公开(公告)号：US5484889A

公开(公告)日：1996-01-16

申请号：US277283

申请日：1994-07-21

申请人： Sylvia Lee-Huang ,  Philip L. Huang ,  Peter L. Nara ,  Hao-Chia Chen ,  Hsiang-fu Kung ,  Peter Huang ,  Henry I. Huang ,  Paul L. Huang

发明人： Sylvia Lee-Huang ,  Philip L. Huang ,  Peter L. Nara ,  Hao-Chia Chen ,  Hsiang-fu Kung ,  Peter Huang ,  Henry I. Huang ,  Paul L. Huang

IPC分类号： A61K36/42 ,  A61K38/00 ,  A61P31/12 ,  A61P35/00 ,  C07K1/00 ,  C07K14/415 ,  C12N1/19 ,  C12N1/21 ,  C12N5/10 ,  C12N15/09 ,  C12N15/29 ,  C12P21/02 ,  C12R1/91

CPC分类号： C07K14/415 ,  A61K38/00

摘要： A protein, in particular MAP 30, obtainable from both the fruit and seeds of Momordica charantia or produced by recombinant means useful for treating tumors and HIV infections is disclosed. In treating HIV infections, the protein is administered alone or in conjunction with conventional AIDS therapies. Also provided are processes for purifying the protein, DNA sequences encoding the protein, and recombinant DNA methods for expressing the protein.

摘要翻译： 公开了可从苦瓜属的水果和种子中获得的蛋白质，特别是MAP 30，或通过用于治疗肿瘤和HIV感染的重组手段产生的蛋白质。 在治疗艾滋病毒感染时，该蛋白质单独或与常规艾滋病治疗联合施用。 还提供了纯化蛋白质的方法，编码蛋白质的DNA序列和用于表达蛋白质的重组DNA方法。

公开(公告)号：US5221732A

公开(公告)日：1993-06-22

申请号：US280363

申请日：1988-12-06

申请人： Hao-Chia Chen ,  Judith H. Brown ,  John L. Morell ,  Charng-Ming Huang

发明人： Hao-Chia Chen ,  Judith H. Brown ,  John L. Morell ,  Charng-Ming Huang

IPC分类号： A61K38/00 ,  C07K14/46

CPC分类号： C07K14/46 ,  A61K38/00

摘要： Peptides which exhibit improved broad spectrum antimicrobial activity are designed and synthesized based on the peptide sequences of magainin or PGS peptides. The modified peptide analogues are synthesized by replacing low helical potential amino acid residues with high helical potential residues and modifying the two termini in order to enhance the amphiphilic structures as well as to prolong antimicrobial activity by lowering their susceptibility to protease degradation. For example, low propensity residues within a strategic region of magainin II, e.g. Ser.sup.8, Gly.sup.13 and Gly.sup.18 are modified with Ala which is known to have high propensity. Amidation of Ser.sup.23, and acylation of Gly.sup.1 with acetyl or beta-alanyl and substitution of Gly.sup.1 with beta-alanine are carried out in order to lower the susceptibility to exopeptidase action. A D-Ala modification for disrupting a stretch of the helical structure is also prepared so as to demonstrate the importance of an amphiphilic helical structure for antimicrobial activity. The modified peptide analogues exhibit an increase of up to two orders of magnitude in antimicrobial activity and, in the most favorable case, no appreciable increase in hemolytic activity over magainin 1.

摘要翻译： 基于magainin或PGS肽的肽序列设计并合成显示出改善的广谱抗微生物活性的肽。 通过用高螺旋电位残基替代低螺旋电位氨基酸残基并修饰两个末端来合成修饰的肽类似物，以增强两亲性结构以及通过降低其对蛋白酶降解的易感性来延长抗微生物活性。 例如，在magainin II的战略区域内的低倾向残基，例如， Ser8，Gly13和Gly18用已知具有高倾向的Ala修饰。 进行Ser23的酰胺化和Gly1与乙酰基或β-丙氨酰的酰化以及用β-丙氨酸取代Gly1以降低对外肽酶作用的易感性。 还制备用于破坏螺旋结构的拉伸的D-Ala修饰，以证明两亲性螺旋结构对于抗微生物活性的重要性。 修饰的肽类似物在抗菌活性中表现出高达两个数量级的增加，并且在最有利的情况下，相对于magainin 1，溶血活性没有明显增加。

公开(公告)号：US4468383A

公开(公告)日：1984-08-28

申请号：US427857

申请日：1982-09-29

申请人： David Rodbard ,  Y. Shimohigashi ,  Hao-Chia Chen ,  Tommaso Costa

发明人： David Rodbard ,  Y. Shimohigashi ,  Hao-Chia Chen ,  Tommaso Costa

IPC分类号： A61K38/00 ,  C07K14/70 ,  A61K37/00 ,  C07C103/52

CPC分类号： C07K14/702 ,  A61K38/00

摘要： The compounds of the invention are symmetrical dimers of enkephalin polypeptides comprising enkephalin polypeptide monomers linked at the C-termini thereof with a difunctional amino bridging group. The compounds are useful as investigative tools for probing the opiate receptor membranes, particularly as radiolabelled ligands for exploring the delta opiate receptor, and also have particular use as narcotic and/or analgesic agents.

摘要翻译： 本发明的化合物是脑啡肽多肽的对称二聚体，其包含在其C-末端与双官能氨基桥连基团连接的脑啡肽多肽单体。 这些化合物可用作探测阿片剂受体膜的研究工具，特别是用作探索δ阿片剂受体的放射性标记的配体，并且还可用作麻醉剂和/或止痛剂。