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公开(公告)号：US5047502A
公开(公告)日：1991-09-10
申请号：US389093
申请日：1989-08-03
IPC分类号： A61K38/00 , C07K14/575
CPC分类号： C07K14/57572 , A61K38/00
摘要： Small cell lung carcinoma cells (SCLC) contain gastrin releasing peptide (GRP) receptors. The response of the cells to GRP is rapid growth. We have found a group of heptapeptides that act as GRP antagonists by blocking the binding of GRP to its receptor thereby inhibiting the growth of cells that are sensitive to the growth promoting acitivity of GRP.
摘要翻译： 小细胞肺癌细胞（SCLC）含有胃泌素释放肽（GRP）受体。 细胞对GRP的反应是快速增长。 我们已经发现一组作为GRP拮抗剂的七肽通过阻断GRP与其受体的结合，从而抑制对促进GRP活性的生长敏感的细胞的生长。
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公开(公告)号：US5019647A
公开(公告)日：1991-05-28
申请号：US197872
申请日：1988-05-24
IPC分类号： A61K38/00 , C07K14/575
CPC分类号： C07K14/575 , A61K38/00
摘要： Small cell lung carcinoma cells (SCLC) contain gastrin releasing peptide (GRP) receptors. The response of the cells to GRP is rapid growth. We have found a group of peptide derivatives that act as GRP antagonists by blocking the binding of GRP to its receptor thereby inhibiting the growth of cells that are sensitive to the growth promoting activity of GRP.
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公开(公告)号：US06130204A
公开(公告)日：2000-10-10
申请号：US51342
申请日：1998-04-06
IPC分类号： C12Q1/37 , A61K38/00 , A61K45/00 , A61K47/48 , A61K49/00 , A61P13/02 , A61P15/00 , A61P35/00 , C07K5/10 , C07K5/107 , C07K7/06 , C07K7/08 , C07K14/47 , A61K38/07 , A61K38/08 , A61K38/48
CPC分类号： C07K14/47 , A61K47/48338 , C07K5/1016 , A61K38/00 , C07K2319/00 , Y10S930/28 , Y10S930/30
摘要： Oligopeptides which comprise amino acid sequences that are recognized and proteolytically cleaved by free prostate specific antigen (PSA) are described. Also described are assays which comprise such oligopeptides useful for determining free PSA protease activity in vitro and in vivo. Therapeutic agents which comprise conjugates of such oligopeptides and known cytotoxic agents are also described.
摘要翻译： PCT No.PCT / US96 / 15713 Sec。 371日期：1998年4月6日 102（e）1998年4月6日PCT PCT 1996年10月2日PCT公布。 出版物WO97 / 12624 日期：1997年4月10日描述了包含被游离前列腺特异性抗原（PSA）识别和蛋白水解切割的氨基酸序列的寡肽。 还描述了包含用于在体外和体内测定游离PSA蛋白酶活性的这种寡肽的测定法。 还描述了包含这种寡肽和已知细胞毒性剂的缀合物的治疗剂。
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公开(公告)号：US06177404B1
公开(公告)日：2001-01-23
申请号：US09051759
申请日：1998-08-03
申请人： Deborah DeFeo-Jones , Raymond E. Jones , Allen I. Oliff , Edward M. Scolnick , Victor M. Garsky
发明人： Deborah DeFeo-Jones , Raymond E. Jones , Allen I. Oliff , Edward M. Scolnick , Victor M. Garsky
IPC分类号： A61K3816
CPC分类号： A61K47/65
摘要： Novel pharmaceutical compositions useful for the treatment of benign prostatic hyperplasia which comprises novel oligopeptides, which are selectively cleaved by enzymatically active PSA, in conjugation with a cytotoxic agent are described. Methods of treating benign prostate hypertrophy are also disclosed.
摘要翻译： 描述了可用于治疗良性前列腺增生的新型药物组合物，其包含通过酶活性PSA选择性切割的与细胞毒性剂缀合的新型寡肽。 还公开了治疗良性前列腺肥大的方法。
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公开(公告)号：US6143864A
公开(公告)日：2000-11-07
申请号：US468161
申请日：1995-06-06
IPC分类号： G01N33/566 , A61K31/195 , A61K38/00 , A61K38/08 , A61K47/48 , A61P13/08 , A61P35/00 , A61P43/00 , C07H15/24 , C07K7/06 , C07K7/08 , C07K14/47 , C07K17/08 , C12Q1/37 , G01N33/574 , A61K38/14 , C07K9/00
CPC分类号： C07K14/47 , A61K47/48238 , A61K47/48338 , A61K38/00
摘要： Oligopeptides which comprise amino acid sequences that are recognized and proteolytically cleaved by free prostate specific antigen (PSA) are described. Also described are assays which comprise such oligopeptides useful for determining free PSA protease activity in vitro and in vivo. Therapeutic agents which comprise conjugates of such oligopeptides and known cytotoxic agents are also described.
