Patents by Inventor Benjamin Cravatt
Benjamin Cravatt has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).
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Publication number: 20240131032Abstract: Disclosed herein are methods, pharmaceutical compositions, and vaccines for modulating an immune response. Also disclosed herein are methods, pharmaceutical compositions, and vaccines for inducing an immune response.Type: ApplicationFiled: October 15, 2020Publication date: April 25, 2024Inventors: Benjamin CRAVATT, Ekaterina VINOGRADOVA, Vincent CROWLEY, Xiaoyu ZHANG, Michael Andreas SCHAFROTH, Minoru YOKOYAMA, Dave REMILLARD, Bruno MELILLO, Stuart SCHREIBER
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Patent number: 11691984Abstract: Disclosed herein are methods and compounds for inducing DDB1- and CUL4-associated factor 16 (DCAF16)-mediated protein degradation in mammalian cells. In some embodiments, also disclosed herein are methods of modulating the substrate selectivity of a DCAF16-CUL4-RBX1-DDB1 complex (CRL4) for modulating protein degradation.Type: GrantFiled: October 11, 2019Date of Patent: July 4, 2023Assignee: THE SCRIPPS RESEARCH INSTITUTEInventors: Benjamin Cravatt, Vincent Crowley, Xiaoyu Zhang
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Publication number: 20210208141Abstract: Cells produce electrophilic products with the potential to modify and affect the function of proteins. Chemoproteomic methods have provided a means to qualitatively inventory proteins targeted by endogenous electrophiles; however, ascertaining the potency and specificity of these reactions to identify the most sensitive sites in the proteome to electrophilic modification requires more quantitative methods. Here, we describe a competitive activity-based profiling method for quantifying the reactivity of electrophilic compounds against 1000+ cysteines in parallel in the human proteome. Using this approach, we identify a select set of proteins that constitute “hot spots” for modification by various lipid-derived electrophiles, including the oxidative stress product 4-hydroxynonenal (HNE).Type: ApplicationFiled: September 15, 2020Publication date: July 8, 2021Inventors: Benjamin Cravatt, Chu Wang, Keriann Backus
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Patent number: 10782295Abstract: Cells produce electrophilic products with the potential to modify and affect the function of proteins. Chemoproteomic methods have provided a means to qualitatively inventory proteins targeted by endogenous electrophiles; however, ascertaining the potency and specificity of these reactions to identify the most sensitive sites in the proteome to electrophilic modification requires more quantitative methods. Here, we describe a competitive activity-based profiling method for quantifying the reactivity of electrophilic compounds against 1000+ cysteines in parallel in the human proteome. Using this approach, we identify a select set of proteins that constitute hot spots for modification by various lipid-derived electrophiles, including the oxidative stress product 4-hydroxnonenal (HNE).Type: GrantFiled: August 13, 2014Date of Patent: September 22, 2020Assignee: The Scripps Research InstituteInventors: Benjamin Cravatt, Chu Wang, Keriann Backus
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Publication number: 20200190105Abstract: Disclosed herein are methods and compounds for inducing DDB1- and CUL4-associated factor 16 (DCAF16)-mediated protein degradation in mammalian cells. In some embodiments, also disclosed herein are methods of modulating the substrate selectivity of a DCAF16-CUL4-RBX1-DDB1 complex (CRL4) for modulating protein degradation.Type: ApplicationFiled: October 11, 2019Publication date: June 18, 2020Inventors: Benjamin CRAVATT, Vincent CROWLEY, Xiaoyu ZHANG
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Publication number: 20160252509Abstract: Cells produce electrophilic products with the potential to modify and affect the function of proteins. Chemoproteomic methods have provided a means to qualitatively inventory proteins targeted by endogenous electrophiles; however, ascertaining the potency and specificity of these reactions to identify the most sensitive sites in the proteome to electrophilic modification requires more quantitative methods. Here, we describe a competitive activity-based profiling method for quantifying the reactivity of electrophilic compounds against 1000+ cysteines in parallel in the human proteome. Using this approach, we identify a select set of proteins that constitute hot spots for modification by various lipid-derived electrophiles, including the oxidative stress product 4-hydroxnonenal (HNE).Type: ApplicationFiled: August 13, 2014Publication date: September 1, 2016Inventors: Benjamin Cravatt, Chu Wang, Keriann Backus
