1995
DOI: 10.1016/0960-894x(95)00441-u
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Kelatorphan and related analogs: potent and selective inhibitors of leukotriene A4 hydrolase

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Cited by 35 publications
(22 citation statements)
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“…In addition, -((-arylalkyl)aryl)alkanoic acids and kelatorphan, a known inhibitor of enkephalin-degrading enzymes, are potent inhibitors (52,53).…”
Section: Lta 4 Hydrolase An Attractive Target For Structure-based Drmentioning
confidence: 99%
“…In addition, -((-arylalkyl)aryl)alkanoic acids and kelatorphan, a known inhibitor of enkephalin-degrading enzymes, are potent inhibitors (52,53).…”
Section: Lta 4 Hydrolase An Attractive Target For Structure-based Drmentioning
confidence: 99%
“…There appears to be a consistent substratedesign motif which specifies a preferred distance between the carboxylate termini of the substrates and the sites of zinccatalyzed chemistry. The distance between the epoxide and carboxylic acid in LTA 4 is very similar to that between the scissile amide bond and the C-terminus of a tripeptide, the preferred substrate size for the enzymes aminopeptidase activity, [13] and also the length of a series of known peptidase inhibitors [37,38] (Figure 7). Site-directed mutagenesis studies published to date further corroborate this view.…”
mentioning
confidence: 99%
“…In contrast to previously described LTA 4 hydrolase inhibitors Hogg et al, 1998), SC-57461A is equipotent as an inhibitor of the hydrolase and peptidase activities. SC-57461A is equipotent with kelatorphan as an inhibitor of LTA 4 hydrolase (Penning et al, 1995).…”
Section: Resultsmentioning
confidence: 96%
“…Hogg et al (1995Hogg et al ( , 1998 reported a series of inverted hydroxamates to be low nanomolar inhibitors of the aminopeptidase activity, but less potent for the epoxide hydrolase activity. Kelatorphan has been shown to be equipotent as an inhibitor of both of the LTA 4 hydrolase activities, but it is not selective for LTA 4 hydrolase (Penning et al, 1995). A very potent ␤-mercaptoamine (Yuan et al, 1993;Ollmann et al, 1995) has been described, but it also inhibits thromboxane B 2 production in human whole blood.…”
Section: Discussionmentioning
confidence: 99%
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