Abstract：
:A sesquiterpene furanoic acid (SFA) marine natural product isolated from soft corals of the genus Sinularia (Bowden et al., Aust J Chem 36: 371-376, 1983) was found to inactivate bee venom phospholipase A2 (bvPLA2, EC 3.1.1.4) in vitro. In this study, we characterized the kinetics of inactivation of bvPLA2 by this compound. The apparent IC50 value was 0.5 microM, and the inactivation of bvPLA2 was time dependent. The drug-enzyme binding appeared to be of a non-competitive, high-affinity nature that was irreversible by aqueous dialysis. The inactivation was prevented by the simultaneous addition of excess lysophosphatidylcholine (lysoPC) during the initial binding step, suggesting that modification of the enzyme by SFA occurs at or near the substrate binding site. Activation of bvPLA2 was observed with lysoPC addition at concentrations equimolar to bvPLA2 and higher. Saturation of activation occurred at concentrations greater than 10 microM lysoPC, and preincubation of bvPLA2 with 100 microM lysoPC did not inhibit the enzyme. Analysis of the post-incubation mixture of SFA-inhibited enzyme in the presence of lysoPC revealed the presence of unaltered enzyme exhibiting typical Michaelis-Menten kinetics. The significance of these observations is discussed in light of the recent discussion by Ortiz on the manoalide binding site on bvPLA2.
journal_name
Biochem Pharmacoljournal_title
Biochemical pharmacologyauthors
Grace KJ,Zavortink D,Jacobs RSdoi
10.1016/0006-2952(94)90343-3subject
Has Abstractpub_date
1994-04-20 00:00:00pages
1427-34issue
8eissn
0006-2952issn
1873-2968pii
0006-2952(94)90343-3journal_volume
47pub_type
杂志文章abstract：:The mitomycin C (MC) analog BMS-181174 (previously designated as BMY25067) has been shown to be active against a variety of solid tumors in mice. The activity of this compound against tumor cell lines resistant to MC and the different toxicity profiles of BMS-181174 and MC suggested that there may be significant diffe...
journal_title：Biochemical pharmacology
pub_type： 杂志文章
doi：10.1016/0006-2952(95)00264-z
更新日期：1995-10-12 00:00:00
abstract：:The crystal structure of the anthraquinone derivative 1,8-bis-(2-diethylaminoethylamino)-anthracene-9,10-dione has been established. This compound was prepared as a potential DNA-intercalating agent based on the proven intercalators doxorubicin and mitoxantrone. Its DNA-binding properties have been examined experiment...
journal_title：Biochemical pharmacology
pub_type： 杂志文章
doi：10.1016/0006-2952(83)90095-3
更新日期：1983-09-15 00:00:00
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journal_title：Biochemical pharmacology
pub_type： 杂志文章
doi：10.1016/j.bcp.2003.12.009
更新日期：2004-04-15 00:00:00
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journal_title：Biochemical pharmacology
pub_type： 杂志文章
doi：10.1016/j.bcp.2005.12.030
更新日期：2006-04-14 00:00:00
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journal_title：Biochemical pharmacology
pub_type： 杂志文章
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pub_type： 杂志文章
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journal_title：Biochemical pharmacology
pub_type： 杂志文章
doi：10.1016/0006-2952(85)90427-7
更新日期：1985-11-01 00:00:00
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journal_title：Biochemical pharmacology
pub_type： 杂志文章
doi：10.1016/0006-2952(92)90559-2
更新日期：1992-02-04 00:00:00
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journal_title：Biochemical pharmacology
pub_type： 杂志文章
doi：10.1016/0006-2952(90)90002-3
更新日期：1990-04-15 00:00:00
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journal_title：Biochemical pharmacology
pub_type： 杂志文章
doi：10.1016/0006-2952(85)90109-1
更新日期：1985-01-01 00:00:00
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journal_title：Biochemical pharmacology
pub_type： 杂志文章
doi：10.1016/0006-2952(84)90364-2
更新日期：1984-01-01 00:00:00
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journal_title：Biochemical pharmacology
pub_type： 杂志文章
doi：10.1016/0006-2952(85)90405-8
更新日期：1985-06-15 00:00:00
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journal_title：Biochemical pharmacology
pub_type： 杂志文章
doi：10.1016/j.bcp.2010.09.024
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journal_title：Biochemical pharmacology
pub_type： 杂志文章
doi：10.1016/0006-2952(85)90260-6
更新日期：1985-03-01 00:00:00
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journal_title：Biochemical pharmacology
pub_type： 杂志文章
doi：10.1016/0006-2952(93)90038-x
更新日期：1993-04-06 00:00:00
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journal_title：Biochemical pharmacology
pub_type： 杂志文章
doi：10.1016/0006-2952(87)90640-x
更新日期：1987-10-01 00:00:00
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pub_type： 杂志文章
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更新日期：2017-02-01 00:00:00
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journal_title：Biochemical pharmacology
pub_type： 杂志文章
doi：10.1016/0006-2952(87)90209-7
更新日期：1987-09-15 00:00:00
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journal_title：Biochemical pharmacology
pub_type： 杂志文章
doi：10.1016/j.bcp.2018.04.014
更新日期：2018-08-01 00:00:00
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journal_title：Biochemical pharmacology
pub_type： 杂志文章
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更新日期：2013-07-01 00:00:00
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journal_title：Biochemical pharmacology
pub_type： 杂志文章
doi：10.1016/j.bcp.2016.09.004
更新日期：2016-11-01 00:00:00
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journal_title：Biochemical pharmacology
pub_type： 杂志文章
doi：10.1016/0006-2952(87)90207-3
更新日期：1987-09-15 00:00:00
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journal_title：Biochemical pharmacology
pub_type： 杂志文章
doi：10.1016/0006-2952(94)90382-4
更新日期：1994-03-29 00:00:00
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journal_title：Biochemical pharmacology
pub_type： 杂志文章
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更新日期：2016-10-15 00:00:00
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journal_title：Biochemical pharmacology
pub_type： 杂志文章
doi：10.1016/j.bcp.2003.08.007
更新日期：2003-12-01 00:00:00
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journal_title：Biochemical pharmacology
pub_type： 杂志文章
doi：10.1016/0006-2952(85)90373-9
更新日期：1985-11-15 00:00:00
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journal_title：Biochemical pharmacology
pub_type： 杂志文章
doi：10.1016/j.bcp.2003.10.031
更新日期：2004-03-15 00:00:00
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journal_title：Biochemical pharmacology
pub_type： 杂志文章
doi：10.1016/s0006-2952(97)00536-4
更新日期：1998-02-15 00:00:00
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journal_title：Biochemical pharmacology
pub_type： 杂志文章
doi：10.1016/0006-2952(88)90025-1
更新日期：1988-04-15 00:00:00
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journal_title：Biochemical pharmacology
pub_type： 杂志文章
doi：10.1016/j.bcp.2009.09.025
更新日期：2010-02-15 00:00:00
