33 results about "Bitter taste receptors" patented technology

Provided herein are methods for treating conditions associated with a chemosensory receptor, including diabetes, obesity, and other metabolic diseases, disorders or conditions by administrating a composition comprising a chemosensory receptor ligand, such as a bitter receptor ligand. Also provided herein are chemosensory receptor ligand compositions, including bitter receptor ligand compositions, and methods for the preparation thereof for use in the methods of the present invention. Also provided herein are compositions comprising metformin and salts thereof and methods of use.

Isolated nucleic acids encoding T2R76 polypeptides, recombinantly expressed T2R76 polypeptides, heterologous expression systems for recombinant expression of T2R76 polypeptides, assay methods employing the same, and methods for altering taste perception via administration of a T2R76 modulator. These T22R76 polypeptides can be expressed alone or co-expressed with another T2R polypeptide, preferably a different human T2R polypeptide.

Isolated nucleic acids encoding T2R76 polypeptides, recombinantly expressed T2R76 polypeptides, heterologous expression systems for recombinant expression of T2R76 polypeptides, assay methods employing the same, and methods for altering taste perception via administration of a T2R76 modulator. These T22R76 polypeptides can be expressed alone or co-expressed with another T2R polypeptide, preferably a different human T2R polypeptide. These T2R76 polypeptides specifcally respond to bitter ligands including brucine and propylthiouracil (PROP) and therefore can be used in assays that identify compounds that modulate, preferably block bitter taste.

Provided herein are methods for treating conditions associated with a chemosensory receptor, including diabetes, obesity, and other metabolic diseases, disorders or conditions by administrating a composition comprising a chemosensory receptor ligand, such as a bitter receptor ligand. Also provided herein are chemosensory receptor ligand compositions, including bitter receptor ligand compositions, and methods for the preparation thereof for use in the methods of the present invention. Also provided herein are compositions comprising metformin and salts thereof and methods of use.

Steviol glycosides have been discovered to bind the bitter taste receptor TAS2R44. Novel methods of identifying modulators and in particular inhibitors to the bitter taste of steviol glycosides and an inhibitor of steviol glycosides are provided.

Identified herein are different forms of bitter receptor genes that occur in different humans. These alleles are generated by numerous coding single nucleotide polymorphisms (cSNP's) that occur within the members of the T2R gene family. Some SNP's cause amino acid substitutions, while others introduce chain termination codons, rendering the allele non-functional. Differences in these genes are believed to have a large effect on those individuals' sense of bitter taste, such that these individuals perceive the taste of bitter substances differently than the rest of the population. The ability to assay this allelic information is useful in the development of flavorings and flavor enhancers, as it can be used to define large groups and populations who perceive bitter tastes differently. This in turn allows the taste preferences of these groups to be addressed at the molecular level for the first time.

Identified herein are different forms of bitter receptor genes that occur in different humans. These alleles are generated by numerous coding single nucleotide polymorphisms (cSNP's) that occur within the members of the T2R gene family. Some SNP's cause amino acid substitutions, while others introduce chain termination codons, rendering the allele non-functional. Differences in these genes are believed to have a large effect on those individuals' sense of bitter taste, such that these individuals perceive the taste of bitter substances differently than the rest of the population. The ability to assay this allelic information is useful in the development of flavorings and flavor enhancers, as it can be used to define large groups and populations who perceive bitter tastes differently. This in turn allows the taste preferences of these groups to be addressed at the molecular level for the first time.

The present invention relates to the discovery that specific human taste receptors in the T2R taste receptor family respond to particular bitter compounds present in hydrolyzed soy protein derived materials. The invention further relates to the use of these T2R receptors in assays for identifying ligands that modulate the activation of these taste receptors by specific bitter ligands present in hydrolyzed soy protein materials and derivatives thereof and related compounds. These compounds may be used as additives and / or removed from soy-based foods, beverages, cosmetics and medicinals in order to modify (block) T2R-associated bitter taste elicited by bitter ligands present in hydrolyzed soy protein materials. Also these T2R ligands potentially may be used as therapeutics to treat and modulate hT2R1 or hT2R67 associated gastrointestinal and metabolic functions such as serum cholesterol levels as well as treat gastrointestinal and metabolic diseases such as eating disorders, food sensing, food absorption, obesity, diabetes, Crohn's disease, celiac disease, et al.

