JP5642060B2 - エクジソン受容体複合体を通して外因性遺伝子の発現を調節するための生物学的利用能のあるジアシルヒドラジン・リガンド - Google Patents
エクジソン受容体複合体を通して外因性遺伝子の発現を調節するための生物学的利用能のあるジアシルヒドラジン・リガンド Download PDFInfo
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- JP5642060B2 JP5642060B2 JP2011286880A JP2011286880A JP5642060B2 JP 5642060 B2 JP5642060 B2 JP 5642060B2 JP 2011286880 A JP2011286880 A JP 2011286880A JP 2011286880 A JP2011286880 A JP 2011286880A JP 5642060 B2 JP5642060 B2 JP 5642060B2
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Description
(a) 非置換又は置換フェニルで、置換体は独立して1から5までのH;ハロ;ニトロ;シアノ;ヒドロキシ;アミノ(‐NRaRb);アルキルアミノアルキル(‐(CH2)nNRaRb);(C1-C6)アルキル;(C1-C6)ハロアルキル;(C1-C6)シアノアルキル;(C1-C6)ヒドロキシアルキル;(C1-C6)アルコキシ;フェノキシ;(C1-C6)ハロアルコキシ;(C1-C6)アルコキシ(C1-C6)アルキル;(C1-C6)アルケニルオキシ(C1-C6)アルキル;(C1-C6)アルコキシ(C1-C6)アルコキシ;(C1-C6)アルカノイルオキシ(C1-C6)アルキル;ハロ、シアノ、(C1-C4)アルキル、又は(C1-C4)アルコキシで選択的に置換した(C2-C6)アルケニル;ハロ又は(C1-C4)アルキルで選択的に置換した(C2-C6)アルキニル;フォルミル;カルボキシ;(C1-C6)アルキルカルボニル;(C1-C6)ハロアルキルカルボニル;ベンゾイル;(C1-C6)アルコキシカルボニル;(C1-C6)ハロアルコキシカルボニル;(C1-C6)アルカノイルオキシ(‐OCORa);カルボキシアミド(‐CONRaRb);アミド(‐N RaCORb);アルコキシカルボニルアミノ(‐NRaCO2Rb);アルキルアミノカルボニルアミノ(‐N RaCONRbRc);メルカプト;(C1-C6)アルキルチオ;(C1-C6)アルキルスルホニル;(C1-C6)アルキルスルホニル(C1-C6)アルキル;(C1-C6)アルキルスルホキシド(‐S(O)Ra);(C1-C6)アルキルスルホキシド(C1-C6)アルキル(‐(CH2)nS(O)Ra);フルファミド(‐SO2NRaRb);‐SO3H;又は非置換又は置換フェニルで、置換体は独立して1から3までのハロ、ニトロ、(C1-C6)アルコキシ、(C1-C6)アルキル、又はアミノ;あるいはフェニル環の隣接する2つの位置の1つ又は両方が置換される場合、付着している原子は、(‐OCH2O-)、(‐OCH(CH3)O-)、(‐CH2CH2O-)、(‐OCH(CH3)CH2O -)、(‐S- CH=N -)、(‐CH2OCH2O‐)、(‐O(CH2)3‐)、(=N-O-N=)、(‐C=CH-NH-)、(‐OCF2O-)、(‐NH-CH=N-)、(‐CH2CH2O-)、及び(‐(CH2)4‐) からなるグループから選ばれた連結のフェニル結合末端を形成する場合があり;
(b)1-3窒素原子及び3-5核炭素原子を持つ非置換6員環ヘテロサイクル又は置換6員環ヘテロサイクルで、置換体は1から3までの同じ又は異なるハロ;ニトロ;ヒドロキシ;(C1-C6)アルキル;(C1-C6)アルコキシ;(C1-C6)チオアルコキシ;カルボキシ;(C1-C6)アルコキシカルボニル;(C1-C6)カルボキシアルキル;各アルキル・グループに独立に定まった数の炭素原子を持つ(C1-C6)アルコキシカルボニルアルキル;‐CONRaRb;アミノ;(C1-C6)アルキルアミノ;各アルキル・グループに独立に定まった数の炭素原子を持つ(C1-C6)ジアルキルアミノ;‐CF3を含むハロアルキル;‐C=N-NHC(O)NRaRb);又は‐C=N-NHC(O)C(O)NRaRb);あるいは
(c) 5−ベンズイミダゾリル;1−トリチル‐5−ベンズイミダゾリル;3−トリチル‐5−ベンズイミダゾリル;1H-インダゾール‐3‐イル;1‐トリチル‐1H‐インダゾール‐3‐イル;又は1‐(C1-C6)アルキル‐1H‐インドール‐2‐イル;
1)Eが非置換又は置換(C4-C10)側鎖アルキルで、置換体が独立に1-4シアノ;ハロ;(C2-C3)アルケニル;カルボキシ;又は(C1-C6)アルコキシカルボニルの場合、
Bは、
(a) 少なくとも1つの‐C=N-NHC(O)NRaRb又は‐C=N-NHC(O)C(O)N RaRbグループを持つ置換フェニル;
(b) 少なくとも1つのハロアルキル・グループを持ち、1-3窒素原子及び3-5核炭素原子を有する置換6員環へテロサイクル;
又は
(c) 5−ベンズイミダゾリル;1−トリチル‐5−ベンズイミダゾリル;3−トリチル‐5−ベンズイミダゾリル;1H-インダゾール‐3‐イル;1‐トリチル‐1H‐インダゾール‐3‐イル;又は1‐(C1-C6)アルキル‐1H‐インドール‐2‐イル;
ここで、Ra、Rbは独立にH、(C1-C6)アルキル、又はフェニルであり;あるいは
2)Eがフェニル、ヒドロキシ、(C1-C6)アルコキシ、又はフォルミルのうち少なくとも1つを有する置換(C4-C10)側鎖アルキルの場合、
Bは、
(a) 少なくとも1つの‐C=N-NHC(O)NRaRb又は‐C=N-NHC(O)C(O)N RaRbグループを持つ置換フェニル;
(b) 1-3窒素原子及び3-5核炭素原子を有する置換又は非置換の6員環へテロサイクル;又は
(c) 5−ベンズイミダゾリル;1−トリチル‐5−ベンズイミダゾリル;3−トリチル‐5−ベンズイミダゾリル;1H-インダゾール‐3‐イル;1‐トリチル‐1H‐インダゾール‐3‐イル;又は1‐(C1-C6)アルキル‐1H‐インドール‐2‐イル;
(i) NaH、KH、あるいはアミドMNRaRbから選ばれる塩基と式(I)の化合物を反応させて生成物IIを得るステップで、ここでMはリチウム、ナトリウム、又はカリウムで、Ra及びRbは独立に(C1-C6)アルキル又はフェニルであり、
(ii) ステップ(i)の生成物(II)と式(III)の化合物との反応で、Rは3から5までの同じ又は異なるクロロ、フルオロ、又はトリフルオロメチルで置換したフェニルであり;
