Matches in SemOpenAlex for { <https://semopenalex.org/work/W2777895384> ?p ?o ?g. }
Showing items 1 to 79 of
79
with 100 items per page.
- W2777895384 abstract "Protein–protein interactions drive every aspect of cell signaling, yet only a few small-molecule inhibitors of these interactions exist. Despite our ability to identify critical residues known as hot spots, little is known about how to effectively engage them to disrupt protein–protein interactions. Here, we take advantage of the ease of preparation and stability of pyrrolinone 1, a small-molecule inhibitor of the tight interaction between the urokinase receptor (uPAR) and its binding partner, the urokinase-type plasminogen activator uPA, to synthesize more than 40 derivatives and explore their effect on the protein–protein interaction. We report the crystal structure of uPAR bound to previously discovered pyrazole 3 and to pyrrolinone 12. While both 3 and 12 bind to uPAR and compete with a fluorescently labeled peptide probe, only 12 and its derivatives inhibit the full uPAR·uPA interaction. Compounds 3 and 12 mimic and engage different hot-spot residues on uPA and uPAR, respectively. Interestingly, 12 i..." @default.
- W2777895384 created "2018-01-05" @default.
- W2777895384 creator A5017353282 @default.
- W2777895384 creator A5022469850 @default.
- W2777895384 creator A5025110808 @default.
- W2777895384 creator A5033159000 @default.
- W2777895384 creator A5039309910 @default.
- W2777895384 creator A5040946263 @default.
- W2777895384 creator A5047569518 @default.
- W2777895384 creator A5055133888 @default.
- W2777895384 date "2017-03-01" @default.
- W2777895384 modified "2023-09-26" @default.
- W2777895384 title "Small Molecules Engage Hot Spots through Cooperative Binding To Inhibit a Tight Protein–Protein Interaction" @default.
- W2777895384 hasPublicationYear "2017" @default.
- W2777895384 type Work @default.
- W2777895384 sameAs 2777895384 @default.
- W2777895384 citedByCount "0" @default.
- W2777895384 crossrefType "book-chapter" @default.
- W2777895384 hasAuthorship W2777895384A5017353282 @default.
- W2777895384 hasAuthorship W2777895384A5022469850 @default.
- W2777895384 hasAuthorship W2777895384A5025110808 @default.
- W2777895384 hasAuthorship W2777895384A5033159000 @default.
- W2777895384 hasAuthorship W2777895384A5039309910 @default.
- W2777895384 hasAuthorship W2777895384A5040946263 @default.
- W2777895384 hasAuthorship W2777895384A5047569518 @default.
- W2777895384 hasAuthorship W2777895384A5055133888 @default.
- W2777895384 hasConcept C107824862 @default.
- W2777895384 hasConcept C11804247 @default.
- W2777895384 hasConcept C12554922 @default.
- W2777895384 hasConcept C161624437 @default.
- W2777895384 hasConcept C170493617 @default.
- W2777895384 hasConcept C185592680 @default.
- W2777895384 hasConcept C2779281246 @default.
- W2777895384 hasConcept C2779679481 @default.
- W2777895384 hasConcept C51639874 @default.
- W2777895384 hasConcept C54355233 @default.
- W2777895384 hasConcept C55493867 @default.
- W2777895384 hasConcept C56219504 @default.
- W2777895384 hasConcept C86803240 @default.
- W2777895384 hasConcept C95444343 @default.
- W2777895384 hasConceptScore W2777895384C107824862 @default.
- W2777895384 hasConceptScore W2777895384C11804247 @default.
- W2777895384 hasConceptScore W2777895384C12554922 @default.
- W2777895384 hasConceptScore W2777895384C161624437 @default.
- W2777895384 hasConceptScore W2777895384C170493617 @default.
- W2777895384 hasConceptScore W2777895384C185592680 @default.
- W2777895384 hasConceptScore W2777895384C2779281246 @default.
- W2777895384 hasConceptScore W2777895384C2779679481 @default.
- W2777895384 hasConceptScore W2777895384C51639874 @default.
- W2777895384 hasConceptScore W2777895384C54355233 @default.
- W2777895384 hasConceptScore W2777895384C55493867 @default.
- W2777895384 hasConceptScore W2777895384C56219504 @default.
- W2777895384 hasConceptScore W2777895384C86803240 @default.
- W2777895384 hasConceptScore W2777895384C95444343 @default.
- W2777895384 hasOpenAccess W2777895384 @default.
- W2777895384 hasRelatedWork W1971014260 @default.
- W2777895384 hasRelatedWork W1988059534 @default.
- W2777895384 hasRelatedWork W2017316435 @default.
- W2777895384 hasRelatedWork W2038910312 @default.
- W2777895384 hasRelatedWork W2058404844 @default.
- W2777895384 hasRelatedWork W2091296857 @default.
- W2777895384 hasRelatedWork W2091737818 @default.
- W2777895384 hasRelatedWork W2152118299 @default.
- W2777895384 hasRelatedWork W2155185154 @default.
- W2777895384 hasRelatedWork W2166301795 @default.
- W2777895384 hasRelatedWork W2168490647 @default.
- W2777895384 hasRelatedWork W2419096704 @default.
- W2777895384 hasRelatedWork W2469259041 @default.
- W2777895384 hasRelatedWork W2811167299 @default.
- W2777895384 hasRelatedWork W2905239553 @default.
- W2777895384 hasRelatedWork W2980579342 @default.
- W2777895384 hasRelatedWork W3011528708 @default.
- W2777895384 hasRelatedWork W3082266363 @default.
- W2777895384 hasRelatedWork W3135323340 @default.
- W2777895384 hasRelatedWork W3138854290 @default.
- W2777895384 isParatext "false" @default.
- W2777895384 isRetracted "false" @default.
- W2777895384 magId "2777895384" @default.
- W2777895384 workType "book-chapter" @default.