Patents by Inventor Brian Kobilka
Brian Kobilka 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).
-
Publication number: 20190383826Abstract: The present invention relates to the field of GPCR structure biology and signaling. In particular, the present invention relates to protein binding domains directed against or capable of specifically binding to a functional conformational state of a G-protein-coupled receptor (GPCR). More specifically, the present invention provides protein binding domains that are capable of increasing the stability of a functional conformational state of a GPCR, in particular, increasing the stability of a GPCR in its active conformational state. The protein binding domains of the present invention can be used as a tool for the structural and functional characterization of G-protein-coupled receptors bound to various natural and synthetic ligands, as well as for screening and drug discovery efforts targeting GPCRs. Moreover, the invention also encompasses the diagnostic, prognostic and therapeutic usefulness of these protein binding domains for GPCR-related diseases.Type: ApplicationFiled: July 1, 2019Publication date: December 19, 2019Inventors: Jan Steyaert, Els Pardon, Soren G.F. Rasmussen, Juan Jose Fung, Brian Kobilka, Toon Laeremans
-
Publication number: 20190383828Abstract: The present invention relates to the field of GPCR structure biology and signaling. In particular, the present invention relates to protein binding domains directed against or capable of specifically binding to a functional conformational state of a G-protein-coupled receptor (GPCR). More specifically, the present invention provides protein binding domains that are capable of increasing the stability of a functional conformational state of a GPCR, in particular, increasing the stability of a GPCR in its active conformational state. The protein binding domains of the present invention can be used as a tool for the structural and functional characterization of G-protein-coupled receptors bound to various natural and synthetic ligands, as well as for screening and drug discovery efforts targeting GPCRs. Moreover, the invention also encompasses the diagnostic, prognostic and therapeutic usefulness of these protein binding domains for GPCR-related diseases.Type: ApplicationFiled: July 30, 2019Publication date: December 19, 2019Inventors: Jan Steyaert, Els Pardon, Soren G.F. Rasmussen, Juan Jose Fung, Brian Kobilka, Toon Laeremans
-
Publication number: 20190338024Abstract: Agents that specifically bind to an opioid receptor in a conformationally specific way can be used to induce a conformational change in the receptor. Such agents have therapeutic applications and can be used in X-ray crystallography studies of the receptor. Such agents can also be used to improve drug discovery via compound screening and/or structure-based drug design.Type: ApplicationFiled: March 15, 2019Publication date: November 7, 2019Inventors: Jan Steyaert, Toon Laeremans, Els Pardon, Brian Kobilka, Aashish Manglik
-
Patent number: 10436796Abstract: The present invention relates to the field of GPCR structure biology and signaling. In particular, the present invention relates to protein binding domains directed against or capable of specifically binding to a functional conformational state of a G-protein-coupled receptor (GPCR). More specifically, the present invention provides protein binding domains that are capable of increasing the stability of a functional conformational state of a GPCR, in particular, increasing the stability of a GPCR in its active conformational state. The protein binding domains of the present invention can be used as a tool for the structural and functional characterization of G-protein-coupled receptors bound to various natural and synthetic ligands, as well as for screening and drug discovery efforts targeting GPCRs. Moreover, the invention also encompasses the diagnostic, prognostic and therapeutic usefulness of these protein binding domains for GPCR-related diseases.Type: GrantFiled: October 26, 2018Date of Patent: October 8, 2019Assignees: LELAND STANFORD JUNIOR UNIVERSITY, VIB VZW, VRIJE UNIVERSITEIT BRUSSELInventors: Jan Steyaert, Els Pardon, Soren G. F. Rasmussen, Juan Jose Fung, Brian Kobilka, Toon Laeremans
-
Patent number: 10233241Abstract: Agents that specifically bind to an opioid receptor in a conformationally specific way can be used to induce a conformational change in the receptor. Such agents have therapeutic applications and can be used in X-ray crystallography studies of the receptor. Such agents can also be used to improve drug discovery via compound screening and/or structure-based drug design.Type: GrantFiled: January 30, 2015Date of Patent: March 19, 2019Assignees: VIB VZW, VRIJE UNIVERSITEIT BRUSSEL, THE BOARD OF TRUSTEES OF THE LELAND STANFORD JUNIOR UNIVERSITYInventors: Jan Steyaert, Toon Laeremans, Els Pardon, Brian Kobilka, Aashish Manglik
-
