Matches in SemOpenAlex for { <https://semopenalex.org/work/W1988695791> ?p ?o ?g. }
- W1988695791 endingPage "8154" @default.
- W1988695791 startingPage "8148" @default.
- W1988695791 abstract "Monoamine oxidases A and B (MAO A and B) catalyze the degradation of neurotransmitters and represent drug targets for the treatment of neurodegenerative disorders. Rasagiline is an irreversible, MAO B-selective inhibitor that has been approved as a novel anti-Parkinson's drug. In this study, we investigate the inhibition of recombinant human MAO A and MAO B by several rasagiline analogues. Different substituents added onto the rasagiline scaffold alter the binding affinity depending on the position on the aminoindan ring and on the size of the substituent. Compounds with a hydroxyl group on either the C4 or the C6 atom inhibit both isozymes, whereas a bulkier substituent such as a carbamate is tolerated only at the C4 position. The 1.7 Å crystal structure of MAO B in complex with 4-(N-methyl-N-ethyl-carbamoyloxy)-N-methyl-N-propargyl-1(R)-aminoindan shows that the binding mode is similar to that of rasagiline with the carbamate moiety occupying the entrance cavity space. 1(R)-Aminoindan, the major metabolic product of rasagiline, and its analogues reversibly inhibit both MAO A and MAO B. The crystal structure of N-methyl-1(R)-aminoindan bound to MAO B shows that its aminoindan ring adopts a different orientation compared to that of rasagiline." @default.
- W1988695791 created "2016-06-24" @default.
- W1988695791 creator A5005754454 @default.
- W1988695791 creator A5006813426 @default.
- W1988695791 creator A5017449175 @default.
- W1988695791 creator A5040990018 @default.
- W1988695791 creator A5042380897 @default.
- W1988695791 creator A5042591457 @default.
- W1988695791 creator A5070368745 @default.
- W1988695791 date "2005-11-10" @default.
- W1988695791 modified "2023-10-16" @default.
- W1988695791 title "Binding of Rasagiline-Related Inhibitors to Human Monoamine Oxidases: A Kinetic and Crystallographic Analysis" @default.
- W1988695791 cites W1493157894 @default.
- W1988695791 cites W1969617718 @default.
- W1988695791 cites W1994912497 @default.
- W1988695791 cites W2001641653 @default.
- W1988695791 cites W2013083986 @default.
- W1988695791 cites W2025204606 @default.
- W1988695791 cites W2035856011 @default.
- W1988695791 cites W2036247273 @default.
- W1988695791 cites W2038840577 @default.
- W1988695791 cites W2042471904 @default.
- W1988695791 cites W2046204255 @default.
- W1988695791 cites W2051176914 @default.
- W1988695791 cites W2068720871 @default.
- W1988695791 cites W2080528351 @default.
- W1988695791 cites W2093781635 @default.
- W1988695791 cites W2103794058 @default.
- W1988695791 cites W2110893691 @default.
- W1988695791 cites W2131915812 @default.
- W1988695791 cites W2136406052 @default.
- W1988695791 cites W2149472336 @default.
- W1988695791 cites W4242482565 @default.
- W1988695791 doi "https://doi.org/10.1021/jm0506266" @default.
- W1988695791 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/2519603" @default.
- W1988695791 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/16366596" @default.
- W1988695791 hasPublicationYear "2005" @default.
- W1988695791 type Work @default.
- W1988695791 sameAs 1988695791 @default.
- W1988695791 citedByCount "95" @default.
- W1988695791 countsByYear W19886957912012 @default.
- W1988695791 countsByYear W19886957912013 @default.
- W1988695791 countsByYear W19886957912014 @default.
- W1988695791 countsByYear W19886957912015 @default.
- W1988695791 countsByYear W19886957912016 @default.
- W1988695791 countsByYear W19886957912017 @default.
- W1988695791 countsByYear W19886957912018 @default.
- W1988695791 countsByYear W19886957912019 @default.
- W1988695791 countsByYear W19886957912020 @default.
- W1988695791 countsByYear W19886957912021 @default.
- W1988695791 countsByYear W19886957912022 @default.
- W1988695791 countsByYear W19886957912023 @default.
- W1988695791 crossrefType "journal-article" @default.
- W1988695791 hasAuthorship W1988695791A5005754454 @default.
- W1988695791 hasAuthorship W1988695791A5006813426 @default.
- W1988695791 hasAuthorship W1988695791A5017449175 @default.
- W1988695791 hasAuthorship W1988695791A5040990018 @default.
- W1988695791 hasAuthorship W1988695791A5042380897 @default.
- W1988695791 hasAuthorship W1988695791A5042591457 @default.
- W1988695791 hasAuthorship W1988695791A5070368745 @default.
- W1988695791 hasBestOaLocation W19886957912 @default.
- W1988695791 hasConcept C142724271 @default.
- W1988695791 hasConcept C178790620 @default.
- W1988695791 hasConcept C185592680 @default.
- W1988695791 hasConcept C2776568683 @default.
- W1988695791 hasConcept C2778565081 @default.
- W1988695791 hasConcept C2778689049 @default.
- W1988695791 hasConcept C2779134260 @default.
- W1988695791 hasConcept C2779734285 @default.
- W1988695791 hasConcept C2780378348 @default.
- W1988695791 hasConcept C2781249495 @default.
- W1988695791 hasConcept C2781311116 @default.
- W1988695791 hasConcept C71240020 @default.
- W1988695791 hasConcept C71924100 @default.
- W1988695791 hasConceptScore W1988695791C142724271 @default.
- W1988695791 hasConceptScore W1988695791C178790620 @default.
- W1988695791 hasConceptScore W1988695791C185592680 @default.
- W1988695791 hasConceptScore W1988695791C2776568683 @default.
- W1988695791 hasConceptScore W1988695791C2778565081 @default.
- W1988695791 hasConceptScore W1988695791C2778689049 @default.
- W1988695791 hasConceptScore W1988695791C2779134260 @default.
- W1988695791 hasConceptScore W1988695791C2779734285 @default.
- W1988695791 hasConceptScore W1988695791C2780378348 @default.
- W1988695791 hasConceptScore W1988695791C2781249495 @default.
- W1988695791 hasConceptScore W1988695791C2781311116 @default.
- W1988695791 hasConceptScore W1988695791C71240020 @default.
- W1988695791 hasConceptScore W1988695791C71924100 @default.
- W1988695791 hasIssue "26" @default.
- W1988695791 hasLocation W19886957911 @default.
- W1988695791 hasLocation W19886957912 @default.
- W1988695791 hasLocation W19886957913 @default.
- W1988695791 hasOpenAccess W1988695791 @default.
- W1988695791 hasPrimaryLocation W19886957911 @default.
- W1988695791 hasRelatedWork W1977240804 @default.
- W1988695791 hasRelatedWork W1988695791 @default.
- W1988695791 hasRelatedWork W2011876025 @default.
- W1988695791 hasRelatedWork W2045778770 @default.
- W1988695791 hasRelatedWork W2065605110 @default.