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1. 发明申请

US20080125354A1 SELECTIVE INHIBITION OF MATRIX METALLOPROTEINASES 审中-公开
标题翻译：选择性抑制基质金属蛋白酶
公开(公告)号：US20080125354A1
公开(公告)日：2008-05-29
申请号：US11562295
申请日：2006-11-21
申请人： Gregg B. Fields , Robert Hammer
发明人： Gregg B. Fields , Robert Hammer
IPC分类号： A61K38/02 , A61P21/00 , A61K31/664 , A61K31/662 , A61P43/00
CPC分类号： A61K38/10 , A61K31/4035 , A61K38/06
摘要： Synthetic triple-helical peptides (THPs) are used for the design and synthesis of triple-helical transition state analog inhibitors. These inhibitors feature a phosphonate ester or phosphinic moiety in place of the scissle bond. These groups inhibit MMPs, and methods been developed for their convenient incorporation within a peptide sequence by solid-phase methods.
摘要翻译：合成三螺旋肽（THP）用于设计和合成三螺旋转移态类似物抑制剂。这些抑制剂的特征在于膦酸酯或次膦酸部分代替硫化物键。这些组抑制MMPs，并且开发了通过固相方法在肽序列中方便地并入其中的方法。

2. 发明申请

US20160053250A1 MATRIX METALLOPROTEINASSES AND USES THEREOF 审中-公开
标题翻译： MATRIX METALLOPROTENESESES及其用途
公开(公告)号：US20160053250A1
公开(公告)日：2016-02-25
申请号：US14782118
申请日：2014-04-04
申请人： Claudia ZYLBERBERG , Gregg B. FIELDS
发明人： Claudia ZYLBERBERG , Gregg B. FIELDS
IPC分类号： C12N9/64 , A61K38/48
CPC分类号： C12N9/6491 , A61K38/4886 , C12N9/6416 , C12Y304/24 , C12Y304/24007 , C12Y304/24017 , C12Y304/24024 , C12Y304/24034 , C12Y304/24035 , C12Y304/24065
摘要： Matrix metalloproteinases (MMPs) compositions, inactive forms of MMPs (e.g. proMMPs), fragments, mutants, variants or combinations thereof. A pharmaceutical composition comprises one or more of the above in a pharmaceutical carrier. A composition comprises at least one of: a matrix metalloproteinase (MMP), an inactive MMP or a proenzyme (proMMP) thereof, wherein the matrix metalloproteinase (MMPs), inactive MMPs or proMMPs thereof, comprise: MMP-1, MMP-2, MMP-3, MMP-7, MMP-8, MMP-9, MMP-10, MMP-11, MMP-12, MMP-13.MMP-14, MMP-15, MMP-16, MMP-17, MMP-18, MMP-19, MMP-20, MMP-21, MMP-23A, MMP-23B, MMP-24, MMP-25, MMP-26, MMP-27, MMP-28, active fragments, mutants, variants or any combinations thereof. The uses include isolation of cells, in particular stem cells, from tissues, dissociation of tissues, proteins and treatment of a variety of conditions.
摘要翻译：基质金属蛋白酶（MMPs）组合物，MMPs的无活性形式（例如proMMP），片段，突变体，变体或其组合。药物组合物在药物载体中包含上述一种或多种。组合物包含以下中的至少一种：基质金属蛋白酶（MMP），非活性MMP或其酶原（proMMP），其中所述基质金属蛋白酶（MMP），其无活性的MMP或其proMMP包含：MMP-1，MMP-2， MMP-3，MMP-7，MMP-8，MMP-9，MMP-10，MMP-11，MMP-12，MMP-13MMP-14，MMP-15，MMP-16， 18，MMP-19，MMP-20，MMP-21，MMP-23A，MMP-23B，MMP-24，MMP-25，MMP-26，MMP-27，MMP-28，活性片段，突变体，其组合。用途包括从组织中分离细胞，特别是干细胞，分解组织，蛋白质以及各种条件的治疗。

