FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2890836587> ?p ?o ?g. }

• W2890836587 abstract "Lecithin:cholesterol acyltransferase (LCAT) and LCAT-activating compounds are being investigated as treatments for coronary heart disease (CHD) and familial LCAT deficiency (FLD). Herein we report the crystal structure of human LCAT in complex with a potent piperidinylpyrazolopyridine activator and an acyl intermediate-like inhibitor, revealing LCAT in an active conformation. Unlike other LCAT activators, the piperidinylpyrazolopyridine activator binds exclusively to the membrane-binding domain (MBD). Functional studies indicate that the compound does not modulate the affinity of LCAT for HDL, but instead stabilizes residues in the MBD and facilitates channeling of substrates into the active site. By demonstrating that these activators increase the activity of an FLD variant, we show that compounds targeting the MBD have therapeutic potential. Our data better define the substrate binding site of LCAT and pave the way for rational design of LCAT agonists and improved biotherapeutics for augmenting or restoring reverse cholesterol transport in CHD and FLD patients." @default.
• W2890836587 created "2018-09-27" @default.
• W2890836587 creator A5013915473 @default.
• W2890836587 creator A5035678820 @default.
• W2890836587 creator A5037144273 @default.
• W2890836587 creator A5039472015 @default.
• W2890836587 creator A5040071159 @default.
• W2890836587 creator A5047533207 @default.
• W2890836587 creator A5059328563 @default.
• W2890836587 creator A5061786031 @default.
• W2890836587 creator A5068951391 @default.
• W2890836587 creator A5074548114 @default.
• W2890836587 creator A5075001959 @default.
• W2890836587 creator A5076285997 @default.
• W2890836587 date "2018-11-27" @default.
• W2890836587 modified "2023-10-02" @default.
• W2890836587 title "Molecular basis for activation of lecithin:cholesterol acyltransferase by a compound that increases HDL cholesterol" @default.
• W2890836587 cites W1134064717 @default.
• W2890836587 cites W1539796472 @default.
• W2890836587 cites W191192140 @default.
• W2890836587 cites W1963554091 @default.
• W2890836587 cites W1965270719 @default.
• W2890836587 cites W1993295279 @default.
• W2890836587 cites W1993577107 @default.
• W2890836587 cites W1996462648 @default.
• W2890836587 cites W2029085242 @default.
• W2890836587 cites W2031850888 @default.
• W2890836587 cites W2046643229 @default.
• W2890836587 cites W2049022217 @default.
• W2890836587 cites W2059356483 @default.
• W2890836587 cites W2069532016 @default.
• W2890836587 cites W2074473216 @default.
• W2890836587 cites W2077706066 @default.
• W2890836587 cites W2088615805 @default.
• W2890836587 cites W2113504642 @default.
• W2890836587 cites W2124026197 @default.
• W2890836587 cites W2131777290 @default.
• W2890836587 cites W2132629607 @default.
• W2890836587 cites W2134201060 @default.
• W2890836587 cites W2144998676 @default.
• W2890836587 cites W2148693064 @default.
• W2890836587 cites W2149632046 @default.
• W2890836587 cites W2154714625 @default.
• W2890836587 cites W2159211495 @default.
• W2890836587 cites W2161615797 @default.
• W2890836587 cites W2180229411 @default.
• W2890836587 cites W2182204189 @default.
• W2890836587 cites W2193771400 @default.
• W2890836587 cites W2201554191 @default.
• W2890836587 cites W2259459296 @default.
• W2890836587 cites W2260638314 @default.
• W2890836587 cites W2277601536 @default.
• W2890836587 cites W2621123160 @default.
• W2890836587 cites W2754097299 @default.
• W2890836587 cites W2763412323 @default.
• W2890836587 cites W2764194391 @default.
• W2890836587 cites W2787305338 @default.
• W2890836587 cites W2804347699 @default.
• W2890836587 doi "https://doi.org/10.7554/elife.41604" @default.
• W2890836587 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/6277198" @default.
• W2890836587 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/30479275" @default.
• W2890836587 hasPublicationYear "2018" @default.
• W2890836587 type Work @default.
• W2890836587 sameAs 2890836587 @default.
• W2890836587 citedByCount "32" @default.
• W2890836587 countsByYear W28908365872019 @default.
• W2890836587 countsByYear W28908365872020 @default.
• W2890836587 countsByYear W28908365872021 @default.
• W2890836587 countsByYear W28908365872022 @default.
• W2890836587 countsByYear W28908365872023 @default.
• W2890836587 crossrefType "journal-article" @default.
• W2890836587 hasAuthorship W2890836587A5013915473 @default.
• W2890836587 hasAuthorship W2890836587A5035678820 @default.
• W2890836587 hasAuthorship W2890836587A5037144273 @default.
• W2890836587 hasAuthorship W2890836587A5039472015 @default.
• W2890836587 hasAuthorship W2890836587A5040071159 @default.
• W2890836587 hasAuthorship W2890836587A5047533207 @default.
• W2890836587 hasAuthorship W2890836587A5059328563 @default.
• W2890836587 hasAuthorship W2890836587A5061786031 @default.
• W2890836587 hasAuthorship W2890836587A5068951391 @default.
• W2890836587 hasAuthorship W2890836587A5074548114 @default.
• W2890836587 hasAuthorship W2890836587A5075001959 @default.
• W2890836587 hasAuthorship W2890836587A5076285997 @default.
• W2890836587 hasBestOaLocation W28908365871 @default.
• W2890836587 hasConcept C107824862 @default.
• W2890836587 hasConcept C170493617 @default.
• W2890836587 hasConcept C181199279 @default.
• W2890836587 hasConcept C185592680 @default.
• W2890836587 hasConcept C2775970874 @default.
• W2890836587 hasConcept C2778163477 @default.
• W2890836587 hasConcept C2779564620 @default.
• W2890836587 hasConcept C2780072125 @default.
• W2890836587 hasConcept C37002583 @default.
• W2890836587 hasConcept C41183919 @default.
• W2890836587 hasConcept C55493867 @default.
• W2890836587 hasConcept C88045685 @default.
• W2890836587 hasConcept C964641 @default.
• W2890836587 hasConceptScore W2890836587C107824862 @default.
• W2890836587 hasConceptScore W2890836587C170493617 @default.
• W2890836587 hasConceptScore W2890836587C181199279 @default.

• next