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Patent number: 9249128Abstract: Serine hydrolases are implicated in malconditions such as cancer, central nervous system disorders, cardiovascular disorders, obesity, and metabolic disorders. Many serine hydrolases expressed in proteomic libraries are of unknown function in vivo. Compounds identified through library versus library screening can be used for treatment of malconditions associated with the specific serine hydrolase KIAA1363 (also known as AADACL1). A library of inhibitors of KIAA1363 was prepared and candidate compounds were identified as a potent inhibitors having submicromolar IC50 values. An exemplary compound of the invention was shown to be an effective inhibitor of prostate cancer pathogenesis. Other inhibitory compounds of the invention comprising fluorophore groups are shown to be effective in spatial and temporal localization of the serine hydrolase in cells and tissues.Type: GrantFiled: October 21, 2011Date of Patent: February 2, 2016Assignee: The Scripps Research InstituteInventors: Benjamin Cravatt, Daniel Nomura, Jae W. Chang
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Patent number: 9108930Abstract: The present invention provides inhibitors of a wide variety of serine hydrolase enzymes. The inhibitors of the present invention are N1- and N2-carbamoyl-1,2,3-triazole compounds such as those of Formula (I): in which N1, N2, and N3 are the nitrogen atoms at positions 1, 2, and 3, respectively, of the triazole ring, and R4, R5, R6 and R7 in Formula (I) are as described herein. Methods of inhibiting serine hydrolase enzymes and methods of preparing carbamoyl-1,2,3-triazole compounds also are described.Type: GrantFiled: April 5, 2012Date of Patent: August 18, 2015Assignee: The Scripps Research InstituteInventors: Benjamin Cravatt, Alexander Adibekian, Katsunori Tsuboi, Ku-Lung Hsu
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Publication number: 20140018318Abstract: The present invention provides inhibitors of a wide variety of serine hydrolase enzymes. The inhibitors of the present invention are N1- and N2-carbamoyl-1,2,3-triazole compounds such as those of Formula (I): in which N1, N2, and N3 are the nitrogen atoms at positions 1, 2, and 3, respectively, of the triazole ring, and R4, R5, R6 and R7 in Formula (I) are as described herein. Methods of inhibiting serine hydrolase enzymes and methods of preparing carbamoyl-1,2,3-triazole compounds also are described.Type: ApplicationFiled: April 5, 2012Publication date: January 16, 2014Applicant: The Scipps Research InstituteInventors: Benjamin Cravatt, Alexander Adibekian, Katsunori Tsuboi, Ku-Lung Hsu
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Publication number: 20130281453Abstract: Serine hydrolases are implicated in malconditions such as cancer, central nervous system disorders, cardiovascular disorders, obesity, and metabolic disorders. Many serine hydrolases expressed in proteomic libraries are of unknown function in vivo. Compounds identified through library versus library screening can be used for treatment of malconditions associated with the specific serine hydrolase KIAA1363 (also known as AADACL1). A library of inhibitors of KIAA1363 was prepared and candidate compounds were identified as a potent inhibitors having submicromolar IC50 values. An exemplary compound of the invention was shown to be an effective inhibitor of prostate cancer pathogenesis. Other inhibitory compounds of the invention comprising fluorophore groups are shown to be effective in spatial and temporal localization of the serine hydrolase in cells and tissues.Type: ApplicationFiled: October 21, 2011Publication date: October 24, 2013Applicant: The Scripps Research InstituteInventors: Benjamin Cravatt, Daniel Nomura, Jae W. Chang, Raymond E. Moellering, Dan Bachovehin, Weiwei Li
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Publication number: 20050287594Abstract: The present invention provides methods for analyzing proteomes, as cells or lysates. The analysis is based on the use of probes that have specificity to the active form of proteins, particularly enzymes and receptors. The probes can be identified in different ways. In accordance with the present invention, a method is provided for generating and screening compound libraries that are used for the identification of lead molecules, and for the parallel identification of their biological targets. By appending specific functionalities and/or groups to one or more binding moieties, the reactive functionalities gain binding affinity and specificity for particular proteins and classes of proteins. Such libraries of candidate compounds, referred to herein as activity-based probes, or ABPs, are used to screen for one or more desired biological activities or target proteins.Type: ApplicationFiled: December 15, 2000Publication date: December 29, 2005Inventors: Benjamin Cravatt, Erik Sorensen, Matthew Patricelli, Martha Lovato, Gregory Adam
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Publication number: 20050266505Abstract: Activity-based compositions for analyzing metalloproteases are disclosed, where the compositions include a chemical compound including a hydroxamate moiety and a benzophenone moiety. Methods for synthesizing these compounds are also disclosed, as well as methods of using them for determining the bioactivity of a compositions comprising active compounds toward a metalloproteases and for determining the potency of an inhibitor against a metalloprotease.Type: ApplicationFiled: June 1, 2005Publication date: December 1, 2005Applicant: THE SCRIPPS RESEARCH INSTITUTEInventors: Benjamin Cravatt, Alan Saghatelian, Nadim Jessani, Arul Joseph