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Volumn 20, Issue 20, 2010, Pages 6030-6033

Discovery of pyrrolopyridazines as novel DGAT1 inhibitors

Author keywords

Acyl CoA:diacylglycerol acyltransferase; DGAT1; DGAT1 inhibitors; Pyrrolopyridazines

Indexed keywords

ACYLTRANSFERASE INHIBITOR; DIACYLGLYCEROL ACYLTRANSFERASE 1; PYRROLOPYRIDAZINE; UNCLASSIFIED DRUG;

EID: 77956914790     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2010.08.066     Document Type: Article
Times cited : (27)

References (21)
  • 15
    • 77956923081 scopus 로고    scopus 로고
    • note
    • 14C acyl coenzyme A (25 μM, such as decanoyl CoA, palmitoyl CoA, oleoyl CoA), and incubated at room temperature for 2 h. The reaction was stopped by adding Wheat Germ Agglutinin (WGA) SPA beads (0.2 mg) in mercuric chloride. Cell membranes were allowed to couple to the beads overnight. The signal was measured using a TopCount device.
  • 16
    • 77956939021 scopus 로고    scopus 로고
    • note
    • 14C oleic acid directly to the cells and the incubation continued for 30 min. Cells were washed two times with 1 ml PBS and air-dried at 37 °C for 10 min. Cell lipids were extracted with 0.5 ml hexane/isopropyl alcohol (3:2 v/v) for 5 min twice. Lipid extracts were evaporated to dryness, dissolved in chloroform and the lipid classes were resolved by TLC using hexane/ether/glacial acetic acid (80:20:1 v/v/v). The plates were exposed to a phosphorimager screen and the amount of radioactivity incorporated in to the triglyceride fraction was determined.
  • 17
    • 77956935235 scopus 로고    scopus 로고
    • note
    • 14C palmitoyl CoA (25 μM), and incubated at ambient temperature for 10 min. The reaction was stopped by adding chloroform (1 mL) and vortexing. After brief centrifugation, the upper aqueous phase was removed and the organic phase applied to an aminopropyl Sep-Pak cartridge. Radioactive product, cholesterol palmitate, was eluted with chloroform (1 mL) into a scintillation vial and counted.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.