Matches in SemOpenAlex for { <https://semopenalex.org/work/W2036005044> ?p ?o ?g. }
- W2036005044 endingPage "475" @default.
- W2036005044 startingPage "465" @default.
- W2036005044 abstract "Urokinase is a serine protease involved in cancer growth and metastasis. Here we present the first urokinase crystal structure in complex with reversible inhibitors at 2.1 and 2.6 Å resolution. These inhibitor complex structures have been obtained from crystals of engineered urokinase type plasminogen activator designed to obtain a crystal form open for inhibitor soaking. The mutant C122S loses its flexible A-chain upon activation cleavage and crystallises in the presence of benzamidine, which was later displaced by the desired inhibitor. This new soakable crystal form turned out to be of great value in the process of structure-based drug design. The evaluated binding mode of amiloride, and UKI-1D revealed a new subsite of the primary specificity pocket of urokinase that will be employed in the future ligand optimisation process." @default.
- W2036005044 created "2016-06-24" @default.
- W2036005044 creator A5015406182 @default.
- W2036005044 creator A5028900839 @default.
- W2036005044 creator A5042947022 @default.
- W2036005044 creator A5061315607 @default.
- W2036005044 creator A5062638493 @default.
- W2036005044 creator A5069108662 @default.
- W2036005044 creator A5088187863 @default.
- W2036005044 date "2000-08-01" @default.
- W2036005044 modified "2023-09-27" @default.
- W2036005044 title "Crystals of the urokinase type plasminogen activator variant βc-uPA in complex with small molecule inhibitors open the way towards structure-based drug design 1 1Edited by A. Fersht" @default.
- W2036005044 cites W157419982 @default.
- W2036005044 cites W1946659263 @default.
- W2036005044 cites W1969211062 @default.
- W2036005044 cites W1969222787 @default.
- W2036005044 cites W1984444278 @default.
- W2036005044 cites W1987576591 @default.
- W2036005044 cites W1989046246 @default.
- W2036005044 cites W1995017064 @default.
- W2036005044 cites W2000008804 @default.
- W2036005044 cites W2001641653 @default.
- W2036005044 cites W2006370393 @default.
- W2036005044 cites W2014577485 @default.
- W2036005044 cites W2019022249 @default.
- W2036005044 cites W2028231353 @default.
- W2036005044 cites W2047039315 @default.
- W2036005044 cites W2052301809 @default.
- W2036005044 cites W2061417741 @default.
- W2036005044 cites W2064012244 @default.
- W2036005044 cites W2075172358 @default.
- W2036005044 cites W2075653464 @default.
- W2036005044 cites W2080476827 @default.
- W2036005044 cites W2080528351 @default.
- W2036005044 cites W2088144279 @default.
- W2036005044 cites W2091969321 @default.
- W2036005044 cites W2103947911 @default.
- W2036005044 cites W2106315897 @default.
- W2036005044 cites W2116275717 @default.
- W2036005044 cites W2127445307 @default.
- W2036005044 cites W2312788277 @default.
- W2036005044 doi "https://doi.org/10.1006/jmbi.2000.3966" @default.
- W2036005044 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/10926521" @default.
- W2036005044 hasPublicationYear "2000" @default.
- W2036005044 type Work @default.
- W2036005044 sameAs 2036005044 @default.
- W2036005044 citedByCount "68" @default.
- W2036005044 countsByYear W20360050442012 @default.
- W2036005044 countsByYear W20360050442014 @default.
- W2036005044 countsByYear W20360050442015 @default.
- W2036005044 countsByYear W20360050442018 @default.
- W2036005044 countsByYear W20360050442019 @default.
- W2036005044 countsByYear W20360050442020 @default.
- W2036005044 countsByYear W20360050442021 @default.
- W2036005044 countsByYear W20360050442022 @default.
- W2036005044 countsByYear W20360050442023 @default.
- W2036005044 crossrefType "journal-article" @default.
- W2036005044 hasAuthorship W2036005044A5015406182 @default.
- W2036005044 hasAuthorship W2036005044A5028900839 @default.
- W2036005044 hasAuthorship W2036005044A5042947022 @default.
- W2036005044 hasAuthorship W2036005044A5061315607 @default.
- W2036005044 hasAuthorship W2036005044A5062638493 @default.
- W2036005044 hasAuthorship W2036005044A5069108662 @default.
- W2036005044 hasAuthorship W2036005044A5088187863 @default.
- W2036005044 hasConcept C104317684 @default.
- W2036005044 hasConcept C115624301 @default.
- W2036005044 hasConcept C12554922 @default.
- W2036005044 hasConcept C134018914 @default.
- W2036005044 hasConcept C143065580 @default.
- W2036005044 hasConcept C151730666 @default.
- W2036005044 hasConcept C170493617 @default.
- W2036005044 hasConcept C175156509 @default.
- W2036005044 hasConcept C181199279 @default.
- W2036005044 hasConcept C185592680 @default.
- W2036005044 hasConcept C2776414213 @default.
- W2036005044 hasConcept C2776714187 @default.
- W2036005044 hasConcept C2776892390 @default.
- W2036005044 hasConcept C2777807008 @default.
- W2036005044 hasConcept C2779288520 @default.
- W2036005044 hasConcept C2779679481 @default.
- W2036005044 hasConcept C43369102 @default.
- W2036005044 hasConcept C54355233 @default.
- W2036005044 hasConcept C55493867 @default.
- W2036005044 hasConcept C56219504 @default.
- W2036005044 hasConcept C71240020 @default.
- W2036005044 hasConcept C8010536 @default.
- W2036005044 hasConcept C86803240 @default.
- W2036005044 hasConcept C88045685 @default.
- W2036005044 hasConceptScore W2036005044C104317684 @default.
- W2036005044 hasConceptScore W2036005044C115624301 @default.
- W2036005044 hasConceptScore W2036005044C12554922 @default.
- W2036005044 hasConceptScore W2036005044C134018914 @default.
- W2036005044 hasConceptScore W2036005044C143065580 @default.
- W2036005044 hasConceptScore W2036005044C151730666 @default.
- W2036005044 hasConceptScore W2036005044C170493617 @default.
- W2036005044 hasConceptScore W2036005044C175156509 @default.
- W2036005044 hasConceptScore W2036005044C181199279 @default.
- W2036005044 hasConceptScore W2036005044C185592680 @default.