Matches in SemOpenAlex for { <https://semopenalex.org/work/W2149353407> ?p ?o ?g. }
Showing items 1 to 97 of
97
with 100 items per page.
- W2149353407 endingPage "82" @default.
- W2149353407 startingPage "80" @default.
- W2149353407 abstract "Based on recent information about the anti‐substrate binding mode of the propeptide portion of procathepsin B and the well established substrate‐like binding of epoxysuccinyl‐dipeptide carboxylates to the S′ subsites of cathepsin B a new endo‐ trans ‐epoxysuccinyl peptide was synthesized that contains the dipeptide moiety Leu‐Pro‐OH for the P1′–P2′ substrate positions and the tripeptide moiety Leu‐Gly‐Gly‐OMe (sequence portion 46–48 of the propeptide) for the P2–P4 positions in anti‐substrate orientation. With an unequivocal (2 S ,3 S ) configuration this new trans ‐epoxysuccinyl peptide derivative was found to inhibit cathepsin B with an apparent second‐order rate constant of 1 520 000 M −1 s −1 which represents so far the most potent inhibitor among E‐64‐derived compounds. Conversely, the (2 R ,3 R ) diastereomer exhibited a significantly lower inhibition potency. This observation fully agrees with our previous findings that inhibitor/enzyme interactions at the S subsites are favored by the (2 S ,3 S ) and reverse interactions at the S′ subsites by the (2 R ,3 R ) configuration of the trans ‐epoxysuccinyl moiety." @default.
- W2149353407 created "2016-06-24" @default.
- W2149353407 creator A5045254763 @default.
- W2149353407 creator A5045745146 @default.
- W2149353407 creator A5052102534 @default.
- W2149353407 creator A5065468362 @default.
- W2149353407 date "1998-01-02" @default.
- W2149353407 modified "2023-10-17" @default.
- W2149353407 title "Substrate/propeptide‐derived endo‐epoxysuccinyl peptides as highly potent and selective cathepsin B inhibitors" @default.
- W2149353407 cites W1588270613 @default.
- W2149353407 cites W1902882579 @default.
- W2149353407 cites W1977620426 @default.
- W2149353407 cites W1981232154 @default.
- W2149353407 cites W1999808993 @default.
- W2149353407 cites W2004794581 @default.
- W2149353407 cites W2011899941 @default.
- W2149353407 cites W2012931700 @default.
- W2149353407 cites W2026014540 @default.
- W2149353407 cites W2028565824 @default.
- W2149353407 cites W2048266624 @default.
- W2149353407 cites W2081577447 @default.
- W2149353407 cites W2089231191 @default.
- W2149353407 cites W2095290410 @default.
- W2149353407 cites W2100288639 @default.
- W2149353407 cites W2109533300 @default.
- W2149353407 cites W2121960150 @default.
- W2149353407 cites W2144077194 @default.
- W2149353407 cites W2148818920 @default.
- W2149353407 cites W2151646462 @default.
- W2149353407 cites W2489736657 @default.
- W2149353407 cites W4232556058 @default.
- W2149353407 cites W4296250016 @default.
- W2149353407 doi "https://doi.org/10.1016/s0014-5793(97)01538-x" @default.
- W2149353407 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/9462845" @default.
- W2149353407 hasPublicationYear "1998" @default.
- W2149353407 type Work @default.
- W2149353407 sameAs 2149353407 @default.
- W2149353407 citedByCount "43" @default.
- W2149353407 countsByYear W21493534072012 @default.
- W2149353407 countsByYear W21493534072013 @default.
- W2149353407 countsByYear W21493534072015 @default.
- W2149353407 countsByYear W21493534072016 @default.
- W2149353407 countsByYear W21493534072018 @default.
- W2149353407 countsByYear W21493534072019 @default.
- W2149353407 countsByYear W21493534072023 @default.
- W2149353407 crossrefType "journal-article" @default.
- W2149353407 hasAuthorship W2149353407A5045254763 @default.
- W2149353407 hasAuthorship W2149353407A5045745146 @default.
- W2149353407 hasAuthorship W2149353407A5052102534 @default.
- W2149353407 hasAuthorship W2149353407A5065468362 @default.
- W2149353407 hasBestOaLocation W21493534071 @default.
- W2149353407 hasConcept C167392928 @default.
- W2149353407 hasConcept C181199279 @default.
- W2149353407 hasConcept C185592680 @default.
- W2149353407 hasConcept C18903297 @default.
- W2149353407 hasConcept C2776568683 @default.
- W2149353407 hasConcept C2777289219 @default.
- W2149353407 hasConcept C2779138802 @default.
- W2149353407 hasConcept C2779281246 @default.
- W2149353407 hasConcept C28021979 @default.
- W2149353407 hasConcept C55493867 @default.
- W2149353407 hasConcept C71240020 @default.
- W2149353407 hasConcept C86803240 @default.
- W2149353407 hasConceptScore W2149353407C167392928 @default.
- W2149353407 hasConceptScore W2149353407C181199279 @default.
- W2149353407 hasConceptScore W2149353407C185592680 @default.
- W2149353407 hasConceptScore W2149353407C18903297 @default.
- W2149353407 hasConceptScore W2149353407C2776568683 @default.
- W2149353407 hasConceptScore W2149353407C2777289219 @default.
- W2149353407 hasConceptScore W2149353407C2779138802 @default.
- W2149353407 hasConceptScore W2149353407C2779281246 @default.
- W2149353407 hasConceptScore W2149353407C28021979 @default.
- W2149353407 hasConceptScore W2149353407C55493867 @default.
- W2149353407 hasConceptScore W2149353407C71240020 @default.
- W2149353407 hasConceptScore W2149353407C86803240 @default.
- W2149353407 hasIssue "1" @default.
- W2149353407 hasLocation W21493534071 @default.
- W2149353407 hasLocation W21493534072 @default.
- W2149353407 hasOpenAccess W2149353407 @default.
- W2149353407 hasPrimaryLocation W21493534071 @default.
- W2149353407 hasRelatedWork W1974977289 @default.
- W2149353407 hasRelatedWork W2083883170 @default.
- W2149353407 hasRelatedWork W2089930841 @default.
- W2149353407 hasRelatedWork W2143567261 @default.
- W2149353407 hasRelatedWork W2145192274 @default.
- W2149353407 hasRelatedWork W2325189328 @default.
- W2149353407 hasRelatedWork W2892225847 @default.
- W2149353407 hasRelatedWork W3126841300 @default.
- W2149353407 hasRelatedWork W412459374 @default.
- W2149353407 hasRelatedWork W4241670312 @default.
- W2149353407 hasVolume "421" @default.
- W2149353407 isParatext "false" @default.
- W2149353407 isRetracted "false" @default.
- W2149353407 magId "2149353407" @default.
- W2149353407 workType "article" @default.