Isolated nucleic acids encoding T2R76 polypeptides, recombinantly expressed T2R76 polypeptides, heterologous expression systems for recombinant expression of T2R76 polypeptides, assay methods employing the same, and methods for altering taste perception via administration of a T2R76 modulator. These T22R76 polypeptides can be expressed alone or co-expressed with another T2R polypeptide, preferably a different human T2R polypeptide.

The invention discloses a sweetening agent compound composition capable of keeping the flavor of momordica grosvenori. The sweetening agent compound composition is prepared from the following raw materials: a momordica grosvenori sweetening agent, white dextrin, a bitterness inhibitor and a functional extract, wherein the bitterness inhibitor comprises adenosine monophosphate, ferulic acid, phosphatidic acid, tannic acid and zinc lactate; the functional natural extract comprises one or a combination of more selected from the group consisting of a honeysuckle extract, a roselle extract, a mulberry leaf extract and a coix seed extract. According to the invention, the compound raw materials and a bitter substance are competitively bonded at the bitter taste acceptor sites of tongue cells, sothe stimuli of bitter taste to the tongue is greatly reduced, and the bitter taste of the momordica grosvenori sweetening agent to the oral cavity can be effectively masked. Moreover, by adding the functional extract, the bitter taste is inhibited, the special sweetness of momordica grosvenori is not influenced and shielded, and the special flavor and taste of a momordica grosvenori beverage are maintained; so the application scope and fields of the momordica grosvenori sweetening agent are expanded, and the product value of the momordica grosvenori sweetening agent is improved.

This invention provides isolated nucleic acid and amino acid sequences of gastrointestinal endocrine cell specific G-protein coupled receptors, methods of detecting such receptors, and methods of screening for ligands of such receptors. Furthermore, this invention demonstrates that SrC-1 enteroendocrine cells express multiple bitter taste receptors as well as a-subunits of G proteins that mediate taste signal transduction and respond to bitter taste compounds initiating changes in intracellular calcium concentration. Given that at present there are no cultured cell model system to determine the functional effects of taste receptor-mediated signaling, our findings identify STC-1 cells as a cell model for studying taste-mediated signal transduction.

The invention belongs to the technical field of daily cosmetics, and discloses a composition for removing acnes and repairing a skin barrier, and a preparation method and application of the composition. The composition comprises the following ingredients in parts by weight: 0.5-5 parts of colloidal sulfur, 1-5 parts of plankton extracts and 1-6 parts of humulus lupulus extracts. The invention discovers that the colloidal sulfur, the plankton extracts and the humulus lupulus extracts have a synergistic effect on the aspects of an anti-inflammatory effect, an antibacterial effect, inhibition of 5 [alpha]-reductase activity and bitter receptor activation. Cosmetics prepared from the composition disclosed by the invention have a good acne removing effect, do not irritate the skin, are high in safety and can enhance the skin barrier.

TAS2R46 was identified as a dextromethorphan-binding bitter taste receptor. Novel methods to identify modulators and in particular inhibitors to the bitter taste of dextromethorphan are provided.

The invention discloses an application of flufenamic acid as an effective component in preparation of an airway smooth muscle relaxation agent. Experiments reveal for the first time that a compound (CID: 3371) can activate bitter taste receptors and strongly relax airway smooth muscle cells, and the relaxation degree of the compound is close to that of isoproterenol and salbutamol; and it is prompted that the compound (CID: 3371) can be used for preparing an airway smooth muscle relaxation medicine and also can be used for preparing the airway smooth muscle relaxation agent, so that the compound is used for asthma, chronic obstructive pulmonary diseases and the like, and has a wide application prospect.

A family of novel feline bitter taste receptors, referred to as feline TAS2R (fTAS2R), are disclosed herein. Isolated polynucleotides encoding the novel feline bitter taste receptors and chimeric polypeptides are also disclosed, as are expression vectors and host cells for expression of the novel feline bitter taste receptors. Methods of identifying compounds that bind to the novel feline bitter taste receptors and modulate their activity are disclosed.

