Development of Light‐Activated LXR Agonists
Abstract: Activation of the oxysterol‐sensing transcription factor liver X receptor (LXR) has been studied as a therapeutic strategy in metabolic diseases and cancer but is compromised by the side effects of LXR agonists. Local LXR activation in cancer treatment may offer an opportunity to overcome this issue suggesting potential uses of photopharmacology. We report the computer‐aided development of photoswitchable LXR agonists based on the T0901317 scaffold, which is a known LXR agonist. Azologization and structure‐guided structure‐activity relationship evaluation enabled the design of an LXR agonist, which activated LXR with low micromolar potency in its light‐induced (Z)‐state and was inactive as (E)‐isomer. This tool sensitized human lung cancer cells to chemotherapeutic treatment in a light‐dependent manner supporting potential of locally activated LXR agonists as adjuvant cancer treatment.
- 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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Development of Light‐Activated LXR Agonists ; day:01 ; month:06 ; year:2023 ; extent:10
ChemMedChem ; (01.06.2023) (gesamt 10)
- Urheber
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Mukhopadhyay, Tufan K.
Willems, Sabine
Arp, Christopher J.
Morstein, Johannes
Haake, Caleb T.
Merk, Daniel
Trauner, Dirk
- DOI
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10.1002/cmdc.202200647
- URN
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urn:nbn:de:101:1-2023060115453202516547
- Rechteinformation
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Open Access; Der Zugriff auf das Objekt ist unbeschränkt möglich.
- Letzte Aktualisierung
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14.08.2025, 11:01 MESZ
Datenpartner
Deutsche Nationalbibliothek. Bei Fragen zum Objekt wenden Sie sich bitte an den Datenpartner.
Beteiligte
- Mukhopadhyay, Tufan K.
- Willems, Sabine
- Arp, Christopher J.
- Morstein, Johannes
- Haake, Caleb T.
- Merk, Daniel
- Trauner, Dirk
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