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SAR and optimizatio...
SAR and optimization of trioxoisothiazole-based liver receptor X (LXR) agonists leading to the clinical candidate AZD3971
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- Johannesson, Petra (author)
- Cardiovascular & Metabolic Diseases Innovative Medicines Unit, AstraZeneca R&D Mölndal, Mölndal, Sweden
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- Bratt, Emma (author)
- Cardiovascular & Metabolic Diseases Innovative Medicines Unit, AstraZeneca R&D Mölndal, Mölndal, Sweden
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- Broo, Anders (author)
- Cardiovascular & Metabolic Diseases Innovative Medicines Unit, AstraZeneca R&D Mölndal, Mölndal, Sweden
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- Evertsson, Emma (author)
- Cardiovascular & Metabolic Diseases Innovative Medicines Unit, AstraZeneca R&D Mölndal, Mölndal, Sweden
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- Judkins, Robert (author)
- Cardiovascular & Metabolic Diseases Innovative Medicines Unit, AstraZeneca R&D Mölndal, Mölndal, Sweden
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- Leandersson, Carina (author)
- Cardiovascular & Metabolic Diseases Innovative Medicines Unit, AstraZeneca R&D Mölndal, Mölndal, Sweden
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- Lutz, Mareike, 1967- (author)
- Cardiovascular & Metabolic Diseases Innovative Medicines Unit, AstraZeneca R&D Mölndal, Mölndal, Sweden
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- Pemberton, Nils (author)
- Cardiovascular & Metabolic Diseases Innovative Medicines Unit, AstraZeneca R&D Mölndal, Mölndal, Sweden
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- Swanson, Marianne (author)
- Cardiovascular & Metabolic Diseases Innovative Medicines Unit, AstraZeneca R&D Mölndal, Mölndal, Sweden
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- Westerlund, Kristina (author)
- Cardiovascular & Metabolic Diseases Innovative Medicines Unit, AstraZeneca R&D Mölndal, Mölndal, Sweden
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- Åkerblad, Peter (author)
- Cardiovascular & Metabolic Diseases Innovative Medicines Unit, AstraZeneca R&D Mölndal, Mölndal, Sweden
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- Lindstedt, Eva-Lotte (author)
- Cardiovascular & Metabolic Diseases Innovative Medicines Unit, AstraZeneca R&D Mölndal, Mölndal, Sweden
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(creator_code:org_t)
- 2014
- 2014
- English.
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In: Division of Medicinal Chemistry. ; , s. 247-247
- Related links:
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https://urn.kb.se/re...
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Abstract
Subject headings
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- The liver X receptors (LXRα and LXRβ) are members of the nuclear receptor family of transcription factors. The activation of LXR induces genes involved in reverse cholesterol transport (RCT), which is believed to be the main effect of LXR agonists in the prevention or treatment of atherosclerosis. However LXR agonists have also been shown to cause hepatic steatosis and hypertriglyceridaemia. The ability to separate beneficial effects from negative effects has been a challenge that so far has hampered the development of LXR agonists for human use. We herein describe the SAR and optimization of a series of trioxoisothiazole-based LXR agonists leading to compounds with nanomolar potencies and a separation of beneficial versus negative effects in vivo. This work ultimately led to the nomination of AZD3971 as a candidate for the treatment of atherosclerosis.
Subject headings
- MEDICIN OCH HÄLSOVETENSKAP -- Medicinska och farmaceutiska grundvetenskaper -- Läkemedelskemi (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Basic Medicine -- Medicinal Chemistry (hsv//eng)
Publication and Content Type
- ref (subject category)
- kon (subject category)
To the university's database
- By the author/editor
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Johannesson, Pet ...
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Bratt, Emma
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Broo, Anders
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Evertsson, Emma
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Judkins, Robert
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Leandersson, Car ...
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show more...
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Lutz, Mareike, 1 ...
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Pemberton, Nils
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Swanson, Mariann ...
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Westerlund, Kris ...
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Åkerblad, Peter
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Lindstedt, Eva-L ...
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- About the subject
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- MEDICAL AND HEALTH SCIENCES
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MEDICAL AND HEAL ...
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and Basic Medicine
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and Medicinal Chemis ...
- Articles in the publication
- Division of Medi ...
- By the university
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Halmstad University