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1. 发明申请

US20170007696A1 SUPRAMOLECULAR HYDROGEL OF FMLF-BASED MOLECULES AND USE THEREOF 审中-公开
标题翻译：基于FMLF的分子的分子水合物及其用途
公开(公告)号：US20170007696A1
公开(公告)日：2017-01-12
申请号：US15115385
申请日：2014-05-29
申请人： Brandeis University , Boston Children's Hospital
发明人： Fan ZHAO , Jingyu LI , Hongbo R. LUO , Bing XU
IPC分类号： A61K39/39 , C07K5/10 , C07K7/06 , C07K7/08 , C07K14/00 , A61K9/06 , A61K38/07 , A61K38/08 , A61K38/10 , A61K38/16 , A61K9/00 , C07K5/08 , A61K38/06
CPC分类号： A61K39/39 , A01N37/46 , A61K9/0019 , A61K9/06 , A61K38/00 , A61K38/06 , A61K38/07 , A61K38/08 , A61K38/10 , A61K38/16 , A61K45/06 , A61K2039/55516 , A61K2039/572 , A61K2039/575 , C07K5/0802 , C07K5/1002 , C07K7/06 , C07K7/08 , C07K14/00 , C07K14/001 , C07K2319/00 , Y02A50/478 , A01N25/04 , A01N25/34
摘要： The invention relates to the application of peptides that can self-assemble to form supramolecular nanofibrils and hydrogels, hydrogel compositions containing the self-assembled supramolecular nanofibrils, and methods of uses and making the hydrogel compositions.
摘要翻译：本发明涉及能够自组装形成超分子纳米原纤维和水凝胶的肽的应用，含有自组装超分子纳米原纤维的水凝胶组合物，以及使用和制备水凝胶组合物的方法。

2. 发明申请

US20220112240A1 BRANCHED PEPTIDES FOR ENZYMATIC ASSEMBLY AND MITOCHONDRIA DRUG DELIVERY 有权
公开(公告)号：US20220112240A1
公开(公告)日：2022-04-14
申请号：US17537418
申请日：2021-11-29
申请人： BRANDEIS UNIVERSITY
发明人： Hongjian HE , Bing XU
IPC分类号： C07K7/06 , C07K7/08 , A61K9/107 , C07K19/00 , A61P9/00 , A61P35/00
摘要： The present invention relates to a branched peptide that includes a first peptide chain and a second peptide chain having its C-terminal amino acid covalently linked to a sidechain of an amino acid residue of the first peptide chain, wherein the first peptide chain includes a plurality of aromatic amino acids and, optionally, an aromatic group linked to an amino terminus of the first peptide chain; and the second peptide chain includes a plurality of hydrophilic amino acids and an enzyme cleavage site. Pharmaceutical compositions containing the branched peptide and one or more therapeutic agents in an aqueous medium are disclosed, where the branched peptides form micelle structures in the aqueous medium. Methods of using the pharmaceutical composition to deliver therapeutic agents, and for treating various disease conditions are also described.

3. 发明申请

US20200023065A1 ENZYMATICALLY ACTIVATABLE PEPTIDE-REDOX MODULATOR CONJUGATES AND USE THEREOF 审中-公开
公开(公告)号：US20200023065A1
公开(公告)日：2020-01-23
申请号：US16476183
申请日：2018-01-04
申请人： BRANDEIS UNIVERSITY
发明人： Bing XU
IPC分类号： A61K47/54 , A61K47/42 , C07K5/107 , A61P35/00
摘要： Disclosed are peptides capable of enzymatically-induced self-assembly to which is conjugated a redox modulator. These peptides are enzymatically responsive hydrogelators, and they can be used to form pericellular hydrogels/nanofibrils upon exposure to target cells that secrete or express a surface bound ectoenzyme having hydrolase activity suitable to induce peptide gelation. These materials, and compositions containing the same, can be used for inhibiting cancer cell migration, inhibiting cancer cell survival, and/or inhibiting cancer cell growth.

