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1.发明授权Crystal structure of hepatocyte growth factor activator complexed with Kunitz domain inhibitor 失效与Kunitz结构域抑制剂复合的肝细胞生长因子激活物的晶体结构公开(公告)号：US07741096B2
公开(公告)日：2010-06-22
申请号：US11721012
申请日：2005-12-09
CPC分类号： C12N9/6424 , C07K14/4753 , C07K2299/00
摘要： The present disclosure provides crystals of and structural coordinates of Hepatocyte growth factor activator with and without bound pseudo-substrate or inhibitor. In a specific embodiment, a crystal structure of activated HGFA complexed with a Kunitz domain inhibitor is provided. The crystals and crystal structures are useful, for example, in the design and synthesis of inhibitors of HGFA.
摘要翻译： 本公开提供具有和不具有结合的假底物或抑制剂的肝细胞生长因子活化剂的晶体和结构坐标。 在具体实施方案中，提供了与Kunitz结构域抑制剂复合的活化HGFA的晶体结构。 晶体和晶体结构在例如HGFA抑制剂的设计和合成中是有用的。
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2.发明申请CRYSTAL STRUCTURE OF HEPATOCYTE GROWTH FACTOR ACTIVATOR COMPLEXED WITH KUNITZ DOMAIN INHIBITOR 审中-公开与昆尼系域抑制剂复合的肝细胞生长因子激活剂的晶体结构公开(公告)号：US20100277473A1
公开(公告)日：2010-11-04
申请号：US12757867
申请日：2010-04-09
IPC分类号： G06T17/00
CPC分类号： C12N9/6424 , C07K14/4753 , C07K2299/00
摘要： The present disclosure provides crystals of and structural coordinates of Hepatocyte growth factor activator with and without bound pseudo-substrate or inhibitor. In a specific embodiment, a crystal structure of activated HGFA complexed with a Kunitz domain inhibitor is provided. The crystals and crystal structures are useful, for example, in the design and synthesis of inhibitors of HGFA.
摘要翻译： 本公开提供具有和不具有结合的假底物或抑制剂的肝细胞生长因子活化剂的晶体和结构坐标。 在具体实施方案中，提供了与Kunitz结构域抑制剂复合的活化HGFA的晶体结构。 晶体和晶体结构在例如HGFA抑制剂的设计和合成中是有用的。
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公开(公告)号：US20100003766A1
公开(公告)日：2010-01-07
申请号：US12427649
申请日：2009-04-21
IPC分类号： G01N33/566
CPC分类号： A61K47/6803 , A01K2267/0331 , A61K45/06 , A61K47/6817 , A61K47/6851 , A61K47/6889 , C07K16/00 , C07K16/32 , C07K2317/21 , C07K2317/51 , C07K2317/52 , C07K2317/55 , C07K2317/624
摘要： Antibodies are engineered by replacing one or more amino acids of a parent antibody with non cross-linked, highly reactive cysteine amino acids. Antibody fragments may also be engineered with one or more cysteine amino acids to form cysteine engineered antibody fragments (ThioFab). Methods of design, preparation, screening, and selection of the cysteine engineered antibodies are provided. Cysteine engineered antibodies (Ab), optionally with an albumin-binding peptide (ABP) sequence, are conjugated with one or more drug moieties (D) through a linker (L) to form cysteine engineered antibody-drug conjugates having Formula I: Ab-(L-D)p I where p is 1 to 4. Diagnostic and therapeutic uses for cysteine engineered antibody drug compounds and compositions are disclosed.
