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Competitive inhibit...
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Mariano, Sandrine
(författare)
Competitive inhibitors of type B ribose 5-phosphate isomerases : design, synthesis and kinetic evaluation of new D-allose and D-allulose 6-phosphate derivatives
- Artikel/kapitelEngelska2009
Förlag, utgivningsår, omfång ...
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Elsevier BV,2009
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printrdacarrier
Nummerbeteckningar
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LIBRIS-ID:oai:DiVA.org:uu-129056
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https://urn.kb.se/resolve?urn=urn:nbn:se:uu:diva-129056URI
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https://doi.org/10.1016/j.carres.2009.02.024DOI
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https://res.slu.se/id/publ/49915URI
Kompletterande språkuppgifter
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Språk:engelska
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Sammanfattning på:engelska
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Ämneskategori:ref swepub-contenttype
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Ämneskategori:art swepub-publicationtype
Anmärkningar
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This study reports syntheses Of D-allose 6-phosphate (All6P), D-allulose (or D-psicose) 6-phosphate (Allu6P), and seven D-ribose 5-phosphate isomerase (Rpi) inhibitors. The inhibitors were designed as analogues of the 6-carbon high-energy intermediate postulated for the All6P to Allu6P isomerization reaction (Allpi activity) catalyzed by type B Rpi from Escherichia coli (EcRpiB). 5-PhosphO-D-ribonate, easily obtained through oxidative cleavage of either All6P or Allu6P, led to the original synthon 5-dihydrogenopliospho-D-ribono-1,4-lactone from which the other inhibitors could be synthesized through nucleophilic addition in one step. Kinetic evaluation on Allpi activity of EcRpiB shows that two of these compounds. 5phospho-D-ribonohydroxamic acid and N-(5-phospho-D-ribonoyl)-methylamine, indeed behave as new efficient inhibitors of EcRpiB; further, 5-phospho-D-ribonohydroxamic acid was demonstrated to have competitive inhibition. Kinetic evaluation on Rpi activity of both EcRpiB and RpiB from Mycobacterium tuberculosis (MtRpiB) shows that several of the designed 6-carbon high-energy intermediate analogues are new competitive inhibitors of both RpiBs. One of them, 5-phospho-D-ribonate, not only appears as the strongest competitive inhibitor of a Rpi ever reported in the literature, with a K-i value of 9 mu M for MtRpiB, but also displays specific inhibition of MtRpiB versus EcRpiB.
Ämnesord och genrebeteckningar
Biuppslag (personer, institutioner, konferenser, titlar ...)
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Roos, Annette K.Uppsala universitet,Institutionen för cell- och molekylärbiologi
(författare)
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Mowbray, Sherry L.Swedish University of Agricultural Sciences,Sveriges lantbruksuniversitet,Institutionen för molekylärbiologi,Department of Molecular Biology(Swepub:slu)51420
(författare)
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Salmon, Laurent
(författare)
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Uppsala universitetInstitutionen för cell- och molekylärbiologi
(creator_code:org_t)
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Sveriges lantbruksuniversitet
Sammanhörande titlar
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Ingår i:Carbohydrate Research: Elsevier BV344:7, s. 869-8800008-62151873-426X
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