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公开(公告)号：US20180051055A1
公开(公告)日：2018-02-22
申请号：US15561230
申请日：2016-03-25
申请人： H. LEE MOFFITT CANCER CENTER AND RESEARCH INTITUTE, INC. , THE ARIZONA BOARD OF REGENTS ON BEHALF OF THE UNIVERSITY OF ARIZONA , UNIVERSITY OF SOUTH FLORIDA
发明人： David L. Morse , Josef Vagner , Mark McLaughlin , Robert Gillies , Amanda Huynh , Michael Doligalski
CPC分类号： C07K5/081 , A61K49/0019 , A61K49/0032 , A61K49/0052 , A61K51/0497
摘要： Disclosed are monoacylated Toll-like receptor 2 ligands which can be used in both the development of targeted agents for the imaging and treatment of pancreatic cancer as well as other cancers, and as an adjuvant for cancer immunotherapy. The monoacylated compounds disclosed herein have a higher binding affinity for TLR2 relative to a known potent diacylated agonists, but only −½ the bioactivity. Competition of the monoacylated compound with the diacylated compound for binding TLR2 was confirmed. Hence, the reported monoacylated compounds are inhibitors/antagonists of TLR2 activation.
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公开(公告)号：US11414455B2
公开(公告)日：2022-08-16
申请号：US17063158
申请日：2020-10-05
申请人： H. LEE MOFFITT CANCER CENTER AND RESEARCH INSTITUTE, INC. , THE ARIZONA BOARD OF REGENTS ON BEHALF OF THE UNIVERSITY OF ARIZONA , UNIVERSITY OF SOUTH FLORIDA
发明人： David L. Morse , Josef Vagner , Mark McLaughlin , Robert Gillies , Amanda Huynh , Michael Doligalski
摘要： Disclosed are monoacylated Toll-like receptor 2 ligands which can be used in both the development of targeted agents for the imaging and treatment of pancreatic cancer as well as other cancers, and as an adjuvant for cancer immunotherapy. The monoacylated compounds disclosed herein have a higher binding affinity for TLR2 relative to a known potent diacylated agonists, but only −½ the bioactivity. Competition of the monoacylated compound with the diacylated compound for binding TLR2 was confirmed. Hence, the reported monoacylated compounds are inhibitors/antagonists of TLR2 activation.
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公开(公告)号：US20210230219A1
公开(公告)日：2021-07-29
申请号：US17063158
申请日：2020-10-05
申请人： H. LEE MOFFITT CANCER CENTER AND RESEARCH INSTITUTE, INC. , THE ARIZONA BOARD OF REGENTS ON BEHALF OF THE UNIVERSITY OF ARIZONA , UNIVERSITY OF SOUTH FLORIDA
发明人： David L. Morse , Josef Vagner , Mark McLaughlin , Robert Gillies , Amanda Huynh , Michael Doligalski
摘要： Disclosed are monoacylated Toll-like receptor 2 ligands which can be used in both the development of targeted agents for the imaging and treatment of pancreatic cancer as well as other cancers, and as an adjuvant for cancer immunotherapy. The monoacylated compounds disclosed herein have a higher binding affinity for TLR2 relative to a known potent diacylated agonists, but only −½ the bioactivity. Competition of the monoacylated compound with the diacylated compound for binding TLR2 was confirmed. Hence, the reported monoacylated compounds are inhibitors/antagonists of TLR2 activation.
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公开(公告)号：US10793595B2
公开(公告)日：2020-10-06
申请号：US16150496
申请日：2018-10-03
申请人： H. LEE MOFFITT CANCER CENTER AND RESEARCH INSTITUTE, INC. , THE ARIZONA BOARD OF REGENTS ON BEHALF OF THE UNIVERSITY OF ARIZONA , UNIVERSITY OF SOUTH FLORIDA
发明人： David L. Morse , Josef Vagner , Mark McLaughlin , Robert Gillies , Amanda Huynh , Michael Doligalski
摘要： Disclosed are monoacylated Toll-like receptor 2 ligands which can be used in both the development of targeted agents for the imaging and treatment of pancreatic cancer as well as other cancers, and as an adjuvant for cancer immunotherapy. The monoacylated compounds disclosed herein have a higher binding affinity for TLR2 relative to a known potent diacylated agonists, but only −½ the bioactivity. Competition of the monoacylated compound with the diacylated compound for binding TLR2 was confirmed. Hence, the reported monoacylated compounds are inhibitors/antagonists of TLR2 activation.
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公开(公告)号：US20190263857A1
公开(公告)日：2019-08-29
申请号：US16150496
申请日：2018-10-03
申请人： H. LEE MOFFITT CANCER CENTER AND RESEARCH INSTITUTE, INC. , THE ARIZONA BOARD OF REGENTS ON BEHALF OF THE UNIVERSITY OF ARIZONA , UNIVERSITY OF SOUTH FLORIDA
发明人： David L. Morse , Josef Vagner , Mark McLaughlin , Robert Gillies , Amanda Huynh , Michael Doligalski
摘要： Disclosed are monoacylated Toll-like receptor 2 ligands which can be used in both the development of targeted agents for the imaging and treatment of pancreatic cancer as well as other cancers, and as an adjuvant for cancer immunotherapy. The monoacylated compounds disclosed herein have a higher binding affinity for TLR2 relative to a known potent diacylated agonists, but only −½ the bioactivity. Competition of the monoacylated compound with the diacylated compound for binding TLR2 was confirmed. Hence, the reported monoacylated compounds are inhibitors/antagonists of TLR2 activation.
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公开(公告)号：US10118942B2
公开(公告)日：2018-11-06
申请号：US15561230
申请日：2016-03-25
申请人： H. LEE MOFFITT CANCER CENTER AND RESEARCH INSTITUTE, INC. , THE ARIZONA BOARD OF REGENTS ON BEHALF OF THE UNIVERSITY OF ARIZONA , UNIVERSITY OF SOUTH FLORIDA
发明人： David L. Morse , Josef Vagner , Mark McLaughlin , Robert Gillies , Amanda Huynh , Michael Doligalski
摘要： Disclosed are monoacylated Toll-like receptor 2 ligands which can be used in both the development of targeted agents for the imaging and treatment of pancreatic cancer as well as other cancers, and as an adjuvant for cancer immunotherapy. The monoacylated compounds disclosed herein have a higher binding affinity for TLR2 relative to a known potent diacylated agonists, but only −½ the bioactivity. Competition of the monoacylated compound with the diacylated compound for binding TLR2 was confirmed. Hence, the reported monoacylated compounds are inhibitors/antagonists of TLR2 activation.
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