Matches in SemOpenAlex for { <https://semopenalex.org/work/W2920116687> ?p ?o ?g. }
- W2920116687 endingPage "2829" @default.
- W2920116687 startingPage "2814" @default.
- W2920116687 abstract "Inhibitors of human p97 (also known as valosin-containing protein) have been actively pursued because of their potential therapeutic applications in cancer and other diseases. However, covalent and irreversible p97 inhibitors have not been well explored. Herein, we report our design, synthesis, and biological evaluation of covalent and irreversible inhibitors of p97. Among an amide and a reverse amide series we synthesized, we have identified a p97 inhibitor whose functional irreversibility has been established both in vitro and in cells. Also importantly, mass spectrometry reveals three potential cysteine residues labeled by this compound, and mutagenesis together with computer modeling suggests Cys522 as a major site, which when modified, could compromise the function of p97. Taken together, this new inhibitor may provide a template for designing more potent p97 inhibitors with covalent and irreversible characteristics." @default.
- W2920116687 created "2019-03-11" @default.
- W2920116687 creator A5002752646 @default.
- W2920116687 creator A5010260308 @default.
- W2920116687 creator A5021345648 @default.
- W2920116687 creator A5046551911 @default.
- W2920116687 creator A5082797965 @default.
- W2920116687 creator A5088174174 @default.
- W2920116687 creator A5088193104 @default.
- W2920116687 creator A5091579621 @default.
- W2920116687 date "2019-03-04" @default.
- W2920116687 modified "2023-10-16" @default.
- W2920116687 title "Discovery of Irreversible p97 Inhibitors" @default.
- W2920116687 cites W146912744 @default.
- W2920116687 cites W1689039642 @default.
- W2920116687 cites W1974256456 @default.
- W2920116687 cites W1983350301 @default.
- W2920116687 cites W1983907437 @default.
- W2920116687 cites W1985286323 @default.
- W2920116687 cites W1989154905 @default.
- W2920116687 cites W1991989590 @default.
- W2920116687 cites W1993450321 @default.
- W2920116687 cites W1994561883 @default.
- W2920116687 cites W1995770177 @default.
- W2920116687 cites W1996718698 @default.
- W2920116687 cites W1999587831 @default.
- W2920116687 cites W2007573706 @default.
- W2920116687 cites W2010993054 @default.
- W2920116687 cites W2012265138 @default.
- W2920116687 cites W2018753611 @default.
- W2920116687 cites W2022558488 @default.
- W2920116687 cites W2029584311 @default.
- W2920116687 cites W2046791391 @default.
- W2920116687 cites W2047422395 @default.
- W2920116687 cites W2048758159 @default.
- W2920116687 cites W2052842467 @default.
- W2920116687 cites W2056730111 @default.
- W2920116687 cites W2068306128 @default.
- W2920116687 cites W2077451485 @default.
- W2920116687 cites W2078594804 @default.
- W2920116687 cites W2080378383 @default.
- W2920116687 cites W2082069715 @default.
- W2920116687 cites W2086781264 @default.
- W2920116687 cites W2087221323 @default.
- W2920116687 cites W2099598643 @default.
- W2920116687 cites W2117313136 @default.
- W2920116687 cites W2131964519 @default.
- W2920116687 cites W2154127938 @default.
- W2920116687 cites W2156739666 @default.
- W2920116687 cites W2171862076 @default.
- W2920116687 cites W2214997168 @default.
- W2920116687 cites W2216848450 @default.
- W2920116687 cites W2259068415 @default.
- W2920116687 cites W2261826202 @default.
- W2920116687 cites W2262506123 @default.
- W2920116687 cites W2287686703 @default.
- W2920116687 cites W2293268779 @default.
- W2920116687 cites W2319201708 @default.
- W2920116687 cites W2322586343 @default.
- W2920116687 cites W2326887417 @default.
- W2920116687 cites W2408495424 @default.
- W2920116687 cites W2430786080 @default.
- W2920116687 cites W248383993 @default.
- W2920116687 cites W2526140753 @default.
- W2920116687 cites W2557917157 @default.
- W2920116687 cites W2559098267 @default.
- W2920116687 cites W2564708666 @default.
- W2920116687 cites W2602529236 @default.
- W2920116687 cites W2615692656 @default.
- W2920116687 cites W2626340527 @default.
- W2920116687 cites W2908143184 @default.
- W2920116687 cites W375413697 @default.
- W2920116687 doi "https://doi.org/10.1021/acs.jmedchem.9b00144" @default.
- W2920116687 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/30830772" @default.
- W2920116687 hasPublicationYear "2019" @default.
- W2920116687 type Work @default.
- W2920116687 sameAs 2920116687 @default.
- W2920116687 citedByCount "15" @default.
- W2920116687 countsByYear W29201166872019 @default.
- W2920116687 countsByYear W29201166872020 @default.
- W2920116687 countsByYear W29201166872021 @default.
- W2920116687 countsByYear W29201166872022 @default.
- W2920116687 countsByYear W29201166872023 @default.
- W2920116687 crossrefType "journal-article" @default.
- W2920116687 hasAuthorship W2920116687A5002752646 @default.
- W2920116687 hasAuthorship W2920116687A5010260308 @default.
- W2920116687 hasAuthorship W2920116687A5021345648 @default.
- W2920116687 hasAuthorship W2920116687A5046551911 @default.
- W2920116687 hasAuthorship W2920116687A5082797965 @default.
- W2920116687 hasAuthorship W2920116687A5088174174 @default.
- W2920116687 hasAuthorship W2920116687A5088193104 @default.
- W2920116687 hasAuthorship W2920116687A5091579621 @default.
- W2920116687 hasConcept C104317684 @default.
- W2920116687 hasConcept C143065580 @default.
- W2920116687 hasConcept C16318435 @default.
- W2920116687 hasConcept C178790620 @default.
- W2920116687 hasConcept C180577832 @default.
- W2920116687 hasConcept C181199279 @default.