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1. 发明授权

US07365221B2 Monoacylated betulin and dihydrobetulin derivatives, preparation thereof and use thereof 失效
标题翻译：单酰化桦木醇和二氢甜菜蛋白衍生物，其制备及其用途
公开(公告)号：US07365221B2
公开(公告)日：2008-04-29
申请号：US10870555
申请日：2004-06-18
申请人： Graham P. Allaway , Carl T. Wild , Yoshiki Kashiwada , Kuo-Hsiung Lee
发明人： Graham P. Allaway , Carl T. Wild , Yoshiki Kashiwada , Kuo-Hsiung Lee
IPC分类号： C07C69/74
CPC分类号： C07J53/00 , A61K31/56 , A61K45/06 , A61K2300/00
摘要： Betulin and dihydrobetulin acyl derivatives according to the present invention have been found to have potent anti-HIV activity. The compounds of the present invention have Formula I as described herein, or pharmaceutically acceptable salts thereof; wherein R1 is a C2-C20 substituted or unsubstituted carboxyacyl or ester thereof; R2 is hydrogen, halogen, hydroxyl or —OR3, R3 is C2-C20 substituted or unsubstituted carboxyacyl; and R4 is hydrogen or C(C6H5)3; wherein the dashed line represents an optional double bond between C20 and C29.
摘要翻译：已经发现根据本发明的桦木醇和二氢甜菜碱酰基衍生物具有有效的抗HIV活性。本发明的化合物具有本文所述的式I或其药学上可接受的盐; 其中R 1是C 2 -C 20 - 取代或未取代的羧酰基或其酯; R 2是氢，卤素，羟基或-OR 3，R 3是C 2 -C 3 取代或未取代的羧酰基; 且R 4是氢或C（C 6 H 5）3 N 3。其中虚线表示C20和C29之间任选的双键。

2. 发明授权

US07345153B2 Compounds capable of inhibiting HIV-1 infection 失效
标题翻译：能够抑制HIV-1感染的化合物
公开(公告)号：US07345153B2
公开(公告)日：2008-03-18
申请号：US11544346
申请日：2006-10-05
申请人： Virginia M. Litwin , Graham P. Allaway , Paul J. Maddon
发明人： Virginia M. Litwin , Graham P. Allaway , Paul J. Maddon
IPC分类号： C07K16/00
CPC分类号： C07K14/705 , A01K2217/05 , A61K38/00 , C07K16/28 , C07K2317/32
摘要： This invention provides an antibody capable of specifically inhibiting the fusion of an HIV-1 envelope glycoprotein+ cell with an appropriate CD4+ cell without cross reacting with the HIV-1 envelope glycoprotein or CD4 and capable of inhibiting infection by one or more strains of HIV-1. This antibody is then used to identify a molecule which is important for HIV infection. Different uses of the antibody and the molecule are described.
摘要翻译：本发明提供能够特异性抑制HIV-1包膜糖蛋白+细胞与适当的CD4 +细胞融合而不与HIV-1包膜糖蛋白交叉反应的抗体或CD4并且能够抑制一种或多种HIV-1毒株的感染。然后将该抗体用于鉴定对HIV感染重要的分子。描述了抗体和分子的不同用途。