3. 发明授权

US5576419A Mild solid-phase synthesis of aligned branched triple-helical peptides 失效
标题翻译：对齐支链三螺旋肽的轻度固相合成
公开(公告)号：US5576419A
公开(公告)日：1996-11-19
申请号：US534342
申请日：1995-09-27
申请人： Gregg B. Fields
发明人： Gregg B. Fields
IPC分类号： C07K1/04 , C07K14/78 , C07K17/06 , C07K1/06 , C07K14/00
CPC分类号： C07K17/06 , C07K1/04 , C07K14/78 , Y10S530/81 , Y10S530/812 , Y10S530/816
摘要： A triple-helical polypeptide of the formula: ##STR1## is provided wherein: Z is Hyp or Pro; each X and Y is an amino acid such that (Gly-X-Y).sub.m is a sequence of a collagen cell adhesion site; said X and Y may be the same or different and each (Gly-X-Y) may be the same or different; O is an amino acid having a single side-chain amino group; J is an amino acid capable of acting as a chromophore; U is an amino acid; u=0 or 1; n.ltoreq.30; m.ltoreq.30; m+n.ltoreq.30; and j.gtoreq.1. Methods of making these compounds and intermediates used in the methods, are also provided.
摘要翻译：提供下式的三螺旋多肽：其中：Z是Hyp或Pro; 每个X和Y是氨基酸，使得（Gly-X-Y）m是胶原细胞粘附位点的序列; 所述X和Y可以相同或不同，并且每个（Gly-X-Y）可以相同或不同; O是具有单个侧链氨基的氨基酸; J是能够作为发色团的氨基酸; U是氨基酸; u = 0或1; n / = 1。还提供了制备这些化合物和方法中使用的中间体的方法。

4. 发明授权

US06096863A Self-assembling amphiphiles for construction of peptide secondary structures 失效
标题翻译：用于构建肽二级结构的自组装两亲物
公开(公告)号：US06096863A
公开(公告)日：2000-08-01
申请号：US702254
申请日：1996-08-23
申请人： Gregg B. Fields , Matthew V. Tirrell
发明人： Gregg B. Fields , Matthew V. Tirrell
IPC分类号： A61K38/00 , C07K14/78 , C07K7/00 , A61K9/127 , C07C55/00 , C07C69/00
CPC分类号： C07K14/78 , A61K38/00
摘要： A peptide-amphiphile complex having a lipophilic portion and a peptide portion, wherein the peptide portion has a secondary structure.
摘要翻译：具有亲油部分和肽部分的肽 - 两亲物复合物，其中所述肽部分具有二级结构。

