Conformationally Restricted Macrocycles as Improved FKBP51 Inhibitors Enabled by Systematic Linker Derivatization Article Swipe
Moritz Spiske
,
Christian Meyners
,
Michael Bauder
,
Maximilian Repity
,
Christian Brudy
,
Wisely Oki Sugiarto
,
Hanaa Achaq
,
Thomas Geiger
,
Felix Hausch
·
YOU?
·
· 2025
· Open Access
·
· DOI: https://doi.org/10.1002/anie.202418511
YOU?
·
· 2025
· Open Access
·
· DOI: https://doi.org/10.1002/anie.202418511
Macrocycles are increasingly considered as promising modalities to target challenging intracellular proteins. However, strategies for transitioning from active linear starting points to improved macrocycles are still underdeveloped. Here we explored the derivatization of linkers as an approach for macrocycle optimization. Using the FK506‐binding protein 51 (FKBP51) as a model system we prepared >140 macrocycles with systematically derivatized linkers. Two backbones were identified as promising frameworks for subsequent optimization. Surprisingly, co‐crystal structure analyses revealed that these chemical templates represent an ensemble of three‐dimensional (3D) conformations that can give rise to several distinct 3D‐scaffolds. This resulted in a set of macrocycles with consistently improved affinity, plasma stability, and aqueous solubility compared to the linear precursors or the non‐functionalized macrocycles. Our results highlight linkers as an opportunity for macrocyclic drug development, show how linker derivatization can improve the performance of macrocycles, and emphasizes the need to track macrocyclic scaffold evolution at a three‐dimensional level.
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- Type
- article
- Language
- en
- Landing Page
- https://doi.org/10.1002/anie.202418511
- OA Status
- hybrid
- Cited By
- 4
- References
- 34
- Related Works
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- OpenAlex ID
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All OpenAlex metadata
Raw OpenAlex JSON
- OpenAlex ID
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https://openalex.org/W4406028502Canonical identifier for this work in OpenAlex
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https://doi.org/10.1002/anie.202418511Digital Object Identifier
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Conformationally Restricted Macrocycles as Improved FKBP51 Inhibitors Enabled by Systematic Linker DerivatizationWork title
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articleOpenAlex work type
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enPrimary language
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2025Year of publication
- Publication date
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2025-01-03Full publication date if available
- Authors
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Moritz Spiske, Christian Meyners, Michael Bauder, Maximilian Repity, Christian Brudy, Wisely Oki Sugiarto, Hanaa Achaq, Thomas Geiger, Felix HauschList of authors in order
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https://doi.org/10.1002/anie.202418511Publisher landing page
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YesWhether a free full text is available
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hybridOpen access status per OpenAlex
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https://doi.org/10.1002/anie.202418511Direct OA link when available
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Derivatization, Linker, Combinatorial chemistry, Chemistry, Computer science, Organic chemistry, High-performance liquid chromatography, Operating systemTop concepts (fields/topics) attached by OpenAlex
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4Total citation count in OpenAlex
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2025: 4Per-year citation counts (last 5 years)
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10Other works algorithmically related by OpenAlex
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