公开(公告)号：US08153386B2

公开(公告)日：2012-04-10

申请号：US11599318

申请日：2006-11-15

Applicant: Jon Elliot Adler

Inventor： Jon Elliot Adler

IPC: G01N33/567 ,  C07K14/705 ,  C12N15/12

CPC classification number: G01N33/74 ,  A01K2217/05 ,  A61K38/00 ,  C07H21/04 ,  C07K14/705 ,  C07K2319/00 ,  G01N33/566 ,  G01N33/582 ,  G01N2333/726 ,  G01N2500/00 ,  G01N2500/04

Abstract: The present invention relates to the discovery of a specific human taste receptor in the T2R taste receptor family, hT2R64 that responds to particular bitter compounds The present invention further relates to the use of this receptor in assays for identifying ligands that modulate the activation of this taste receptor. These compounds may be used as additives and/or removed from foods, beverages and medicinals in order to modify (block) T2R-associated bitter taste. A preferred embodiment is the use of the identified compounds as additives in foods, beverages and medicinals for blocking bitter taste.

Abstract translation: 本发明涉及T2R味觉受体家族中特异性人体受体的发现，hT2R64对特定苦味化合物的响应本发明还涉及这种受体在用于鉴别调节该味道的活化的配体的测定中的应用 受体。 这些化合物可以用作添加剂和/或从食品，饮料和药物中去除，以便改变（阻断）T2R相关的苦味。 优选的实施方案是使用所鉴定的化合物作为食品，饮料和药物中的添加剂来阻止苦味。

公开(公告)号：US08148544B2

公开(公告)日：2012-04-03

申请号：US13051052

申请日：2011-03-18

Applicant: Xiaodong Li ,  Andrew Patron ,  Catherine Tachdjian ,  Hong Xu ,  Qing Li ,  Alexey Pronin ,  Guy Servant ,  Lan Zhang ,  Thomas Brady ,  Vincent Darmohusodo ,  Melissa Arellano ,  Victor Selchau ,  Brett Weylan Ching ,  Donald S. Karanewsky ,  Paul Brust ,  Jing Ling ,  Wen Zhao ,  Chad Priest

Inventor： Xiaodong Li ,  Andrew Patron ,  Catherine Tachdjian ,  Hong Xu ,  Qing Li ,  Alexey Pronin ,  Guy Servant ,  Lan Zhang ,  Thomas Brady ,  Vincent Darmohusodo ,  Melissa Arellano ,  Victor Selchau ,  Brett Weylan Ching ,  Donald S. Karanewsky ,  Paul Brust ,  Jing Ling ,  Wen Zhao ,  Chad Priest

IPC: C07D261/06

CPC classification number: C07C311/17 ,  A23L27/86 ,  A61K8/46 ,  A61K8/466 ,  A61K8/4933 ,  A61K8/494 ,  A61K8/4973 ,  A61K8/498 ,  A61K8/4986 ,  A61K31/135 ,  A61K31/4439 ,  A61K31/485 ,  A61K31/60 ,  A61K31/704 ,  A61K45/06 ,  A61Q11/00 ,  C07C233/73 ,  C07C311/04 ,  C07C311/13 ,  C07C311/16 ,  C07C311/18 ,  C07C311/19 ,  C07C311/20 ,  C07C311/21 ,  C07C311/29 ,  C07C311/46 ,  C07C323/49 ,  C07C335/16 ,  C07C335/18 ,  C07D213/42 ,  C07D213/71 ,  C07D217/08 ,  C07D223/18 ,  C07D307/14 ,  C07D307/52 ,  C07D317/58 ,  C07D333/20 ,  C07D333/34 ,  A61K2300/00

Abstract: 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, e.g., coffee. Also, the invention relates to the discovery of specific compounds and compositions containing that function as bitter taste blockers and the use thereof as bitter taste blockers or flavor modulators in, e.g., coffee and coffee flavored foods, beverages and medicaments. Also, the present invention relates to the discovery of a compound that antagonizes numerous different human T2Rs and the use thereof in assays and as a bitter taste blocker in compositions for ingestion by humans and animals.

