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Volumn 13, Issue 24, 2003, Pages 4273-4276

KMI-008, a novel β-Secretase inhibitor containing a hydroxymethylcarbonyl isostere as a transition-State mimic: Design and synthesis of substrate-based octapeptides

Author keywords

[No Author keywords available]

Indexed keywords

BETA SECRETASE INHIBITOR; ENZYME INHIBITOR; KMI 008; OCTAPEPTIDE; PHENYLNORSTATINE; UNCLASSIFIED DRUG;

EID: 0344927114     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2003.09.053     Document Type: Article
Times cited : (89)

References (20)
  • 17
    • 85030945277 scopus 로고    scopus 로고
    • note
    • 3COOH, NaOH (pH 5.0), 7% DMSO. After incubation for 60 min at 37 °C, the reaction was stopped by addition of trichloroacetic acid. The N-terminal cleavage fragment [(7-methoxycoumarin-4-yl)acetyl-Ser-Glu-Val- Asn-Leu-OH] was analyzed by RP-HPLC with the detection of fluorescence intensity (Ex, 328 nm; Em, 393 nm).
  • 19
    • 85030945308 scopus 로고    scopus 로고
    • note
    • COS-7 cells were grown in DMEM containing 10% FBS and co-transfected with wild-type APP and full-length BACE1. As a control, pcDNA3HA empty vector was used. 48 h post-transfection, conditioned medium was replaced by new serum-free medium in the presence or absence of KMI-008, and incubated for 6 h. The culture media was concentrated by the TCA method and dissolved in SDS sample buffer. Samples were run on 7.5% SDS-PAGE and western blotted. The blots were probed with anti-sAPPβ antibody. The amount of the secreted proteins was normalized by the cell number.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.