CREB/CBP
The CBP protein was described as a factor binding to protein kinase A (PKA)-phosphorylated forms of CREB. Since phospshorylation of CREB enhances transcription of downstream target promoters, it was hypothesized that CBP functions as a transcription co-activator. A variety of sequence-specific, DNA-binding factors are found in complex with CBP: these include nuclear steroid receptors, c-Jun, Fos, p53, Sap1, Stat1 and Stat2, MyoD, Ets-1, NFkB, HIF1 , GATA 1, cMyb, and Smad proteins. Further, CBP interact with TBP, TFIIB, TFIID, RNA helicase A, and with RNA poymerase II itself, suggesting that they are recruited to RNA polymerase II holoenzyme. In transient transfection assays increased expression levels of CBP leads to inhibition of cellular growth. The viral oncoproteins Tag and E1a require the association with p300 and CBP to induce entry into S-phase and also inhibit the transcription activity of both proteins on several cellular enhancers/promoter elements. Deletions, translocations and point mutations within the CBP genes have been found in human tumors.
References
1.Dyson HJ,et al. J Biol Chem. 2016 Mar 25;291(13):6714-22.
References
1.Dyson HJ,et al. J Biol Chem. 2016 Mar 25;291(13):6714-22.
Nuclear Receptor/Transcription Factor
CREB/CBP
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Naphthol AS-E
产品货号 : M16643
cas no: 92-78-4
KIX-KID 相互作用和 CREB 介导的基因转录的细胞渗透性抑制剂 (IC50=2.26 uM)。 -
NCGC 00067819
产品货号 : M16148
cas no: 847163-23-9
NCGC 00067819 是一种小分子化合物,可增强 CREB 信号传导,初步筛选中的 EC50 为 16 nM,CHO CRE-β-内酰胺酶确认测定中的 EC50 为 79 nM。 -
KG-501
产品货号 : M12812
cas no: 18228-17-6
CREB-CBP 相互作用的小分子拮抗剂,通过 CREB 抑制细胞基因的 cAMP 依赖性激活。 -
XX-650-23
产品货号 : M10601
cas no: 117739-40-9
XX-650-23 是 CREB 的小分子抑制剂,阻断 CREB/CBP 相互作用 (IC50=3.2 uM) 并破坏 CREB 驱动的基因表达。