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Volumn 19, Issue 19, 2009, Pages 5684-5688

Diphenylmethylene hydroxamic acids as selective class IIa histone deacetylase inhibitors

Author keywords

HDAC class IIa selective inhibitors; HDAC inhibitors; HDAC4 inhibitors; HDAC5 inhibitors; HDAC7 inhibitors

Indexed keywords

HISTONE DEACETYLASE 1; HISTONE DEACETYLASE 2; HISTONE DEACETYLASE 7; HISTONE DEACETYLASE INHIBITOR; HYDROXAMIC ACID; HYDROXAMIC ACID DERIVATIVE; N HYDROXY 2,2 DIPHENYLACETAMIDE; N HYDROXY 9H XANTHENE 9 CARBOXAMIDE; OXYGEN; UNCLASSIFIED DRUG;

EID: 69949090550     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2009.08.010     Document Type: Article
Times cited : (55)

References (39)
  • 35
    • 69949101365 scopus 로고    scopus 로고
    • note
    • -1) versus HDAC1, 2, 3, 4, 5, 7, and 8 enzymes utilizing both acetyl-Boc-lysine and Boc-Lys-(ε-trifluormethylacetyl)-MCA substrates clearly demonstrated the extraordinary specificity of the Boc-Lys-(ε-trifluormethylacetyl)-MCA substrate for HDAC4, 5, and 7 enzymes (class IIa).
  • 37
    • 69949091932 scopus 로고    scopus 로고
    • note
    • (a) For details of the HDAC class I whole cell assay see: Li, Z.; Besterman, J.M.; and Bonfils, C. International Patent application WO 2007/135471 A1, 2007; (b) For details of the HDAC class II whole cell assay see Jubrail Rahil, Aihua Lu Patent Application US 2008/0199897, 2008; (c) The whole cell assay was done in cultured Human Embryonic Kidney cells (293T), which were treated with inhibitors for 16 h and then incubated with the substrate Boc-Ac-Lys-AMC, for measuring class I HDAC activity or Boc-Lys-(ε-trifluormethylacetyl)-AMC for measuring HDAC class IIa activity. After 90 min at 37 °C, the reaction was quenched with trypsin and TSA to a final concentration of 1 mg/mL and 1 μM, respectively. The cells were lysed with 1% NP-40. Fluorescence was read at Ex 360 nm, Em 470 nm, using GeminiXS fluorimeter.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.