Patents by Inventor Stephen B. H. Kent
Stephen B. H. Kent 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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Methods and Compositions for Identifying D-Peptidic Compounds that Specifically Bind Target Proteins
Publication number: 20160223560Abstract: Methods and compositions for identifying D-peptidic compounds that specifically bind target proteins are provided. Aspects of the methods include screening libraries of 20 residue or more L-peptidic compounds for specific binding to 40 residue or more D-target proteins. Once a L-peptidic compound has been identified that specifically binds to the D-target protein, the D-enantiomer of that compound may be produced.Type: ApplicationFiled: February 1, 2016Publication date: August 4, 2016Inventors: Dana Ault-Riche, Stephen B.H. Kent, Sachdev S. Sidhu, Maruti Uppalapati -
Methods and compositions for identifying D-peptidic compounds that specifically bind target proteins
Patent number: 9285372Abstract: Methods and compositions for identifying D-peptidic compounds that specifically bind target proteins are provided. Aspects of the methods include screening libraries of 20 residue or more L-peptidic compounds for specific binding to 40 residue or more D-target proteins. Once a L-peptidic compound has been identified that specifically binds to the D-target protein, the D-enantiomer of that compound may be produced.Type: GrantFiled: November 10, 2011Date of Patent: March 15, 2016Assignees: Reflexion Pharmaceuticals, Inc., The Governing Council of the University of TorontoInventors: Dana Ault-Riche, Stephen B. H. Kent, Sachdev S. Sidhu, Maruti Uppalapati -
Patent number: 8618049Abstract: Compositions and methods related to ester insulin or derivatives thereof are provided. The compositions include GluA4-ThrB30 ester insulin, in which side chains of GluA4 and ThrB30 of native human insulin or an insulin analogue such as insulin lispro are covalently linked via a single ester bond. The ester insulin is efficiently folded, forming the desired disulfides. The ThrB30-GluA4 ester bond can be cleaved in vitro or in vivo to give the desired folded insulin with full biological activity. The ester insulin is readily prepared by total chemical synthesis, and amendable to cost-effective, large scale manufacturing. Also provided are pharmaceutical compositions and kits for use in practicing the subject methods. Also provided are methods of using the subject compositions and kits in the treatment of a variety of different disease conditions, particularly glucose metabolic disorders such as diabetes and obesity.Type: GrantFiled: September 7, 2010Date of Patent: December 31, 2013Inventors: Stephen B. H. Kent, Youhei Soma
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Publication number: 20120220522Abstract: Compositions and methods related to ester insulin or derivatives thereof are provided. The compositions include GluA4-ThrB30 ester insulin, in which side chains of GluA4 and ThrB30 of native human insulin or an insulin analogue such as insulin lispro are covalently linked via a single ester bond. The ester insulin is efficiently folded, forming the desired disulfides. The ThrB30-GluA4 ester bond can be cleaved in vitro or in vivo to give the desired folded insulin with full biological activity. The ester insulin is readily prepared by total chemical synthesis, and amendable to cost-effective, large scale manufacturing. Also provided are pharmaceutical compositions and kits for use in practicing the subject methods. Also provided are methods of using the subject compositions and kits in the treatment of a variety of different disease conditions, particularly glucose metabolic disorders such as diabetes and obesity.Type: ApplicationFiled: September 7, 2010Publication date: August 30, 2012Inventors: Stephen B.H. Kent, Yohei Soma
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METHODS AND COMPOSITIONS FOR IDENTIFYING D-PEPTIDIC COMPOUNDS THAT SPECIFICALLY BIND TARGET PROTEINS
Publication number: 20120178643Abstract: Methods and compositions for identifying D-peptidic compounds that specifically bind target proteins are provided. Aspects of the methods include screening libraries of 20 residue or more L-peptidic compounds for specific binding to 40 residue or more D-target proteins. Once a L-peptidic compound has been identified that specifically binds to the D-target protein, the D-enantiomer of that compound may be produced.Type: ApplicationFiled: November 10, 2011Publication date: July 12, 2012Inventors: DANA AULT-RICHE, STEPHEN B. H. KENT, SACHDEV S. SIDHU, MARUTI UPPALAPATI -
Patent number: 8034900Abstract: Water-soluble thioester and selenoester compounds, their generators, as well as methods for making and using the same, are provided. The subject thioester and selenoester compounds are characterized by including an amino acid synthon having a C-terminal group bonded to a water-soluble polymer through a thioester or selenoester linkage. Solid phase resins and protocols for generating the subject compounds are also provided. The subject water soluble thioester and selenoester compounds and generators find use in a variety of different applications, including thioester or selenoester mediated chemical ligation reactions.Type: GrantFiled: December 30, 2003Date of Patent: October 11, 2011Assignee: Amylin Pharmaceuticals, Inc.Inventors: Leslie Philip Miranda, Stephen B. H. Kent
