Enzo潜在的癌症治疗靶点-去泛素化酶（DUBs）
自从蛋白酶体抑制剂硼替佐米(bortezomib, Velcade))批准用于治疗多发性骨髓瘤后，作为治疗癌症的新方法——泛素蛋白酶体途径备受关注。在信号通道中去泛素化酶(DUBs)是一种特殊的“可用药物靶点”，许多科研人员开发其抑制剂作为潜在的抗癌药物。西班牙巴塞罗那瓦尔德希伯伦肿瘤研究所Dr. Joan Seoane和许多学者都证实DUB——泛素特异性肽酶15(USP15)，在恶性胶质瘤和其它恶性肿瘤中对转化生长因子β(TGF-β)起重要调节作用(Eichhorn et al (2012) Nat Med, doi: 10.1038/nm.2619)。TGF-β是中晚期肿瘤的致癌因子，促使TGF-β受体I型和II型(TβR-I和TβR-II)形成异质二聚体复合物，最终激活信号级联反应。这种信号途径可由泛素化来调节，而USP15会抑制泛素化。在胶质瘤的小鼠模型中通过抑制USP15，可降低TGF-β活性，减少肿瘤生长。从人类肿瘤疾病模型中可以看出，USP15基因大量扩增，不利于患者的诊断治疗。
Enzo Life Sciences可提供全面的产品，用于检测DUBs在药物治疗上起何种关键性调控作用。
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Product |
Highlight |
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USP15 (human), (recombinant) (His-tag) |
>95% purity by SDS-PAGE |
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USP15 (human), pAb |
Recognizes human and mouse USP15. |
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Deubiquitinylating enzyme probes, sampler pack |
Active site-directed probes for detection of DUBs |
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Ubiquitin aldehyde, (recombinant) |
High purity inhibitor of deubiquitinylating enzymes (DUBs). |
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Ubiquitin-AMC |
Fluorogenic substrate for a wide range of DUBs |
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Ubiquitin vinyl sulfone, (HA-tag) |
Potent and irreversible inhibitor of DUBs |
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Ubiquitin vinyl methyl ester, HA-tagged |
Active site-directed probe for detection of DUBs. |
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Chloroethyl-ubiquitin, HA-tagged |
Active site-directed probe for detection of DUBs. |
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Bromoethyl-ubiquitin, HA-tagged |
Active site-directed probe for detection of DUBs. |
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TGF-β1 ELISA kit |
Reliably measures as little as 3.3 pg/ml |
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TGF-β1 (human platelets) |
>95% purity by SDS-PAGE |
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ALK5 Inhibitor I |
Cell permeable, potent, selective and ATP-competitive inhibitor of TGF-β RI kinase (IC50=51nM). |