FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2095092334> ?p ?o ?g. }

• W2095092334 endingPage "1008" @default.
• W2095092334 startingPage "1003" @default.
• W2095092334 abstract "POP (prolyl oligopeptidase) specifically hydrolyses a number of small proline-containing peptides at the carboxy end of the proline residue and POP inhibitors have been shown to have cognition-enhancing properties. It has been noted that certain functional groups at the P1 site of the inhibitor, which correspond to the substrate residue on the N-terminal side of the bond to be cleaved, increase the inhibitory potency. However, detailed mechanistic and kinetic analysis of the inhibition has not been studied. In the present study, we examined the effect of different functional groups at the P1 site of the parent inhibitor isophthalic acid bis-(L-prolylpyrrolidine) amide on the binding kinetics to POP. Addition of CHO, CN or COCH2OH groups to the P1 site increased the inhibitory potency by two orders of magnitude (Ki=11.8–0.1 nM) and caused a clear slow-binding inhibition. The inhibitor containing a CHO group had the lowest association rate constant, kon=(2.43±0.12)×105 M−1·s−1, whereas the inhibitor with a CN group exhibited the fastest binding, kon=(12.0±0.08)×105 M−1·s−1. In addition, the dissociation rate was found to be crucially dependent on the type of the functional group. Compounds with COCH2OH and CHO groups had much longer half-lives of dissociation (over 5 h) compared with the compound with the CN group (25 min), although the Ki values of the compounds were relatively similar. A possibility to optimize the duration of inhibition by changing the functional group at the P1 site is important when planning therapeutically useful POP inhibitors." @default.
• W2095092334 created "2016-06-24" @default.
• W2095092334 creator A5015022975 @default.
• W2095092334 creator A5022729685 @default.
• W2095092334 creator A5024765402 @default.
• W2095092334 creator A5038405908 @default.
• W2095092334 creator A5040013014 @default.
• W2095092334 creator A5042266669 @default.
• W2095092334 creator A5044379426 @default.
• W2095092334 creator A5068021509 @default.
• W2095092334 date "2004-09-07" @default.
• W2095092334 modified "2023-10-18" @default.
• W2095092334 title "Slow-binding inhibitors of prolyl oligopeptidase with different functional groups at the P1 site" @default.
• W2095092334 cites W1501954618 @default.
• W2095092334 cites W1573122700 @default.
• W2095092334 cites W1764151989 @default.
• W2095092334 cites W1969398979 @default.
• W2095092334 cites W1985068557 @default.
• W2095092334 cites W1988940766 @default.
• W2095092334 cites W1999514420 @default.
• W2095092334 cites W2000290970 @default.
• W2095092334 cites W2004235172 @default.
• W2095092334 cites W2019030450 @default.
• W2095092334 cites W2020535330 @default.
• W2095092334 cites W2067570041 @default.
• W2095092334 cites W2070467580 @default.
• W2095092334 cites W2075814487 @default.
• W2095092334 cites W2083076197 @default.
• W2095092334 cites W2084525598 @default.
• W2095092334 cites W2086147088 @default.
• W2095092334 cites W2166113206 @default.
• W2095092334 cites W2273901504 @default.
• W2095092334 cites W73894140 @default.
• W2095092334 doi "https://doi.org/10.1042/bj20040992" @default.
• W2095092334 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/1133977" @default.
• W2095092334 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/15217351" @default.
• W2095092334 hasPublicationYear "2004" @default.
• W2095092334 type Work @default.
• W2095092334 sameAs 2095092334 @default.
• W2095092334 citedByCount "22" @default.
• W2095092334 countsByYear W20950923342012 @default.
• W2095092334 countsByYear W20950923342013 @default.
• W2095092334 countsByYear W20950923342017 @default.
• W2095092334 countsByYear W20950923342018 @default.
• W2095092334 countsByYear W20950923342020 @default.
• W2095092334 crossrefType "journal-article" @default.
• W2095092334 hasAuthorship W2095092334A5015022975 @default.
• W2095092334 hasAuthorship W2095092334A5022729685 @default.
• W2095092334 hasAuthorship W2095092334A5024765402 @default.
• W2095092334 hasAuthorship W2095092334A5038405908 @default.
• W2095092334 hasAuthorship W2095092334A5040013014 @default.
• W2095092334 hasAuthorship W2095092334A5042266669 @default.
• W2095092334 hasAuthorship W2095092334A5044379426 @default.
• W2095092334 hasAuthorship W2095092334A5068021509 @default.
• W2095092334 hasBestOaLocation W20950923342 @default.
• W2095092334 hasConcept C107824862 @default.
• W2095092334 hasConcept C170493617 @default.
• W2095092334 hasConcept C181199279 @default.
• W2095092334 hasConcept C185592680 @default.
• W2095092334 hasConcept C202751555 @default.
• W2095092334 hasConcept C2778439535 @default.
• W2095092334 hasConcept C2779815552 @default.
• W2095092334 hasConcept C2780043585 @default.
• W2095092334 hasConcept C515207424 @default.
• W2095092334 hasConcept C55493867 @default.
• W2095092334 hasConcept C57992300 @default.
• W2095092334 hasConcept C71240020 @default.
• W2095092334 hasConcept C74998103 @default.
• W2095092334 hasConceptScore W2095092334C107824862 @default.
• W2095092334 hasConceptScore W2095092334C170493617 @default.
• W2095092334 hasConceptScore W2095092334C181199279 @default.
• W2095092334 hasConceptScore W2095092334C185592680 @default.
• W2095092334 hasConceptScore W2095092334C202751555 @default.
• W2095092334 hasConceptScore W2095092334C2778439535 @default.
• W2095092334 hasConceptScore W2095092334C2779815552 @default.
• W2095092334 hasConceptScore W2095092334C2780043585 @default.
• W2095092334 hasConceptScore W2095092334C515207424 @default.
• W2095092334 hasConceptScore W2095092334C55493867 @default.
• W2095092334 hasConceptScore W2095092334C57992300 @default.
• W2095092334 hasConceptScore W2095092334C71240020 @default.
• W2095092334 hasConceptScore W2095092334C74998103 @default.
• W2095092334 hasIssue "3" @default.
• W2095092334 hasLocation W20950923341 @default.
• W2095092334 hasLocation W20950923342 @default.
• W2095092334 hasLocation W20950923343 @default.
• W2095092334 hasLocation W20950923344 @default.
• W2095092334 hasOpenAccess W2095092334 @default.
• W2095092334 hasPrimaryLocation W20950923341 @default.
• W2095092334 hasRelatedWork W1968014007 @default.
• W2095092334 hasRelatedWork W1976150075 @default.
• W2095092334 hasRelatedWork W1990080839 @default.
• W2095092334 hasRelatedWork W2003599828 @default.
• W2095092334 hasRelatedWork W2003776559 @default.
• W2095092334 hasRelatedWork W2064279248 @default.
• W2095092334 hasRelatedWork W2215143303 @default.
• W2095092334 hasRelatedWork W2413943946 @default.
• W2095092334 hasRelatedWork W2949825340 @default.
• W2095092334 hasRelatedWork W2952903803 @default.

• next