3. 发明授权

US06737267B2 Non-peptidyl moiety-conjugated CD4-gamma2 and CD4-IgG2 immunoconjugates, and uses thereof 失效
标题翻译：非肽基部分结合的CD4-γ2和CD4-IgG2免疫缀合物及其用途
公开(公告)号：US06737267B2
公开(公告)日：2004-05-18
申请号：US09766995
申请日：2001-01-22
申请人： Paul J. Maddon , Graham P. Allaway
发明人： Paul J. Maddon , Graham P. Allaway
IPC分类号： C12N1574
CPC分类号： C07K16/00 , A61K38/00 , A61K47/6425 , A61K47/6803 , A61K47/6849 , A61K51/10 , A61K51/1093 , C07K14/70514 , C07K2319/00 , C07K2319/30
摘要： This invention provides an immunoconjugate which comprises 1) a non-peptidyl toxin and 2) a CD4-gamma2 chimeric heavy chain homodimer linked thereto. This invention also provides an immunoconjugate which comprises 1) a gamma radiation-emitting radionuclide of low to moderate cytotoxicity and 2) a CD4-gamma2 chimeric heavy chain homodimer linked thereto. This invention further provides an immunoconjugate which comprises 1) a non-peptidyl toxin and 2) a heterotetramer comprising two heavy chains and two light chains, both heavy chains being either a) IgG2 heavy chains or b) chimeric CD4-IgG2 heavy chains, and both light chains being either a) kappa light chains or b) chimeric CD4-kappa light chains. This invention further provides an immunoconjugate which comprises 1) a gamma radiation-emitting radionuclide of low to moderate cytotoxicity and 2) a heterotetramer comprising two heavy chains and two light chains, both heavy chains being either a) IgG2 heavy chains or b) chimeric CD4-IgG2 heavy chains, and both light chains being either a) kappa light chains or b) chimeric CD4-kappa light chains. Finally, this invention provides methods of using the immunoconjugates of the subject invention.
摘要翻译：本发明提供免疫偶联物，其包含1）非肽基毒素和2）与其连接的CD4-γ2嵌合重链同源二聚体。本发明还提供免疫偶联物，其包含1）低至中等细胞毒性的γ辐射发射放射性核素，和2）与其连接的CD4-γ2嵌合重链同源二聚体。本发明还提供了免疫偶联物，其包含1）非肽基毒素和2）包含两条重链和两条轻链的异源四聚体，两条重链均为a）IgG2重链或b）嵌合型CD4-IgG2重链，以及两条轻链都是a）κ轻链或b）嵌合的CD4-κ轻链。本发明进一步提供免疫偶联物，其包含1）低至中等细胞毒性的γ辐射发射放射性核素，以及2）包含两条重链和两条轻链的异源四聚体，两条重链均为a）IgG2重链或b）嵌合CD4 -IgG2重链，两条轻链均为a）κ轻链或b）嵌合型CD4-κ轻链。最后，本发明提供了使用本发明的免疫偶联物的方法。

4. 发明申请

US20130211043A1 METHOD FOR PREVENTING HIV-1 INFECTION OF CD4+ CELLS 审中-公开
标题翻译：用于预防HIV-1感染CD4 +细胞的方法
公开(公告)号：US20130211043A1
公开(公告)日：2013-08-15
申请号：US13093331
申请日：2011-04-25
申请人： Graham P. Allaway , Virginia M. Litwin , Paul J. Maddon , William C. Olson
发明人： Graham P. Allaway , Virginia M. Litwin , Paul J. Maddon , William C. Olson
IPC分类号： C07K2/00
CPC分类号： C07K2/00 , C07K16/2866 , C07K2317/76 , G01N33/566 , G01N33/56988 , G01N2333/162 , G01N2333/70514 , G01N2333/7158 , G01N2500/10
摘要： This invention provides methods for inhibiting fusion of HIV-1 to CD4+ cells, comprising contacting CD4+ cells with a non-chemokine agent capable of binding to a chemokine receptor in an amount and under conditions such that fusion of HIV-1 to CD4+ cells is inhibited. Also provided are methods for inhibiting HIV-1 infection of CD4+ cells, comprising contacting CD4+ cells with a non-chemokine agent capable of binding to a chemokine receptor in an amount and under conditions such that fusion of HIV-1 to CD4+ cells is inhibited, thereby inhibiting the HIV-1 infection. This invention provides non-chemokine agents capable of binding to the chemokine receptor and inhibiting fusion of HIV-1 to CD4+ cells and pharmaceutical compositions comprising an amount of the non-chemokine agent capable of binding to the chemokine receptor and inhibiting fusion of HIV-1 to CD4+ cells effective to prevent fusion of HIV-1 to CD4+ cells and a pharmaceutically acceptable carrier.
摘要翻译：本发明提供了用于抑制HIV-1与CD4 +细胞融合的方法，包括使CD4 +细胞与能够结合趋化因子受体的非趋化因子试剂以一定量和在使得HIV-1与CD4 +细胞融合被抑制的条件下接触。还提供了用于抑制CD4 +细胞的HIV-1感染的方法，包括使CD4 +细胞与能够结合趋化因子受体的非趋化因子试剂以及在使得HIV-1与CD4 +细胞融合被抑制的条件下接触，从而抑制HIV-1感染。本发明提供了能够结合趋化因子受体并抑制HIV-1与CD4 +细胞融合的非趋化因子试剂和包含一定量的能够结合趋化因子受体并抑制HIV-1融合的非趋化因子试剂的药物组合物对于有效防止HIV-1与CD4 +细胞融合的CD4 +细胞和药学上可接受的载体。

