hh.sePublications
Change search
CiteExportLink to record
Permanent link

Direct link
Cite
Citation style
  • apa
  • ieee
  • modern-language-association-8th-edition
  • vancouver
  • Other style
More styles
Language
  • de-DE
  • en-GB
  • en-US
  • fi-FI
  • nn-NO
  • nn-NB
  • sv-SE
  • Other locale
More languages
Output format
  • html
  • text
  • asciidoc
  • rtf
SAR and optimization of trioxoisothiazole-based liver receptor X (LXR) agonists leading to the clinical candidate AZD3971
Cardiovascular & Metabolic Diseases Innovative Medicines Unit, AstraZeneca R&D Mölndal, Mölndal, Sweden.
Cardiovascular & Metabolic Diseases Innovative Medicines Unit, AstraZeneca R&D Mölndal, Mölndal, Sweden.
Cardiovascular & Metabolic Diseases Innovative Medicines Unit, AstraZeneca R&D Mölndal, Mölndal, Sweden.
Cardiovascular & Metabolic Diseases Innovative Medicines Unit, AstraZeneca R&D Mölndal, Mölndal, Sweden.
Show others and affiliations
2014 (English)In: Division of Medicinal Chemistry: Scientific Abstracts for the 248th National Meeting and Exposition: August 10-14, 2014: San Francisco, CA, 2014, Vol. 248, 247-247 p.Conference paper, Abstract (Refereed)
Abstract [en]

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.

Place, publisher, year, edition, pages
2014. Vol. 248, 247-247 p.
National Category
Medicinal Chemistry
Identifiers
URN: urn:nbn:se:hh:diva-26706ISI: 000349167402150OAI: oai:DiVA.org:hh-26706DiVA: diva2:754575
Conference
248th ACS (American Chemical Society) National Meeting, San Francisco, CA, USA, August 10-14, 2014
Available from: 2014-10-10 Created: 2014-10-10 Last updated: 2017-03-21Bibliographically approved

Open Access in DiVA

No full text

Other links

Abstracts

Search in DiVA

By author/editor
Lutz, Mareike
Medicinal Chemistry

Search outside of DiVA

GoogleGoogle Scholar

Total: 129 hits
CiteExportLink to record
Permanent link

Direct link
Cite
Citation style
  • apa
  • ieee
  • modern-language-association-8th-edition
  • vancouver
  • Other style
More styles
Language
  • de-DE
  • en-GB
  • en-US
  • fi-FI
  • nn-NO
  • nn-NB
  • sv-SE
  • Other locale
More languages
Output format
  • html
  • text
  • asciidoc
  • rtf