KR970703780A - 신규한 펩타이드(Novel Peptides) - Google Patents

신규한 펩타이드(Novel Peptides)

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KR970703780A
KR970703780A KR1019960707514A KR19960707514A KR970703780A KR 970703780 A KR970703780 A KR 970703780A KR 1019960707514 A KR1019960707514 A KR 1019960707514A KR 19960707514 A KR19960707514 A KR 19960707514A KR 970703780 A KR970703780 A KR 970703780A
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seq
ser
amide
oligopeptide
alaasnlysilesertyrgln
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데보라 데페오-존스
동-메이 펭
빅터 엠 가르스키
레이몬드 이 존스
알렌 아이 올리프
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위노커 멜빈
머크 앤드 캄파니, 인코포레이티드
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Abstract

본원에는 유리 전립선 특이 항원(PSA)에 의해 인식되고 단백질분해로 절단되는 아미노산 서열을 포함하는 올리고펩타이드가 기술되어 있다. 또한, 시험관내 및 생체내에서 유리 PSA프로타아제를 측정하는데 유용한 올리고펩타이드를 포함하는 검정물이 기술된다. 이러한 올리고펩타이드와 공지된 세포 독성제의 결합제를 포함하는 치료제가 기술되어 있다.

Description

신규한 펩타이드(Novel Peptides)
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (20)