5. 发明授权

US5853744A Solid-phase method for attaching a biomolecule to a substrate surface with a photoreactive crosslinking agent 失效
标题翻译：用光反应性交联剂将生物分子附着到基材表面的固相方法
公开(公告)号：US5853744A
公开(公告)日：1998-12-29
申请号：US699965
申请日：1996-08-20
申请人： Daniel L. Mooradian , Gregg B. Fields
发明人： Daniel L. Mooradian , Gregg B. Fields
IPC分类号： A61L27/34 , A61L27/50 , C12N5/00 , A61F2/06 , C07K17/06 , C12N11/06
CPC分类号： C12N5/0068 , A61L27/34 , A61L27/507 , C12N2533/30 , C12N2533/50 , Y10S530/81 , Y10S530/812 , Y10S530/815 , Y10S530/816
摘要： A method for making a medical device having a biomolecule immobilized on a substrate surface is provided. The method includes: providing an immobilized biomolecule comprising a biomolecule covalently attached to a support material; attaching a photoreactive crosslinking agent to the immobilized biomolecule to form a photoreactive analog of the biomolecule; and removing the photoreactive analog of the biomolecule from the support material. The photoreactive analog of the biomolecule can then be attached to a substrate surface, such as a biomaterial that forms part of a medical device. The immobilized biomolecule may contain a peptide having an N.sup..alpha. -terminus. The photoreactive crosslinking agent is attached to the peptide at the N.sup..alpha. -terminus to form the photoreactive analog of the biomolecule. The peptide can be an adhesion peptide containing the sequence Trp-Gln-Pro-Pro-Arg-Ala-Arg-Ile. Attachment of the peptide to a substrate surface promotes cell adhesion to the surface. The photoreactive crosslinking agent can be heterobifunctional or contain two photoreactive groups. The photoreactive analog of the biomolecule is attached to the substrate surface by activating a photoreactive group of the analog such as by exposing the analog to UV radiation.
摘要翻译：提供一种制造具有固定在基板表面上的生物分子的医疗装置的方法。该方法包括：提供固定化的生物分子，其包含共价连接到载体材料上的生物分子; 将光反应性交联剂附着到固定化的生物分子上以形成生物分子的光反应性类似物; 并从载体材料中除去生物分子的光反应性类似物。然后可以将生物分子的光反应性类似物连接到基底表面，例如形成医疗装置的一部分的生物材料。固定化的生物分子可以含有具有Nα末端的肽。光反应性交联剂以Nα末端连接到肽上以形成生物分子的光反应性类似物。肽可以是含有序列Trp-Gln-Pro-Pro-Arg-Ala-Arg-Ile的粘附肽。将肽附着到基底表面促进细胞对表面的粘附。光反应性交联剂可以是异双官能的或含有两个光反应性基团。生物分子的光反应性类似物通过激活类似物的光反应性基团（例如通过将类似物暴露于紫外线辐射）而附着到基底表面。

6. 发明授权

US5731409A Polypeptides with type I collagen activity 失效
标题翻译：具有I型胶原活性的多肽
公开(公告)号：US5731409A
公开(公告)日：1998-03-24
申请号：US330599
申请日：1994-10-28
申请人： Gregg B. Fields , Leo T. Furcht , James B. McCarthy
发明人： Gregg B. Fields , Leo T. Furcht , James B. McCarthy
IPC分类号： A61K47/48 , C07K14/78 , A61K38/00 , C07K1/00 , C07K5/00 , C07K7/00
CPC分类号： A61K47/48292 , C07K14/78
摘要： Polypeptides are provided that have a sequence of at least about four amino acids corresponding substantially to an amino acid sequence within the triple-helical domain of Type I collagen. The polypeptides promote cell adhesion and/or cell migration. Cell culture substrates coated with the polypeptides are also provided. Prosthetic devices and methods for identifying and distinguishing cells of different types are also provided.
摘要翻译：提供多肽，其具有至少约四个氨基酸的序列，其基本上对应于I型胶原的三螺旋结构域内的氨基酸序列。多肽促进细胞粘附和/或细胞迁移。还提供了用多肽包被的细胞培养物底物。还提供了用于识别和区分不同类型的细胞的假体装置和方法。

7. 发明授权

US5770691A Discriminatory substrates for MMP hydrolysis 失效
标题翻译： MMP水解的歧视底物
公开(公告)号：US5770691A
公开(公告)日：1998-06-23
申请号：US464337
申请日：1995-06-05
申请人： Gregg B. Fields , Hideaki Nagase
发明人： Gregg B. Fields , Hideaki Nagase
IPC分类号： C07K7/06 , C12Q1/37 , A61K38/04 , A61K7/16 , A61K38/00
CPC分类号： C07K7/06 , C12Q1/37 , C12Q2337/22 , G01N2333/96486
摘要： A method of screening a sample for the presence of a matrix metalloproteinase employing discriminatory peptide substrates is provided. The method involves providing a peptide substrate of 6-14 amino acid residues containing at least one matrix metalloproteinase cleavage site. The peptide substrate contains Mca as a fluorogenic group and Lys(Dnp) as a quenching group separated by at least four amino acid residues, wherein the peptide substrate is specific for the matrix metalloproteinase of interest. The peptide substrate is combined with a sample containing at least one matrix metalloproteinase to form a mixture. The fluorescence of the mixture is monitored to determine if the matrix metalloproteinase of interest is present.
摘要翻译：提供了使用鉴别性肽底物筛选样品存在基质金属蛋白酶的方法。该方法包括提供含有至少一个基质金属蛋白酶切割位点的6-14个氨基酸残基的肽底物。肽底物含有作为荧光基团的Mca，并且由至少四个氨基酸残基分开的作为猝灭基团的Lys（Dnp），其中肽底物对感兴趣的基质金属蛋白酶是特异性的。将肽底物与含有至少一种基质金属蛋白酶的样品组合以形成混合物。监测混合物的荧光以确定感兴趣的基质金属蛋白酶是否存在。