Publication number: 20190076398Abstract: Described herein, inter alia, are compositions and methods for modulating mu opioid receptor activity.Type: ApplicationFiled: June 30, 2016Publication date: March 14, 2019Inventors: Brian K. Shoichet, Henry Lin, Peter Gmeiner, Aashish Manglik, Brian Kobilka, Bryan L. Roth, Daniela Gisela Dengler
-
Publication number: 20190055208Abstract: Described herein, inter alia, are compositions and methods for modulating mu opioid receptor activity.Type: ApplicationFiled: August 17, 2018Publication date: February 21, 2019Inventors: Brian K. Shoichet, Anat Levit, Aashish Manglik, Brian Kobilka, Peter Gmeiner, Harald Hübner, Daniela Gisela Dengler
-
Publication number: 20190049463Abstract: The present invention relates to the field of GPCR structure biology and signaling. In particular, the present invention relates to protein binding domains directed against or capable of specifically binding to a functional conformational state of a G-protein-coupled receptor (GPCR). More specifically, the present invention provides protein binding domains that are capable of increasing the stability of a functional conformational state of a GPCR, in particular, increasing the stability of a GPCR in its active conformational state. The protein binding domains of the present invention can be used as a tool for the structural and functional characterization of G-protein-coupled receptors bound to various natural and synthetic ligands, as well as for screening and drug discovery efforts targeting GPCRs. Moreover, the invention also encompasses the diagnostic, prognostic and therapeutic usefulness of these protein binding domains for GPCR-related diseases.Type: ApplicationFiled: October 26, 2018Publication date: February 14, 2019Inventors: Jan Steyaert, Els Pardon, Soren G.F. Rasmussen, Juan Jose Fung, Brian Kobilka, Toon Laeremans
-
Publication number: 20190041400Abstract: The present invention relates to the field of GPCR structure biology and signaling. In particular, the present invention relates to protein binding domains directed against or capable of specifically binding to a functional conformational state of a G-protein-coupled receptor (GPCR). More specifically, the present invention provides protein binding domains that are capable of increasing the stability of a functional conformational state of a GPCR, in particular, increasing the stability of a GPCR in its active conformational state. The protein binding domains of the present invention can be used as a tool for the structural and functional characterization of G-protein-coupled receptors bound to various natural and synthetic ligands, as well as for screening and drug discovery efforts targeting GPCRs. Moreover, the invention also encompasses the diagnostic, prognostic and therapeutic usefulness of these protein binding domains for GPCR-related diseases.Type: ApplicationFiled: July 26, 2018Publication date: February 7, 2019Inventors: Jan Steyaert, Els Pardon, Soren G.F. Rasmussen, Juan Jose Fung, Brian Kobilka, Toon Laeremans
-
Patent number: 10078088Abstract: The present invention relates to the field of GPCR structure biology and signaling. In particular, the present invention relates to protein binding domains directed against or capable of specifically binding to a functional conformational state of a G-protein-coupled receptor (GPCR). More specifically, the present invention provides protein binding domains that are capable of increasing the stability of a functional conformational state of a GPCR, in particular, increasing the stability of a GPCR in its active conformational state. The protein binding domains of the present invention can be used as a tool for the structural and functional characterization of G-protein-coupled receptors bound to various natural and synthetic ligands, as well as for screening and drug discovery efforts targeting GPCRs. Moreover, the invention also encompasses the diagnostic, prognostic and therapeutic usefulness of these protein binding domains for GPCR-related diseases.Type: GrantFiled: November 17, 2017Date of Patent: September 18, 2018Assignees: VIB VZW, Vrije Universiteit Brussel, The Board of Trustees of the leland Stanford Junior UniversityInventors: Jan Steyaert, Els Pardon, Soren G. F. Rasmussen, Juan Jose Fung, Brian Kobilka, Toon Laeremans
-
Patent number: 10054598Abstract: The present invention relates to the field of GPCR structure biology and signaling. In particular, the present invention relates to protein binding domains directed against or capable of specifically binding to a functional conformational state of a G-protein-coupled receptor (GPCR). More specifically, the present invention provides protein binding domains that are capable of increasing the stability of a functional conformational state of a GPCR, in particular, increasing the stability of a GPCR in its active conformational state. The protein binding domains of the present invention can be used as a tool for the structural and functional characterization of G-protein-coupled receptors bound to various natural and synthetic ligands, as well as for screening and drug discovery efforts targeting GPCRs. Moreover, the invention also encompasses the diagnostic, prognostic and therapeutic usefulness of these protein binding domains for GPCR-related diseases.Type: GrantFiled: November 21, 2017Date of Patent: August 21, 2018Assignees: VIB VZW, VRIJE UNIVERSITEIT BRUSSEL, THE BOARD OF TRUSTEES OF THE LELAND STANFORD JUNIOR UNIVERSITYInventors: Jan Steyaert, Els Pardon, Soren G. F. Rasmussen, Juan Jose Fung, Brian Kobilka, Toon Laeremans