ここで、
A及びBは独立に、
(a) 非置換又は置換フェニルで、置換体は独立して1から5までのH; ハロ;ニトロ;シアノ;アミノ(‐NRaRb);アルキルアミノアルキル(‐(CH2)nNRaRb);(C1-C6)アルキル;(C1-C6)ハロアルキル;(C1-C6)シアノアルキル;(C1-C6)アルコキシ;フェノキシ;(C1-C6)ハロアルコキシ;(C1-C6)アルコキシ(C1-C6)アルキル;(C1-C6)アルケニルオキシ(C1-C6)アルキル;(C1-C6)アルコキシ(C1-C6)アルコキシ;ハロ、シアノ、(C1-C4)アルキル、又は(C1-C4)アルコキシで選択的に置換した(C2-C6)アルケニル;ハロ又は(C1-C4)アルキルで選択的に置換した(C2-C6)アルキニル;フォルミル;(C1-C6)ハロアルキルカルボニル;ベンゾイル;(C1-C6)アルコキシカルボニル;(C1-C6)ハロアルコキシカルボニル;(C1-C6)アルカノイルオキシ(‐OCORa);カルボキシアミド(‐CONRaRb);アミド(‐N RaCORb);アルコキシカルボニルアミノ(‐N(CH2)nCO2Rb);アルキルアミノカルボニルアミノ(‐N(CH2)nCONRbRc);(C1-C6)アルキルチオ;フルファミド(‐SO2NRaRb);又は非置換又は置換フェニルで、置換体は独立して1から3までのハロ、ニトロ、(C1-C6)アルコキシ、(C1-C6)アルキル、又は(‐NRaRb);あるいはフェニル環の隣接する2つの位置の1つ又は両方が置換される場合、付着している原子は、(‐OCH2O‐)、(‐OCH(CH3)O-)、(‐CH2CH2O-)、(‐OCH(CH3)CH2O -)、(‐S- CH=N -)、(‐CH2OCH2O‐)、(‐O(CH2)3‐)、(=N-O-N=)、(‐C=CH-NH-)、(‐OCF2O-)、(‐NH-CH=N-)、(‐CH2CH2O-)、及(‐(CH2)4‐)からなるグループから選ばれた連結のフェニル結合末端を形成する場合があり;あるいは
(b) 1-3窒素原子を持つ非置換5又は6員環ヘテロサイクル又は置換5又は6員環ヘテロサイクルで、置換体は1から4までの同じ又は異なるハロ;ニトロ;(C1-C6)アルキル;(C1-C6)アルケニル;(C1-C6)アルコキシ;(C1-C6)チオアルコキシ;(C1-C6)アルコ
キシカルボニル;(C1-C6)カルボキシアルキル;‐CONRaRb;アミノ(‐NRaRb);‐CF3を含むハロアルキル;トリアルキルシリル(-SiRaRb Rc);トリチル(C(Ph)3);あるいは非置換又は置換のフェニルで、置換体は独立に1から3までのハロ、ニトロ、(C1-C6)アルコキシ、(C1-C6)アルキル、又は(‐NRaRb);あるいは2つの隣接する位置が置換される場合、これらの位置はベンゾ環融合を形成する場合があり、そして
Eはフェニル、あるいは非置換又は置換(C1-C10)直鎖又は側鎖のアルキルで、置換体は独立に1-4シアノ;ハロ;(C5-C6)シクロアルキル;フェニル;(C2-C3)アルケニル;(C1-C6)アルコキシ;(C1-C6)アルコキシカルボニル;(C1-C6)アルカノイルオキシ(-OCORa);フォルミル;各アルキル・グループに独立に所定の炭素数を持っている(C1-C6)トリアルキルシリルオキシ;又は‐C=N-ORaで、
ここで、Ra、Rb、及びRcは独立に(C1-C4)アルキル又はフェニルで、n=1-4である。
a)エクジソン受容体複合体に含まれるもの:
1)DNA結合ドメイン
2)リガンドのための結合ドメイン
3)トランスアクティベーション・ドメイン
b)DNAコンストラクトに含まれるもの
1)外因性遺伝子
2)応答要素
ここで外因性遺伝子は応答要素のコントロール下にあり、リガンドの存在下でDNA結合ドメインと応答要素と結合する事により、遺伝子の活性化又は抑制が起きる。
a)本発明の化合物を含むリガンドと接触しても殆ど何も感じない細胞を選択
b)細胞への導入
1)DNAコンストラクトに含まれるもの
i)ポリペプチドをコード化している外因性遺伝子
ii)応答要素
ここで、遺伝子は応答要素のコントロール下にある。
2)エクジソン受容体複合体に含まれるもの:
i)DNA結合ドメイン
ii)リガンドのための結合ドメイン
iii)トランスアクティベーション・ドメイン
c)細胞をリガンドに接触させる。
一般的方法
した。濾液を蒸発乾固すると、1.62gの粗ベンジルアルコールが得られた。生成物をシリカゲル・カラムクロマトグラフィーで精製した。50-60%の酢酸エチル/ヘキサンで溶出すると、1.25gの白色固体である3,5-ジメチル安息香酸N-tert-ブチル-N’-(2-ヒドロキシメチル-3-メトキシ-ベンゾイル)-ヒドラジドが得られた。1HNMR (CDCl3, 300 MHz)δ(ppm): 7.1 (t, 1H), 7.05 (s, 2H), 6.98 (s,1H), 6.9 (d, 1H), 6.5 (d, 1H), 4.2(q, 2H), 3.79 (s, 3H), 2.23 (s, 6H), 1.57(s, 9H). TLC (1:1酢酸エチル:ヘキサン) Rf=0.20.
を示していた。100mgの塩化アセチルと適量のピリジンを加え、1時間還流した。反応混合物はCH2Cl2に注ぎ、希釈したK2CO3水溶液、次に希塩酸水溶液で抽出した。CH2Cl2抽出物を乾燥し、濃縮すると、粗酢酸塩が得られた。物質はシリカゲル・カラムクロマトグラフィーを使い、1:1酢酸エチル:ヘキサンで溶出する事により精製した。1HNMR (CDCl3, 300 MHz)δ(ppm): 7.3-6.9 (m, 6H), 6.4 (d, 1H), 4.8 (d,1H), 4.6 (d, 1H), 3.795 (s, 3H),2.3 (s, 6H), 2.03 (s, 3H), 1.58 (s, 9H).
し、CH2Cl2で抽出した。(別の実験では、弱NaOHで洗浄し、過剰の酸と酸塩化物を除去した)。抽出物を乾燥し、蒸発させると、約1gの白色の固体が得られた。これをシリカゲル・クロマトグラフィーで精製した。15%の酢酸エチル・ヘキサン溶液で溶出すると、精製された生成物である3,5-ジメチル安息香酸N’-(2,3-ジメチル-ベンゾイル)-N-(1-エチル-2,2-ジメチル-プロピル)-ヒドラジドを得た(0.62g、70%)。1HNMR (500 MHz, CDCl3) δ=(ppm):6.95-7.4 (m, 7H), 4.61 (m, 1H),2.2-2.4 (multiple s, 9H), 1.81 (s, 3H), 1.6-1.8(m, 2H), 1.3 (br t, 3H), 1.08(multiple br s, 9H).
