The Pseudo‐Natural Product Rhonin Targets RHOGDI
Abstract: For the discovery of novel chemical matter generally endowed with bioactivity, strategies may be particularly efficient that combine previous insight about biological relevance, e.g., natural product (NP) structure, with methods that enable efficient coverage of chemical space, such as fragment‐based design. We describe the de novo combination of different 5‐membered NP‐derived N‐heteroatom fragments to structurally unprecedented “pseudo‐natural products” in an efficient complexity‐generating and enantioselective one‐pot synthesis sequence. The pseudo‐NPs inherit characteristic elements of NP structure but occupy areas of chemical space not covered by NP‐derived chemotypes, and may have novel biological targets. Investigation of the pseudo‐NPs in unbiased phenotypic assays and target identification led to the discovery of the first small‐molecule ligand of the RHO GDP‐dissociation inhibitor 1 (RHOGDI1), termed Rhonin. Rhonin inhibits the binding of the RHOGDI1 chaperone to GDP‐bound RHO GTPases and alters the subcellular localization of RHO GTPases.
- Standort
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Deutsche Nationalbibliothek Frankfurt am Main
- Umfang
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Online-Ressource
- Sprache
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Englisch
- Erschienen in
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The Pseudo‐Natural Product Rhonin Targets RHOGDI ; day:02 ; month:03 ; year:2022 ; extent:1
Angewandte Chemie ; (02.03.2022) (gesamt 1)
- Urheber
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Akbarzadeh, Mohammad
Flegel, Jana
Patil, Sumersing
Shang, Erchang
Narayan, Rishikesh
Buchholzer, Marcel
Kazemein Jasemi, Neda S.
Grigalunas, Michael
Krzyzanowski, Adrian
Abegg, Daniel
Shuster, Anton
Potowski, Marco
Karatas, Hacer
Karageorgis, George
Mosaddeghzadeh, Niloufar
Zischinsky, Mia‐Lisa
Merten, Christian
Golz, Christopher
Brieger, Lucas
Strohmann, Carsten
Antonchick, Andrey P.
Janning, Petra
Adibekian, Alexander
Goody, Roger S.
Ahmadian, Mohammad Reza
Ziegler, Slava
Waldmann, Herbert
- DOI
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10.1002/ange.202115193
- URN
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urn:nbn:de:101:1-2022030314042584254526
- Rechteinformation
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Open Access; Der Zugriff auf das Objekt ist unbeschränkt möglich.
- Letzte Aktualisierung
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15.08.2025, 07:32 MESZ
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Beteiligte
- Akbarzadeh, Mohammad
- Flegel, Jana
- Patil, Sumersing
- Shang, Erchang
- Narayan, Rishikesh
- Buchholzer, Marcel
- Kazemein Jasemi, Neda S.
- Grigalunas, Michael
- Krzyzanowski, Adrian
- Abegg, Daniel
- Shuster, Anton
- Potowski, Marco
- Karatas, Hacer
- Karageorgis, George
- Mosaddeghzadeh, Niloufar
- Zischinsky, Mia‐Lisa
- Merten, Christian
- Golz, Christopher
- Brieger, Lucas
- Strohmann, Carsten
- Antonchick, Andrey P.
- Janning, Petra
- Adibekian, Alexander
- Goody, Roger S.
- Ahmadian, Mohammad Reza
- Ziegler, Slava
- Waldmann, Herbert
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