VSE knjižnice (vzajemna bibliografsko-kataložna baza podatkov COBIB.SI)
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Efficient and selective biosynthesis of a precursor-directed FK506 analogue : paving the way for click chemistryGoranovič, Dušan ...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.Vir: Journal of natural products. - ISSN 0163-3864 (Vol. 88, iss. 3, 2025, str. 619-630)Vrsta gradiva - članek, sestavni del ; neleposlovje za odrasleLeto - 2025Jezik - angleškiCOBISS.SI-ID - 228597507
Digitalne vsebine: dCOBISS
| Avtor | Goranovič, Dušan ... |
| Naslov | Efficient and selective biosynthesis of a precursor-directed FK506 analogue : paving the way for click chemistry |
| Datum objave | 2025-03-10 |
| COBISS.SI-ID | 228597507 |
| Verzija objave v repozitoriju | Založnikova različica |
| Licenca objave v repozitoriju | Creative Commons Priznanje avtorstva 4.0 Mednarodna |
| Embargo | Takojšnja javna objava |
Projekti in financerji, navedeni v objavi
| Naziv | Akronim | Številka projekta | Financer |
|---|---|---|---|
| Mikrobiologija in biotehnologija živil in okolja | P4-0116-2022 |
Javna agencija za znanstvenoraziskovalno in inovacijsko dejavnost Republike Slovenije |
|
| Nova tehnologija za pridobivanje novih poliketidnih vodnic s kemijsko reaktivnimi skupinami | L4-5530-2013 |
Javna agencija za znanstvenoraziskovalno in inovacijsko dejavnost Republike Slovenije |
|
| Analitika in kemijska karakterizacija materialov ter procesov | P1-0034-2020 |
Javna agencija za znanstvenoraziskovalno in inovacijsko dejavnost Republike Slovenije |
|
| Targeting convergent mechanisms of inefficient immunity in tumors and chronic infections | SFB 1292 TP18 | 318346496 |
Deutsche Forschungsgemeinschaft |
| Heterogeneity and functional specialization of regulatory T cells in distinct microenvironments | SFB355 TPA4 | 490846870 |
Deutsche Forschungsgemeinschaft |
| Young Researcher Grant | 53621 |
Javna agencija za znanstvenoraziskovalno in inovacijsko dejavnost Republike Slovenije |
Datoteke, ki spadajo k objavi
https://d.cobiss.net/repository/si/files/228597507/155395/Efficient-and-selective-biosynthesis-of-a-precursor-directed.pdf
Vir: Osebne bibliografije
in: SICRIS
