Matches in SemOpenAlex for { <https://semopenalex.org/work/W2327887515> ?p ?o ?g. }
- W2327887515 endingPage "2330" @default.
- W2327887515 startingPage "2320" @default.
- W2327887515 abstract "DNA-damaging agents are among the most frequently used anticancer drugs. However, they provide only modest benefit in most cancers. This may be attributed to a genome maintenance network, the DNA damage response (DDR), that recognizes and repairs damaged DNA. ATR is a major regulator of the DDR and an attractive anticancer target. Herein, we describe the discovery of a series of aminopyrazines with potent and selective ATR inhibition. Compound 45 inhibits ATR with a Ki of 6 nM, shows >600-fold selectivity over related kinases ATM or DNA-PK, and blocks ATR signaling in cells with an IC50 of 0.42 μM. Using this compound, we show that ATR inhibition markedly enhances death induced by DNA-damaging agents in certain cancers but not normal cells. This differential response between cancer and normal cells highlights the great potential for ATR inhibition as a novel mechanism to dramatically increase the efficacy of many established drugs and ionizing radiation." @default.
- W2327887515 created "2016-06-24" @default.
- W2327887515 creator A5026334555 @default.
- W2327887515 creator A5029248074 @default.
- W2327887515 creator A5032442215 @default.
- W2327887515 creator A5051770888 @default.
- W2327887515 creator A5060587798 @default.
- W2327887515 creator A5062276884 @default.
- W2327887515 creator A5066925736 @default.
- W2327887515 creator A5071540554 @default.
- W2327887515 creator A5071642924 @default.
- W2327887515 creator A5079058393 @default.
- W2327887515 creator A5081671018 @default.
- W2327887515 creator A5085072340 @default.
- W2327887515 creator A5089100496 @default.
- W2327887515 creator A5091175904 @default.
- W2327887515 date "2011-03-17" @default.
- W2327887515 modified "2023-10-14" @default.
- W2327887515 title "Discovery of Potent and Selective Inhibitors of Ataxia Telangiectasia Mutated and Rad3 Related (ATR) Protein Kinase as Potential Anticancer Agents" @default.
- W2327887515 cites W1564224574 @default.
- W2327887515 cites W1965239527 @default.
- W2327887515 cites W1967630574 @default.
- W2327887515 cites W1967743500 @default.
- W2327887515 cites W1968552183 @default.
- W2327887515 cites W1983632171 @default.
- W2327887515 cites W1985555097 @default.
- W2327887515 cites W1985857665 @default.
- W2327887515 cites W1987698532 @default.
- W2327887515 cites W1992876574 @default.
- W2327887515 cites W2000303122 @default.
- W2327887515 cites W2004718750 @default.
- W2327887515 cites W2007208661 @default.
- W2327887515 cites W2012752748 @default.
- W2327887515 cites W2013341646 @default.
- W2327887515 cites W2014894784 @default.
- W2327887515 cites W2023568503 @default.
- W2327887515 cites W2032020572 @default.
- W2327887515 cites W2033346155 @default.
- W2327887515 cites W2048916500 @default.
- W2327887515 cites W2051808614 @default.
- W2327887515 cites W2058606238 @default.
- W2327887515 cites W2065335379 @default.
- W2327887515 cites W2074631079 @default.
- W2327887515 cites W2078663612 @default.
- W2327887515 cites W2086333179 @default.
- W2327887515 cites W2087497348 @default.
- W2327887515 cites W2097186309 @default.
- W2327887515 cites W2098457059 @default.
- W2327887515 cites W2101988823 @default.
- W2327887515 cites W2107614388 @default.
- W2327887515 cites W2109805150 @default.
- W2327887515 cites W2110017381 @default.
- W2327887515 cites W2118346657 @default.
- W2327887515 cites W2120932387 @default.
- W2327887515 cites W2126854707 @default.
- W2327887515 cites W2133318290 @default.
- W2327887515 cites W2145200068 @default.
- W2327887515 cites W2156625590 @default.
- W2327887515 cites W2162730779 @default.
- W2327887515 cites W2163798887 @default.
- W2327887515 cites W2167589496 @default.
- W2327887515 cites W2313488879 @default.
- W2327887515 cites W2324773916 @default.
- W2327887515 cites W2949405598 @default.
- W2327887515 cites W2951742598 @default.
- W2327887515 cites W3093265161 @default.
- W2327887515 doi "https://doi.org/10.1021/jm101488z" @default.
- W2327887515 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/21413798" @default.
- W2327887515 hasPublicationYear "2011" @default.
- W2327887515 type Work @default.
- W2327887515 sameAs 2327887515 @default.
- W2327887515 citedByCount "216" @default.
- W2327887515 countsByYear W23278875152012 @default.
- W2327887515 countsByYear W23278875152013 @default.
- W2327887515 countsByYear W23278875152014 @default.
- W2327887515 countsByYear W23278875152015 @default.
- W2327887515 countsByYear W23278875152016 @default.
- W2327887515 countsByYear W23278875152017 @default.
- W2327887515 countsByYear W23278875152018 @default.
- W2327887515 countsByYear W23278875152019 @default.
- W2327887515 countsByYear W23278875152020 @default.
- W2327887515 countsByYear W23278875152021 @default.
- W2327887515 countsByYear W23278875152022 @default.
- W2327887515 countsByYear W23278875152023 @default.
- W2327887515 crossrefType "journal-article" @default.
- W2327887515 hasAuthorship W2327887515A5026334555 @default.
- W2327887515 hasAuthorship W2327887515A5029248074 @default.
- W2327887515 hasAuthorship W2327887515A5032442215 @default.
- W2327887515 hasAuthorship W2327887515A5051770888 @default.
- W2327887515 hasAuthorship W2327887515A5060587798 @default.
- W2327887515 hasAuthorship W2327887515A5062276884 @default.
- W2327887515 hasAuthorship W2327887515A5066925736 @default.
- W2327887515 hasAuthorship W2327887515A5071540554 @default.
- W2327887515 hasAuthorship W2327887515A5071642924 @default.
- W2327887515 hasAuthorship W2327887515A5079058393 @default.
- W2327887515 hasAuthorship W2327887515A5081671018 @default.
- W2327887515 hasAuthorship W2327887515A5085072340 @default.
- W2327887515 hasAuthorship W2327887515A5089100496 @default.