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Substrate activity screening with kinases: discovery of small-molecule substrate-competitive c-Src inhibitors.
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2
Bivalent Inhibitors of c-Src Tyrosine Kinase That Bind a Regulatory Domain.
Bioconjug Chem. 2016 Jul 20;27(7):1745-9. doi: 10.1021/acs.bioconjchem.6b00243. Epub 2016 Jun 22.
3
Exquisitely specific bisubstrate inhibitors of c-Src kinase.
ACS Chem Biol. 2015 Jun 19;10(6):1387-91. doi: 10.1021/cb501048b. Epub 2015 Mar 31.
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Irreversible inhibitors of c-Src kinase that target a nonconserved cysteine.
ACS Chem Biol. 2012 Nov 16;7(11):1910-7. doi: 10.1021/cb300337u. Epub 2012 Sep 5.
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ATP-phosphopeptide conjugates as inhibitors of Src tyrosine kinases.
Bioorg Med Chem. 2004 Nov 15;12(22):5753-66. doi: 10.1016/j.bmc.2004.08.043.
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Allosteric Modulation of Src Family Kinases with ATP-Competitive Inhibitors.
Methods Mol Biol. 2017;1636:79-89. doi: 10.1007/978-1-4939-7154-1_6.
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Discovery of selective irreversible inhibitors of B-Lymphoid tyrosine kinase (BLK).
Eur J Med Chem. 2022 Feb 5;229:114051. doi: 10.1016/j.ejmech.2021.114051. Epub 2021 Dec 16.

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The prospect of substrate-based kinase inhibitors to improve target selectivity and overcome drug resistance.
Chem Sci. 2024 Jul 13;15(33):13130-13147. doi: 10.1039/d4sc01088d. eCollection 2024 Aug 22.
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Fluorogenic structure activity library pinpoints molecular variations in substrate specificity of structurally homologous esterases.
J Biol Chem. 2018 Sep 7;293(36):13851-13862. doi: 10.1074/jbc.RA118.003972. Epub 2018 Jul 13.
5
Bivalent Inhibitors of c-Src Tyrosine Kinase That Bind a Regulatory Domain.
Bioconjug Chem. 2016 Jul 20;27(7):1745-9. doi: 10.1021/acs.bioconjchem.6b00243. Epub 2016 Jun 22.
6
Conformation-Selective Analogues of Dasatinib Reveal Insight into Kinase Inhibitor Binding and Selectivity.
ACS Chem Biol. 2016 May 20;11(5):1296-304. doi: 10.1021/acschembio.5b01018. Epub 2016 Mar 1.
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Discovery of Bivalent Kinase Inhibitors via Enzyme-Templated Fragment Elaboration.
ACS Med Chem Lett. 2015 Jul 13;6(8):898-901. doi: 10.1021/acsmedchemlett.5b00167. eCollection 2015 Aug 13.
8
Exquisitely specific bisubstrate inhibitors of c-Src kinase.
ACS Chem Biol. 2015 Jun 19;10(6):1387-91. doi: 10.1021/cb501048b. Epub 2015 Mar 31.
10
Small molecule substrate phosphorylation site inhibitors of protein kinases: approaches and challenges.
ACS Chem Biol. 2015 Jan 16;10(1):175-89. doi: 10.1021/cb5008376. Epub 2014 Dec 23.

本文引用的文献

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Metrics other than potency reveal systematic variation in responses to cancer drugs.
Nat Chem Biol. 2013 Nov;9(11):708-14. doi: 10.1038/nchembio.1337. Epub 2013 Sep 8.
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The Substrate-Activity-Screening methodology applied to receptor tyrosine kinases: a proof-of-concept study.
Eur J Med Chem. 2012 Nov;57:1-9. doi: 10.1016/j.ejmech.2012.08.038. Epub 2012 Sep 4.
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Development of a highly selective c-Src kinase inhibitor.
ACS Chem Biol. 2012 Aug 17;7(8):1393-8. doi: 10.1021/cb300172e. Epub 2012 Jun 4.
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Comprehensive analysis of kinase inhibitor selectivity.
Nat Biotechnol. 2011 Oct 30;29(11):1046-51. doi: 10.1038/nbt.1990.
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ADP-Glo: A Bioluminescent and homogeneous ADP monitoring assay for kinases.
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Bisubstrate inhibitors of protein kinases: from principle to practical applications.
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Targeting cancer with small molecule kinase inhibitors.
Nat Rev Cancer. 2009 Jan;9(1):28-39. doi: 10.1038/nrc2559.
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Small molecule recognition of c-Src via the Imatinib-binding conformation.
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