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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# P, D3 r/ \; l9 z, U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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* W4 `, Q# d0 ]! `- K# l+ }) U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。
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《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)。

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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, c; q$ q+ a7 u' G# }" i( o1、《Targeting Oncogenic Super Enhancers in MYC-Dependent AML Using a Small Molecule Activator of NR4A Nuclear Receptors》

“MYC was identified as the most statistically repressed gene by DHE”



; {7 i. s5 o( M5 V% S) V- h9 }2、《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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  R4 ?1 Q+ A: K4 y3、《Involvement of MCL1, c-myc, and cyclin D2 protein degradation in ponatinib-induced cytotoxicity against T315I(+) Ph+leukemia cells》
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) A! z7 c9 R& _8 [9 F! z“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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1 ^* S1 x* J2 p" X/ o( H* B4 `  d4、《 Synergistic effect of eribulin and CDK inhibition for the treatment of triple negative breast cancer》

3 `1 R4 q+ j# V3 H: T0 d Additionally, treatment with eribulin resulted in a decrease in c-myc expression and a trend
- W! h! \* z& Y; i6 o. m$ Etoward an increase in cdki p15。


8 m  ^# b0 T' {" u# B) b: ]/ p4 f5、《Atovaquone: an antiprotozoal drug suppresses primary and resistant breast tumor growth by inhibiting HER2/β-catenin signaling》

“We also observed a decrease in c-Myc expression in the tumors of atovaquone-treated mice”