-
Publication number: 20180222978Abstract: Agents that specifically bind to a muscarinic acetylcholine receptor in a conformationally specific way can be used to induce a conformational change in the receptor. Such agents have therapeutic applications and can be used in X-ray crystallography studies of the receptor. Such agents can also be used to improve drug discovery via compound screening and/or structure based drug design.Type: ApplicationFiled: March 29, 2018Publication date: August 9, 2018Inventors: Jan Steyaert, Els Pardon, Brian Kobilka, Aaron Ring, Andrew Kruse, Aashish Manglik
-
Publication number: 20180100865Abstract: The present invention relates to the field of GPCR structure biology and signaling. In particular, the present invention relates to protein binding domains directed against or capable of specifically binding to a functional conformational state of a G-protein-coupled receptor (GPCR). More specifically, the present invention provides protein binding domains that are capable of increasing the stability of a functional conformational state of a GPCR, in particular, increasing the stability of a GPCR in its active conformational state. The protein binding domains of the present invention can be used as a tool for the structural and functional characterization of G-protein-coupled receptors bound to various natural and synthetic ligands, as well as for screening and drug discovery efforts targeting GPCRs. Moreover, the invention also encompasses the diagnostic, prognostic and therapeutic usefulness of these protein binding domains for GPCR-related diseases.Type: ApplicationFiled: November 21, 2017Publication date: April 12, 2018Applicants: VIB VZW, The Board of Trustees of the Leland Stanford Junior University, Vrije Universiteit Brussel, The Board of Trustees of the Leland Stanford Junior UniversityInventors: Jan Steyaert, Els Pardon, Soren G.F. Rasmussen, Juan Jose Fung, Brian Kobilka, Toon Laeremans
-
Publication number: 20180067126Abstract: The present invention relates to the field of GPCR structure biology and signaling. In particular, the present invention relates to protein binding domains directed against or capable of specifically binding to a functional conformational state of a G-protein-coupled receptor (GPCR). More specifically, the present invention provides protein binding domains that are capable of increasing the stability of a functional conformational state of a GPCR, in particular, increasing the stability of a GPCR in its active conformational state. The protein binding domains of the present invention can be used as a tool for the structural and functional characterization of G-protein-coupled receptors bound to various natural and synthetic ligands, as well as for screening and drug discovery efforts targeting GPCRs. Moreover, the invention also encompasses the diagnostic, prognostic and therapeutic usefulness of these protein binding domains for GPCR-related diseases.Type: ApplicationFiled: November 17, 2017Publication date: March 8, 2018Inventors: Jan Steyaert, Els Pardon, Soren G.F. Rasmussen, Juan Jose Fung, Brian Kobilka, Toon Laeremans
-
Patent number: 9880179Abstract: Provided herein are several methods for selecting agents that bind to transmembrane receptors in a conformationally-selective way. In some embodiments, the method may comprise producing: a transmembrane receptor in an active conformation; and said transmembrane receptor in an inactive conformation and using cell sorting to select, from a population of cells comprising a library of cell surface-tethered extracellular capture agents, cells that are specifically bound to either the transmembrane receptor in its active conformation or the transmembrane receptor in its inactive conformation, but not both. In other embodiments, the method may comprise: contacting a GPCR with a population of cells that comprise a library of surface-tethered extracellular proteins; labeling the cell population with a conformationally-specific binding agent, e.g., a G-protein or mimetic thereof; and using cell sorting to select from the cell population cells that bind to the agent.Type: GrantFiled: February 5, 2014Date of Patent: January 30, 2018Assignee: The Board of Trustees of the Leland Stanford Junior UniversityInventors: Aaron Michael Ring, Aashish Manglik, Andrew Kruse, Brian Kobilka
-