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Patent number: 7482425Abstract: The present invention relates to methods and compositions for lipid matrix-assisted chemical ligation and synthesis of membrane polypeptides that are incorporated in a lipid matrix. The invention is exemplified in production of a prefolded membrane polypeptide embedded within a lipid matrix via stepwise chemoselective chemical ligation of unprotected peptide segments, where at least one peptide segment is embedded in a lipid matrix. Any chemoselective reaction chemistry amenable for ligation of unprotected peptide segments can be employed. Suitable lipid matrices include liposomes, micelles, cell membrane patches and optically isotropic cubic lipidic phase matrices. Prefolded synthetic and semi-synthetic membrane polypeptides synthesized according to the methods and compositions of the invention also permit site-specific incorporation of one or more detectable moieties, such as a chromophore, which can be conveniently introduced during synthesis.Type: GrantFiled: July 30, 2002Date of Patent: January 27, 2009Assignee: Amylin Pharmaceuticals, Inc.Inventors: Gerd. G. Kochendoerfer, Christie L. Hunter, Stephen B. H. Kent, Paolo Botti
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Patent number: 7408026Abstract: Proteins of moderate size having native peptide backbones are produced by a method of native chemical ligation. Native chemical ligation employs a chemoselective reaction of two unprotected peptide segments to produce a transient thioester-linked intermediate. The transient thioester-linked intermediate then spontaneously undergoes a rearrangement to provide the full length ligation product having a native peptide bond at the ligation site. Full length ligation products are chemically identical to proteins produced by cell free synthesis. Full length ligation products may be refolded and/or oxidized, as allowed, to form native disulfide-containing protein molecules. The technique of native chemical ligation is employable for chemically synthesizing full length proteins.Type: GrantFiled: November 8, 2000Date of Patent: August 5, 2008Assignee: The Scripps Research InstituteInventors: Stephen B. H. Kent, Tom W. Muir, Philip E. Dawson
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Patent number: 7341874Abstract: This invention provides for novel methods of identifying covalent modifications of an amino acid residue in a polypeptide chain by detecting mass differences.Type: GrantFiled: March 2, 2004Date of Patent: March 11, 2008Assignees: The Rockefeller University, The Scripps Research InstituteInventors: Brian T. Chait, Ronald Beavis, Rong Wang, Stephen B. H. Kent
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Patent number: 7118737Abstract: The present invention relates to methods and compositions for modifying peptides, polypeptides and proteins with polymers, especially glyco-mimetic polymers, so as to improve their biological activity or pharmacokinetic properties. The invention further provides methods and uses for such polymer-modified peptides, polypeptides and proteins. The invention is particularly suitable for use in the synthesis of polymer-modified synthetic bioactive proteins (FIG. 1D), and of pharmaceutical compositions that contain such proteins.Type: GrantFiled: July 12, 2001Date of Patent: October 10, 2006Assignee: Amylin Pharmaceuticals, Inc.Inventors: Gerd G. Kochendoerfer, Paolo Botti, James A. Bradburne, Shiah-yun Chen, Sonya Cressman, Christie L. Hunter, Stephen B. H. Kent, Donald W. Low, Jill G. Wilken
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Patent number: 7094871Abstract: The present invention provides methods, apparatus and kits for synthesizing assembled peptides and proteins on a solid phase with sequential ligation of three or more unprotected peptide segments using chemoselective and mild ligation chemistries in aqueous solution. Also provided are methods of monitoring solid phase sequential ligation reactions using MALDI or electrospray ionization mass spectrometry of reaction products.Type: GrantFiled: November 15, 2001Date of Patent: August 22, 2006Assignee: Gryphon TherapeuticsInventors: Lynne Canne, Stephen B. H. Kent, Reyna Simon
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Patent number: 7030218Abstract: The present invention concerns methods and compositions for extending the technique of native chemical ligation of a wider range of peptides, polypeptides, other polymers and other molecules via an amide bond (see FIG. 1). The invention further provides methods and uses for such proteins and derivatized proteins. The invention is particularly suitable for use in the synthesis of optionally polymer-modified, synthetic bioactive proteins, and of pharmaceutical compositions that contain such proteins.Type: GrantFiled: July 12, 2001Date of Patent: April 18, 2006Assignee: Gryphon TherapeuticsInventors: Christie L. Hunter, Paolo Botti, James A. Bradburne, Shiah-yun Chen, Sonya Cressman, Stephen B. H. Kent, Gerd G. Kochendoerfer, Donald W. Low
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Patent number: 7030217Abstract: The present invention provides methods, apparatus and kits for synthesizing assembled peptides and proteins on a solid phase with sequential ligation of three or more unprotected peptide segments using chemoselective and mild ligation chemistries in aqueous solution. Also provided are methods of monitoring solid phase sequential ligation reactions using MALDI or electrospray ionization mass spectrometry of reaction products.Type: GrantFiled: November 15, 2001Date of Patent: April 18, 2006Assignee: Gryphon Therapeutics, Inc.Inventors: Lynne Canne, Stephen B. H. Kent, Reyna Simon
