IP Library Granted Patent US 8,796,233
Granted Patent B2
US 8,796,233 · App. 13/163,638 · Granted Aug 5, 2014

Methods and systems for modulating hormones and related methods, agents and compositions

Inventors: William A. Goddard, III (Pasadena, CA); Mark Menna (Los Angeles, CA); Stephen Pandol (Los Angeles, CA); Ravinder Abrol (Arcadia, CA)
Assignees: California Institute of Technology; The Regents of the University of California; The United States of America as represented by the Department of Veterans Affairs
A61K31/10A61K31/12A61K31/122A61K47/4823
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Quick Facts
Patent No.
US 8,796,233
App. No.
13/163,638
Granted
Aug 5, 2014
Kind
B2
Abstract

Provided herein are bitter taste receptor ligands, related agents, combinations, compositions, methods and systems for modulating release of a metabolic hormone in vitro or in vivo from cells of the GI tract of an individual.

Claims (14)

1. A method for modulating release of a bitter taste receptor mediated metabolic hormone in an individual, the method comprising:

administering to the individual one or more GI bitter taste receptor ligands selected from the group consisting of 6-n-propylthiouracil, phenylthiocarbamide, denatonium benzoate, Glycyrrhizic acid ammonium salt, Epigallocatechin gallate, Hyperforin, Berberine chloride, Coptisine Chloride, Allyl methyl sulfide, Rottlerin, Curcumin, Ellagic acid, Embelin and/or a derivative thereof, wherein the one or more GI bitter taste receptor ligands are conjugated with a complementary molecule and are configured for interfering with systemic absorption and release of the one or more GI bitter taste receptor ligands, in an effective amount to allow binding of the one or more GI bitter taste receptor ligands to the one or more GI bitter taste receptors in the individual, the binding resulting in modulating release of the bitter taste receptor-mediated metabolic hormone, wherein the metabolic hormone is GLP-1, PYY and/or CCK, wherein the administering is performed by enteral administration.

2. The method of claim 1 , wherein the one or more GI bitter taste receptor ligands is selected from the group consisting of 6-n-propylthiouracil, phenylthiocarbamide, denatonium benzoate, Glycyrrhizic acid ammonium salt, Epigallocatechin gallate,Hyperforin, Berberine chloride, Coptisine Chloride, Allyl methyl sulfide, Rottlerin, Curcumin, Ellagic acid, and Embelin and/or and an agonist derivative thereof and the binding results in increasing release of GLP-1, PYY and/or CCK.

3. The method of claim 1 , wherein the one or more GI bitter taste receptor ligands is selected from the group consisting of denatonium benzoate and an agonist derivative thereof and the binding results in increasing release of CCK.

4. The method of claim 1 , wherein the complementary molecule is cellulose, polyethylene glycol, monosaccharides, oligosaccharides, amino acids, and/or peptides.

5. The method of claim 1 , wherein the administering of the one or more GI bitter taste receptor ligands is performed in a composition formulated to minimize systemic absorption of the one or more GI bitter taste receptor ligands across GI epithelium.

6. A method for activating a target bitter taste receptor in an individual, the method comprising:

administering to the individual an effective amount of one or more bitter tastant ligands that are conjugated with a complementary molecule, wherein the complementary molecule is configured for interfering with systemic absorption and release of the bitter tastant receptor ligand, wherein the administering is performed by enteral administration.

7. The method of claim 1 , wherein the binding resulting in modulating release of metabolic hormone GLP-1, PYY and/or CCK is effective for treatment of a metabolic condition, the condition being obesity and/or diabetes.

8. The method of claim 1 , wherein the GI bitter taste receptor ligand is 6-n-propylthiouracil.

9. The method of claim 1 , wherein the administering of the one or more GI bitter taste receptor ligands is performed in a composition formulated to minimize systemic absorption of the one or more GI bitter taste receptor ligands and/or to deliver the bitter tastant specifically to the vicinity of or directly to an L-cell of the small or large intestine.

10. The method of claim 1 , wherein the one or more bitter tastant ligands are selected from the group consisting of Epigallocatechin gallate, Hyperforin, Berberine chloride, Coptisin, Rottlerin, Curcumin, Ellagic acid, Embelin and derivative thereof.

11. The method of claim 1 , wherein the enteral administration is oral administration.

12. The method of claim 6 , wherein the enteral administration is oral administration.

Assignments (6)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 25, 2014
From: GODDARD, WILLIAM A., III
To: CALIFORNIA INSTITUTE OF TECHNOLOGY
Reel/Frame 033179/0720 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 25, 2014
From: PANDOL, STEPHEN
To: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA; UNITED STATES GOVERNMENT REPRESENTED BY THE DEPARTMENT OF VETERANS AFFAIRS
Reel/Frame 033244/0457 →
RESCISSION AGREEMENT Recorded Jun 16, 2014
From: CALIFORNIA INSTITUTE OF TECHNOLOGY
To: PANDOL, STEPHEN
Reel/Frame 033153/0927 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 20, 2011
From: ABROL, RAVINDER
To: CALIFORNIA INSTITUTE OF TECHNOLOGY
Reel/Frame 027095/0504 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 13, 2011
From: GODDARD, WILLIAM A., III; PANDOL, STEPHEN
To: CALIFORNIA INSTITUTE OF TECHNOLOGY
Reel/Frame 027058/0194 →
CONFIRMATORY LICENSE Recorded Jul 11, 2011
From: CALIFORNIA INSTITUTE OF TECHNOLOGY
To: NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT
Reel/Frame 026571/0278 →
Continuity (2)
Provisional Application 61397940 · Jun 17, 2010
Related Publication 20120058965A1 · Mar 8, 2012