Patent number: 9863959Abstract: The present invention relates to the field of GPCR structure biology and signaling. In particular, the present invention relates to protein binding domains directed against or capable of specifically binding to a functional conformational state of a G-protein-coupled receptor (GPCR). More specifically, the present invention provides protein binding domains that are capable of increasing the stability of a functional conformational state of a GPCR, in particular, increasing the stability of a GPCR in its active conformational state. The protein binding domains of the present invention can be used as a tool for the structural and functional characterization of G-protein-coupled receptors bound to various natural and synthetic ligands, as well as for screening and drug discovery efforts targeting GPCRs. Moreover, the invention also encompasses the diagnostic, prognostic and therapeutic usefulness of these protein binding domains for GPCR-related diseases.Type: GrantFiled: January 18, 2017Date of Patent: January 9, 2018Assignees: VIB VZW, VRIJE UNIVERSITEIT BRUSSEL, THE BOARD OF TRUSTEES OF THE LELAND STANFORD JUNIOR UNIVERSITYInventors: Jan Steyaert, Els Pardon, Soren G. F. Rasmussen, Juan Jose Fung, Brian Kobilka, Toon Laeremans
-
Publication number: 20170253644Abstract: The present disclosure relates to the field of G protein coupled receptor (GPCR) structural biology and signaling. In particular, the present disclosure relates to binding domains directed against and/or specifically binding to GPCR:G protein complexes. Also provided are nucleic acid sequences encoding such binding domains and cells expressing or capable of expressing such binding domains. The binding domains of the present disclosure can be used as universal tools for the structural and functional characterization of G-protein coupled receptors in complex with downstream heterotrimeric G proteins and bound to various natural or synthetic ligands, for investigating the dynamic features of G protein activation, as well as for screening and drug discovery efforts that make use of GPCR:G protein complexes.Type: ApplicationFiled: May 1, 2017Publication date: September 7, 2017Applicants: VIB VZW, Vrije Universiteit Brussel, The Board of Trustees of the Leland Stanford Junior University, The Regents of the University of MichiganInventors: Jan Steyaert, Els Pardon, Toon Laeremans, Brian Kobilka, Soren G.F. Rasmussen, Sebastien Granier, Roger K. Sunahara
-
Patent number: 9695227Abstract: The present invention relates to the field of G protein coupled receptor (GPCR) structural biology and signaling. In particular, the present invention relates to binding domains directed against and/or specifically binding to GPCR:G protein complexes. Also provided are nucleic acid sequences encoding such binding domains and cells expressing or capable of expressing such binding domains. The binding domains of the present invention can be used as universal tools for the structural and functional characterization of G-protein coupled receptors in complex with downstream heterotrimeric G proteins and bound to various natural or synthetic ligands, for investigating the dynamic features of G protein activation, as well as for screening and drug discovery efforts that make use of GPCR:G protein complexes.Type: GrantFiled: June 21, 2012Date of Patent: July 4, 2017Assignees: Vrije Universiteit Brussel, VIB VZW, The Board of Trustees of the Leland Stanford Junior Universitv, The Regents of the University of MichiganInventors: Jan Steyaert, Els Pardon, Toon Laeremans, Brian Kobilka, Søren Rasmussen, Sebastian Granier, Roger K. Sunahara
-
Publication number: 20170183404Abstract: Agents that specifically bind to an opioid receptor in a conformationally specific way can be used to induce a conformational change in the receptor. Such agents have therapeutic applications and can be used in X-ray crystallography studies of the receptor. Such agents can also be used to improve drug discovery via compound screening and/or structure-based drug design.Type: ApplicationFiled: January 30, 2015Publication date: June 29, 2017Applicant: VIB VZWInventors: Jan Steyaert, Toon Laeremans, Els Pardon, Brian Kobilka, Aashish Manglik
-
Patent number: 9689872Abstract: The present invention relates to the field of GPCR structure biology and signaling. In particular, the present invention relates to protein binding domains directed against or capable of specifically binding to a functional conformational state of a G-protein-coupled receptor (GPCR). More specifically, the present invention provides protein binding domains that are capable of increasing the stability of a functional conformational state of a GPCR, in particular, increasing the stability of a GPCR in its active conformational state. The protein binding domains of the present invention can be used as a tool for the structural and functional characterization of G-protein-coupled receptors bound to various natural and synthetic ligands, as well as for screening and drug discovery efforts targeting GPCRs. Moreover, the invention also encompasses the diagnostic, prognostic and therapeutic usefulness of these protein binding domains for GPCR-related diseases.Type: GrantFiled: August 13, 2016Date of Patent: June 27, 2017Assignees: VIB VZW, Vrije Universiteit Brussel, The Board of Trustees of the Leland Stanford Junior UniversityInventors: Jan Steyaert, Juan Jose Fung, Brian Kobilka, Toon Laeremans, Els Pardon, Soren G. F. Rasmussen