  1. 유리 전립선 특히 항원에 의해 인식되고 선택적인 단백질분해로 절단되는 아미노산 서열을 포함하는 올리고펩타이드.
  2. 제1항에 있어서, 아미노산 서열이
    a)AsnLysIleSerTyrGln│Ser (서열13),
    b)LysIleSerTyrGln│Ser (서열14),
    c)GlnGluAsnGlyValGlnLysAspValSerGlnXaaSerIleTyr│SerGlnThrGlu (서열15),
    d)GlyLysGlyIleSerSerGlnTyr│SerAsnThrGluGluArgLeu (서열2),
    e)AsnLysIleSerTyrTyr│Ser (서열127),
    f)AsnLysAlaSerTyrGln│Ser (서열128),
    g)SerTyrGln│SerSer(서열129)
    h)LysTyrGln│SerSer(서열 140); 또는
    i)hArgTyrGln│SerSer(서열141)(상기 서열식에서, hArg는 호모아르기닌이고, Xaa는 임의의 천연아미노산이다)인 올리고펩타이드.
  3. 제2항에 있어서, 아미노산 서열이
    a)AsnLysIleSerTyrGln│SerSer (서열16),
    b)AsnLysIleSerTyrGln│SerAla (서열130),
    c)AsnLysIleSerTyrGln│SerSerSer (서열17),
    d)AlaAsnLysIleSerTyrGln│SerSerSer (서열18),
    e)LysIleSerTyrGln│SerSerSerThrGlu (서열19),
    f)GlyGluAsnGlyValGlnLysAspValSerGlnArgSerIleTyr│SerGlnThrGlu (서열4),
    g)GlyGluAsnGlyValGlnLysAspValSerGlnArgSerIleTyr│SerGlnThrGlu (서열5),
    h)AlaAsnLysIleSerTyrTyr│Ser (서열131),
    i)AlaAsnLysAlaSerTyrGln│Ser (서열132),
    j)SerTyrGln│SerSerThr (서열133),
    k)SerTyrGln│SerSerSer (서열134),
    l)LysTyrGln│SerSerSer (서열142),
    m)hArgTyrGln│SerSerSer (서열143)또는
    n)SerTyrGln│SerSerLeu (서열135)인 올리고펩타이드.
  4. 제2항에 있어서, 아미노산 서열이
    a)AsnLysIleSerTyrGln│SerSerSerThr (서열10),
    b)AlaAsnLysIleSerTyrGln│SerAla (서열136),
    c)AsnLysIleSerTyrGln│SerSerSerThrGlu (서열3),
    d)AlaAsnLysIleSerTyrGln│SerSerSerThrGlu (서열11),
    e)GlyGluAsnGlyValGlnLysAspValSerGlnArgSerIleTyr│SerGlnThrGlu (서열4),
    f)AlaAsnLysIleSerTyrTyr│SerSer (서열137),
    g)AlaAsnLysIleSerTyrTyr│SerAla (서열138),
    h)AlaAsnLysAlaSerTyrGln│SerAla (서열139),
    i)AlaSerTyrGln│SerSerLeu (서열94)인 올리고펩타이드.
  5. 제2항에 있어서, 아미노산 서열이
    a)GlyArgLysAlaAsnLysIleSerTyrGln│SerSerSerThrGluGluArgArgLeuHisTyrGlyGluAsnGly( 서열6)인 올리고펩타이드.
  6. 제1항에 있어서,
    AsnArgIleSerTyrGln│Ser (서열21),
    AsnLysValSerTyrGln│Ser (서열22),
    AsnLysMetSerTyrGln│SerSer (서열23),
    AsnLysLeuSerTyrGln│SerSer (서열24),
    AsnLysIleSerTyrGln│SerSerSer (서열25),
    AsnLysIleSerPheGln│SerSerSer (서열26),
    AsnLysIleSerTrpGln│SerSerSerThr (서열27),
    AsnLysIleSerTyrAsn│SerSerSerThr (서열28),
    AsnLysIleSerTyrGln│ThrSerSer (서열29),
    AsnLysIleSerTyrGln│Ser (서열30),
    GlnLysIleSerTyrGln│SerSer (서열31),
    AsnArgIleThrGln│SerSerSer (서열32),
    AsnArgIleSerPheGln│SerSerSerThr (서열33),
    AsnArgIleSerTrpGln│SerSerSerThr (서열35),
    AsnArgIleSerTrpGln│ThrSerSerThr (서열36),
    AsnLysIleThrTyrGln│ThrSerSerThr (서열37),
    AsnLysLeuSerTyrGln│ThrSerSerThr (서열38),
    GlnLysLeuSerTyrGln│SerSerSerThr (서열39),
    AsnArgLeuSerTyrGln│ThrSerSerThr (서열40),
    AsnLysValSerPheGln│SerSerSerThr (서열41),
    AsnArgValSerTrpGln│SerSerSerThr (서열42),
    GlnLysValSerTyrGln│SerSerSerThr (서열43),
    GlnLysIleSerTyrGln│ThrSerSerThr (서열34),
    또는 AsnLysIleThrTyrGln│SerSerSerThr (서열44),중에서 선택되는 올리고펩타이드.
  7. 제1항에 있어서, AlaAsnLysIleSerTyrGln│SerSerSerThrGlu-아미드(서열11),
    Ac-AlaAsnLysIleSerTyrGln│SerSerSerThrLeu (서열70),
    Ac-AlaAsnLysIleSerTyrGln│SerSerSerThrGlu-아미드 (서열11),
    Ac-AlaAsnLysIleSerTyrGln│SerSerSerThrLeu-아미드 (서열70),
    Ac-AlaAsnLysIleSerTyrGln│SerAlaSerThrGlu-아미드 (서열73),
    Ac-AlaAsnLysIleSerTyrGln│SerSerLysThrGlu-아미드 (서열74),
    Ac-AlaAsnLysIleSerTyrGln│SerSerThrGlu-아미드 (서열75),
