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公开(公告)号：US11834520B2
公开(公告)日：2023-12-05
申请号：US16766201
申请日：2018-12-13
摘要： This disclosure features structurally-stabilized and/or cysteine-reactive peptide inhibitors for selective targeting of BFL-1, or dual targeting of BFL-1 and MCL-1. Also disclosed are methods of using such structurally-stabilized and cysteine-reactive peptides in the treatment of BFL-1- and/or MCL-1-expressing or -dependent cancers or diseases of cellular excess (e.g., autoimmune or inflammatory conditions). Also provided are combination therapies comprising such structurally-stabilized and/or cysteine-reactive peptides and inhibitors of the DNA damage response pathway, such as an ATM kinase inhibitor, ATR kinase inhibitor, CHK1/2 inhibitor, or PARP inhibitor; or an inhibitor of MCL-1, or a selective inhibitor of BCL-2, or an inhibitor of BCL-2/BCL-XL, for the treatment of BFL-1-expressing or -dependent cancers (e.g., AML), BFL-1 and MCL-1-expressing or -dependent cancers, or diseases of cellular excess (e.g., autoimmune or inflammatory conditions).
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公开(公告)号：US20230183309A1
公开(公告)日：2023-06-15
申请号：US17786157
申请日：2020-12-18
发明人： Loren D. Walensky , Gregory H. Bird
IPC分类号： C07K14/605 , A61P3/10 , A61K9/00
CPC分类号： C07K14/605 , A61K9/0019 , A61P3/10
摘要： This disclosure features structurally-stabilized peptides that target glucagon-like peptide 1 receptor (GLP-1R), compositions comprising same, and methods for using such peptides in the treatment of diabetes, hyperglycemia, cardiovascular disease, obesity, Alzheimer’s disease, Huntington’s disease, and other conditions that can benefit from increased GLP-1 agonist activity and in increasing cAMP levels
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公开(公告)号：US20230132372A9
公开(公告)日：2023-04-27
申请号：US17387888
申请日：2021-07-28
发明人： Craig Braun , Wilhelm Haas , Steven P. Gygi , Gregory H. Bird , Loren D. Walensky , Martin Helmut Wuhr , Brian K. Erickson
IPC分类号： G01N33/58 , C07D207/46 , C07C237/22 , C07K1/13 , C07K5/02 , G01N33/68
摘要： In some embodiments, a mass spectrometry tag may comprise a linker region, a mass balance region, and a reporter region. The mass spectrometry tag may be configured to fragment in a mass spectrometer via an energy dependent process to produce multiple reporter molecules. For example, the reporter region of the tag may be configured to produce at least two reporter molecules via fragmentation. In some embodiments, one or more regions of the tag may comprise at least one heavy isotope. In some such embodiments, the ability to fragment into multiple reporter molecules as well as the placement and/or number of heavy isotope(s) allows the mass spectrometry tag to be distinguished from other similar mass spectrometry tags. In some such embodiments, the ability to distinguish between tags having the same or substantially similar total mass to charge ratio and reporter region mass may allow the system to have a greater multiplexing capacity than conventional systems.
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公开(公告)号：US11466064B2
公开(公告)日：2022-10-11
申请号：US16326493
申请日：2017-08-25
发明人： Rosalind Segal , Loren D. Walensky , Lisa Vaughn Goodrich , Sarah Elizabeth Raissi , Maria F. Murphy , Gregory H. Bird
IPC分类号： A61K38/16 , A61K38/10 , A61K38/00 , A61P25/04 , A61K38/04 , C07K5/00 , C07K7/00 , C07K16/00 , C07K17/00 , C07K14/47 , A61P35/00 , A61K31/337 , A61P25/02 , C07K7/08 , A61K45/06 , A61K38/17
摘要： Compositions and methods are provided for the treatment or prevention of chemotherapy-induced peripheral neuropathy and hearing loss in a subject in need thereof. The methods involve administering to the subject a bclw protein, a BH4 domain-containing fragment thereof, or a bclw mimetic. Also provided are exemplary bclw mimetics.
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公开(公告)号：US20210002336A1
公开(公告)日：2021-01-07
申请号：US16876779
申请日：2020-05-18
摘要： The invention provides structurally-constrained peptides by hydrocarbon stapling of a BCL9 HD2 helix for use as a therapeutic agent. The invention further provides methods and kits for use of the structurally-constrained peptide of the instant invention. The invention is based, at least in part, on the results provided herein demonstrating that hydrocarbon stapled helical peptides display excellent proteolytic, acid, and thermal stability, restore the native helical structure of the peptide, possess superior pharmacokinetic properties compared to the corresponding unmodified peptides, and are highly effective in binding to β-catenin in vitro, in cellulo, and in vivo, disrupting the BCL-9/β-catenin interaction, and thereby interfering with deregulated Wnt/β-catenin signaling for therapeutic benefit in a variety of human diseases including human cancer.
