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Discovery of phenyl...
Discovery of phenyl acetic acid substituted quinolines as novel liver X receptor agonists for the treatment of atherosclerosis
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Hu, Baihua (author)
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Collini, Michael (author)
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Unwalla, Rayomand (author)
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Miller, Christopher (author)
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Singhaus, Robert (author)
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Quinet, Elaine (author)
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Savio, Dawn (author)
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Halpern, Anita (author)
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Basso, Michael (author)
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Keith, James (author)
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Clerin, Valerie (author)
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Chen, Liang (author)
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Resmini, Christine (author)
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Liu, Qiang-Yuan (author)
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Feingold, Irene (author)
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Huselton, Christine (author)
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Azam, Farooq (author)
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Farnegardh, Mathias (author)
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- Enroth, Cristofer (author)
- Örebro universitet,Institutionen för naturvetenskap,Molekylär biokemi
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Bonn, Tomas (author)
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Goos-Nilsson, Annika (author)
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Wilhelmsson, Anna (author)
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Nambi, Ponnal (author)
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Wrobel, Jay (author)
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(creator_code:org_t)
- 2006-09-09
- 2006
- English.
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In: Journal of Medicinal Chemistry. - : American Chemical Society (ACS). - 0022-2623 .- 1520-4804. ; 49:21, s. 6151-6154
- Related links:
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https://urn.kb.se/re...
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https://doi.org/10.1...
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Abstract
Subject headings
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- A structure-based approach was used to optimize our new class of quinoline LXR modulators leading to phenyl acetic acid substituted quinolines 15 and 16. Both compounds displayed good binding affinity for LXRâ and LXRR and were potent activators in LBD transactivation assays. The compounds also increased expression of ABCA1 and stimulated cholesterol efflux in THP-1 cells. Quinoline 16 showed good oral bioavailability and in vivo efficacy in a LDLr knockout mouse model for lesions.
Subject headings
- MEDICIN OCH HÄLSOVETENSKAP -- Medicinska och farmaceutiska grundvetenskaper -- Farmaceutiska vetenskaper (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Basic Medicine -- Pharmaceutical Sciences (hsv//eng)
Keyword
- Pharmaceutical biochemistry
- Farmaceutisk biokemi
- Biochemistry
- Biokemi
Publication and Content Type
- ref (subject category)
- art (subject category)
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To the university's database
- By the author/editor
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Hu, Baihua
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Collini, Michael
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Unwalla, Rayoman ...
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Miller, Christop ...
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Singhaus, Robert
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Quinet, Elaine
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show more...
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Savio, Dawn
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Halpern, Anita
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Basso, Michael
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Keith, James
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Clerin, Valerie
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Chen, Liang
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Resmini, Christi ...
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Liu, Qiang-Yuan
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Feingold, Irene
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Huselton, Christ ...
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Azam, Farooq
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Farnegardh, Math ...
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Enroth, Cristofe ...
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Bonn, Tomas
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Goos-Nilsson, An ...
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Wilhelmsson, Ann ...
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Nambi, Ponnal
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Wrobel, Jay
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show less...
- 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 Pharmaceutical S ...
- Articles in the publication
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Journal of Medic ...
- By the university
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Örebro University