摘要翻译： 描述了包含被游离前列腺特异性抗原（PSA）识别和蛋白水解切割的氨基酸序列的寡肽。 还描述了包含用于在体外和体内测定游离PSA蛋白酶活性的这种寡肽的测定法。 还描述了包含这种寡肽和已知细胞毒性剂的缀合物的治疗剂。
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公开(公告)号：US5866679A
公开(公告)日：1999-02-02
申请号：US540412
申请日：1995-10-06
IPC分类号： C12Q1/37 , A61K38/00 , A61K45/00 , A61K47/48 , A61K49/00 , A61P13/02 , A61P15/00 , A61P35/00 , C07K5/10 , C07K5/107 , C07K7/06 , C07K7/08 , C07K14/47 , C07K5/09
CPC分类号： C07K14/47 , A61K47/48338 , C07K5/1016 , A61K38/00 , C07K2319/00 , Y10S930/28 , Y10S930/30
摘要： Oligopeptides which comprise amino acid sequences that are recognized and proteolytically cleaved by free prostate specific antigen (PSA) are described. Also described are assays which comprise such oligopeptides useful for determining free PSA protease activity in vitro and in vivo. Therapeutic agents which comprise conjugates of such oligopeptides and known cytotoxic agents are also described.
摘要翻译： 描述了包含被游离前列腺特异性抗原（PSA）识别和蛋白水解切割的氨基酸序列的寡肽。 还描述了包含用于在体外和体内测定游离PSA蛋白酶活性的这种寡肽的测定法。 还描述了包含这种寡肽和已知细胞毒性剂的缀合物的治疗剂。
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公开(公告)号：US5690928A
公开(公告)日：1997-11-25
申请号：US224422
申请日：1994-04-11
IPC分类号： A61K38/00 , A61K47/48 , A61P35/00 , C07K1/22 , C07K1/30 , C07K14/00 , C07K14/195 , C07K14/21 , C07K14/41 , C07K14/415 , C07K14/495 , C07K14/52 , C07K19/00 , C12N5/10 , C12N15/09 , C12P21/02 , C12R1/19 , A61K38/45
CPC分类号： C07K14/495 , A61K47/48261 , A61K47/48269 , C07K14/21 , A61K38/00 , C07K2319/00
摘要： Methods and compositions for treating bladder cancer using TGF-alpha or EGF fused to PE.sub.40 or cysteine modified derivatives are taught. Also, a method of producing TGF-alpha-PE.sub.40 derivatives of enhanced potency is described.
摘要翻译： 教导了使用与PE40或半胱氨酸修饰的衍生物融合的TGF-α或EGF治疗膀胱癌的方法和组合物。 另外，描述了提高效能的TGF-α-PE40衍生物的生产方法。
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公开(公告)号：US06391305B1
公开(公告)日：2002-05-21
申请号：US09254892
申请日：1999-06-28
IPC分类号： A61K3814
CPC分类号： C07K7/06 , A61K38/00 , C07K5/1016
摘要： Chemical conjugates which comprise oligopeptides, having amino acid sequences that are selectively proteolytically cleaved by free prostate specific antigen (PSA), hydrophilic oligopeptide blocking groups and known cytotoxic agents are disclosed. Such conjugates are useful in the treatment of prostatic cancer and benign prostatic hypertrophy (BPH).
摘要翻译： 公开了包含具有由游离前列腺特异性抗原（PSA）选择性蛋白水解切割的氨基酸序列，亲水寡肽封闭基团和已知的细胞毒性剂的寡肽的化学共轭物。 这种缀合物可用于治疗前列腺癌和良性前列腺肥大（BPH）。
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公开(公告)号：US5599686A
公开(公告)日：1997-02-04
申请号：US267092
申请日：1994-06-28
CPC分类号： C07K14/47 , A61K47/48338 , A61K38/00
摘要： Assays which comprise oligopeptides and which are useful for determining free PSA protease activity in vitro and in vivo are described. Such oligopeptides comprise amino acid sequences that are recognized and proteolytically cleaved by free prostrate specific antigen (PSA). Also described are assays useful in identifying inhibitors of free PSA.
摘要翻译： 描述了包含寡肽并且其可用于在体外和体内测定游离PSA蛋白酶活性的测定。 这样的寡肽包括由游离的前列腺特异性抗原（PSA）识别和蛋白水解切割的氨基酸序列。 还描述了可用于鉴定游离PSA的抑制剂的测定法。
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公开(公告)号：US5473056A
公开(公告)日：1995-12-05
申请号：US136119
申请日：1993-10-13
CPC分类号： C07K14/4738 , A61K38/00 , C07K2319/00
摘要： The present invention is directed to a novel protein with E2F-like properties and the cDNA that encodes for that protein. The purified protein exhibits biological activity which is deemed important to medical science in the study of cell cycle regulation in general and the specific study of the Rb rumor suppressor protein and certain viral oncogenes. The protein may be employed in a complex with pRb or other cellular proteins to study inhibitors of biochemical transformations of those proteins, such as for example the phosphorylation of the pRb portion of the complex, therefore aiding in the study of potential pharmaceutical agents useful against certain oncoproteins encoded by DNA tumor viruses.
摘要翻译： 本发明涉及具有E2F样特性的新蛋白质和编码该蛋白质的cDNA。 纯化的蛋白质表现出生物活性，这在生物活性中被认为对于医学科学在一般的细胞周期调控的研究和Rb肿瘤抑制蛋白和某些病毒致癌基因的具体研究中是重要的。 蛋白质可以用于与pRb或其它细胞蛋白质的复合物中，以研究这些蛋白质的生物化学转化的抑制剂，例如复合物的pRb部分的磷酸化，因此有助于研究对某些有用的潜在药剂 由DNA肿瘤病毒编码的癌蛋白。
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