5. 发明授权

US06342586B1 Non-peptidyl moiety-conjugated CD4-gamma2 and CD4-IgG2 immunoconjugates and uses thereof 失效
标题翻译：非肽基部分结合的CD4-γ2和CD4-IgG2免疫缀合物及其用途
公开(公告)号：US06342586B1
公开(公告)日：2002-01-29
申请号：US09409006
申请日：1999-09-29
申请人： Graham P. Allaway , Paul J. Maddon
发明人： Graham P. Allaway , Paul J. Maddon
IPC分类号： C07K1600
CPC分类号： C07K14/70514 , C07K2319/00 , C07K2319/30
摘要： This invention provides an immunoconjugate which comprises 1) a non-peptidyl toxin and 2) a CD4-gamma2 chimeric heavy chain homodimer linked thereto. This invention also provides an immunoconjugate which comprises 1) a gamma radiation-emitting radionuclide of low to moderate cytotoxicity and 2) a CD4-gamma2 chimeric heavy chain homodimer linked thereto. This invention further provides an immunoconjugate which comprises 1) a non-peptidyl toxin and 2) a heterotetramer comprising two heavy chains and two light chains, both heavy chains being either 1) IgG2 heavy chains or b) chimeric CD4-IgG2 heavy chains, and both light chains being either a) kappa light chains or b) chimeric CD4-kappa light chains. This invention further provides an immunoconjugate which comprises 1) a gamma radiation-emitting radionuclide of low to moderate cytotoxicity and 2) a heterotetramer comprising two heavy chains and two light chains, both heavy chains being either a) IgG2 heavy chains or b) chimeric CD4-IgG2 heavy chains, and both light chains being either a) kappa light chains or b) chimeric CD4-kappa light chains. Finally, this invention provides methods of using the immunoconjugates of the subject invention.
摘要翻译：本发明提供免疫偶联物，其包含1）非肽基毒素和2）与其连接的CD4-γ2嵌合重链同源二聚体。本发明还提供免疫偶联物，其包含1）低至中等细胞毒性的γ辐射发射放射性核素，和2）与其连接的CD4-γ2嵌合重链同源二聚体。本发明还提供了免疫偶联物，其包含1）非肽基毒素和2）包含两条重链和两条轻链的异源四聚体，两条重链均为1）IgG2重链或b）嵌合型CD4-IgG2重链，以及两条轻链都是a）κ轻链或b）嵌合的CD4-κ轻链。本发明进一步提供免疫偶联物，其包括1）低至中等细胞毒性的γ射线辐射放射性核素，以及2）包含两条重链和两条轻链的异源四聚体，两条重链均为a）IgG2重链或b）嵌合CD4 -IgG2重链，两条轻链均为a）κ轻链或b）嵌合型CD4-κ轻链。最后，本发明提供了使用本发明的免疫偶联物的方法。

6. 发明授权

US06177549B1 Non-peptidyl moiety-conjugated CD4-gamma2 and CD4-IgG2 immunoconjugates, and uses thereof 失效
标题翻译：非肽基部分结合的CD4-γ2和CD4-IgG2免疫缀合物及其用途
公开(公告)号：US06177549B1
公开(公告)日：2001-01-23
申请号：US09329916
申请日：1999-06-10
申请人： Paul J. Maddon , Graham P. Allaway
发明人： Paul J. Maddon , Graham P. Allaway
IPC分类号： C07K1600
CPC分类号： C07K16/00 , A61K38/00 , A61K47/6425 , A61K47/6803 , A61K47/6849 , A61K51/10 , A61K51/1093 , C07K14/70514 , C07K2319/00 , C07K2319/30
摘要： This invention provides an immunoconjugate which comprises 1) a non-peptidyl toxin and 2) a CD4-gamma2 chimeric heavy chain homodimer linked thereto. This invention also provides an immunoconjugate which comprises 1) a gamma radiation-emitting radionuclide of low to moderate cytotoxicity and 2) a CD4-gamma2 chimeric heavy chain homodimer linked thereto. This invention further provides an immunoconjugate which comprises 1) a non-peptidyl toxin and 2) a heterotetramer comprising two heavy chains and two light chains, both heavy chains being either a) IgG2 heavy chains or b) chimeric CD4-IgG2 heavy chains, and both light chains being either a) kappa light chains or b) chimeric CD4-kappa light chains. This invention further provides an immunoconjugate which comprises 1) a gamma radiation-emitting radionuclide of low to moderate cytotoxicity and 2) a heterotetramer comprising two heavy chains and two light chains, both heavy chains being either a) IgG2 heavy chains or b) chimeric CD4-IgG2 heavy chains, and both light chains being either a) kappa light chains or b) chimeric CD4-kappa light chains. Finally, this invention provides methods of using the immunoconjugates of the subject invention.
摘要翻译：本发明提供免疫偶联物，其包含1）非肽基毒素和2）与其连接的CD4-γ2嵌合重链同源二聚体。本发明还提供免疫偶联物，其包含1）低至中等细胞毒性的γ辐射发射放射性核素，和2）与其连接的CD4-γ2嵌合重链同源二聚体。本发明还提供了免疫偶联物，其包含1）非肽基毒素和2）包含两条重链和两条轻链的异源四聚体，两条重链均为a）IgG2重链或b）嵌合型CD4-IgG2重链，以及两条轻链都是a）κ轻链或b）嵌合的CD4-κ轻链。本发明进一步提供免疫偶联物，其包含1）低至中等细胞毒性的γ辐射发射放射性核素，以及2）包含两条重链和两条轻链的异源四聚体，两条重链均为a）IgG2重链或b）嵌合CD4 -IgG2重链，两条轻链均为a）κ轻链或b）嵌合型CD4-κ轻链。最后，本发明提供了使用本发明的免疫偶联物的方法。

