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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.
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2014 (Engelska)Ingår i: Division of Medicinal Chemistry: Scientific Abstracts for the 248th National Meeting and Exposition: August 10-14, 2014: San Francisco, CA, 2014, Vol. 248, s. 247-247Konferensbidrag, Muntlig presentation med publicerat abstract (Refereegranskat)
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.

Ort, förlag, år, upplaga, sidor
2014. Vol. 248, s. 247-247
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URN: urn:nbn:se:hh:diva-26706ISI: 000349167402150OAI: oai:DiVA.org:hh-26706DiVA, id: diva2:754575
Konferens
248th ACS (American Chemical Society) National Meeting, San Francisco, CA, USA, August 10-14, 2014
Tillgänglig från: 2014-10-10 Skapad: 2014-10-10 Senast uppdaterad: 2018-03-22Bibliografiskt granskad

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