)、反応混合物に加え、反応混合物は再び0℃に冷やした。3.63g(mmol)の5-エチル-2,3-ジヒドロ-ベンゾ[1,4]ジオキシン-6-カルボニル塩化物を40mLのCH2Cl2に溶解し、分離
漏斗から15分かけて滴下した。反応混合物は室温で3日間撹拌した。反応混合物はCH2Cl2と水を使って分離漏斗へ移した。水の層はCH2Cl2で十分に抽出した。CH2Cl2抽出物は0.5NHClで抽出し、乾燥し、蒸発させた。残渣を真空オーブンで更に乾燥すると、5.15gの黄褐色の固体であるN’-(5-エチル-2,3-ジヒドロ-ベンゾ[1,4]ジオキシン-6-カルボニル)-ヒドラジン安息香酸tert-ブチルエステルが得られた。TLC(1:1酢酸エチル:ヘキサン)はRf=0.43に単一のスポットを示し、NMRは極めて精製された生成物である事を示していた。1H NMR(CDCl3, 500 MHz) δ (ppm): 7.5 (br, 1H), 7.0 (br,1H), 6.75 (d, 2H),4.28 (br, 4H), 2.76 (m, 2H), 1.5 (s, 9H), 1.18 (t, 3H).
に加え、室温で24時間撹拌した。反応混合物は分離漏斗へ移し、希NaHCO3とCH2Cl2を加えた。CH2Cl2層は分離し、水の層をCH2Cl2で2度抽出した。CH2Cl2抽出物をMgSO4上で乾燥し、蒸発させると、0.59gの白色の残渣を得た。カラムクロマトグラフィーを使い、15mLの20%酢酸エチル/ヘキサンで溶出すると、約350mgの3,5-ジメチル安息香酸N’-(5-エチル-2,3-ジヒドロ-ベンゾ[1,4]ジオキシン-6-カルボニル)-N-(1-エチル-2,2-ジメチル-プロピル)-ヒドラジドが得られた(TLC:Rf=0.56、1:1酢酸エチル:ヘキサンにより、95%精製)。1HNMR (CDCl3, 500 MHz) δ(ppm): 7.05 (s, 1H), 7.0 (s, 2H),6.6 (d, 1H),6. 27 (d, 1H), 4.65 (d, 1H), 4.25 (s, 4H), 2.9 (m, 1H), 2.3 (s,6H), 2.0 (m, 1H),1. 55-1.7 (m, 2H), 1.25 (m, 3H), 0.9-1.2 (3s, 9H), 0.9 (t, 3H).
見掛けの透過度、PaPP、回収%は以下の方法で計算された:
Papp= (dCr /dt) x Vr/(A x C0) (1)
回収%=100 x((Vr x Cr final) + (Vdx Cd final))/(Vdx C0) (2)
ここで、
dCr/dtは受け器室の蓄積濃度対時間(単位:Ms-1)
Vrは受け器室の容積(単位:cm3)
Vdはドナー室の容積(単位:cm3)
Aは細胞単層の面積(12ウェル・トランスウェルに関しては1.13cm2)
Coは投与溶液の濃度(単位:M)
Cr finalは培養期間終了時点の受け器蓄積濃度(単位:M)
Cd finalは培養期間終了時点のドナー蓄積濃度(単位:M)
遺伝子発現カセット
安定細胞株
遺伝子発現カセット
Claims (23)
- 5-メチル-2,3-ジヒドロ-ベンゾ[1,4]ジオキシン-6-カルボン酸N’-(3,5-ジメチル-ベンゾイル)-N’-(1-エチル-2,2-ジメチル-プロピル)-ヒドラジド、
5-メチル-2,3-ジヒドロ-ベンゾ[1,4]ジオキシン-6-カルボン酸N’-(1-tert-ブチル-ブチル)-N’-(3,5-ジメチル-ベンゾイル)-ヒドラジド、
5-メチル-2,3-ジヒドロ-ベンゾ[1,4]ジオキシン-6-カルボン酸N’-(1-tert-ブチル-ブチル)-N’-(3,5-ジメトキシ-4-メチル-ベンゾイル)-ヒドラジド、
5-エチル-2,3-ジヒドロ-ベンゾ[1,4]ジオキシン-6-カルボン酸N’-(3,5-ジメチル-ベンゾイル)-N’-(1-エチル-2,2-ジメチル-プロピル)-ヒドラジド、
5-エチル-2,3-ジヒドロ-ベンゾ[1,4]ジオキシン-6-カルボン酸N’-(3,5-ジメトキシ-4-メチル-ベンゾイル)-N’-(1-エチル-2,2-ジメチル-プロピル)-ヒドラジド、
5-エチル-2,3-ジヒドロ-ベンゾ[1,4]ジオキシン-6-カルボン酸N’-(1-tert-ブチル-ブチル)-N’-(3,5-ジメチル-ベンゾイル)-ヒドラジド、
3,5-ジメチル安息香酸N-(1-エチル-2,2-ジメチル-プロピル)-N’-(3-メトキシ-2-メチル-ベンゾイル)-ヒドラジド、
3,5-ジメトキシ-4-メチル安息香酸N-(1-エチル-2,2-ジメチル-プロピル)-N’-(3-メトキシ-2-メチル-ベンゾイル)-ヒドラジド、
3,5-ジメチル安息香酸N-(1-tert-ブチル-ブチル)-N’-(3-メトキシ-2-メチル-ベンゾイル)-ヒドラジド、
3,5-ジメトキシ-4-メチル安息香酸N-(1-tert-ブチル-ブチル)-N’-(3-メトキシ-2-メチル-ベンゾイル)-ヒドラジド、
3,5-ジメチル安息香酸N-(1-エチル-2,2-ジメチル-プロピル)-N’-(2-エチル-3-メトキシ-ベンゾイル)-ヒドラジド、
3,5-ジメトキシ-4-メチル安息香酸N-(1-エチル-2,2-ジメチル-プロピル)-N’-(2-エチル-3-メトキシ-ベンゾイル)-ヒドラジド、
3,5-ジメチル安息香酸N-(1-tert-ブチル-ブチル)-N’-(2-エチル-3-メトキシ-ベンゾイル)-ヒドラジド、
3,5-ジメトキシ-4-メチル安息香酸N-(1-tert-ブチル-ブチル)-N’-(2-エチル-3-メトキシ-ベンゾイル)-ヒドラジド、
3,5-ジメチル安息香酸N-(1-tert-ブチル-ペンチル)-N’-(4-エチル-ベンゾイル)-ヒドラジド、
3,5-ジメチル安息香酸N-(2,2-ジメチル-1-フェニル-プロピル)-N’-(4-エチル-ベンゾイル)-ヒドラジド、
3,5-ジメチル安息香酸N-(1-tert-ブチル-ペンチル)-N’-(3-メトキシ-2-メチル-ベンゾイル)-ヒドラジド、及び
3,5-ジメトキシ-4-メチル安息香酸N-(1-tert-ブチル-ペンチル)-N’-(3-メトキシ-2-メチル-ベンゾイル)-ヒドラジド
から構成されるグループから選ばれる化合物又はその製薬的に容認できる塩。 - 3,5-ジメチル安息香酸N-(1-tert-ブチル-ブチル)-N’-(2-エチル-3-メトキシ-ベンゾイル)-ヒドラジド又はその製薬的に容認できる塩である、請求項1に記載の化合物。
- 3,5-ジメチル安息香酸N-(1-エチル-2,2-ジメチル-プロピル)-N’-(3-メトキシ-2-メチル-ベンゾイル)-ヒドラジド又はその製薬的に容認できる塩である、請求項1に記載の化合物。
- 5-メチル-2,3-ジヒドロ-ベンゾ[1,4]ジオキシン-6-カルボン酸N’-(3,5-ジメチル-ベンゾイル)-N’-(1-エチル-2,2-ジメチル-プロピル)-ヒドラジドである、請求項1に記載の化合物。
- 3,5-ジメチル安息香酸N-(1-tert-ブチル-ブチル)-N’-(3-メトキシ-2-メチル-ベンゾイル)-ヒドラジドである、請求項1に記載の化合物。
- 製薬的に容認できる担体としての、請求項1〜5のいずれか一項に記載の化合物。
- 細胞に於いて遺伝子の発現をインビトロで調節する方法であり、
前記細胞は、
(i)トランスアクティベーション・ドメイン、
(ii)DNA結合ドメイン、及び
(iii)グループH核受容体リガンド結合ドメイン、
を含む、第1ポリペプチドをコード化する第1ポリヌクレオチドを含む第1遺伝子発現カセ
ット、並びに
(i)前記DNA結合ドメインに結合できる応答要素、
(ii)前記トランスアクティベーション・ドメインにより活性化されるプロモーター、及び
(iii)前記遺伝子、
を含む、第2遺伝子発現カセットを含み、
前記方法は、前記細胞と、請求項1〜5のいずれか一項に記載の化合物とを、接触させることを含む、
方法。 - 請求項1〜5のいずれか一項に記載の化合物を含み、細胞に於いて遺伝子の発現を調節するための薬剤であり、
前記細胞は、
(i)トランスアクティベーション・ドメイン、
(ii)DNA結合ドメイン、及び
(iii)グループH核受容体リガンド結合ドメイン、
を含む、第1ポリペプチドをコード化する第1ポリヌクレオチドを含む第1遺伝子発現カセット、並びに
(i)前記DNA結合ドメインに結合できる応答要素、
(ii)前記トランスアクティベーション・ドメインにより活性化されるプロモーター、及び
(iii)前記遺伝子、
を含む、第2遺伝子発現カセットを含む、
薬剤。 - 請求項1〜5のいずれか一項に記載の化合物を含み、対象の中で1つ又はそれ以上の外因性遺伝子の発現を調節するための薬剤。
- 前記1つ又はそれ以上の外因性遺伝子が、分泌性蛋白質、酵素、調節蛋白質、細胞表面受容体、血液凝固因子、ホルモン、サイトカイン、阻害物質、ジフテリアの毒、コレラの毒、癌治療に有益な物質、又は遺伝子疾患の治療に有益な物質をコード化する、
請求項9に記載の薬剤。 - 前記1つ又はそれ以上の外因性遺伝子が、サイトカインをコード化する、
請求項10に記載の薬剤。 - 前記サイトカインがリンフォカインである、
請求項11に記載の薬剤。 - 前記サイトカインが、インターフェロン、顆粒細胞マクロファージ・コロニー刺激因子、コロニー刺激因子‐1、腫瘍壊死因子又はエリスロポイエチンである、
請求項11に記載の薬剤。 - 前記1つ又はそれ以上の外因性遺伝子が、ホルモンをコード化する、
請求項10に記載の薬剤。 - 前記ホルモンは、インシュリン、副甲状腺ホルモン、黄体ホルモン放出因子、アルファ及びベータ精インヒビン又はヒト成長ホルモンである、
請求項14に記載の薬剤。 - 前記1つ又はそれ以上の外因性遺伝子が、阻害物質をコード化する、
請求項10に記載の薬剤。 - 前記阻害物質が、アルファ1‐アンチトリプシンである、
請求項16に記載の薬剤。 - 請求項1〜5のいずれか一項に記載の化合物を含み、対象の細胞内でエクジソン受容体複合体を前記化合物に接触させて、遺伝子導入された対象の中で、内因性又は非相同性の遺伝子発現を調節するための薬剤であり、
前記細胞は、前記化合物と結合する時に、エクジソン受容体複合体のDNA結合配列をさらに含み、エクジソン受容体複合体/前記化合物/DNA結合配列複合体は前記遺伝子の発現を誘導する、
薬剤。 - 前記エクジソン受容体複合体はキメラ・エクジソン受容体複合体であり、前記DNAコンストラクトはプロモーターをさらに含む、請求項18に記載の薬剤。
- 対象が植物である、請求項18に記載の薬剤。
- 対象が哺乳類である、請求項18に記載の薬剤。
- 請求項1〜5のいずれか一項に記載の化合物を含み、細胞の遺伝子の発現を調節するための薬剤であって、
前記細胞は遺伝子発現調節システムを含み、
前記遺伝子調節システムは、
