About: Transition-state mimicking inhibitors of human betaine: homocysteine S-methyltransferase     Goto   Sponge   NotDistinct   Permalink

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  • We propose the design, synthesis and biological characterization of new inhibitors of human betaine: homocysteine S-methyltransferase (BHMT). These new inhibitors will mimic the structure of the hypothetical transition-state of substrates upon binding to the enzyme active site. There classes of compounds mimicking the transition-state are planned to be synthesized: (i) sulfur containing compounds, (ii) phosphorus containing compounds of phosphinate, phosphonate and phosphodiester type and (iii) phosphorus containing compounds substituted by nitjrogen or sulfur containing moieties. The accent will be directed to both potency and selectivity of inhibitors towards BHMT and related enzymes, namely methionine synthase and cystathionine beta-synthetase. Potential metabolic stability of compounds will also be taken into account. The most promising inhibitors should be used in pharmacological experiments for studying the role of BHMT in vivo. (en)
  • Navrhujeme design, syntézu a biologickou charakterizaci nových inhibitorů lidského enzymu betain: homocystein S-methyltransferázy (BHMT). Tyto nové inhibitory budou napodobovat hypotetický tranzitní stav substrátů během jejich vazby do aktivního místa enzymu. Plánujeme syntézu tří skupin látek napodobujících tranzitní stav: (i) síru obsahující sloučeniny, (ii) fosfor obsahující sloučeniny fosfinátového, fosfonátového a fosfodiesterového typu a (iii) fosfor obsahující sloučeniny substituované skupinami obsahujícími dusík nebo síru. Důraz bude kladen jednak na potenci ale i selektivitu inhibitorů vůči BHMT a příbuzným enzymům methionin syntháze a cystathionin beta-synthetáze. V úvahu budeme brát i potencionální metabolickou stabilitu látek. Nejslibnější inhibitory by měly být farmakologicky testovány za účelem studia role BHMT in vivo.
Title
  • Transition-state mimicking inhibitors of human betaine: homocysteine S-methyltransferase (en)
  • Tranzitní stav napodobující inhibitory lidského enzymu betain: homocystein S-methyltransferázy
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  • IAA4055302
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  • betaine: homocysteine S-methyltransferase; inhibitors; transition-state inhibitors; phosphinates; phosphonates; thiols; thioethers; sznthesis (en)
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  • We synthesized and characterized a series of new inhibitors of human BHMT. The most potent inhibitors were used to study intrinsic fluorescence of BHMT and tested in mice in vivo. We confirmed the role of BHMT in the metabolism of sulfur amino acids. (en)
  • Připravili jsme a charakterizovali sérii nových inhibitorů lidské BHMT. Nejsilnější inhibitory byly použity ke studiu flurorescence BHMT a testovány na myších in vivo. Podařilo se nám potvrdit roli BHMT v metabolismu sirných aminokyselin. (cs)
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  • inhibitors
  • phosphonates
  • phosphinates
  • thioethers
  • thiols
  • transition-state inhibitors
  • betaine: homocysteine S-methyltransferase
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