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Volumn 9, Issue 16, 2007, Pages 3045-3048

19-epi-okadaic acid, a novel protein phosphatase inhibitor with enhanced selectivity

Author keywords

[No Author keywords available]

Indexed keywords

19 EPI OKADAIC ACID; 19-EPI-OKADAIC ACID; DRUG DERIVATIVE; ENZYME INHIBITOR; OKADAIC ACID; PHOSPHOPROTEIN PHOSPHATASE; UNCLASSIFIED DRUG;

EID: 34547942018     PISSN: 15237060     EISSN: None     Source Type: Journal    
DOI: 10.1021/ol071099i     Document Type: Article
Times cited : (36)

References (27)
  • 12
    • 34547942987 scopus 로고    scopus 로고
    • NMR experiments were acquired in deuterated methanol at 400 and 500 MHz at a temperature of 298 K. HSQC, COSY, 1D/2D TOCSY, HMBC, and ROESY experiments were performed using standard pulse sequences. Data were processed using MestRec software. The integrals of the individually assigned NOE cross-peaks were converted into distance constrains using the isolated spin pair approximation, taking into account the offset effect.
    • NMR experiments were acquired in deuterated methanol at 400 and 500 MHz at a temperature of 298 K. HSQC, COSY, 1D/2D TOCSY, HMBC, and ROESY experiments were performed using standard pulse sequences. Data were processed using MestRec software. The volume integrals of the individually assigned NOE cross-peaks were converted into distance constrains using the isolated spin pair approximation, taking into account the offset effect.
  • 20
    • 0039820322 scopus 로고
    • Bioactive polyethers
    • Scheuer, P. J, Ed, Springer-Verlag: New York
    • Uemura, D. Bioactive polyethers. In Biorganic Marine Chemistry; Scheuer, P. J., Ed.; Springer-Verlag: New York, 1991; Vol. 4, pp 1-31.
    • (1991) Biorganic Marine Chemistry , vol.4 , pp. 1-31
    • Uemura, D.1
  • 22
    • 34547962191 scopus 로고    scopus 로고
    • PP1c was purchased from New England Biolabs, and PP2Ac was purchased from Sigma. Protein phosphatase activity was assayed at 37°C using 0.025 units/μL of protein and 100 μM of fluorescein diphosphate as substrate. The reaction was followed by fluorescence spectroscopy at 485-535 nM. Data were fitted to a one-site binding model. Assays with 19-epi-okadaic acid were performed in quintuplicate (n = 5), while for okadaic acid only duplicates (n = 2) were used.
    • PP1c was purchased from New England Biolabs, and PP2Ac was purchased from Sigma. Protein phosphatase activity was assayed at 37°C using 0.025 units/μL of protein and 100 μM of fluorescein diphosphate as substrate. The reaction was followed by fluorescence spectroscopy at 485-535 nM. Data were fitted to a one-site binding model. Assays with 19-epi-okadaic acid were performed in quintuplicate (n = 5), while for okadaic acid only duplicates (n = 2) were used.
  • 23
    • 0037061628 scopus 로고    scopus 로고
    • Assays adding BSA (0.125 mg/mL) to the media were also undertaken in order to explore the possibility that 19-epi-OA could be a phony hit as described in McGovern, S. L.; Caselli, E.; Grigorieff, N.; Shoichet, B. K. J. Med. Chem. 2002, 45, 1712-1722, but no significant differences were seen, leaving out such possibility.
    • Assays adding BSA (0.125 mg/mL) to the media were also undertaken in order to explore the possibility that 19-epi-OA could be a "phony" hit as described in McGovern, S. L.; Caselli, E.; Grigorieff, N.; Shoichet, B. K. J. Med. Chem. 2002, 45, 1712-1722, but no significant differences were seen, leaving out such possibility.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.