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公开(公告)号：US06908617B1
公开(公告)日：2005-06-21
申请号：US09446799
申请日：1998-11-10
CPC分类号： C07K14/005 , C07K2319/21 , C07K2319/50 , C12N2740/16122
摘要： A modified polypeptide corresponding to an envelope glycoprotein of a primate lentivirus is described. The polypeptide has been modified from the wild-type structure so that it has at least two of the glycosylation sites proximal to the CD4 binding site or chemokine receptor site altered so that the alteration prevents glycosylation at that site or where glycosylation sites distal to these sites have been derivatized with a molecular adjuvant, while retaining the overall 3-dimensional structure of a discontinuous conserved epitope of the wild-type protein. Preferably, the polypeptide has both changes. Preferably, the primate lentivirus is HIV, and the protein is HIV-1 gp 120.
摘要翻译： 描述了与灵长类慢病毒的包膜糖蛋白相应的修饰的多肽。 已经从野生型结构修饰了多肽，使得其具有至少两个接近CD4结合位点或趋化因子受体位点的糖基化位点被改变，使得该改变防止在该位点处的糖基化，或者在这些位点远侧的糖基化位点 已经用分子佐剂衍生化，同时保留野生型蛋白质的不连续保守表位的整体3维结构。 优选地，多肽具有两个改变。 优选地，灵长类动物慢病毒是HIV，蛋白质是HIV-1gp120。
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公开(公告)号：US07048929B1
公开(公告)日：2006-05-23
申请号：US09446820
申请日：1998-11-10
IPC分类号： A61K39/21
CPC分类号： C07K14/005 , C07K2319/00 , C12N2740/16122 , C12N2740/16134
摘要： A modified polypeptide corresponding to an envelope glycoprotein of a primate lentivirus is described. The polypeptide has been modified from the wild-type structure so that it has cysteine amino acid residues introduced to create disulfide bonds, a cavity is filled with hydrophobic amino acids, a Proresidue is introduced at a defined turn structure of the protein, or the hydrophobicity is increased across the interface between different domains, while retaining the overall 3-dimensional structure of a discontinuous conserved epitope of the wild-type protein. Preferably, the polypeptide has more than one of those characteristics. Preferably, the primate lentivirus is HIV, and the protein is HIV-1 gp120.
摘要翻译： 描述了与灵长类慢病毒的包膜糖蛋白相应的修饰的多肽。 已经从野生型结构修饰了多肽，使得其具有引入的半胱氨酸氨基酸残基以产生二硫键，空洞填充疏水性氨基酸，在定义的蛋白质结构引入前体，或疏水性 在不同结构域之间的界面上增加，同时保留野生型蛋白质的不连续保守表位的整体3维结构。 优选地，多肽具有多于一种特征。 优选地，灵长类动物慢病毒是HIV，蛋白质是HIV-1 gp120。
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公开(公告)号：US09776963B2
公开(公告)日：2017-10-03
申请号：US13128549
申请日：2009-11-10
申请人： Joseph G. Sodroski , Navid Madani , Arne Schön , Judith M. LaLonde , Joel R. Courter , Takahiro Soeta , Danny Ng , Ernesto Freire , Amos B. Smith, III , Amy M. Princiotto , Matthew Le-Khac , Wayne A. Hendrickson
发明人： Joseph G. Sodroski , Navid Madani , Arne Schön , Judith M. LaLonde , Joel R. Courter , Takahiro Soeta , Danny Ng , Ernesto Freire , Amos B. Smith, III , Amy M. Princiotto , Matthew Le-Khac , Wayne A. Hendrickson
IPC分类号： A61K31/397 , C07D211/58 , C07D205/04 , C07D207/09 , C07D207/16 , C07D207/22 , C07D211/26 , C07D211/44 , C07D211/56 , C07D217/14 , C07D223/04 , C07D231/56 , C07D233/64 , C07D235/02 , C07D235/14 , C07D237/32 , C07D239/42 , C07D239/47 , C07D239/90 , C07D249/08 , C07D265/36 , C07D295/13 , C07D307/52 , C07D317/28 , C07D333/20 , C07D333/48 , C07D401/04 , C07D401/06 , C07D405/06 , C07D409/14 , C07D455/02 , C07D471/08 , C07D473/18 , C07D487/04 , C07D495/04
CPC分类号： C07D211/58 , C07D205/04 , C07D207/09 , C07D207/16 , C07D207/22 , C07D211/26 , C07D211/44 , C07D211/56 , C07D217/14 , C07D223/04 , C07D231/56 , C07D233/64 , C07D235/02 , C07D235/14 , C07D237/32 , C07D239/42 , C07D239/47 , C07D239/90 , C07D249/08 , C07D265/36 , C07D295/13 , C07D307/52 , C07D317/28 , C07D333/20 , C07D333/48 , C07D401/04 , C07D401/06 , C07D405/06 , C07D409/14 , C07D455/02 , C07D471/08 , C07D473/18 , C07D487/04 , C07D495/04
摘要： The invention provides for compounds of formula I: wherein Z is absent or (CRARB)nW; each RA and RB is independently (i) H, alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, aralkyl, heteroaralkyl, haloalkyl, each of which may be optionally substituted; (ii) OH, ORc, NH2, NHRc, NRcRc, SH, S(O)mRc; or (iii) RA and RB together form C(O); W is absent, C(O), C(O)O, C(O)NRcRc, O, S(O)m, or NRcRc; Y is an optionally substituted heterocyclic, optionally substituted heteroaryl, optionally substituted cycloalkyl, optionally substituted aryl, or NRXRY; wherein Rx and Ry are each independently H, alkyl or aryl; X1 is selected from the group consisting of halogen, methyl, and hydroxyl; X2 is a halogen; each Rc is independently alkyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, aralkyl, or heteroaralkyl, each of which may be optionally substituted; m is O, 1, or 2; and n is 1, 2, 3, 4, 5, or 6; and pharmaceutically acceptable salts thereof.