i) (a) 発現調節の対象となっている遺伝子に関連した応答要素を認識するDNA結合ドメイン、及び
(b) エクジソン受容体リガンド結合ドメイン、
を含む、第1ハイブリッド・ポリペプチドをコード化するポリヌクレオチド配列を含む、前記細胞の中で発現させることができる第1遺伝子発現カセット、
ii) (a) トランスアクティベーション・ドメイン、及び
(b) キメラ・レチノイドX受容体リガンド結合ドメイン、
を含む、第2ハイブリッド・ポリペプチドをコード化するポリヌクレオチド配列を含む、前記細胞の中で発現させることができる第2遺伝子発現カセット、並びに
iii) (a) 第1ハイブリッド・ポリペプチドのDNA結合ドメインにより認識される応答エレメント、
(b) 第2ハイブリッド・ポリペプチドのトランスアクティベーション・ドメインが活性化するプロモーター、及び
(c) 発現調節の対象である遺伝子、
を含む、ポリヌクレオチド配列を含む、前記細胞の中で発現させることができる第3遺伝子発現カセット、
を含む、
薬剤。 - 請求項1〜5のいずれか一項に記載の化合物を含み、細胞内でポリペプチドを生産するための薬剤であって、
前記細胞は、
1)i) ポリペプチドをコード化する外因性遺伝子、及び
ii) 応答要素、
を含むDNAコンストラクトで、前記遺伝子が前記応答要素のコントロール下にあるもの、並びに
2)i) DNA結合ドメイン、
ii) エクジソン受容体リガンド結合ドメイン、及び
iii) トランスアクティベーション・ドメイン、
を含むエクジソン受容体複合体をコード化するDNAコンストラクト、
を含む、
薬剤。
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Families Citing this family (39)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US20040033600A1 (en) * | 2001-03-21 | 2004-02-19 | Palli Subba Reddy | Ecdysone receptor-based inducible gene expression system |
US8105825B2 (en) * | 2000-10-03 | 2012-01-31 | Intrexon Corporation | Multiple inducible gene regulation system |
US8715959B2 (en) | 2001-02-20 | 2014-05-06 | Intrexon Corporation | Substitution mutant receptors and their use in a nuclear receptor-based inducible gene expression system |
US9249207B2 (en) | 2001-02-20 | 2016-02-02 | Intrexon Corporation | Substitution mutant receptors and their use in an ecdysone receptor-based inducible gene expression system |
JP4955905B2 (ja) * | 2001-02-20 | 2012-06-20 | イントレキソン コーポレーション | キメラレチノイドx受容体および新規エクジソン受容体−ベースの誘導性遺伝子発現システムにおけるそれらの使用 |
US9493540B2 (en) | 2001-02-20 | 2016-11-15 | Intrexon Corporation | Ecdysone receptor/invertebrate retinoid X receptor-based inducible gene expression system |
EP1436394A4 (en) | 2001-09-26 | 2004-12-29 | Rheo Gene Holdings Inc | CICADA ECDYSON RECEPTOR NUCLEIC ACIDS, POLYPEPTIDES AND THEIR USE |
US7304161B2 (en) * | 2003-02-10 | 2007-12-04 | Intrexon Corporation | Diaclhydrazine ligands for modulating the expression of exogenous genes in mammalian systems via an ecdysone receptor complex |
US7456315B2 (en) * | 2003-02-28 | 2008-11-25 | Intrexon Corporation | Bioavailable diacylhydrazine ligands for modulating the expression of exogenous genes via an ecdysone receptor complex |
US7935510B2 (en) * | 2004-04-30 | 2011-05-03 | Intrexon Corporation | Mutant receptors and their use in a nuclear receptor-based inducible gene expression system |
BRPI0811348B1 (pt) | 2007-05-29 | 2022-02-08 | Intrexon Corporation | Composto, (n-(1-ter-butil-butil)-n'-(2-etil-3-metóxi benzoil)-hidrazida de ácido (r)-3,5-dimetilbenzóico e composição farmacêutica |
AU2013204101B2 (en) * | 2007-05-29 | 2015-07-02 | Intrexon Corporation | Chiral diacylhydrazine ligands for modulating the expression of exogenous genes via an ecdysone receptor complex |
MX2010001993A (es) * | 2007-08-23 | 2010-03-11 | Intrexon Corp | Metodos y composiciones para diagnosticar una enfermedad. |
CA2715080C (en) * | 2007-09-28 | 2021-09-28 | Intrexon Corporation | Therapeutic gene-switch constructs and bioreactors for the expression of biotherapeutic molecules, and uses thereof |
EP2207874B1 (en) | 2007-10-08 | 2014-12-03 | Intrexon Corporation | Engineered dendritic cells and uses for the treatment of cancer |
BRPI0908747A2 (pt) | 2008-03-14 | 2023-04-18 | Intrexon Corp | Ligantes esteróides e seu uso em modulação de comutador genético |
DE102008038222A1 (de) * | 2008-08-18 | 2010-02-25 | Merck Patent Gmbh | Indazol-5-carbonsäurehydrazid-derivate |
BRPI0920679A2 (pt) | 2008-10-08 | 2022-05-17 | Intrexon Corp | Células construídas expressando múltiplos imunomoduladores e usos das mesmas |
BRPI1009792A2 (pt) * | 2009-03-05 | 2015-08-25 | Rohm & Haas | Sistema de expressão de gene para inibir controlavelmente o acúmulo em uma célula de planta, composição, e , métodos para produzir um planta transgênica e para modular a sensibilidade de etileno em uma planta. |
TWI688395B (zh) | 2010-03-23 | 2020-03-21 | 英翠克頌公司 | 條件性表現治療性蛋白質之載體、包含該載體之宿主細胞及彼等之用途 |
DE102010055499A1 (de) * | 2010-12-22 | 2011-06-16 | W.C. Heraeus Gmbh | Prozess zur Herstellung von Bendamustinalkylester, Bendarmustin sowie Derivaten davon |
EP2681327B1 (en) | 2011-03-04 | 2018-11-21 | Intrexon Corporation | Vectors conditionally expressing protein |
TWI586640B (zh) * | 2011-09-08 | 2017-06-11 | 英翠克頌公司 | 結晶狀二醯基肼及其用途 |
AU2014227571B2 (en) | 2013-03-15 | 2017-02-02 | Intrexon Corporation | Boron-containing diacylhydrazines |
US11053513B2 (en) | 2013-07-15 | 2021-07-06 | Donald Danforth Plant Science Center | Enhanced oil production and stress tolerance in plants |
WO2016044390A1 (en) | 2014-09-17 | 2016-03-24 | Intrexon Corporation | Boron-containing diacylhydrazine compounds |
