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Träfflista för sökning "WFRF:(Corbet R.) srt2:(2020-2023)"

Sökning: WFRF:(Corbet R.) > (2020-2023)

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1.
  • Corbet, Brian P., et al. (författare)
  • Peptide Conjugated Dihydroazulene/Vinylheptafulvene Photoswitches in Aqueous Environment
  • 2023
  • Ingår i: European Journal of Organic Chemistry. - : John Wiley & Sons. - 1434-193X .- 1099-0690. ; 26:1
  • Tidskriftsartikel (refereegranskat)abstract
    • Light-responsive molecules have seen a major advance in modulating biological functions in recent years. Especially photoswitches are highly attractive building blocks due to the reversible nature of their light-mediated reactivity. They are frequently used to affect both the properties of small bioactive compounds and biomacromolecules if incorporated suitably. Despite their success in a plethora of applications, only a limited set of photochromic core structures is routinely employed and a large number of photochromic couples are under-investigated in biological context. Broadening the toolbox of photoswitches available to modulate biological activity would open new avenues and unlock the full potential of photoswitchable molecules for biological studies. In this work, we explore the photochemical and thermal properties of the dihydroazulene/vinylheptafulvene photochromic couple as peptide conjugates in aqueous environment.
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2.
  • Spillier, Q, et al. (författare)
  • Structure-Activity Relationships (SARs) of α-Ketothioamides as Inhibitors of Phosphoglycerate Dehydrogenase (PHGDH)
  • 2020
  • Ingår i: Pharmaceuticals (Basel, Switzerland). - : MDPI AG. - 1424-8247. ; 13:2
  • Tidskriftsartikel (refereegranskat)abstract
    • For many years now, targeting deregulation within cancer cells’ metabolism has appeared as a promising strategy for the development of more specific and efficient cancer treatments. Recently, numerous reports highlighted the crucial role of the serine synthetic pathway, and particularly of the phosphoglycerate dehydrogenase (PHGDH), the first enzyme of the pathway, to sustain cancer progression. Yet, because of very weak potencies usually in cell-based settings, the inhibitors reported so far failed to lay ground on the potential of this approach. In this paper, we report a structure–activity relationship study of a series of α-ketothioamides that we have recently identified. Interestingly, this study led to a deeper understanding of the structure–activity relationship (SAR) in this series and to the identification of new PHGDH inhibitors. The activity of the more potent compounds was confirmed by cellular thermal shift assays and in cell-based experiments. We hope that this research will eventually provide a new entry point, based on this promising chemical scaffold, for the development of therapeutic agents targeting PHGDH.
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