7. 发明授权

US07858298B1 Methods of inhibiting human immunodeficiency virus type 1 (HIV-1) infection through the administration of CCR5 chemokine receptor antagonists 有权
标题翻译：通过施用CCR5趋化因子受体拮抗剂来抑制1型（HIV-1）感染的人类免疫缺陷病毒的方法
公开(公告)号：US07858298B1
公开(公告)日：2010-12-28
申请号：US09460216
申请日：1999-12-13
申请人： Graham P. Allaway , Virginia M. Litwin , Paul J. Maddon , William C. Olson
发明人： Graham P. Allaway , Virginia M. Litwin , Paul J. Maddon , William C. Olson
IPC分类号： C12Q1/70 , A61K39/42
CPC分类号： C07K2/00 , C07K16/2866 , C07K2317/76 , G01N33/566 , G01N33/56988 , G01N2333/162 , G01N2333/70514 , G01N2333/7158 , G01N2500/10
摘要： This invention provides methods for inhibiting fusion of HIV-1 to CD4+ cells which comprise contacting CD4+ cells with a non-chemokine agent capable of binding to a chemokine receptor in an amount and under conditions such that fusion of HIV-1 to the CD4+ cells is inhibited. This invention also provides methods for inhibiting HIV-1 infection of CD4+ cells which comprise contacting CD4+ cells with a non-chemokine agent capable of binding to a chemokine receptor in an amount and under conditions such that fusion of HIV-1 to the CD4+ cells is inhibited, thereby inhibiting the HIV-1 infection. This invention provides non-chemokine agents capable of binding to the chemokine receptor and inhibiting fusion of HIV-1 to CD4+ cells. This invention also provides pharmaceutical compositions comprising an amount of the non-chemokine agent capable of binding to the chemokine receptor and inhibiting fusion of HIV-1 to CD4+ cells effective to prevent fusion of HIV-1 to CD4+ cells and a pharmaceutically acceptable carrier.
摘要翻译：本发明提供了用于抑制HIV-1与CD4 +细胞融合的方法，其包括使CD4 +细胞与能够结合趋化因子受体的非趋化因子试剂以一定量和在使HIV-1与CD4 +细胞融合的条件下抑制。本发明还提供了用于抑制CD4 +细胞的HIV-1感染的方法，其包括使CD4 +细胞与能够结合趋化因子受体的非趋化因子试剂接触，其量和条件使得HIV-1与CD4 +细胞的融合是抑制，从而抑制HIV-1感染。本发明提供能够结合趋化因子受体并抑制HIV-1与CD4 +细胞融合的非趋化因子试剂。本发明还提供药物组合物，其包含一定量的能够结合趋化因子受体的非趋化因子剂，并且抑制HIV-1与有效预防HIV-1与CD4 +细胞融合的CD4 +细胞和药学上可接受的载体的融合。

