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公开(公告)号:US20210269863A1
公开(公告)日:2021-09-02
申请号:US17323695
申请日:2021-05-18
发明人: Casey J. Krusemark , Kyle Denton , Dongwook Kim , Rachael Jetson
IPC分类号: C12Q1/6823 , C12N15/10 , C07H21/04 , C12Q1/686 , G01N33/68
摘要: Systems, kits, and methods for detecting and quantifying proteomic activity using DNA-encoded probes are provided, where the proteomic activity may be enzymatic activity or ligand binding affinity. Such systems and methods encode quantitative proteomic activity information into DNA sequence populations and utilize DNA-linked substrates or ligands as activity probes. The systems, kits, and methods that are directed to detecting ligand affinity further include crosslinking steps to ensure the integrity of the DNA-linked ligands during purification and washing. Signal detection involves the chemical manipulation of a probe population downstream of sample exposure and application of purifying, selective pressure for desired products. Selection-induced changes in DNA abundance between the initial pool and the purified pool indicate sample activity.
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公开(公告)号:US20220098643A1
公开(公告)日:2022-03-31
申请号:US17472756
申请日:2021-09-13
发明人: Casey J. Krusemark , Bo Cai
摘要: The present application relates to an assay method using affinity crosslinking of DNA-linked ligands to proteins to enable small molecule screening and determination of apparent affinity constants of ligands to the proteins. This method has been applied to determine 96 compounds' dissociation constants to a protein target simultaneously, and directly determine a compound's IC50 against five protein targets concurrently in crude cell lysates. Additionally, this approach was used to screen a Library of Pharmacologically Active Compounds (LOPAC) library against dihydrofolate reductase (eDHFR), enabling the discovery of a novel eDHFR inhibitor (IC50=7.9 μM). An assay kit and the method of uses are within the scope of this disclosure.
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公开(公告)号:US12071652B2
公开(公告)日:2024-08-27
申请号:US17323695
申请日:2021-05-18
发明人: Casey J. Krusemark , Kyle Denton , Dongwook Kim , Rachael Jetson
IPC分类号: C12Q1/6823 , C07H21/04 , C12N15/10 , C12Q1/686 , G01N33/68
CPC分类号: C12Q1/6823 , C07H21/04 , C12N15/1065 , C12N15/1075 , C12Q1/686 , G01N33/68 , C12N2310/3517 , C12N2320/10 , C12N15/1075 , C12Q2521/537 , C12Q2563/179 , C12Q1/6823 , C12Q2521/537 , C12Q2563/179
摘要: Systems, kits, and methods for detecting and quantifying proteomic activity using DNA-encoded probes are provided, where the proteomic activity may be enzymatic activity or ligand binding affinity. Such systems and methods encode quantitative proteomic activity information into DNA sequence populations and utilize DNA-linked substrates or ligands as activity probes. The systems, kits, and methods that are directed to detecting ligand affinity further include crosslinking steps to ensure the integrity of the DNA-linked ligands during purification and washing. Signal detection involves the chemical manipulation of a probe population downstream of sample exposure and application of purifying, selective pressure for desired products. Selection-induced changes in DNA abundance between the initial pool and the purified pool indicate sample activity.
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公开(公告)号:US20230257421A1
公开(公告)日:2023-08-17
申请号:US18103694
申请日:2023-01-31
CPC分类号: C07K7/06 , A61P35/02 , C07K5/1016 , A61K38/00
摘要: The present invention relates to series of peptidomimetic compounds selectively targeting CBX8 of polycomb chromobox protein homolog proteins. Pharmaceutical compositions of those compounds and methods of using them in the treatment of diseases involved CBX8 pharmacology, including various cancers and leukemia, by administering therapeutically effective amounts of such compound alone or together with other therapeutics, are within the scope of this disclosure.
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公开(公告)号:US11028427B2
公开(公告)日:2021-06-08
申请号:US15753317
申请日:2016-08-18
IPC分类号: C12Q1/6823 , C12N15/10 , C07H21/04 , C12Q1/686 , G01N33/68
摘要: Systems, kits, and methods for detecting and quantifying proteomic activity using DNA-encoded probes are provided, where the proteomic activity may be enzymatic activity or ligand binding affinity. Such systems and methods encode quantitative proteomic activity information into DNA sequence populations and utilize DNA-linked substrates or ligands as activity probes. The systems, kits, and methods that are directed to detecting ligand affinity further include crosslinking steps to ensure the integrity of the DNA-linked ligands during purification and washing. Signal detection involves the chemical manipulation of a probe population downstream of sample exposure and application of purifying, selective pressure for desired products. Selection-induced changes in DNA abundance between the initial pool and the purified pool indicate sample activity.
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公开(公告)号:US11566046B2
公开(公告)日:2023-01-31
申请号:US16894036
申请日:2020-06-05
摘要: The present invention relates to series of peptidomimetic compounds selectively targeting CBX8 of polycomb chromobox protein homolog proteins. Pharmaceutical compositions of those compounds and methods of using them in the treatment of diseases involved CBX8 pharmacology, including various cancers and leukemia, by administering therapeutically effective amounts of such compound alone or together with other therapeutics, are within the scope of this disclosure.
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公开(公告)号:US20180237831A1
公开(公告)日:2018-08-23
申请号:US15753317
申请日:2016-08-18
IPC分类号: C12Q1/6823 , G01N33/68 , C12Q1/686 , C07H21/04 , C12N15/10
CPC分类号: C12Q1/6823 , C07H21/04 , C12N15/1065 , C12N15/1075 , C12N2310/3517 , C12N2320/10 , C12Q1/686 , G01N33/68 , C12Q2521/537 , C12Q2563/179
摘要: Systems, kits, and methods for detecting and quantifying proteomic activity using DNA-encoded probes are provided, where the proteomic activity may be enzymatic activity or ligand binding affinity. Such systems and methods encode quantitative proteomic activity information into DNA sequence populations and utilize DNA-linked substrates or ligands as activity probes. The systems, kits, and methods that are directed to detecting ligand affinity further include crosslinking steps to ensure the integrity of the DNA-linked ligands during purification and washing. Signal detection involves the chemical manipulation of a probe population downstream of sample exposure and application of purifying, selective pressure for desired products. Selection-induced changes in DNA abundance between the initial pool and the purified pool indicate sample activity.
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