MTAP deletions in cancer create vulnerability to targeting of the MAT2A/PRMT5/RIOK1 axis

Marjon, Katya, Cameron, Michael J., Quang, Phong, Clasquin, Michelle F., Mandley, Everton, Kunii, Kaiko, McVay, Michael, Choe, Sung +9 more·2016·Cell Reports

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  78. BindingDB Entry 50023341: From DNA-Encoded Library Screening to AM-9747: An MTA-Cooperative PRMT5 Inhibitor with Potent Oral In Vivo Efficacy.
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  86. BindingDB Entry 50021728: Discovery of TNG908: A Selective, Brain Penetrant, MTA-Cooperative PRMT5 Inhibitor That Is Synthetically Lethal with MTAP-Deleted Cancers.
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  87. BindingDB Entry 50020883: Discovery of Potent and Oral Bioavailable MAT2A Inhibitors for the Treatment of MTAP-Deleted Tumors.
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  88. BindingDB Entry 50006690: Discovery of Potent and Selective Covalent Protein Arginine Methyltransferase 5 (PRMT5) Inhibitors.
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  89. BindingDB Entry 50014417: Discovery of AG-270, a First-in-Class Oral MAT2A Inhibitor for the Treatment of Tumors with Homozygous
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  90. BindingDB Entry 50022533: Activation of the p53-MDM4 regulatory axis defines the anti-tumour response to PRMT5 inhibition through its role in regulating cellular splicing.
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  91. BindingDB Entry 50015922: Design and evaluation of achiral, non-atropisomeric 4-(aminomethyl)phthalazin-1(2H)-one derivatives as novel PRMT5/MTA inhibitors.
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  92. BindingDB Entry 50021894: Discovery and In Vivo Efficacy of AZ-PRMT5i-1, a Novel PRMT5 Inhibitor with High MTA Cooperativity.
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  93. BindingDB Entry 50012652: Exploiting binding-site arginines in drug design: Recent examples.
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  94. BindingDB Entry 50020264: Identification of a Protein Arginine Methyltransferase 7 (PRMT7)/Protein Arginine Methyltransferase 9 (PRMT9) Inhibitor.
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  95. BindingDB Entry 50019870: Targeting Arginine Methyltransferase PRMT5 for Cancer Therapy: Updated Progress and Novel Strategies.
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  96. BindingDB Entry 50020979: New Horizons of Synthetic Lethality in Cancer: Current Development and Future Perspectives.
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