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Volumn 22, Issue 8, 2012, Pages 2963-2967

From ApoA1 upregulation to BET family bromodomain inhibition: Discovery of I-BET151

Author keywords

7 Isoxazoloquinolines; ApoA1 upregulators; BET family; Bromodomains inhibitors

Indexed keywords

7 ISOXAZOLOQUINOLINE; APOLIPOPROTEIN A1; CARDIOVASCULAR AGENT; UNCLASSIFIED DRUG;

EID: 84859443655     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2012.01.125     Document Type: Article
Times cited : (107)

References (17)
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    • references cited therein
    • P.P. Toth Circulation 111 2005 e89 and references cited therein
    • (2005) Circulation , vol.111 , pp. 89
    • Toth, P.P.1
  • 5
    • 84859441784 scopus 로고    scopus 로고
    • The luciferase cellular assay was used as a primary screen. We also measured ApoA1 secretion as a secondary assay in the same cell type. A very nice correlation between the two readouts was observed, indicating that compounds were truly upregulators of ApoA1 production by hepatic cells. See Supplementary data for details
    • The luciferase cellular assay was used as a primary screen. We also measured ApoA1 secretion as a secondary assay in the same cell type. A very nice correlation between the two readouts was observed, indicating that compounds were truly upregulators of ApoA1 production by hepatic cells. See Supplementary data for details.
  • 6
    • 2942705774 scopus 로고    scopus 로고
    • A combination of our ApoA1 upregulators with statins has been envisaged. Since Cytochrome P450 (CYP) isoenzymes are involved in the oxidative metabolism of the statins, with CYP3A4 and CYP2C9 isoenzymes being the most dominant, we wanted to discharge any risk of drug-drug interactions with our compounds being CYP inhibitors. See Bellosta, S.; Paoletti, R.; and Corsini A. Circulation 2004, 109, III-50
    • A combination of our ApoA1 upregulators with statins has been envisaged. Since Cytochrome P450 (CYP) isoenzymes are involved in the oxidative metabolism of the statins, with CYP3A4 and CYP2C9 isoenzymes being the most dominant, we wanted to discharge any risk of drug-drug interactions with our compounds being CYP inhibitors. See Bellosta, S.; Paoletti, R.; and Corsini A. Circulation 2004, 109, III-50.
  • 8
    • 34548803525 scopus 로고
    • Organic Syntheses
    • 1948, 28, 38
    • C.C. Price, and R.M. Roberts Organic Syntheses Coll. 3 1955 272 1948, 28, 38
    • (1955) Coll. , vol.3 , pp. 272
    • Price, C.C.1    Roberts, R.M.2


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.