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公开(公告)号：US4943561A
公开(公告)日：1990-07-24
申请号：US276985
申请日：1988-11-28
CPC分类号： C07K14/57572 , A61K38/00
摘要： Small cell lung carcinoma (SCLC) cells 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：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：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：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：US6103487A
公开(公告)日：2000-08-15
申请号：US140557
申请日：1998-08-26
IPC分类号： A61K31/00 , A61K31/4174 , A61K31/4178 , A61K31/4439 , A61K31/454 , A61K31/495 , A61K31/496 , A61K31/5513 , A61K38/00 , A61K38/05 , C12Q1/48
CPC分类号： C12Q1/48 , A61K31/00 , A61K31/4174 , A61K31/4178 , A61K31/4439 , A61K31/454 , A61K31/495 , A61K31/496 , A61K31/5513 , A61K38/005 , A61K38/05 , G01N2407/00 , G01N2500/00 , Y10S436/815 , Y10T436/15 , Y10T436/153333 , Y10T436/156666 , Y10T436/16
摘要： The instant invention provides for a method of inhibiting prenyl-protein transferases and treating cancer which comprises administering to a mammal a prenyl-protein transferase inhibitor which is efficacious in vivo as an inhibitor of geranylgeranyl-protein transferase type I (GGTase-I). The invention also provides for a method of inhibiting farnesyl-protein transferase and geranylgeranyl-protein transferase type I by administering a compound that is a dual inhibitor of both of those prenyl-protein transferases. The invention also provides for a method of identifying such a compound, the method comprising a modified inhibitory assay that incorporates a modulator anion that alters the in vitro potency of prenyl-protein transferase inhibitors in a way that predicts their potency in vivo, thus providing convenient identification of compounds that possess such in vivo activity.
摘要翻译： 本发明提供一种抑制异戊烯基 - 蛋白转移酶和治疗癌症的方法，其包括对哺乳动物施用作为er牛儿基anyl anyl anyl蛋白转移酶I型（GGTase-I）抑制剂的体内有效的异戊烯基 - 蛋白转移酶抑制剂。 本发明还提供了通过施用作为这些异戊烯基 - 蛋白质转移酶两者的双重抑制剂的化合物来抑制法呢基蛋白转移酶和er牛儿基ger牛蛋白转移酶I型的方法。 本发明还提供鉴定这种化合物的方法，所述方法包括修饰的抑制性测定法，其包含改变异戊烯基 - 蛋白质转移酶抑制剂的体外效力的调节剂阴离子，以预测其体内效力的方式，从而提供方便 鉴定具有这种体内活性的化合物。
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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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