8. 发明授权

US5726243A Mild solid-phase synthesis of aligned, branched triple-helical peptides 失效
标题翻译：对齐，支链三螺旋肽的轻度固相合成
公开(公告)号：US5726243A
公开(公告)日：1998-03-10
申请号：US675140
申请日：1996-07-03
申请人： Gregg B. Fields
发明人： Gregg B. Fields
IPC分类号： C07K1/04 , C07K14/78 , C07K17/06 , C07K1/06 , C08G69/10
CPC分类号： C07K17/06 , C07K1/04 , C07K14/78 , Y10S530/81 , Y10S530/812 , Y10S530/816
摘要： A triple-helical polypeptide of the formula: ##STR1## is provided wherein: Z is Hyp or Pro; each X and Y is an amino acid such that (Gly-X-Y).sub.m is a sequence of a collagen cell adhesion site; said X and Y may be the same or different and each (Gly-X-Y) may be the same or different; O is an amino acid having a single side-chain amino group; J is an amino acid capable of acting as a chromophore; U is an amino acid; u=0 or 1; n.ltoreq.30; m.ltoreq.30; m+n.ltoreq.30; and j.gtoreq.1. Methods of making these compounds and intermediates used in the methods, are also provided.
摘要翻译：提供下式的三螺旋多肽：其中：Z是Hyp或Pro; 每个X和Y是氨基酸，使得（Gly-X-Y）m是胶原细胞粘附位点的序列; 所述X和Y可以相同或不同，并且每个（Gly-X-Y）可以相同或不同; O是具有单个侧链氨基的氨基酸; J是能够作为发色团的氨基酸; U是氨基酸; u = 0或1; n / = 1。还提供了制备这些化合物和方法中使用的中间体的方法。

9. 发明申请

US20090062211A1 CONOPEPTIDES AND METHODS OF USE 审中-公开
标题翻译：配合及使用方法
公开(公告)号：US20090062211A1
公开(公告)日：2009-03-05
申请号：US12101002
申请日：2008-04-10
申请人： Frank Mari , Gregg B. Fields
发明人： Frank Mari , Gregg B. Fields
IPC分类号： A61K38/08 , C07K7/06 , C12N5/02
CPC分类号： C07K7/06 , A61K38/00 , C07K14/43504
摘要： Isolation, synthesis and therapeutic use of conotoxin and conophan compounds and related compositions including a new class of conopeptides including the modified amino acid D-γ-hydro-oxyvalinie (D-Hyv=V*) are described herein. These isolated peptides are the first known example of a naturally occurring polypeptide chain containing D-Hyv. The active peptides, termed γ-Hydroxyconophans are heavily hydroxylated small peptides. These peptides contain a definitive structural motif which is a double modification of the polypeptide chain (γ-D-OH-Hyv-Trp).
摘要翻译：本文描述了分泌，合成和治疗用途的萜类毒素和科普汉化合物以及相关组合物，包括新类型的包括修饰的氨基酸D-γ-羟基氧化血红蛋白（D-Hyv = V *）的肽。这些分离的肽是含有D-Hyv的天然存在的多肽链的第一个已知实例。称为γ-羟基半胱氨酸的活性肽是高羟基化的小肽。这些肽含有确定的结构基序，其是多肽链（γ-D-OH-Hyv-Trp）的双重修饰。

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