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Patent number: 6977292Abstract: The invention is directed to nucleophile-stable thioester generating compounds comprising a carboxyester thiol. The compounds have wide applicability in organic synthesis, including the generation of peptide-, polypeptide- and other polymer-thioesters. The invention is particularly useful for generating activated-thioesters from precursors that are made under conditions in which strong nucleophiles are employed, such as peptides or polypeptides made using Fmoc SPPS, as well as multi-step ligation or conjugation schemes that require (or benefit from the use of) compatible selective approaches for directing a specific ligation or conjugation reaction of interest.Type: GrantFiled: August 30, 2001Date of Patent: December 20, 2005Assignee: Gryphon TherapeuticsInventors: Paolo Botti, James A. Bradburne, Stephen B. H. Kent
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Patent number: 6844161Abstract: Novel proteins and protein libraries are disclosed. The proteins possess one or more functional protein modules from different parent protein molecules. The proteins and protein libraries are exemplified by the preparation of cross-over chemokines that contain various combinations of peptide segments derived from RANTES, SDS-1 and vMIP-I and to vMIP-II. The proteins and libraries are extremely pure and can be provided in non-limiting high yields suitable for diagnostic and high-throughput screening assays.Type: GrantFiled: August 31, 1998Date of Patent: January 18, 2005Assignee: Gryphon Therapeutics, Inc.Inventors: Michael A. Siani, Jill Wilken, Reyna Simon, Stephen B. H. Kent
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Publication number: 20040265944Abstract: Method is described for sequencing polypeptides by forming peptide ladders comprising a series of polypeptides in which adjacent members of the series vary by one amino acid residue and determining the identity and position of each amino acid in the polypeptide by mass spectroscopy.Type: ApplicationFiled: March 2, 2004Publication date: December 30, 2004Applicants: The Rockefeller University, The Scripps Research InstituteInventors: Brian T. Chait, Ronald Beavis, Rong Wang, Stephen B. H. Kent
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Publication number: 20040138412Abstract: The invention is directed to methods and compositions for chemical ligation of components comprising a first component having a carboxythioester, and preferable an &agr;-carboxythioester, moiety and a second component having an N-substituted, and preferably an N&agr;-substituted, 2 or 3 carbon chain alkyl or aryl thiol to give a ligation product having an N-substituted amide bond at the ligation site. The reactants of the invention are chemoselective, and the alkyl or aryl thiol moiety is removable from the ligation product. Removal of the alkyl or aryl thiol gives a native amide bond at the ligation site. The methods and compositions of the invention are particularly useful for ligation of peptides and polypeptides. The ligation system of the invention is applicable to a wide variety of molecules, and thus can be exploited to generate peptides, polypeptides and other amino acid containing polymers having a native amide bond at the ligation site.Type: ApplicationFiled: January 15, 2003Publication date: July 15, 2004Inventors: Paolo Botti, James A Bradburne, Stephen B H Kent, Donald W Low
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Publication number: 20040115774Abstract: The present invention relates to methods and compositions for modifying peptides, polypeptides and proteins with polymers, especially glyco-mimetic polymers, so as to improve their biological activity or pharmacokinetic properties. The invention further provides methods and uses for such polymer-modified peptides, polypeptides and proteins. The invention is particularly suitable for use in the synthesis of polymer-modified synthetic bioactive proteins (FIG. 1D), and of pharmaceutical compositions that contain such proteins.Type: ApplicationFiled: January 8, 2003Publication date: June 17, 2004Inventors: Gerd G Kochendoerfer, Paolo Botti, James A Bradburne, Shiah-yun Chen, Sonya Cressman, Christie L Hunter, Stephen B H Kent, Donald W Low, Jill G Wilken
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Patent number: 6750061Abstract: Method is described for sequencing polypeptides by forming peptide ladders comprising a series of polypeptides in which adjacent members of the series vary by one amino acid residue and determining the identity and position of each amino acid in the polypeptide by mass spectroscopy.Type: GrantFiled: April 5, 2001Date of Patent: June 15, 2004Assignees: The Rockefeller University, The Scripps Research InstituteInventors: Brian T. Chait, Ronald Beavis, Rong Wang, Stephen B. H. Kent
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Publication number: 20030208046Abstract: The present invention concerns methods and compositions for extending the technique of native chemical ligation of a wider range of peptides, polypeptides, other polymers and other molecules via an amide bond (see FIG. 1). The invention further provides methods and uses for such proteins and derivatized proteins. The invention is particularly suitable for use in the synthesis of optionally polymer-modified, synthetic bioactive proteins, and of pharmaceutical compositions that contain such proteins.Type: ApplicationFiled: January 8, 2003Publication date: November 6, 2003Inventors: Christie L. Hunter, Paolo Botti, James A. Bradburne, Shiah-yun Chen, Sonya Cressman, Stephen B.H. Kent, Gerd G. Kochendoerfer, Donald W. Low