4. 发明申请

US20170037082A1 SYNTHETIC PEPTIDES, ENZYMATIC FORMATION OF PERICELLULAR HYDROGELS/NANOFIBRILS, AND METHODS OF USE 审中-公开
标题翻译：合成肽，环状水凝胶/纳米纤维的酶促形成及其使用方法
公开(公告)号：US20170037082A1
公开(公告)日：2017-02-09
申请号：US15303172
申请日：2015-04-09
申请人： BRANDEIS UNIVERSITY
发明人： Bing XU , Junfeng SHI , Yi KUANG
IPC分类号： C07K5/087 , G01N33/58 , G01N33/573 , A61K49/00
CPC分类号： C07K5/0812 , A61K49/0056 , C07K5/06078 , C07K5/1013 , C07K5/1016 , C07K14/001 , G01N33/573 , G01N33/582
摘要： Disclosed are peptides that contain up to about 35 amino acids, including a plurality of aromatic amino acid residues and either (i) an amino acid residue that is phosphorylated or sulfated, or (ii) an amino acid comprising an ester-moiety linked via peptide bond, or both (i) and (ii), wherein the peptide is capable of self-assembly to form nanofibrils in the presence of an enzyme that hydrolyzes the phosphate group, the sulfate group, or the ester-moiety. These peptides are enzymatically responsive hydrogelators, and they can be used to form pericellular hydrogels/nanofibrils upon exposure to target cells that secrete or express a surface bound ectoenzyme having hydrolase activity suitable to induce peptide gelation. These materials, and compositions containing the same, can be used for in vitro and in vivo cellular imaging, treating cancerous conditions, collecting a secretome from a cell upon which the pericellular hydrogels/nanofibrils form, and screening the collected secretome.
摘要翻译：公开了含有多至约35个氨基酸的肽，包括多个芳族氨基酸残基和（i）被磷酸化或硫酸化的氨基酸残基，或（ii）包含通过肽连接的酯部分的氨基酸键，或（i）和（ii）两者，其中肽在能水解磷酸基，硫酸基或酯部分的酶存在下能够自组装形成纳米原纤维。这些肽是酶促反应性水凝胶剂，并且它们可以用于在暴露于分泌或表达具有适于诱导肽凝胶化的水解酶活性的表面结合的外消旋体的靶细胞时形成细胞周围水凝胶/纳米原纤维。这些材料和含有它们的组合物可用于体外和体内细胞成像，治疗癌症，从形成细胞周围水凝胶/纳米原纤维的细胞收集分泌物，并筛选收集的分泌物。

5. 发明申请

US20160016994A1 INHIBITION OF TUMOR GROWTH WITH AGGREGATES OF SMALL MOLECULES 审中-公开
标题翻译：抑制肿瘤生长与小分子聚集
公开(公告)号：US20160016994A1
公开(公告)日：2016-01-21
申请号：US14773690
申请日：2014-03-06
申请人： BRANDEIS UNIVERSITY
发明人： Bing XU , Kuang YI
IPC分类号： C07K5/072
CPC分类号： C07K5/06121 , A61K31/195
摘要： Disclosed herein are fibrillar molecular aggregates, which are morphologically and phenotypically similar to oligomers of aberrant proteins. The molecular aggregates, formed by self-assembly of small hydrophobic molecules, prevent the growth of microtubules. This unprecedented mechanism of “self-assembly to interfere with self-organization” allows inhibition of the growth of cancer cells.
摘要翻译：本文公开了纤维状分子聚集体，其在形态学和表型上类似于异常蛋白质的寡聚体。通过小疏水分子的自组装形成的分子聚集体阻止了微管的生长。这种前所未有的“自组装干扰自组织”的机制允许抑制癌细胞的生长。

6. 发明申请

US20210128745A1 RAPID FORMATION OF SUPRAMOLECULAR HYDROGELS BY SHORT PEPTIDE AND BIOACTIVE SMALL MOLECULES 有权
公开(公告)号：US20210128745A1
公开(公告)日：2021-05-06
申请号：US16639467
申请日：2018-08-15
申请人： BRANDEIS UNIVERSITY
发明人： Bing XU , Huaimin WANG
IPC分类号： A61K47/69 , A61K45/06 , A61K39/39 , A61K9/00 , A61P35/00 , A61K31/573 , A61K31/704 , C07K7/06 , C07K7/08
摘要： Disclosed are a peptide capable of induced self-assembly by a bioactive molecule comprising a (i) hydrogelation-promoting amino acid sequence and (ii) an oligomerization sequence; compositions containing the peptide and, optionally, bioactive molecule; hydrogels formed thereby; and various methods of using the same