WO2017012966A1 (de) * | 2015-07-17 | 2017-01-26 | Bayer Cropscience Aktiengesellschaft | Substituierte aryl- und heteroarylcarbonsäurehydrazide oder deren salze und ihre verwendung zur steigerung der stresstoleranz in pflanzen |
SG11201802912PA (en) | 2015-10-10 | 2018-05-30 | Intrexon Corp | Improved therapeutic control of proteolytically sensitive, destabilized forms of interleukin-12 |
CA3004742A1 (en) | 2015-11-11 | 2017-05-18 | Intrexon Corporation | Compositions and methods for expression of multiple biologically active polypeptides from a single vector for treatment of cardiac conditions and other pathologies |
US11446398B2 (en) | 2016-04-11 | 2022-09-20 | Obsidian Therapeutics, Inc. | Regulated biocircuit systems |
UY37343A (es) | 2016-07-25 | 2018-02-28 | Intrexon Corp | Control del fenotipo en plantas |
CN106565531A (zh) * | 2016-10-31 | 2017-04-19 | 苏州汉德创宏生化科技有限公司 | 烷基肼的药学可接受盐的合成方法 |
CN110139933B (zh) | 2016-11-09 | 2024-03-08 | 英特瑞克斯顿股份有限公司 | 共济蛋白表达构建体 |
IL310711A (en) | 2017-01-10 | 2024-04-01 | Intrexon Corp | Modulation of expression of polypeptides through a new system for changing gene expression |
CA3092935A1 (en) | 2018-03-06 | 2019-09-12 | Precigen, Inc. | Hepatitis b vaccines and uses of the same |
CN109134354B (zh) * | 2018-09-19 | 2022-03-25 | 天津科技大学 | 2-吡啶甲基硫醚的合成方法及相关药物的合成工艺 |
WO2020206056A1 (en) | 2019-04-04 | 2020-10-08 | Greenvenus Llc | Peptides and methods of plant protection |
CN110423210B (zh) * | 2019-07-19 | 2021-07-27 | 暨南大学 | 一种苄基芳基硫醚衍生物及其制备方法和应用 |
CN114150032A (zh) * | 2021-11-01 | 2022-03-08 | 丁庆 | 一种基于蝗虫特有肽的蝗虫水解物的制造方法及应用 |
Family Cites Families (127)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4631211A (en) | 1985-03-25 | 1986-12-23 | Scripps Clinic & Research Foundation | Means for sequential solid phase organic synthesis and methods using the same |
US5117057A (en) | 1985-10-21 | 1992-05-26 | Rohm And Haas Company | Insecticidal N' substituted-N-N'-disubstituted-hydrazines |
US5424333A (en) * | 1985-10-21 | 1995-06-13 | Rohm And Haas Company | Anthelmintic N'-substituted-N,N'-disubstitutedhydrazines |
US5354762A (en) | 1986-07-14 | 1994-10-11 | Rohm And Haas Company | Six-membered heterocyclic derivatives of N'-substituted N,N'-diacylhydrazines |
DK483586A (da) * | 1985-10-21 | 1987-04-22 | Rohm & Haas | Insecticide n'-substituerede-n,n'-diacylhydraziner |
US4985461A (en) * | 1985-10-21 | 1991-01-15 | Rohm And Haas Company | Insecticidal N'-substituted-N,N'-diacylhydrazines |
DE3683749D1 (de) * | 1985-12-09 | 1992-03-12 | American Cyanamid Co | Insektentoetende diacylhydrazinverbindungen. |
US4814349A (en) * | 1985-12-09 | 1989-03-21 | American Cyanamid Company | Insecticidal substituted and unsubstituted benzoic acid 1-alkyl, 2 alkyl and 2-cycloalkylhydrazides |
CA1338289C (en) | 1986-01-22 | 1996-04-30 | Raymond August Murphy | Insecticidal n'-substituted-n-alkylcarbonyl- n'-acylhydrazines |
CA1295618C (en) | 1986-02-28 | 1992-02-11 | Adam Chi-Tung Hsu | Insecticidal n'-substituted-n-acyl -n'-alkylcarbonylhydrazines |
JPH0820680B2 (ja) | 1986-03-04 | 1996-03-04 | ミノルタ株式会社 | 複写機の露光量制御方法 |
US4859609A (en) | 1986-04-30 | 1989-08-22 | Genentech, Inc. | Novel receptors for efficient determination of ligands and their antagonists or agonists |
US5225443A (en) * | 1986-05-01 | 1993-07-06 | Rohm And Haas Company | Insecticidal N'-substituted-N'-substituted N,N'-diacylhydrazines |
CA1281716C (en) | 1986-05-01 | 1991-03-19 | Raymond August Murphy | Insecticidal n-substituted-n'-substituted-n,n'- diacylhydrazines |
JPS62293150A (ja) | 1986-06-13 | 1987-12-19 | Amada Co Ltd | 同期整流回路 |
ES2037709T3 (es) | 1986-07-14 | 1996-07-16 | Rohm & Haas | Derivados heterociclicos de seis miembros de n,n'-diacilhidrazinas n'-sustituidas. |
US5071773A (en) | 1986-10-24 | 1991-12-10 | The Salk Institute For Biological Studies | Hormone receptor-related bioassays |
EP0286746B1 (en) | 1987-04-15 | 1991-02-27 | Rohm And Haas Company | Insecticidal n-(optionally substituted) - n'-substituted-n,n'-disubstituted- hydrazines |
US4906280A (en) * | 1987-10-14 | 1990-03-06 | Pennwalt Corporation | Tertiary butylhydrazides as plant growth regulators |
US4981784A (en) | 1987-12-02 | 1991-01-01 | The Salk Institute For Biological Studies | Retinoic acid receptor method |
US5171671A (en) | 1987-12-02 | 1992-12-15 | The Salk Institute For Biological Studies | Retinoic acid receptor composition |
US5429952A (en) | 1988-02-02 | 1995-07-04 | Biocode, Inc. | Marking of products to establish identity and source |
US5110986A (en) | 1988-04-26 | 1992-05-05 | Rohm And Haas Company | Synthesis of n-t-alkyl-1,2-diacylhydrazines |
US5010175A (en) | 1988-05-02 | 1991-04-23 | The Regents Of The University Of California | General method for producing and selecting peptides with specific properties |
