JP2017096944A5 - - Google Patents

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JP2017096944A5
JP2017096944A5 JP2016221254A JP2016221254A JP2017096944A5 JP 2017096944 A5 JP2017096944 A5 JP 2017096944A5 JP 2016221254 A JP2016221254 A JP 2016221254A JP 2016221254 A JP2016221254 A JP 2016221254A JP 2017096944 A5 JP2017096944 A5 JP 2017096944A5
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test compound
ezh2
ratio
trimethylation
trimethylated
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Claims (7)

  1. 非メチル化H3-K27、モノメチル化H3-K27、ジメチル化H3-K27、およびそれらの任意の組み合わせからなる群より選択されるH3-K27の形態を含むヒストン基質、メチル基供与体、ならびに試験化合物と、単離されたEZH2ポリペプチドのY641変異体とを混ぜ合わせて、試験混合物を形成させる段階; および
    ヒストン基質におけるH3-K27のメチル化を検出し、それによって、試験化合物の存在下でのH3-K27のメチル化が試験化合物の非存在下でのH3-K27のメチル化よりも少ない場合に、試験化合物をEZH2のY641変異体の阻害剤と特定する段階
    を含む方法。
  2. ヒストン基質におけるトリメチル化H3-K27の形成を検出し、それによって、試験化合物の存在下でのトリメチル化H3-K27の形成が試験化合物の非存在下でのトリメチル化H3-K27の形成よりも少ない場合に、試験化合物をEZH2のY641変異体の阻害剤と特定する段階
    をさらに含む、請求項1記載の方法。
  3. モノメチル化H3-K27、ジメチル化H3-K27、およびモノメチル化H3-K27とジメチル化H3-K27との組み合わせからなる群より選択されるH3-K27の形態を含むヒストン基質、メチル基供与体、ならびに試験化合物と、単離された野生型EZH2とを混ぜ合わせ、それによって対照混合物を形成させる段階;
    試験混合物および対照混合物のそれぞれにおけるヒストン基質のトリメチル化を検出する段階;
    (a)試験化合物ありでのEZH2のY641変異体(M+)によるトリメチル化と(b)試験化合物なしでのEZH2のY641変異体(M-)によるトリメチル化の比率を算出する段階;
    (c)試験化合物ありでの野生型EZH2(WT+)によるトリメチル化と(d)試験化合物なしでの野生型EZH2(WT-)によるトリメチル化の比率を算出する段階;
    比率(a)/(b)を比率(c)/(d)と比較する段階; ならびに
    比率(a)/(b)が比率(c)/(d)未満である場合に、試験化合物をEZH2のY641変異体の選択的阻害剤と特定する段階
    をさらに含む、請求項2記載の方法。
  4. EZH2ポリペプチドのY641変異体が、Y641F、Y641H、Y641N、およびY641Sからなる群より選択される変異を有する、請求項1〜3のいずれか一項記載の方法。
  5. 検出する段階が、標識されたメチル基の取り込みを測定することを含む、請求項1〜4記載の方法。
  6. 標識されたメチル基が同位体で標識されたメチル基である、請求項5記載の方法。
  7. 検出する段階が、ヒストン基質を、トリメチル化H3-K27に特異的に結合する抗体と接触させることを含む、請求項1〜3のいずれか一項記載の方法。
JP2016221254A 2010-09-10 2016-11-14 ヒトｅｚｈ２の阻害剤、およびその使用方法 Active JP6496296B2 (ja)

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JP2018218823A Pending JP2019070653A (ja) 2010-09-10 2018-11-22 ヒトｅｚｈ２の阻害剤、およびその使用方法
JP2021096308A Pending JP2021169450A (ja) 2010-09-10 2021-06-09 ヒトｅｚｈ２の阻害剤、およびその使用方法
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US (6) US8895245B2 (ja)
EP (1) EP2614369B1 (ja)
JP (5) JP6389036B2 (ja)
KR (3) KR102373074B1 (ja)
CN (2) CN103261890B (ja)
AU (4) AU2011298987B2 (ja)
BR (1) BR112013005806B1 (ja)
CA (2) CA3176977A1 (ja)
DK (1) DK2614369T3 (ja)
ES (1) ES2570380T3 (ja)
HU (1) HUE028977T2 (ja)
PL (1) PL2614369T3 (ja)
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