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Št. zadetkov: 3
3,1-benzothiazines, 1,4-benzodioxines, 1,4-benzoxazines as inhibitors of matriptase-2
Polya G. Roydeva, Anna-Madeleine Beckmann, Marit Stirnberg, Jožko Cesar, Danijel Kikelj, Janez Ilaš, Michael Gütschow
Izvirni znanstveni članek
Oznake: marine alkaloid;Agelas;clathrodin;oroidin;pyrrole-2-aminoimidazole;antibacterial;benzamidines;4H-3,1-benzothiazin-4-ones;2,3-dihydro-1,4-benzodioxines;3,4-dihydro- 2H-1,4-benzoxazines;matriptase-2;protease inhibition;
The liver enzyme matriptase-2 is a multi-domain, transmembrane serine protease with an extracellular, C-terminal catalytic domain. Synthetic low-molecular weight inhibitors of matriptase-2 have potential as therapeutics to treat iron overload syndromes, in particular in patients with %-thalassemia. ...
Leto: 2016 Vir: Fakulteta za farmacijo (UL FFA)
Heterobifunctional ligase recruiters enable pan-degradation of inhibitor of apoptosis proteins
Yuen Lam Dora Ng, Aleša Bricelj, Jacqueline A. Jansen, Arunima Murgai, Kirsten Peter, Katherine A. Donovan, Michael Gütschow, Jan Krönke, Christian Steinebach, Izidor Sosič
Izvirni znanstveni članek
Oznake: antagonists;degradation;ligands;mixtures;peptides;proteins;
Proteolysis targeting chimeras (PROTACs) represent a new pharmacological modality to inactivate disease-causing proteins. PROTACs operate via recruiting E3 ubiquitin ligases, which enable the transfer of ubiquitin tags onto their target proteins, leading to proteasomal degradation. However, several ...
Leto: 2023 Vir: Fakulteta za farmacijo (UL FFA)
Accessing three-branched high-affinity cereblon ligands for molecular glue and protein degrader design
Robert Kuchta, Christopher Heim, Alexander Herrmann, Samuel Maiwald, Yuen Lam Dora Ng, Izidor Sosič, Tim Keuler, Jan Krönke, Michael Gütschow, Marcus D. Hartmann, Christian Steinebach
Izvirni znanstveni članek
Oznake: the Petasis borono-Mannich reaction;Strecker synthesis;CRBN ligands;
The Petasis borono-Mannich reaction was employed for an alternative entry towards three-branched cereblon ligands. Such compounds are capabable of making multiple interactions with the protein surface and possess a suitable linker exit vector. The high-affinity ligands were used to assemble prototyp ...
Leto: 2023 Vir: Fakulteta za farmacijo (UL FFA)
Št. zadetkov: 3
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