SG50681A1 (en) | 1988-06-13 | 1998-07-20 | American Biogenetic Sciences | Method for the production of monoclonal antibodies utilizing a germfree animal |
MY107431A (en) | 1988-06-15 | 1995-12-30 | Rohm & Haas | Insecticidal n''''substituted-n-alkylcarbonyl-n''''-acylhydra zines and n''''substituted-n-acyl-n''''-alkylcarbonylhydrazines. |
AU637573B2 (en) | 1988-06-16 | 1993-06-03 | Dow Agrosciences Llc | Hydrazine derivatives for pharmaceutical use |
US4857550A (en) * | 1988-08-29 | 1989-08-15 | American Cyanamid Company | Novel insecticidal dibenzoyl-tert-butylcarbazonitrile compounds and method for the preparation thereof |
JPH02207066A (ja) | 1989-02-07 | 1990-08-16 | Ishihara Sangyo Kaisha Ltd | ヒドラジン系化合物、それらの製造方法及びそれらを含有する有害動物防除剤 |
US5354844A (en) | 1989-03-16 | 1994-10-11 | Boehringer Ingelheim International Gmbh | Protein-polycation conjugates |
US5693622A (en) | 1989-03-21 | 1997-12-02 | Vical Incorporated | Expression of exogenous polynucleotide sequences cardiac muscle of a mammal |
US5703055A (en) | 1989-03-21 | 1997-12-30 | Wisconsin Alumni Research Foundation | Generation of antibodies through lipid mediated DNA delivery |
US4950666A (en) * | 1989-03-30 | 1990-08-21 | Fmc Corporation | Difluoroalkane and difluoroalkenylalkane pesticides |
US4954655A (en) * | 1989-03-31 | 1990-09-04 | Rohm And Haas Company | Preparation of alkylhydrazines |
EP0395581A1 (de) | 1989-04-27 | 1990-10-31 | Ciba-Geigy Ag | N-Sulfenyl- und N-sulfinyl-N,N'-diacylhydrazide |
NZ228936A (en) | 1989-05-01 | 1992-04-28 | Rohm & Haas | Method for treating insect infestation in rice plants comprising applying diacylhydrazine derivatives |
JPH03141245A (ja) | 1989-10-24 | 1991-06-17 | Ishihara Sangyo Kaisha Ltd | ヒドラジン系化合物、それらの製造方法及びそれらを含有する有害動物防除剤 |
JPH03145447A (ja) | 1989-10-31 | 1991-06-20 | Nissan Chem Ind Ltd | ジベンゾイルヒドラジン化合物および殺虫剤 |
US5283173A (en) | 1990-01-24 | 1994-02-01 | The Research Foundation Of State University Of New York | System to detect protein-protein interactions |
CA2075182C (en) | 1990-02-09 | 2003-03-25 | David J. Mangelsdorf | Retinoid receptor compositions and methods |
CA2076386C (en) * | 1990-02-26 | 2003-04-22 | David S. Hogness | Identification and expression of insect steroid receptor dna sequence |
WO1991014695A1 (en) * | 1990-03-22 | 1991-10-03 | The Salk Institute For Biological Studies | Insect retinoid receptor compositions and methods |
US7119077B1 (en) | 1990-03-22 | 2006-10-10 | The Salk Institute For Biological Studies | Multimeric forms of members of the steroid/thyroid superfamily of receptors with the ultraspiracle receptor |
US5688691A (en) | 1990-03-22 | 1997-11-18 | The Salk Institute For Biological Studies | Insect retinoid-like receptor compositions and methods |
US5264618A (en) | 1990-04-19 | 1993-11-23 | Vical, Inc. | Cationic lipids for intracellular delivery of biologically active molecules |
CA2043775A1 (en) | 1990-06-14 | 1991-12-15 | Dat P. Le | Dibenzoylakylcyanohydrazines |
JP3068846B2 (ja) | 1990-08-01 | 2000-07-24 | 日本化薬株式会社 | 新規ヒドラジン誘導体およびそれを有効成分とする殺虫組成物 |
JP2885902B2 (ja) | 1990-08-01 | 1999-04-26 | 日本化薬株式会社 | N’―tert―ブチル―N―ハロゲノメチルスルフェニル―N,N’―ジベンゾイルヒドラジン誘導体およびそれを有効成分とする殺虫組成物 |
JPH0539252A (ja) | 1990-08-01 | 1993-02-19 | Nippon Kayaku Co Ltd | N,N’−ジベンゾイル−tert−ブチルヒドラジン誘導体およびそれを有効成分とする殺虫組成物 |
US5075471A (en) * | 1990-10-09 | 1991-12-24 | Rohm And Haas Company | Insecticidal ferrocenoyl acylhydrazines |
JP3087854B2 (ja) | 1991-01-09 | 2000-09-11 | 日本化薬株式会社 | 新規ヒドラジン誘導体及びそれを有効成分とする殺虫組成物 |
IL100643A (en) * | 1991-01-25 | 1996-10-31 | Nippon Kayaku Kk | History of hydrazine and pesticides containing these histories as an active ingredient |
EP0600028B1 (en) | 1991-08-23 | 2001-11-07 | The Salk Institute For Biological Studies | Use of selective ligands for treatment of disease states responsive to steroid or steroid-like hormones |
US5668175A (en) | 1991-08-23 | 1997-09-16 | The Salk Institute For Biological Studies | Use of selective ligands for treatment of disease states responsive to steroid or steroid-like retinoids |
ATE215601T1 (de) | 1991-09-17 | 2002-04-15 | Salk Inst For Biological Studi | Rezeptoren der steroid/thyroid superfamilie von rezeptoren |
JPH0539252U (ja) | 1991-10-31 | 1993-05-28 | 株式会社 神戸鋳鉄所 | 樹木保護構造体 |
CA2121800A1 (en) | 1991-12-06 | 1993-06-10 | Ronald M. Evans | Multimeric forms of members of the steroid/thyroid superfamily of receptors |
US6013836A (en) * | 1992-02-28 | 2000-01-11 | Rohm And Haas Company | Insecticidal N'-substituted-N,N'-disubstitutedhydrazines |
US5530028A (en) * | 1992-11-23 | 1996-06-25 | Rohm And Haas Company | Insecticidal N'-substituted-N,N'-diacylhydrazines |
US5344958A (en) | 1992-11-23 | 1994-09-06 | Rohm And Haas Company | Insecticidal N'-substituted-N,N'-diacylhydrazines |