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公开(公告)号：US10308926B2
公开(公告)日：2019-06-04
申请号：US14772143
申请日：2014-03-13
发明人： Loren D. Walensky , Gregory H. Bird , Woojin Kim , Stuart Orkin
IPC分类号： C12N9/96 , A61K38/00 , A61K35/00 , A61K38/12 , C07K5/00 , C07K7/00 , C07K16/00 , C07K17/00 , C07K14/47 , C12N9/10
摘要： Provided herein are polypeptides containing stabilized therapeutic peptides related to enhancer of zeste homolog 2 (EZH2), histone lysine N-methyltransferase. Also provided are compositions containing these polypeptides and methods of using such peptides in the treatment of cancer that include administering to a subject one of the polypeptides.
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公开(公告)号：US11982674B2
公开(公告)日：2024-05-14
申请号：US17387888
申请日：2021-07-28
发明人： Craig Braun , Wilhelm Haas , Steven P. Gygi , Gregory H. Bird , Loren D. Walensky , Martin Helmut Wuhr , Brian K. Erickson
IPC分类号： C07D207/46 , C07C237/22 , C07K1/13 , C07K5/02 , G01N33/58 , G01N33/68
CPC分类号： G01N33/58 , C07C237/22 , C07D207/46 , C07K1/13 , C07K5/0202 , G01N33/6848 , C07B2200/07 , G01N2458/15
摘要： In some embodiments, a mass spectrometry tag may comprise a linker region, a mass balance region, and a reporter region. The mass spectrometry tag may be configured to fragment in a mass spectrometer via an energy dependent process to produce multiple reporter molecules. For example, the reporter region of the tag may be configured to produce at least two reporter molecules via fragmentation. In some embodiments, one or more regions of the tag may comprise at least one heavy isotope. In some such embodiments, the ability to fragment into multiple reporter molecules as well as the placement and/or number of heavy isotope(s) allows the mass spectrometry tag to be distinguished from other similar mass spectrometry tags. In some such embodiments, the ability to distinguish between tags having the same or substantially similar total mass to charge ratio and reporter region mass may allow the system to have a greater multiplexing capacity than conventional systems.
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公开(公告)号：US20210070802A1
公开(公告)日：2021-03-11
申请号：US16766201
申请日：2018-12-13
IPC分类号： C07K7/08
摘要： This disclosure features structurally-stabilized and/or cysteine-reactive peptide inhibitors for selective targeting of BFL-1, or dual targeting of BFL-1 and MCL-1. Also disclosed are methods of using such structurally-stabilized and cysteine-reactive peptides in the treatment of BFL-1- and/or MCL-1-expressing or -dependent cancers or diseases of cellular excess (e.g., autoimmune or inflammatory conditions). Also provided are combination therapies comprising such structurally-stabilized and/or cysteine-reactive peptides and inhibitors of the DNA damage response pathway, such as an ATM kinase inhibitor, ATR kinase inhibitor, CHK1/2 inhibitor, or PARP inhibitor; or an inhibitor of MCL-1, or a selective inhibitor of BCL-2, or an inhibitor of BCL-2/BCL-XL, for the treatment of BFL-1-expressing or -dependent cancers (e.g., AML), BFL-1 and MCL-1-expressing or -dependent cancers, or diseases of cellular excess (e.g., autoimmune or inflammatory conditions).
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公开(公告)号：US20200231638A1
公开(公告)日：2020-07-23
申请号：US16551102
申请日：2019-08-26
摘要： The present invention provides methods of designing and making structurally stabilized anti-microbial peptides for the prophylaxis and treatment of infection. Methods are also disclosed for designing stabilized anti-microbial peptides that are selectively lytic/cytotoxic to bacteria, allowing for internal use of anti-microbial peptides without mammalian membrane disruption and cytotoxicity.
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公开(公告)号：US10464975B2
公开(公告)日：2019-11-05
申请号：US15201235
申请日：2016-07-01
摘要： The present invention provides methods of designing and making structurally stabilized anti-microbial peptides for the prophylaxis and treatment of infection. Methods are also disclosed for designing stabilized anti-microbial peptides that are selectively lytic/cytotoxic to bacteria, allowing for internal use of anti-microbial peptides without mammalian membrane disruption and cytotoxicity.
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