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8. Editors' choise - The effect of anchor group and alkyl backbone chain on performance of organic compounds as corrosion inhibitors for aluminum investigated using an Integrative experimental-modeling approachIngrid Milošev, Dolores Zimerl, Charly Carrière, Sandrine Zanna, Antoine Seyeux, Jernej Iskra, Stojan Stavber, Fatah Chiter, Matic Poberžnik, Dominique Costa, Anton Kokalj, Philippe Marcus, 2020, izvirni znanstveni članek Objavljeno v DiRROS: 14.05.2025; Ogledov: 214; Prenosov: 46
 Celotno besedilo (5,21 MB) |
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10. Efficient and selective biosynthesis of a precursor-directed FK506 analogue : paving the way for click chemistryDušan Goranovič, Branko Jenko, Barbara Ramšak, Ajda Podgoršek Berke, Leon Bedrač, Jaka Horvat, Martin Šala, Damjan Makuc, Guilhermina M. Carriche, Luana Silva, Aleksandra Lopez Krol, Alen Pšeničnik, Maria Beatriz Duran Alonso, Martina Avbelj, Stojan Stavber, Janez Plavec, Tim Sparwasser, Rolf Müller, Gregor Kosec, Štefan Fujs, Hrvoje Petković, 2025, izvirni znanstveni članek Povzetek: The medically important immunosuppressant FK506 is a structurally complex macrolactone biosynthesized by a combined polyketide synthase and a nonribosomal peptide synthetase enzyme complex. Its acyltransferase domain 4 (AT4) selects an unusual extender unit, resulting in an allyl moiety on carbon 21 of the macrolactone backbone. Based on the AT4 domain, chemobiosynthetic processes have been developed that enable the introduction of diverse moieties at the carbon 21 position. However, the novel moieties that were introduced into the polyketide backbone are chemically inert. Reported here is a novel and efficient chemobiosynthetic approach that ensures high titer of an FK506 analogue containing a propargyl moiety. The novel FK506 analogue displays lower immunosuppression activity than FK506 with significantly reduced cytotoxicity. More importantly, the propargyl moiety contains a terminal alkyl group, which makes click chemistry reactions possible; this approach may potentially be translated to other medically important drugs of polyketide origin.
Objavljeno v DiRROS: 15.04.2025; Ogledov: 228; Prenosov: 58
Celotno besedilo (3,26 MB) |