JPH06172342A (ja) | 1992-12-07 | 1994-06-21 | Nippon Kayaku Co Ltd | 新規ヒドラジン誘導体およびそれを有効成分とする殺虫組成物 |
JP3298954B2 (ja) | 1992-12-16 | 2002-07-08 | 三共株式会社 | 新規n,n’−ジベンゾイルヒドラジン誘導体及び殺虫組成物 |
JPH06298755A (ja) * | 1993-04-20 | 1994-10-25 | Nippon Kayaku Co Ltd | 新規ヒドラジン誘導体およびそれを有効成分とする殺虫組成物 |
KR0149048B1 (ko) | 1993-05-21 | 1998-08-17 | 박성희 | 인체의 피질흉선세포에 표현되는 단백질 |
ATE232882T1 (de) | 1993-05-27 | 2003-03-15 | Selectide Corp | Topologisch getrennte kodierende festphasen- bibliotheken |
US5358966A (en) * | 1993-06-08 | 1994-10-25 | Rohm And Haas Company | Turfgrass insecticides |
ES2109613T3 (es) | 1993-08-19 | 1998-01-16 | Rohm & Haas | Preparacion de 1,2-diacil-2-(t-alquil)hidrazinas. |
FR2714830B1 (fr) | 1994-01-10 | 1996-03-22 | Rhone Poulenc Rorer Sa | Composition contenant des acides nucléiques, préparation et utilisations. |
FR2715847B1 (fr) | 1994-02-08 | 1996-04-12 | Rhone Poulenc Rorer Sa | Composition contenant des acides nucléiques, préparation et utilisations. |
US5482962A (en) * | 1994-07-22 | 1996-01-09 | Rohm And Haas Company | Insecticidal N,N'-disubstituted-N-N'-diacylhydrazines |
FR2727679B1 (fr) | 1994-12-05 | 1997-01-03 | Rhone Poulenc Rorer Sa | Nouveaux agents de transfection et leurs applications pharmaceutiques |
CA2210248A1 (en) | 1995-01-13 | 1996-07-18 | Ronald M. Evans | Allosteric control of nuclear hormone receptors |
FR2730637B1 (fr) | 1995-02-17 | 1997-03-28 | Rhone Poulenc Rorer Sa | Composition pharmaceutique contenant des acides nucleiques, et ses utilisations |
JP3600298B2 (ja) | 1995-02-27 | 2004-12-15 | 日本化薬株式会社 | 新規ヒドラジン誘導体およびそれを有効成分とする殺虫組成物 |
JPH08231529A (ja) | 1995-02-27 | 1996-09-10 | Nippon Kayaku Co Ltd | ヒドラジン誘導体およびそれを有効成分とする殺虫組成物 |
WO1996027673A1 (en) | 1995-03-03 | 1996-09-12 | Novartis Ag | Control of gene expression in plants by receptor mediated transactivation in the presence of a chemical ligand |
TR200003861T2 (tr) | 1995-05-26 | 2001-04-20 | Zeneca Limited | Bir ekdison reseptörünü içeren bir gen anahtarı. |
JPH09100262A (ja) | 1995-06-06 | 1997-04-15 | Rohm & Haas Co | N,N’−ジアシル−N’−t−アルキルヒドラジン化合物の製造方法 |
CA2200423C (en) | 1996-03-26 | 2006-12-19 | Sietse Mosselman | Novel estrogen receptor |
EP0910652B1 (en) | 1996-04-05 | 2014-10-08 | The Salk Institute For Biological Studies | Hormone-mediated methods for modulating expression of exogenous genes in mammalian systems, and products related thereto |
US6723531B2 (en) * | 1996-04-05 | 2004-04-20 | The Salk Institute For Biological Studies | Method for modulating expression of exogenous genes in mammalian systems, and products related thereto |
US6025483A (en) | 1996-06-05 | 2000-02-15 | The Regents Of The University Of California | Maize and cauliflower apetalai gene products and nucleic acid molecules encoding same |
US5919667A (en) | 1996-06-20 | 1999-07-06 | The Salk Institute For Biological Studies | Modular assembly retroviral vectors and uses thereof |
US5948406A (en) | 1996-08-12 | 1999-09-07 | Rohm And Haas Company | Immunogens, antibodies formed therefrom, and coating antigens useful in a diacylhydrazine immunoassay method |
CA2296093A1 (en) | 1997-07-10 | 1999-01-21 | The Salk Institute For Biological Studies | Modified lepidopteran receptors and hybrid multifunctional proteins for use in regulation of transgene expression |
US6300488B1 (en) * | 1997-07-10 | 2001-10-09 | The Salk Institute For Biological Studies | Modified lepidopteran receptors and hybrid multifunctional proteins for use in transcription and regulation of transgene expression |
DE19837620A1 (de) | 1997-08-22 | 1999-02-25 | Novartis Ag | Organische Verbindungen |
EP1017829A2 (en) | 1997-08-26 | 2000-07-12 | Ariad Gene Therapeutics, Inc. | Fusion proteins comprising a dimerization, trimerization or tetramerization domain and an additional heterologous transcription activation, transcription repression, dna binding or ligand binding domain |
US6756491B2 (en) | 1998-01-09 | 2004-06-29 | The Salk Institute For Biological Studies | Steroid-activated nuclear receptors and uses therefor |
AUPP135698A0 (en) | 1998-01-15 | 1998-02-05 | Commonwealth Scientific And Industrial Research Organisation | Insectical modalities |
US6333318B1 (en) * | 1998-05-14 | 2001-12-25 | The Salk Institute For Biological Studies | Formulations useful for modulating expression of exogenous genes in mammalian systems, and products related thereto |
US6258603B1 (en) * | 1998-06-17 | 2001-07-10 | Rohm And Haas Company | Ligands for modulating the expression of exogenous genes via an ecdysone receptor complex |
JP2000026423A (ja) | 1998-07-09 | 2000-01-25 | Otsuka Chem Co Ltd | イソニコチノイルヒドラジン誘導体及び該誘導体を有効成分として含有する害虫防除剤 |