The invention particularly relates to an active peptide with a bitterness blocking effect. The amino acid sequence of the active peptide is Asp-Asp-Asn-Lys (DDNK). The invention provides an active peptide with a bitterness blocking effect, which can be effectively combined with a bitterness receptor T2R14, has a continuous and stable masking effect on bitterness substances, and has the outstanding advantages of safety, non-toxic and side effects, easy absorption, industrialization and the like. The active peptide DDNK can be used in food, medicines and health care products with bitterness, and has wide application prospects and very important significance.

The invention relates to a bitter receptor agonist and application thereof in prevention and treatment of SARS-CoV-2 related infectious diseases. Specifically, the invention relates to application of a bitter receptor stimulant as a 2019 novel coronavirus (SARS-CoV-2) inhibitor in preparation of medicines for treating and / or preventing and relieving related diseases such as respiratory tract infection and pneumonia caused by 2019 novel coronavirus infection.

The invention relates to the field of medicine, in particular to an application of quinine and pharmaceutically acceptable salts thereof to preparation of a drug for treating AD (atopic dermatitis) and the drug for treating AD. A mouse model of AD is established by an embodiment, a skin lesion region of a mouse is smeared with a physiological saline solution of quinine, and the skin lesion is found to be obviously reduced. Further research shows that quinine can obviously reduce the pathological injury of the mouse, activate expression of a bitter taste receptor and silk polymerization protein, inhibit IgE in blood of the mouse and secretion of cytokines such as IL-1beta, IL-4, IL-5, IL-13 and IL-33 in skin lesion tissue, and thus, improve the skin condition, enhance the skin barrier function, inhibit occurrence of allergic reaction, relieve skin damage caused by immune reaction, and play a safe and effective role in treating the skin damage caused by AD. The invention expands medicalapplications of quinine and provides a new direction for treatment of AD.

The presently disclosed subject matter relates to methods of screening raw materials and pet food products to manufacture a palatable pet food product. The presently disclosed subject matter also relates to methods for identifying compounds that modulate the activity and / or expression of a bitter taste receptor.

The invention provides a levofloxacin oral administration solution and a preparation method thereof. The levofloxacin oral administration solution is prepared from levofloxacin, corrigents, a pH regulating agent and a solvent, wherein the content of the levofloxacin is 2.5g / 100ml, the pH regulating agent is (5mL to 7mL) to 100mL of the using consumption of hydrochloric acid; the corrigent is a mixture of sucrose and saccharin sodium, the content of the sucrose is 48g / 100mL to 58g / 100mL, and the content of the saccharin sodium is 0.2g / 100mL to 0.6g / 100mL; and the solvent is a mixture of glycerol, propylene glycol and purified water. The levofloxacin oral administration solution disclosed by the invention adopts the corrigents including the sucrose and the saccharin sodium, and due to cooperation between the two corrigents, the bitter taste of the levofloxacin oral administration solution can be reduced; and because competitive combination of the contained flavor masking agents includingalanine and taurine and the bitter taste receptor in an oral cavity, the bitter taste of levofloxacin can be further reduced, so that the levofloxacin oral administration solution has a better taste;and due to the contained beta-carotene, the photosensitivity adverse effect caused by the levofloxacin can be reduced, and the safety of a preparation is improved.

The invention provides methods and compositions for the diagnosis, prognosis and treatment of respiratory tract diseases. Specifically, the invention provides diagnosis, prognosis and treatment of respiratory infections using bitter and sweet taste signal transduction pathways. In one aspect, the invention relates to a method for treating a respiratory infection by administering a composition to the respiratory tract of a subject in an amount capable of activating bitter taste signaling and / or inhibiting sweet taste signaling. The composition comprises at least a bitter receptor agonist and, optionally, a pharmaceutically acceptable carrier for delivering the composition to the respiratory tract. In another aspect, the invention relates to a composition for treatment of a respiratory infection. Such composition comprises at least a bitter receptor agonist and, optionally, a pharmaceutically acceptable carrier for delivering the composition to the respiratory tract.