摘要翻译： 通过用非交联的高反应性半胱氨酸氨基酸替代亲本抗体的一个或多个氨基酸来设计抗体。 抗体片段也可以用一个或多个半胱氨酸氨基酸进行工程化以形成半胱氨酸改造的抗体片段（ThioFab）。 提供了设计，制备，筛选和选择半胱氨酸改造的抗体的方法。 任选与白蛋白结合肽（ABP）序列的半胱氨酸改造的抗体（Ab）通过接头（L）与一个或多个药物部分（D）缀合，形成具有式I：Ab- （LD）p I，其中p为1至4.披露了半胱氨酸改造的抗体药物化合物和组合物的诊断和治疗用途。
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公开(公告)号：US07855275B2
公开(公告)日：2010-12-21
申请号：US12399241
申请日：2009-03-06
IPC分类号： C07K16/00
CPC分类号： A61K47/6803 , A01K2267/0331 , A61K45/06 , A61K47/6817 , A61K47/6851 , A61K47/6889 , C07K16/00 , C07K16/32 , C07K2317/21 , C07K2317/51 , C07K2317/52 , C07K2317/55 , C07K2317/624
摘要： Antibodies are engineered by replacing one or more amino acids of a parent antibody with non cross-linked, highly reactive cysteine amino acids. Antibody fragments may also be engineered with one or more cysteine amino acids to form cysteine engineered antibody fragments (ThioFab). Methods of design, preparation, screening, and selection of the cysteine engineered antibodies are provided. Cysteine engineered antibodies (Ab), optionally with an albumin-binding peptide (ABP) sequence, are conjugated with one or more drug moieties (D) through a linker (L) to form cysteine engineered antibody-drug conjugates having Formula I: Ab-(L-D)p I where p is 1 to 4. Diagnostic and therapeutic uses for cysteine engineered antibody drug compounds and compositions are disclosed.
摘要翻译： 通过用非交联的高反应性半胱氨酸氨基酸替代亲本抗体的一个或多个氨基酸来设计抗体。 抗体片段也可以用一个或多个半胱氨酸氨基酸进行工程化以形成半胱氨酸改造的抗体片段（ThioFab）。 提供了设计，制备，筛选和选择半胱氨酸改造的抗体的方法。 任选与白蛋白结合肽（ABP）序列的半胱氨酸改造的抗体（Ab）通过接头（L）与一个或多个药物部分（D）缀合，形成具有式I：Ab- （LD）p I，其中p为1至4.披露了半胱氨酸改造的抗体药物化合物和组合物的诊断和治疗用途。
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5.发明申请公开(公告)号：US20080195366A1
公开(公告)日：2008-08-14
申请号：US12057291
申请日：2008-03-27
IPC分类号： G06G7/60
CPC分类号： C07K14/4753 , C07K2299/00 , G16B15/00 , G16B20/00
摘要： The disclosure provides a crystal and crystal structure of the Hepatocyte Growth Factor Beta (HGF β) Chain, as well as use of the crystal structure in the design, identification, and selection of modulators of HGF or Met activity.
摘要翻译： 本公开提供了肝细胞生长因子β（HGFβ）链的晶体和晶体结构，以及在HGF或Met活性调节剂的设计，鉴定和选择中使用晶体结构。
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公开(公告)号：US20110137017A1
公开(公告)日：2011-06-09
申请号：US12971197
申请日：2010-12-17
CPC分类号： A61K47/6803 , A01K2267/0331 , A61K45/06 , A61K47/6817 , A61K47/6851 , A61K47/6889 , C07K16/00 , C07K16/32 , C07K2317/21 , C07K2317/51 , C07K2317/52 , C07K2317/55 , C07K2317/624
摘要： Antibodies are engineered by replacing one or more amino acids of a parent antibody with non cross-linked, highly reactive cysteine amino acids. Antibody fragments may also be engineered with one or more cysteine amino acids to form cysteine engineered antibody fragments (ThioFab). Methods of design, preparation, screening, and selection of the cysteine engineered antibodies are provided. Cysteine engineered antibodies (Ab), optionally with an albumin-binding peptide (ABP) sequence, are conjugated with one or more drug moieties (D) through a linker (L) to form cysteine engineered antibody-drug conjugates having Formula I: Ab-(L-D)p I where p is 1 to 4. Diagnostic and therapeutic uses for cysteine engineered antibody drug compounds and compositions are disclosed.