7. 发明申请

US20150306232A1 HYDROGELATORS COMPRISING D-AMINO ACIDS 审中-公开
标题翻译：包含D-氨基酸的氢化剂
公开(公告)号：US20150306232A1
公开(公告)日：2015-10-29
申请号：US14441773
申请日：2013-11-08
申请人： BRANDEIS UNIVERSITY
发明人： Bing XU , Jiayang LI , Kuang YI
IPC分类号： A61K47/42 , A61K9/00 , A61K31/192 , C07K5/107
CPC分类号： A61K47/42 , A61K9/0014 , A61K9/0092 , A61K9/06 , A61K31/192 , A61K31/196 , A61K31/337 , A61K31/403 , A61K31/407 , C07K5/1016
摘要： Described herein are compounds comprising an oligopeptide and a non-steroidal antiinflammatory agent. The compounds self-assemble into supramolecular hydrogels and can be used as topical treatments for inflammatory conditions, such as osteoarthritis. Also described herein are oligopeptides compounds made from D-amino acid residues that form supramolecular hydrogels. The compounds may be functionalized with active agents, such as anticancer therapeutic agents, antiinflammatory agents, or imaging agents, therefore providing new mechanisms for delivery of active agents.
摘要翻译：本文描述的是包含寡肽和非甾体抗炎剂的化合物。化合物自组装成超分子水凝胶，可用作炎性病症如骨关节炎的局部治疗。本文还描述了由形成超分子水凝胶的D-氨基酸残基制备的寡肽化合物。化合物可以用活性剂如抗癌治疗剂，抗炎剂或显像剂进行官能化，因此提供新的递送活性剂的机制。

8. 发明申请

US20220387610A1 PEPTIDE-CONJUGATED PRODRUGS 有权
公开(公告)号：US20220387610A1
公开(公告)日：2022-12-08
申请号：US17761496
申请日：2020-09-18
申请人： BRANDEIS UNIVERSITY
发明人： Bing XU , Jiaqing WANG
IPC分类号： A61K47/64 , A61P31/04
摘要： The present disclosure relates to a conjugated prodrug comprising a peptide conjugated to an antibiotic molecules via a cleavable linker and pharmaceutical compositions thereof. Also disclosed are methods of enhancing the intracellular concentration of an antibiotic agent in a bacterium and methods of treating a patient for a bacterial infection.

9. 发明申请

US20200281854A1 BRANCHED PEPTIDES FOR ENZYMATIC ASSEMBLY AND MITOCHONDRIA DRUG DELIVERY 审中-公开
公开(公告)号：US20200281854A1
公开(公告)日：2020-09-10
申请号：US16648295
申请日：2018-09-18
申请人： BRANDEIS UNIVERSITY
发明人： Hongjian HE , Bing XU
IPC分类号： A61K9/107 , C07K7/06 , A61P35/00 , A61K47/42 , A61K47/69 , A61K31/704
摘要： The present invention relates to a branched peptide that includes a first peptide chain and a second peptide chain having its C-terminal amino acid covalently linked to a sidechain of an amino acid residue of the first peptide chain, wherein the first peptide chain includes a plurality of aromatic amino acids and, optionally, an aromatic group linked to an amino terminus of the first peptide chain; and the second peptide chain includes a plurality of hydrophilic amino acids and an enzyme cleavage site. Pharmaceutical compositions containing the branched peptide and one or more therapeutic agents in an aqueous medium are disclosed, where the branched peptides form micelle structures in the aqueous medium. Methods of using the pharmaceutical composition to deliver therapeutic agents, and for treating various disease conditions are also described.

10. 发明申请

US20190224330A1 AMINO ACID- AND PEPTIDE-STEROID CONJUGATES AND USE THEREOF 审中-公开
公开(公告)号：US20190224330A1
公开(公告)日：2019-07-25
申请号：US16097325
申请日：2017-04-28
申请人： BRANDEIS UNIVERSITY
发明人： Huaimin WANG , Bing XU
IPC分类号： A61K47/64 , A61K47/54 , A61P35/04
摘要： This invention relates to a conjugate of formula (I): (A-Z1-)n-Q-Z2-D (I), wherein Z1, Z2, Q, A, D, and n are as described herein. This invention also relates to a pharmaceutical composition including a pharmaceutically acceptable carrier and a conjugate of formula (I). This invention also relates to a method making a conjugate of formula (I), and the use of the conjugate for treating cancerous conditions, modulating cell membrane microheterogeneity, stimulating an immunoresponse, and forming a network on or near the inner or outer surface of target cells.

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