II by mannostatin A.
Article in Chembiochem : a European journal of chemical biology, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. An erratum has been issued. Cited by 12 papers.
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Who cites it
12 citing papers in PubMed, 37 citations in OpenAlex.
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- 1,4-Dideoxy-1,4-imino-D- and L-lyxitol-based inhibitors bind to Golgi α-mannosidase II in different protonation forms.Organic & biomolecular chemistry · 2022Article
- Structure based virtual screening of natural product molecules as glycosidase inhibitors.In silico pharmacology · 2021Article
- Impact of cell culture media additives on IgG glycosylation produced in Chinese hamster ovary cells.Biotechnology and bioengineering · 2019Article
- Identification of a potential allosteric site of Golgi α-mannosidase II using computer-aided drug design.PloS one · 2019Article
- N-Benzyl Substitution of Polyhydroxypyrrolidines: The Way to Selective Inhibitors of Golgi α-Mannosidase II.ChemMedChem · 2018Article
- 'Click chemistry' synthesis of 1-(α-D-mannopyranosyl)-1,2,3-triazoles for inhibition of α-mannosidases.Carbohydrate research · 2015Article
- Mutations in four glycosyl hydrolases reveal a highly coordinated pathway for rhodopsin biosynthesis and N-glycan trimming in Drosophila melanogaster.PLoS genetics · 2014Article
- Characterisation of class I and II α-mannosidases from Drosophila melanogaster.Glycoconjugate journal · 2013Article
- Structure and kinetic investigation of Streptococcus pyogenes family GH38 alpha-mannosidase.PloS one · 2010Article
- Mechanistic insights into a Ca2+-dependent family of alpha-mannosidases in a human gut symbiont.Nature chemical biology · 2010Article
- Analysis of carbohydrates and glycoconjugates by matrix-assisted laser desorption/ionization mass spectrometry: an update for 2009-2010.Mass spectrometry reviewsReview
Corrections and comments
- Erratum issued
Authors and funding
5 authors at 3 institutions in 2 countries.
Funding
Abstract
Mannostatin A is a potent inhibitor of the mannose-trimming enzyme, Golgi alpha-mannosidase II (GMII), which acts late in the N-glycan processing pathway. Inhibition of this enzyme provides a route to blocking the transformation-associated changes in cancer cell surface oligosaccharide structures. Here, we report on the synthesis of new Mannostatin derivatives and analyze their binding in the active site of Drosophila GMII by X-ray crystallography. The results indicate that the interaction with the backbone carbonyl of Arg876 is crucial to the high potency of the inhibitor-an effect enhanced by the hydrophobic interaction between the thiomethyl group and an aromatic pocket vicinal to the cleavage site. The various structures indicate that differences in the hydration of protein-ligand complexes are also important determinants of plasticity as well as selectivity of inhibitor binding.
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Registered trials
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.