摘要翻译： 通过用非交联的高反应性半胱氨酸氨基酸替代亲本抗体的一个或多个氨基酸来设计抗体。 抗体片段也可以用一个或多个半胱氨酸氨基酸进行工程化以形成半胱氨酸改造的抗体片段（ThioFab）。 提供了设计，制备，筛选和选择半胱氨酸改造的抗体的方法。 任选与白蛋白结合肽（ABP）序列的半胱氨酸改造的抗体（Ab）通过接头（L）与一个或多个药物部分（D）缀合，形成具有式I：Ab- （LD）p I，其中p为1至4.披露了半胱氨酸改造的抗体药物化合物和组合物的诊断和治疗用途。
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公开(公告)号：US20090175865A1
公开(公告)日：2009-07-09
申请号：US12399241
申请日：2009-03-06
IPC分类号： A61K39/395 , C07K16/46 , A61P35/00
CPC分类号： A61K47/6803 , A01K2267/0331 , A61K45/06 , A61K47/6817 , A61K47/6851 , A61K47/6889 , C07K16/00 , C07K16/32 , C07K2317/21 , C07K2317/51 , C07K2317/52 , C07K2317/55 , C07K2317/624
摘要： Antibodies are engineered by replacing one or more amino acids of a parent antibody with non cross-linked, highly reactive cysteine amino acids. Antibody fragments may also be engineered with one or more cysteine amino acids to form cysteine engineered antibody fragments (ThioFab). Methods of design, preparation, screening, and selection of the cysteine engineered antibodies are provided. Cysteine engineered antibodies (Ab), optionally with an albumin-binding peptide (ABP) sequence, are conjugated with one or more drug moieties (D) through a linker (L) to form cysteine engineered antibody-drug conjugates having Formula I: Ab-(L-D)p I where p is 1 to 4. Diagnostic and therapeutic uses for cysteine engineered antibody drug compounds and compositions are disclosed.
摘要翻译： 通过用非交联的高反应性半胱氨酸氨基酸替代亲本抗体的一个或多个氨基酸来设计抗体。 抗体片段也可以用一个或多个半胱氨酸氨基酸进行工程化以形成半胱氨酸改造的抗体片段（ThioFab）。 提供了设计，制备，筛选和选择半胱氨酸改造的抗体的方法。 任选与白蛋白结合肽（ABP）序列的半胱氨酸改造的抗体（Ab）通过接头（L）与一个或多个药物部分（D）缀合以形成具有式I的半胱氨酸改造的抗体 - 药物共轭物： in-line-formula description =“In-line Formulas”end =“lead”？> Ab-（LD）p I <？in-line-formula description =“In-line Formulas”end =“tail”？> where p是1至4.公开了半胱氨酸改造的抗体药物化合物和组合物的诊断和治疗用途。
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公开(公告)号：US07521541B2
公开(公告)日：2009-04-21
申请号：US11233258
申请日：2005-09-22
IPC分类号： C07K16/00
CPC分类号： A61K47/6803 , A01K2267/0331 , A61K45/06 , A61K47/6817 , A61K47/6851 , A61K47/6889 , C07K16/00 , C07K16/32 , C07K2317/21 , C07K2317/51 , C07K2317/52 , C07K2317/55 , C07K2317/624
摘要： Antibodies are engineered by replacing one or more amino acids of a parent antibody with non cross-linked, highly reactive cysteine amino acids. Antibody fragments may also be engineered with one or more cysteine amino acids to form cysteine engineered antibody fragments (ThioFab). Methods of design, preparation, screening, and selection of the cysteine engineered antibodies are provided. Cysteine engineered antibodies (Ab), optionally with an albumin-binding peptide (ABP) sequence, are conjugated with one or more drug moieties (D) through a linker (L) to form cysteine engineered antibody-drug conjugates having Formula I: Ab-(L-D)p I where p is 1 to 4. Diagnostic and therapeutic uses for cysteine engineered antibody drug compounds and compositions are disclosed.
摘要翻译： 通过用非交联的高反应性半胱氨酸氨基酸替代亲本抗体的一个或多个氨基酸来设计抗体。 抗体片段也可以用一个或多个半胱氨酸氨基酸进行工程化以形成半胱氨酸改造的抗体片段（ThioFab）。 提供了设计，制备，筛选和选择半胱氨酸改造的抗体的方法。 任选与白蛋白结合肽（ABP）序列的半胱氨酸改造的抗体（Ab）通过接头（L）与一个或多个药物部分（D）缀合以形成具有式I的半胱氨酸改造的抗体 - 药物共轭物： in-line-formula description =“In-line Formulas”end =“lead”？> Ab-（LD）p I <？in-line-formula description =“In-line Formulas”end =“tail”？> where p是1至4.公开了半胱氨酸改造的抗体药物化合物和组合物的诊断和治疗用途。
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