    Ac-AlaAsnLysIleSerTyrGln│SerSerGluThrGlu-아미드 (서열78),
    Ac-AlaAsnLysIleSerTyrGln│SerAlaLysThrGlu-아미드 (서열79),
    Ac-AlaAsnLysIleSerTyrGln│SerThrGlu-아미드 (서열81),
    Ac-AlaAsnLysSerTyrGln│SerSerThrGlu-아미드 (서열82),
    Ac-AlaAsnLysAlaSerTyrGln│SerAlaSerThrGlu-아미드 (서열84),
    Ac-AlaAsnGluIleSerTyrGln│SerAlaSerThrGlu-아미드 (서열85),
    Ac-AlaLysIleSerTyrGln│SerSer-아미드 (서열16),
    Ac-LysIleSerTyrGln│SerSer-아미드 (서열86),
    Ac-SerTyrGln│SerSerThrGlu-아미드 (서열87),
    Ac-AlaSerTyrGln│SerSerThrGlu-아미드 (서열89),
    Ac-AlaAsnLysIleSerTyrTyr│SerSerSerThrGlu-아미드 (서열92),
    Ac-AlaAsnLysIleSerTyrTyr│SerAlaSerThrGlu-아미드 (서열93),
    Ac-AlaSerTyrGln│SerSerLeu--아미드 (서열94),
    Ac-AlaAsnSerTyrGln│SerSerSerThrGlu-아미드 (서열95),
    Ac-AlaSerTyrGln│SerSerSerThrGlu-아미드 (서열96),
    Ac-SerTyrGln│SerSerSerThrGlu-아미드 (서열97)또는
    Ac-AlaAsnLysAlaSerTyrGln│SerAlaSerCys--아미드 (서열98)인 올리고펩타이드.
  8. (a)유리 전립선 특이 항원에 의해 인식되고 선택적인 단백질분해로 절단되는 아미노산 서열을 포함하는 올리고펩타이드인 기질을 샘플과 반응시키는 단계 및 (b)기질이 절단되었는지를 검출하는 단계를 포함하여, 샘플에서 유리 전립선 특이 항원의 단백질분해 활성을 검출하기 위한 검정 방법.
  9. 제8항에 있어서, 기질이 절단되었는지를 측정하는 단계가 고성능 액체 크로마토그래피로 검정 혼합물을 분석하는 단계를 포함하는 검정 방법.
  10. (a)유리 전립선 특이 항원에 의해 인식되고 선택적인 단백질분해로 절단되는 아미노산 서열을 포함하는 기질을 유리 전립선 특히 항원과 시험 물질의 존재하에 반응시키는 단계 및 (b)전립선 특이 항원의 단백질분해 활성을 억제하는 시험물질의 능력이 시험 물질의 부재하에서의 기질의 절단과 비교하여 기질 절단의 감소로 나타남으로써 기질이 절단되었는지를 검출하는 단계를 포함하여, 전립선 특이 항원의 단백질분해 활성을 억제하는 화합물을 동정하는 검정 방법.
  11. 제10항에 있어서, 기질이 절단되었는지를 검출하는 단계가 고성능 액체 크로마토그래피로 검정 혼합물을 분석하는 단계를 포함하는 검정 방법.
  12. 유리 전립선 특이 항원에 의해 인식되고 선택적인 단백질분해로 절단되는 아미노산 서열을 포함하는 올리고펩타이드에 공유결합 또는 화학적 링커에 의해 부착된 세포독성제를 포함하는, 전립선암의 치료에 유용한 결합체.
  13. 제12항에 있어서, 세포독성제가 a)안트라사이클린계 약물,b)빈카 알칼로이드 약물, c)미토마이신, d)블레오마이신, e)세포 독성 뉴클레오사이드, f)프테리딘계 약물, g)디이넨, h)에스트라무스틴, i)사이클로포스프아미드 및 j)포도필로톡신 부류 중에서 선택되는 세포독성계 부류중 일원인 결합체.
  14. 제12항에 있어서, 세포독성제가 a)독소루비신, b)카미노마이신 c)다우노루비신, d)아미노프테린, e)메토트렉세이트,f)메토프테린, g)디클로로-메토트렉세이트, h)미토마이신 C, i)포피로마이신, j)5-플루오르 우라실, k)6-머캅토푸린, l)시토신 아라비노사이드, m)포도필로톡신, n)에토포사이드,o)에토포사이드 포스페이트, p)멜팔란, q)빈블라스틴, r)빈크리스틴, s)류로시딘, t)빈데신, u)에스트라무스틴, v)시스플라틴, w)사이클로포스프아미드 및 x)류로신중에서 선택되는 결합체.
  15. 제12항에 있어서, 세포독성제가 독소루비신 및 빈블라스틴 또는 이의 세포독성유도체중에서 선택되는 결합체.
  16. 제12항에 있어서, 세포독성제가 독소루비신 또는 이의 세포 독성유도체인 결합체.
  17. 제16항에 있어서, 화학식 I인 결합식.
    상기식에서, 올리고펩타이드는 유리 전립선 특이 항원(PSA)에 의해 특이적으로 인식되고 유리 전립선 특이 항원의 효소 활성에 의해 단백질분해로 절단될 수 있는 올리고펩타이드이고, XL은 부재하거나, a)페닐알라닌,b)루이신,c)발린, d)이소루이신,e)(2-나프틸)알라닌,f)사이클로헥실알리닌, g)디페닐알라닌, h)노르바린 및 j)노르루이신중에서 선택되는 아미노산이며, R은 수소 또는-(C=O)R1이고,R1은 C1-C6-알킬 또는 아릴이다.
  18. 제17항에 있어서, 올리고펩타이드가 a)AsnLysIleSerTyrGln│Ser (서열13), b)LysIleSerTyrGln│Ser (서열14), c)GlyGluAsnValGlnLysAspValSerGlnXaaSerIleTyr│SerGlnThrGlu (서열15),d)GlyLysGlyIleSerSerGlnTyr│SerAsnThrGluGluArgLeu (서열2),e)AsnLysIleSerTyrTyr│Ser (서열127),f)AsnLysAlaSerTyrGln│Ser (서열128) g)SerTyrGln│SerSer(서열129) 및 h)hArgTyrGln│SerSer(서열141)(여기서, hArg는 호모아르기닌이고, Xaa는 임의의 천연아미노산이다)중에서 선택되는 아미노산 서열을 포함하는 올리고머이고, XL는 부재하거나, a)루이신, b)이소루이신 및, d)발린중에서 선택되는 아미노산이며, R이 아세틸, 피발로일 또는 벤조일인 결합체.
  19. 제16항에 있어서, X가
    중에서 선택되는 결합체.
  20. 제15항에 있어서, 화학식 Ⅱ인 결합체.
    상기 식에서, 올리고펩타이드는 유리 전립선 특이 항원(PSA)에 의해 특이적으로 인식되고 유리 전립선 특이 항원의 효소 활성에 의해 단백질분해로 절단될 수 있는 올리고펩타이드이다.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
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