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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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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：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：US11078235B2
公开(公告)日：2021-08-03
申请号：US16025382
申请日：2018-07-02
申请人： H. Lee Moffitt Cancer Center And Research Institute, Inc. , University of South Florida , The Scripps Research Institute , Modulation Therapeutics
发明人： Lori Hazlehurst , Christoph Rader , Xiuling Li , Mark McLaughlin
IPC分类号： C07K7/06 , C07K7/08 , C07K14/705 , C07K1/00 , A61K38/00
摘要： The present invention concerns cyclic compounds, compositions comprising the cyclic compounds, linkers, a method of preparing a carrying agent:cyclic compound adduct, a method for treating disorders such as proliferation disorders (e.g., malignancies), bone deficiency diseases, and autoimmune diseases, and a method for suppressing the growth of, or inducing apoptosis in, cells (e.g., malignant cells).
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公开(公告)号：US10556928B2
公开(公告)日：2020-02-11
申请号：US16157174
申请日：2018-10-11
发明人： Mark McLaughlin , Amod A. Sarnaik
摘要： The current invention pertains to stabilized peptoids or peptoid-peptide hybrids. The peptoids or peptoid-peptide hybrids are stabilized by side chain-side to side chain linkages and/or backbone cyclization. The current invention also provides a positional library scanning method for identification of peptoids or peptoid-peptide hybrids having a desired biological activity.
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公开(公告)号：US10197575B2
公开(公告)日：2019-02-05
申请号：US15300451
申请日：2015-03-31
发明人： Mark McLaughlin , Amod A. Sarnaik
摘要： The current invention pertains to stabilized peptoids or peptoid-peptide hybrids. The peptoids or peptoid-peptide hybrids are stabilized by side chain-side to side chain linkages and/or backbone cyclization. The current invention also provides a positional library scanning method for identification of peptoids or peptoid-peptide hybrids having a desired biological activity.
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公开(公告)号：US20180362583A1
公开(公告)日：2018-12-20
申请号：US16113869
申请日：2018-08-27
摘要： Integrin interaction inhibitors using a beta-turn promoter are described herein. These peptides are useful in treating cancer, such as multiple myeloma, by administering a therapeutically effective amount of the integrin interaction inhibitor. Data show that integrin interaction inhibitors act synergistically or additively interact with anti-proliferative agents such as doxorubicin, SAHA, arsenic trioxide, and etoposide.
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