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4.发明授权Non-naturally occurring targeted lipolytic compounds and related compositions and methods 失效非天然存在的靶向脂肪分解化合物及相关组合物和方法公开(公告)号：US06399355B1
公开(公告)日：2002-06-04
申请号：US08483228
申请日：1995-06-07
IPC分类号： C12N706
CPC分类号： C12N9/16 , A61K47/68 , A61K47/6815 , A61K47/6889 , C07K14/70514 , C07K19/00 , C07K2319/00
摘要： This invention provides a non-naturally occurring targeted lipolytic compound comprising a lipolytic agent linked to a targeting agent. In an embodiment, the lipolytic agent is covalently attached to the targeting agent. In an embodiment, the lipolytic agent is a phospholipase and the targeting agent is a viral receptor. This invention further provides for therapeutic uses of the non-naturally occurring targeted lipolytic compound. In an embodiment, the non-naturally occurring targeted lipolytic compound neutralizes virions of the human immunodeficiency virus (HIV).
摘要翻译： 本发明提供一种非天然存在的靶向脂肪分解化合物，其包含与靶向剂连接的脂肪分解剂。 在一个实施方案中，所述脂肪分解剂共价连接到所述靶向剂上。 在一个实施方案中，脂肪分解剂是磷脂酶，靶向剂是病毒受体。 本发明进一步提供非天然存在的目标脂肪分解化合物的治疗用途。 在一个实施方案中，非天然存在的靶向脂肪分解化合物中和人免疫缺陷病毒（HIV）的病毒粒子。
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5.发明授权公开(公告)号：US06904369B1
公开(公告)日：2005-06-07
申请号：US09609027
申请日：2000-06-29
CPC分类号： C07K14/005 , A61K38/00 , C07H21/04 , C07K1/1077 , C12N2760/16022 , G06F19/16
摘要： This invention provides a computer based method for preparing a stem cell factor (SCF) analog comprising the steps of: (a) providing computer expression of the three dimensional structure of an SCF molecule using its crystal structure; (b) selecting from the computer expression of step (a) at least one site on the SCF molecule for alteration; (c) preparing a SCF molecule having an alteration at said at least one selected site; and (d) optionally, testing the SCF molecule for a desired characteristic. This invention also provides SCF analogs and SCF ligand analogs prepared according to the above-described method. Compositions comprising SCF analogs or SCF ligand analogs prepared according to the above-described method effective to treat a subject and a pharmaceutically acceptable carrier are provided, as are methods of treating a subject comprising administration of pharmaceutical compositions comprising the prepared SCF analogs and SCF ligand analogs prepared by the described methods. This invention also provides methods for designing compounds capable of binding to the SCF receptor site and compounds designed by the above-described methods.
摘要翻译： 本发明提供了一种用于制备干细胞因子（SCF）类似物的基于计算机的方法，包括以下步骤：（a）使用其晶体结构提供SCF分子的三维结构的计算机表达; （b）选自步骤（a）的计算机表达，SCF分子上的至少一个位点用于改变; （c）制备在所述至少一个所选位点具有改变的SCF分子; 和（d）任选地，测试SCF分子的期望特性。 本发明还提供了根据上述方法制备的SCF类似物和SCF配体类似物。 提供了包含根据有效治疗受试者和药学上可接受的载体的上述方法制备的SCF类似物或SCF配体类似物的组合物，治疗受试者的方法包括施用包含制备的SCF类似物和SCF配体类似物的药物组合物 通过描述的方法准备。 本发明还提供了设计能够结合SCF受体位点的化合物和通过上述方法设计的化合物的方法。
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公开(公告)号：US20090247734A1
公开(公告)日：2009-10-01
申请号：US12086675
申请日：2006-12-14
申请人： Wayne A. Hendrickson , Hui Xie , Amos B. Smith , Danny Ng
发明人： Wayne A. Hendrickson , Hui Xie , Amos B. Smith , Danny Ng
CPC分类号： C07K14/70514
摘要： This invention provides two soluble polypeptides which comprise a portion of CD4 comprising all HIV gp120-binding epitopes present on intact CD4, wherein the polypeptide has a cysteine substitution at a residue which, in intact CD4, interfaces with HIV gp120. This invention also provides a method for making a derivatized soluble polypeptide and a method for obtaining a structural model useful in the design of an agent for inhibiting CD4 binding to HIV gp120.
摘要翻译： 本发明提供两种可溶性多肽，其包含一部分CD4，其包含存在于完整CD4上的所有HIV gp120结合表位，其中该多肽在完整的CD4与HIV gp120接合的残基处具有半胱氨酸置换。 本发明还提供了制备衍生化的可溶性多肽的方法和获得用于设计抑制CD4结合HIV gp120的药物的结构模型的方法。
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