8. 发明申请

US20100221264A1 Inhibition of HIV-1 Replication by Disruption of the Processing of the Viral Capsid-Spacer Peptide 1 Protein 有权
标题翻译：通过破坏病毒衣壳间隔肽1蛋白的加工来抑制HIV-1复制
公开(公告)号：US20100221264A1
公开(公告)日：2010-09-02
申请号：US12498157
申请日：2009-07-06
申请人： Karl Salzwedel , Feng Li , Carl T. Wild , Graham P. Allaway , Eric O. Freed
发明人： Karl Salzwedel , Feng Li , Carl T. Wild , Graham P. Allaway , Eric O. Freed
IPC分类号： A61K39/395 , A61K31/655 , A61K38/16 , A61P31/18 , A61K31/56
CPC分类号： A61K45/06 , A61K31/56 , C07K14/005 , C12N2740/16043 , C12N2740/16222 , G01N2333/161 , A61K2300/00
摘要： Inhibition of HIV-1 replication by disrupting the processing of the viral Gag capsid (CA) protein (p24) from the CA-spacer peptide 1 (SP1) protein precursor (p25) is disclosed. Amino acid sequences containing a mutation in the Gag p25 protein, with the mutation resulting in a decrease in the inhibition of processing of p25 to p24 by dimethylsuccinyl betulinic acid or dimethylsuccinyl betulin, polynucleotides encoding such mutated sequences and antibodies that selectively bind such mutated sequences are also included. Methods of inhibiting, inhibitory compounds and methods of discovering inhibitory compounds that target proteolytic processing of the HIV Gag protein are included. In one embodiment, such compounds inhibit the interaction of the HIV protease enzyme with Gag by binding to the Gag proteolytic cleavage site rather than to the protease enzyme. In another embodiment, viruses or recombinant proteins that contain mutations in the region of the Gag proteolytic cleavage site can be used in screening assays to identify compounds that target proteolytic processing.
摘要翻译：公开了通过破坏来自CA-间隔肽1（SP1）蛋白前体（p25）的病毒Gag衣壳（CA）蛋白（p24））的加工来抑制HIV-1复制。含有Gag p25蛋白突变的氨基酸序列，突变导致二甲基琥珀酰桦树酸或二甲基琥珀酰基桦木醇处理p25至p24的抑制作用降低，编码这种突变序列的多核苷酸和选择性结合这种突变序列的抗体是也包括在内。包括抑制，抑制化合物的方法和发现靶向HIV Gag蛋白的蛋白水解加工的抑制性化合物的方法。在一个实施方案中，这样的化合物通过结合Gag蛋白水解切割位点而不是蛋白酶抑制HIV蛋白酶与Gag的相互作用。在另一个实施方案中，在Gag蛋白水解切割位点区域中含有突变的病毒或重组蛋白质可用于筛选测定以鉴定靶向蛋白水解加工的化合物。

9. 发明申请

US20090155774A1 Fluorescence resonance energy transfer screening assay for the identification of HIV-1 envelope glycoprotein-medicated cell 审中-公开
标题翻译：用于鉴定HIV-1包膜糖蛋白药物细胞的荧光共振能量转移筛选测定
公开(公告)号：US20090155774A1
公开(公告)日：2009-06-18
申请号：US12378572
申请日：2009-02-17
申请人： Graham P. Allaway , Virginia M. Litwin , Paul J. Maddon
发明人： Graham P. Allaway , Virginia M. Litwin , Paul J. Maddon
IPC分类号： C12Q1/70
CPC分类号： C07K14/005 , A61K38/00 , C07K16/2812 , C12N2740/16122 , G01N33/56972 , G01N33/56988 , G01N2500/02
摘要： This invention provides: agents determined to be capable of specifically inhibiting the fusion of a macrophage-tropic primary isolate of HIV-1 to a CD4+ cell, but not a T cell-tropic isolate of HIV-1 to a CD4+ cell; and agents determined to be capable of specifically inhibiting the fusion of a T cell-tropic isolate of HIV-1 to a CD4+ cell, but not a macrophage-tropic primary isolate of HIV-1 to a CD4+ cell. This invention also provides: agents capable of specifically inhibiting the fusion of a macrophage tropic primary isolate of HIV-1 with a CD+ cell susceptible to infection by a macrophage-tropic primary isolate of HIV-1; and agents capable of specifically inhibiting the fusion of a T cell-tropic isolate of HIV-1 with a CD4+ cell susceptible to infection by a T cell-tropic isolate of HIV-1. The agents include but are not limited to antibodies. This invention further provides: methods of inhibiting fusion of a macrophage-tropic primary isolate of HIV-1 with a CD4+ cell susceptible to infection by a macrophage-tropic primary isolate of HIV-1 which comprises contacting the CD4+ cell with an amount of an agent capable of specifically inhibiting such fusion so as to thereby inhibit such fusion; and methods of inhibiting fusion of a T cell-tropic isolate of HIV-1 with a CD4+ cell susceptible to infection by a T cell-tropic isolate of HIV-1 which comprises contacting the CD4+ cell with an amount of an agent capable of specifically inhibiting such fusion so as to thereby inhibit such fusion.
摘要翻译：本发明提供：确定能够特异性抑制HIV-1的巨噬细胞 - 初级分离物与CD4 +细胞而不是CD4 +细胞的HIV-1的T细胞分泌物的融合的药剂; 并且确定能够特异性抑制HIV-1的T细胞分泌物与CD4 +细胞而不是CD4 +细胞的HIV-1的巨噬细胞 - 初级分离物融合的药剂。本发明还提供：能够特异性抑制HIV-1的巨噬细胞回归初级分离物与易受HIV-1巨噬细胞 - 初级分离株感染的CD +细胞的融合的试剂; 以及能够特异性抑制HIV-1的T细胞分泌物与CD4 +细胞融合的试剂，所述CD4 +细胞对HIV-1的T细胞分泌物敏感。这些试剂包括但不限于抗体。本发明进一步提供：抑制HIV-1的巨噬细胞 - 初级分离物与HIV-1巨噬细胞 - 初级分离株感染易感染的CD4 +细胞融合的方法，其包括将CD4 +细胞与一定量的试剂接触能够特异性地抑制这种融合，从而抑制这种融合; 以及抑制HIV-1的T细胞分泌物与CD4 +细胞融合的方法，所述CD4 +细胞易感染HIV-1的T细胞分泌物，其包括将CD4 +细胞与一定量的能够特异性抑制的药剂接触这样的融合从而抑制这种融合。