DE19831710A1 (de) | 1998-07-15 | 2000-01-20 | Merck Patent Gmbh | Diacylhydrazinderivate |
EP0984009A1 (en) | 1998-08-25 | 2000-03-08 | Rohm And Haas Company | Benzodioxincarboxylic acid hydrazides as insecticides |
US6117639A (en) | 1998-08-31 | 2000-09-12 | Vertex Pharmaceuticals Incorporated | Fusion proteins, DNA molecules, vectors, and host cells useful for measuring protease activity |
US5989863A (en) | 1998-10-14 | 1999-11-23 | Incyte Pharmaceuticals, Inc. | Human ankyrin family protein |
CN1177813C (zh) | 1999-09-06 | 2004-12-01 | 华东理工大学 | 1,2-烷(芳)酰基芳酰基肼类昆虫生长调节剂及制备和应用 |
US7057015B1 (en) | 1999-10-20 | 2006-06-06 | The Salk Institute For Biological Studies | Hormone receptor functional dimers and methods of their use |
EP1214070A4 (en) * | 2000-02-18 | 2008-07-16 | Arch Dev Corp | COMPOUNDS WITH POLY-HYDROXYLATED BENZENE |
WO2001062780A1 (en) | 2000-02-24 | 2001-08-30 | The Salk Institute For Biological Studies | Gene expression system based on chimeric receptors |
CA2404253C (en) | 2000-03-22 | 2014-05-13 | Rohm And Haas Company | Novel ecdysone receptor-based inducible gene expression system |
US20040033600A1 (en) * | 2001-03-21 | 2004-02-19 | Palli Subba Reddy | Ecdysone receptor-based inducible gene expression system |
DE20012351U1 (de) | 2000-07-14 | 2001-11-15 | Siegenia Frank Kg | Fenster oder Tür mit Entlastungseinrichtung |
US8105825B2 (en) | 2000-10-03 | 2012-01-31 | Intrexon Corporation | Multiple inducible gene regulation system |
AU2002247644A1 (en) | 2001-02-16 | 2002-09-04 | Degussa Ag | Nucleotide sequences of the ribosomal protein s12 gene (rpsl) from corynebacterium glutamicum |
JP4955905B2 (ja) * | 2001-02-20 | 2012-06-20 | イントレキソン コーポレーション | キメラレチノイドx受容体および新規エクジソン受容体−ベースの誘導性遺伝子発現システムにおけるそれらの使用 |
US8715959B2 (en) * | 2001-02-20 | 2014-05-06 | Intrexon Corporation | Substitution mutant receptors and their use in a nuclear receptor-based inducible gene expression system |
US9249207B2 (en) | 2001-02-20 | 2016-02-02 | Intrexon Corporation | Substitution mutant receptors and their use in an ecdysone receptor-based inducible gene expression system |
US9493540B2 (en) | 2001-02-20 | 2016-11-15 | Intrexon Corporation | Ecdysone receptor/invertebrate retinoid X receptor-based inducible gene expression system |
CN1161325C (zh) | 2001-03-26 | 2004-08-11 | 江苏省农药研究所 | 作为杀虫剂的二酰基肼类化合物及制备此种化合物的中间体以及它们的制备方法 |
FR2827678B1 (fr) | 2001-07-23 | 2003-12-12 | Photonetics | Attenuateur optique multicanal pour signal multiplexe |
EP1436394A4 (en) * | 2001-09-26 | 2004-12-29 | Rheo Gene Holdings Inc | CICADA ECDYSON RECEPTOR NUCLEIC ACIDS, POLYPEPTIDES AND THEIR USE |
CA2459807C (en) * | 2001-09-26 | 2013-09-03 | Jianzhong Zhang | Whitefly ecdysone receptor nucleic acids, polypeptides, and uses thereof |
US20050228016A1 (en) | 2002-06-13 | 2005-10-13 | Enrique Michelotti | Tetrahydroquinolines for modulating the expression of exogenous genes via an ecdysone receptor complex |
US7375093B2 (en) | 2002-07-05 | 2008-05-20 | Intrexon Corporation | Ketone ligands for modulating the expression of exogenous genes via an ecdysone receptor complex |
US7304161B2 (en) | 2003-02-10 | 2007-12-04 | Intrexon Corporation | Diaclhydrazine ligands for modulating the expression of exogenous genes in mammalian systems via an ecdysone receptor complex |
US7304162B2 (en) | 2003-02-21 | 2007-12-04 | Intrexon Corporation | Oxadiazoline ligands for modulating the expression of exogenous genes via an ecdysone receptor complex |
US7456315B2 (en) | 2003-02-28 | 2008-11-25 | Intrexon Corporation | Bioavailable diacylhydrazine ligands for modulating the expression of exogenous genes via an ecdysone receptor complex |
DE10324799A1 (de) * | 2003-06-02 | 2004-12-23 | Bayer Cropscience Ag | Ligandenbindedomäne des Ecdyson-Rezeptors |
US7935510B2 (en) | 2004-04-30 | 2011-05-03 | Intrexon Corporation | Mutant receptors and their use in a nuclear receptor-based inducible gene expression system |
JP4412051B2 (ja) * | 2004-05-10 | 2010-02-10 | パナソニック株式会社 | 電子部品装着装置および電子部品装着方法 |
US9034650B2 (en) | 2005-02-02 | 2015-05-19 | Intrexon Corporation | Site-specific serine recombinases and methods of their use |
BRPI0811348B1 (pt) | 2007-05-29 | 2022-02-08 | Intrexon Corporation | Composto, (n-(1-ter-butil-butil)-n'-(2-etil-3-metóxi benzoil)-hidrazida de ácido (r)-3,5-dimetilbenzóico e composição farmacêutica |
JP5508625B2 (ja) | 2009-12-14 | 2014-06-04 | トヨタ自動車株式会社 | 車両の制御装置及び車両の制御方法 |
US9331524B1 (en) | 2010-07-03 | 2016-05-03 | Best Energy Reduction Technologies, Llc | Method, system and apparatus for monitoring and measuring power usage |
US9814215B2 (en) | 2014-03-11 | 2017-11-14 | Little Big Cat, Inc. | Pet toy with telescoping wand with metallic wire |
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