FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2915291231> ?p ?o ?g. }

• W2915291231 abstract "Protein palmitoylation is an essential post-translational modification necessary for trafficking and localization of regulatory proteins that play key roles in cell growth and signaling. Multiple oncogenes, including HRAS and SRC, require palmitoylation for malignant transformation. Lysophospholipase 1 (LYPLA1) has been identified as a candidate protein palmitoyl thioesterase responsible for HRAS depalmitoylation in mammalian cells. Seeking chemical tools to investigate biochemical pathway involvement and potential roles in cancer pathogenesis, we conducted a fluorescence polarization-based competitive activity-based protein profiling (fluopol-ABPP) HTS campaign to identify inhibitors of LYPLA1 and the structurally related LYPLA2. HTS identified a lead triazole urea micromolar inhibitor, which we optimized as dual LYPLA1/LYPLA2 inhibitor ML211, and reversible compounds ML348 and ML349 that act as selective LYPLA1 and LYPLA2 inhibitors, respectively. Using an advanced competitive ABPP strategy employing ABPP probes with controlled reactivity rates, we successfully confirmed potent and selective target engagement of these reversible compounds in living systems as detailed here for ML348 and in the accompanying ML349 Probe Report. Together, these compounds should greatly aid investigations into the biological function of LYPLA1 and LYPLA2." @default.
• W2915291231 created "2019-03-02" @default.
• W2915291231 creator A5000381341 @default.
• W2915291231 creator A5001446294 @default.
• W2915291231 creator A5003203423 @default.
• W2915291231 creator A5006260657 @default.
• W2915291231 creator A5014739166 @default.
• W2915291231 creator A5016869942 @default.
• W2915291231 creator A5019762035 @default.
• W2915291231 creator A5034348335 @default.
• W2915291231 creator A5034784760 @default.
• W2915291231 creator A5051431581 @default.
• W2915291231 creator A5054637908 @default.
• W2915291231 creator A5057561024 @default.
• W2915291231 creator A5061974401 @default.
• W2915291231 creator A5085356292 @default.
• W2915291231 date "2014-01-13" @default.
• W2915291231 modified "2023-09-26" @default.
• W2915291231 title "Characterization of a Selective, Reversible Inhibitor of Lysophospholipase 1 (LYPLA1)" @default.
• W2915291231 cites W1575071875 @default.
• W2915291231 cites W1597678601 @default.
• W2915291231 cites W1970696723 @default.
• W2915291231 cites W1972907910 @default.
• W2915291231 cites W1974374321 @default.
• W2915291231 cites W1983926699 @default.
• W2915291231 cites W1991219570 @default.
• W2915291231 cites W2003180508 @default.
• W2915291231 cites W2004104748 @default.
• W2915291231 cites W2021790986 @default.
• W2915291231 cites W2023364037 @default.
• W2915291231 cites W2024201380 @default.
• W2915291231 cites W2033333594 @default.
• W2915291231 cites W2036043110 @default.
• W2915291231 cites W2046370400 @default.
• W2915291231 cites W2051554315 @default.
• W2915291231 cites W2078410070 @default.
• W2915291231 cites W2079340910 @default.
• W2915291231 cites W2092991098 @default.
• W2915291231 cites W2110112655 @default.
• W2915291231 cites W2120821369 @default.
• W2915291231 cites W2129105333 @default.
• W2915291231 cites W2131774390 @default.
• W2915291231 cites W2134450626 @default.
• W2915291231 cites W2140946052 @default.
• W2915291231 cites W2141676388 @default.
• W2915291231 cites W2150209094 @default.
• W2915291231 cites W2150700075 @default.
• W2915291231 cites W2162884305 @default.
• W2915291231 cites W2163824404 @default.
• W2915291231 cites W2171494192 @default.
• W2915291231 cites W2399531612 @default.
• W2915291231 hasPublicationYear "2014" @default.
• W2915291231 type Work @default.
• W2915291231 sameAs 2915291231 @default.
• W2915291231 citedByCount "2" @default.
• W2915291231 countsByYear W29152912312018 @default.
• W2915291231 countsByYear W29152912312021 @default.
• W2915291231 crossrefType "journal-article" @default.
• W2915291231 hasAuthorship W2915291231A5000381341 @default.
• W2915291231 hasAuthorship W2915291231A5001446294 @default.
• W2915291231 hasAuthorship W2915291231A5003203423 @default.
• W2915291231 hasAuthorship W2915291231A5006260657 @default.
• W2915291231 hasAuthorship W2915291231A5014739166 @default.
• W2915291231 hasAuthorship W2915291231A5016869942 @default.
• W2915291231 hasAuthorship W2915291231A5019762035 @default.
• W2915291231 hasAuthorship W2915291231A5034348335 @default.
• W2915291231 hasAuthorship W2915291231A5034784760 @default.
• W2915291231 hasAuthorship W2915291231A5051431581 @default.
• W2915291231 hasAuthorship W2915291231A5054637908 @default.
• W2915291231 hasAuthorship W2915291231A5057561024 @default.
• W2915291231 hasAuthorship W2915291231A5061974401 @default.
• W2915291231 hasAuthorship W2915291231A5085356292 @default.
• W2915291231 hasConcept C104317684 @default.
• W2915291231 hasConcept C1167327 @default.
• W2915291231 hasConcept C146727910 @default.
• W2915291231 hasConcept C181199279 @default.
• W2915291231 hasConcept C185592680 @default.
• W2915291231 hasConcept C204628709 @default.
• W2915291231 hasConcept C2779201268 @default.
• W2915291231 hasConcept C2781187634 @default.
• W2915291231 hasConcept C501734568 @default.
• W2915291231 hasConcept C55493867 @default.
• W2915291231 hasConcept C86803240 @default.
• W2915291231 hasConcept C95444343 @default.
• W2915291231 hasConceptScore W2915291231C104317684 @default.
• W2915291231 hasConceptScore W2915291231C1167327 @default.
• W2915291231 hasConceptScore W2915291231C146727910 @default.
• W2915291231 hasConceptScore W2915291231C181199279 @default.
• W2915291231 hasConceptScore W2915291231C185592680 @default.
• W2915291231 hasConceptScore W2915291231C204628709 @default.
• W2915291231 hasConceptScore W2915291231C2779201268 @default.
• W2915291231 hasConceptScore W2915291231C2781187634 @default.
• W2915291231 hasConceptScore W2915291231C501734568 @default.
• W2915291231 hasConceptScore W2915291231C55493867 @default.
• W2915291231 hasConceptScore W2915291231C86803240 @default.
• W2915291231 hasConceptScore W2915291231C95444343 @default.
• W2915291231 hasLocation W29152912311 @default.
• W2915291231 hasOpenAccess W2915291231 @default.
• W2915291231 hasPrimaryLocation W29152912311 @default.
• W2915291231 hasRelatedWork W1988750150 @default.

• next