The invention relates to new use of piperine and application of the piperine in preparation of an agonist of a human bitter receptor 14 subtype (hTAS2R14). The piperine can be used for increasing an mRNA level and protein expression of the hTAS2R14 in enteroendocrine cell cells Caco-2, increasing protein expression of downstream phospholipase C beta 2 and transient receptor potential ion channel protein M5, and increasing mobilization of intracellular calcium, and then, the gene expression of a glucagon-like peptide 1 (GLP-1) precursor proglucagon and the secretion of the GLP-1 are improved. The hTAS2R14 agonist 6-methoxyflavone does not weaken the mobilization effect of the piperine on the intracellular calcium, but promotes the mobilization of the piperine on the intracellular calcium. A G beta gamma subunit inhibitor of the G protein coupled with the hTAS2R14 obviously weakens the secretion of the piperine to the GLP-1, and the phospholipase C beta 2 inhibitor obviously weakens the secretion of the piperine to the GLP-1. The research shows that the piperine is an efficient agonist of the hTAS2R14.

The present invention discloses two active peptides with bitter taste inhibitory effect, the amino acid sequences of which are Ala-Asp-Met and Ala-Asp-Trp respectively. The two active peptides with bitter taste inhibitory effect provided by the present invention can effectively combine with the bitter taste receptor T2R14, have a sustained and stable inhibitory effect on bitter substances, and have the characteristics of safety, non-toxic side effects, good water solubility, etc., and can be used for It has broad application prospects and very important significance in food, medicine and health care products.

The presently disclosed subject matter relates to methods of screening raw materials and pet food products to manufacture a palatable pet food product. The presently disclosed subject matter also relates to methods for identifying compounds that modulate the activity and / or expression of a bitter taste receptor.

Steviol glycosides have been discovered to bind the bitter taste receptor TAS2R44. Novel methods of identifying modulators and in particular inhibitors to the bitter taste of steviol glycosides and an inhibitor of steviol glycosides are provided.

Beef protein was hydrolyzed with each of six commercial enzymes (alcalase, chymotrypsin, trypsin, pepsin, flavourzyme, and thermoase). Electronic tongue measurements showed that the hydrolysates had significantly (p<0.05) lower bitter scores than quinine. Addition of the hydrolysates to quinine led to reduced bitterness intensity of quinine with trypsin and pepsin hydrolysates being the most effective. Addition of the hydrolysates to HEK293T cells that heterologously express one of the bitter taste receptors (T2R4) showed alcalase, thermoase, pepsin and trypsin hydrolysates as the most effective in reducing calcium mobilization. Eight peptides that were identified from the alcalase and chymotrypsin hydrolysates also suppressed bitter agonist-dependent calcium release from T2R4 and T2R14 with AGDDAPRAVF and ETSARHL being the most effective.

The invention discloses a tilmicosin premix and a preparation method thereof. The tilmicosin premix comprises the following raw materials in percentage by mass: 10-30% of tilmicosin, 1-5% of a bitter receptor inhibitor, 20-50% of an enteric carrier material and 15-69% of a diluent, according to the tilmicosin premix provided by the invention, the medicine and the bitter receptor blocker are mixed, so that on one hand, the tilmicosin premix can compete for a bitter receptor with tilmicosin, and on the other hand, transmission of a bitter signal to the brain is blocked, the irritant bitter taste of the tilmicosin is covered, the taste of the tilmicosin is improved, the clinical use compliance is improved, and the tilmicosin premix is beneficial to ingestion of treated animals; the treatment effect of the veterinary drug is improved.

The invention belongs to the technical field of medicines and the field of foods and particularly relates to a novel application of 2,6-disubstituted pyridine-4-thioformamide to preparation of a bitterness inhibiting drug or food. The invention firstly discloses that 2,6-disubstituted pyridine-4-thioformamide has an effect on inhibiting a bitterness receptor hTAS2R38 and is obvious in inhibiting effect. 2,6-disubstituted pyridine-4-thioformamide disclosed by the invention can be applied to the preparation of the bitterness inhibiting drug alone, can also be used as a drug preparation additive to be compounded to form a composition for reducing the bitterness of a drug and can be prepared into any one of dosage forms including a tablet, powder, an oral solution or a spray and the like suitable for clinic use. Meanwhile, 2,6-disubstituted pyridine-4-thioformamide can also be used as a food additive for regulating the taste of the food.