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    • 3. 发明授权
    • Acetylation of pRb by p300 assay method for compounds which modulate this process
    • 通过p300测定方法对调节此过程的化合物进行pRb的乙酰化
    • US07238493B2
    • 2007-07-03
    • US10344243
    • 2001-08-09
    • Nicholas Barrie la ThangueHo Man Chan
    • Nicholas Barrie la ThangueHo Man Chan
    • C12Q1/00C12C1/02C12C1/04G01N33/573
    • G01N33/5011
    • The present invention is based upon the finding that the protein p300 has acetylation activity which is directed to the retinoblastoma tumour suppressor protein pRb by the presence in the cell of the adenovirus E1A protein. This represents a target for modulators of the cell cycle, to which end the invention provides an assay for a modulator of acetylation of pRb by p300, which comprises: a) bringing into contact a p300 protein a pRb protein and a putative modulator compound under conditions where the p300 protein, in the absence of said modulator is capable of acetylating the pRb protein; b) providing conditions for acetylation of said pRb protein; and c) measuring the degree of inhibition of acetylation caused by said modulator compound.
    • 本发明基于蛋白质p300具有通过在腺病毒E1A蛋白质的细胞中的存在而导向视网膜母细胞瘤肿瘤抑制蛋白质pRb的乙酰化活性的发现。 这表示细胞周期的调节剂的靶标,本发明的最后本发明提供了p300对pRb的乙酰化调节剂的测定法,其包括:a)在条件下使p300蛋白与推定的调节剂化合物接触 其中p300蛋白在没有所述调节剂的情况下能够乙酰化pRb蛋白; b)提供所述pRb蛋白的乙酰化条件; 和c)测量由所述调节剂化合物引起的乙酰化抑制程度。