10. 发明申请

US20080233559A1 Inhibition of HIV-1 Replication by Disruption of the Processing of the Viral Capsid-Spacer Peptide 1 Protein 审中-公开
标题翻译：通过破坏病毒衣壳间隔肽1蛋白的加工来抑制HIV-1复制
公开(公告)号：US20080233559A1
公开(公告)日：2008-09-25
申请号：US11962315
申请日：2007-12-21
申请人： Karl SALZWEDEL , Feng Li , Carl T. Wild , Graham P. Allaway , Eric O. Freed
发明人： Karl SALZWEDEL , Feng Li , Carl T. Wild , Graham P. Allaway , Eric O. Freed
IPC分类号： C12Q1/70
CPC分类号： A61K31/215 , A61K31/56 , A61K31/567 , A61K45/06 , C07K14/005 , C12N2740/16043 , C12N2740/16222 , G01N33/56988 , G01N2333/161 , A61K2300/00
摘要： Inhibition of HIV-1 replication by disrupting the processing of the viral Gag capsid (CA) protein (p24) from the CA-spacer peptide 1 (SP1) protein precursor (p25) is disclosed. Amino acid sequences containing a mutation in the Gag p25 protein, with the mutation resulting in a decrease in the inhibition of processing of p25 to p24 by dimethylsuccinyl betulinic acid or dimethylsuccinyl betulin, polynucleotides encoding such mutated sequences and antibodies that selectively bind such mutated sequences are also included. Methods of inhibiting, inhibitory compounds and methods of discovering inhibitory compounds that target proteolytic processing of the HIV Gag protein are included. In one embodiment, such compounds inhibit the interaction of the HIV protease enzyme with Gag by binding to Gag rather than to the protease enzyme. In another embodiment, viruses or recombinant proteins that contain mutations in the region of the Gag proteolytic cleavage site can be used in screening assays to identify compounds that target proteolytic processing.
摘要翻译：公开了通过破坏来自CA-间隔肽1（SP1）蛋白前体（p25）的病毒Gag衣壳（CA）蛋白（p24））的加工来抑制HIV-1复制。含有Gag p25蛋白突变的氨基酸序列，突变导致二甲基琥珀酰桦树酸或二甲基琥珀酰基桦木醇处理p25至p24的抑制作用降低，编码这种突变序列的多核苷酸和选择性结合这种突变序列的抗体是也包括在内。包括抑制，抑制化合物的方法和发现靶向HIV Gag蛋白的蛋白水解加工的抑制性化合物的方法。在一个实施方案中，这些化合物通过结合Gag而不是蛋白酶抑制HIV蛋白酶与Gag的相互作用。在另一个实施方案中，在Gag蛋白水解切割位点区域中含有突变的病毒或重组蛋白质可用于筛选测定以鉴定靶向蛋白水解加工的化合物。

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