与myc结合亲和力高的已上市药物

MYC有所谓不可成药性，还没有专门的靶向药上市。
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目前针对myc实际可行的治疗策略是根据患者除myc突变扩增外的其他突变，抑制其他靶点，如mtor、hsp90等，实现合成致死或蛋白降解。自救群里部分myc扩增的乳腺癌患者用了mtor抑制剂，确有疗效。
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针对治疗myc还有一种办法是通过计算机虚拟筛选等办法，在已上市药物里找与myc结合亲和力高的药物。

9 E) {/ ~4 W( o+ F' k7 q《In Silico, In Vitro, and In Vivo Investigations on Adapalene as Repurposed Third Generation Retinoid against Multiple Myeloma and Leukemia》这篇论文，通过Virtual Screening、Molecular Docking Analyses and Microscale Thermophoresis的办法，从FDA已经批准上市的1578种药物里，筛选出一些与MYC结合亲和力高的药物；其中一些药物与MYC的结合亲和力超过常用的c-MYC 抑制剂试剂 10058-F4 和 10074-G5(LBEs of −4.92 kcal/mol and −6.24 kcal/mol)。

) z3 s$ ]  }8 U3 b. k7 i1 a- o6 |5 I下面是结合亲和力比较强的一些药物：

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其他一些研究的结论与这篇论文的结论是相印证的，试举几例如下：
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1、《Targeting Oncogenic Super Enhancers in MYC-Dependent AML Using a Small Molecule Activator of NR4A Nuclear Receptors》
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“MYC was identified as the most statistically repressed gene by DHE”
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! W7 h  P: W: z% J1 V2、《Drug repurposing and prediction of multiple interaction types via graph embedding》

“Two FDA approved drugs, Dihydroergotamine (CHEMBL1732) and Indinavir Sulfate (CHEMBL1735), which are predicted by the DT2Vec+, might be able to target MYC and decrease its expression. ”

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) s: N( `3 f/ R- y8 V, W% H2 x3、《Involvement of MCL1, c-myc, and cyclin D2 protein degradation in ponatinib-induced cytotoxicity against T315I(+) Ph+leukemia cells》

, K7 ?* i; x# y# Z) b“PNT induced apoptosis (increased sub G1 cells, and cleaved caspase3 and PARP), and suppressed protein expression of MCL1, cyclin D2 and c-myc, which were reversed by a proteasome inhibitor, MG132, suggesting enhanced proteasomal degradation by PNT. ”
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4、《 Synergistic effect of eribulin and CDK inhibition for the treatment of triple negative breast cancer》
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% C4 i6 E6 Q7 Z4 U0 f- ? Additionally, treatment with eribulin resulted in a decrease in c-myc expression and a trend
( j5 z! u! {6 a3 y/ t1 ctoward an increase in cdki p15。
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5、《Atovaquone: an antiprotozoal drug suppresses primary and resistant breast tumor growth by inhibiting HER2/β-catenin signaling》
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“We also observed a decrease in c-Myc expression in the tumors of atovaquone-treated mice”