KMI-358 and KMI-370, highly potent and small-sized BACE1 inhibitors containing phenylnorstatine

Bioorganic and Medicinal Chemistry Letters

Volumn 14, Issue 6, 2004, Pages 1527-1531

  Kimura, Tooru ^a   Shuto, Daisuke ^a   Kasai, Soko ^a   Liu, Ping ^a   Hidaka, Koushi ^a   Hamada, Takashi ^a   Hayashi, Yoshio ^a   Hattori, Chinatsu ^b   Asai, Masashi ^b   Kitazume, Shinobu ^c   Saido, Takaomi C ^d   Ishiura, Shoichi ^b   Kiso, Yoshiaki ^a  

^a KYOTO PHARMACEUTICAL UNIVERSITY   (Japan)

^b UNIVERSITY OF TOKYO   (Japan)

^c Frontier Research System   (Japan)

^d RIKEN BRAIN SCIENCE INSTITUTE   (Japan)

Author keywords

[No Author keywords available]

Indexed keywords

BETA SECRETASE; BETA SECRETASE 1; BETA SECRETASE INHIBITOR; KMI 008; KMI 358; KMI 370; OCTAPEPTIDE; PHENYLNORSTASTINE; STATINE DERIVATIVE; UNCLASSIFIED DRUG;

ARTICLE; DRUG DESIGN; DRUG POTENCY; DRUG STRUCTURE; DRUG SYNTHESIS; EMBRYO; HUMAN; HUMAN CELL; IC 50;

AMYLOID PRECURSOR PROTEIN SECRETASES; ASPARTIC ENDOPEPTIDASES; CELL LINE; DOSE-RESPONSE RELATIONSHIP, DRUG; ENDOPEPTIDASES; HUMANS; PHENYLBUTYRATES; PROTEASE INHIBITORS;

EID: 10744219775     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2003.12.088     Document Type: Article

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16. BACE1-HEK293 cells (80-100% confluent) were replaced with new serum-free medium (DMEM containing 1 mg/mL G418) with 100 μM/10 μM/1 μM/100 nM of KMI-358 or KMI-370, followed by cell incubation for 6 h. The sAPPβ in the culture was concentrated, ran on 7.5% SDS-PAGE and western blotted. The blots were proved with anti-sAPPβ antibody.