Abstract translation: 本发明涉及T2R味觉受体家族中的特定人味受体对存在于例如咖啡中的特定苦味化合物的反应的发现。 此外，本发明涉及含有作为苦味抑制剂的特定化合物和组合物的发现，以及其作为例如咖啡和咖啡风味食品，饮料和药物中的苦味抑制剂或风味调节剂的用途。 此外，本发明涉及一种拮抗多种不同人类T2R的化合物的发现及其在测定中的用途以及用于摄取人类和动物的组合物中的苦味阻滞剂。

公开(公告)号：US08124121B2

公开(公告)日：2012-02-28

申请号：US12257017

申请日：2008-10-23

Applicant: Catherine Tachdjian ,  Andrew P. Patron ,  Sara L. Adamski-Werner ,  Farid Bakir ,  Qing Chen ,  Vincent Darmohusodo ,  Stephen Terrence Hobson ,  Xiaodong Li ,  Ming Qi ,  Daniel H. Rogers ,  Marketa Rinnova ,  Guy Servant ,  Xiao-Qing Tang ,  Mark Zoller ,  David Wallace ,  Amy Xing ,  Klaus Gubernator

Inventor： Catherine Tachdjian ,  Andrew P. Patron ,  Sara L. Adamski-Werner ,  Farid Bakir ,  Qing Chen ,  Vincent Darmohusodo ,  Stephen Terrence Hobson ,  Xiaodong Li ,  Ming Qi ,  Daniel H. Rogers ,  Marketa Rinnova ,  Guy Servant ,  Xiao-Qing Tang ,  Mark Zoller ,  David Wallace ,  Amy Xing ,  Klaus Gubernator

IPC: A61K47/00 ,  A61K31/4965

CPC classification number: G01N33/543 ,  A23L2/56 ,  A23L27/202 ,  A23L27/203 ,  A23L27/2054 ,  A23L27/88 ,  A23V2002/00 ,  A61K8/4973 ,  A61K8/55 ,  A61K47/22 ,  A61K47/24 ,  C07C233/65 ,  C07C235/54 ,  C07C275/30 ,  C07C275/34 ,  C07D307/84 ,  C07D317/68 ,  C07D405/12 ,  C07F9/65517 ,  G01N33/5041 ,  G01N33/566 ,  G01N33/74 ,  G01N2333/726

Abstract: The present invention relates to the discovery that certain non-naturally occurring, non-peptide amide compounds and amide derivatives, such as oxalamides, ureas, and acrylamides, are useful flavor or taste modifiers, such as a flavoring or flavoring agents and flavor or taste enhancer, more particularly, savory (the “umami” taste of monosodium glutamate) or sweet taste modifiers, —savory or sweet flavoring agents and savory or sweet flavor enhancers, for food, beverages, and other comestible or orally administered medicinal products or compositions.

Abstract translation: 本发明涉及某些非天然存在的非肽酰胺化合物和酰胺衍生物，例如草酰胺，脲和丙烯酰胺，是有用的风味或调味剂，例如调味剂或调味剂和风味或味道 增强剂，更特别地，用于食品，饮料和其它可食用或口服给药的药物产品或组合物的美味（味道味道）或甜味调节剂，美味或甜味调味剂和咸味或甜味增味剂。

公开(公告)号：US08119359B2

公开(公告)日：2012-02-21

申请号：US13016887

申请日：2011-01-28

Applicant: Jon E. Adler ,  Xiaodong Li ,  Lena Staszewski ,  Hong Xu ,  Fernando Echeverri

Inventor： Jon E. Adler ,  Xiaodong Li ,  Lena Staszewski ,  Hong Xu ,  Fernando Echeverri

IPC: G01N33/567 ,  G01N33/53 ,  C07K1/00 ,  C07K14/00 ,  C07K17/00

CPC classification number: G01N33/5041 ,  C07K14/723 ,  G01N33/5008 ,  G01N33/5023 ,  G01N33/74 ,  G01N2333/705 ,  G01N2333/726 ,  G01N2500/00

Abstract: Newly identified mammalian taste-cell-specific G protein-coupled receptors which function as hetero-oligomeric complexes in the sweet taste transduction pathway, and the genes and cDNA encoding said receptors are described. Specifically, T1R G protein-coupled receptors active in sweet taste signaling as hetero-oligomeric complexes, and the genes and cDNA encoding the same, are described, along with methods for isolating such genes and for isolating and expressing such receptors. Methods for identifying putative taste modulating compounds using such hetero-oligomeric complexes also described, as is a novel surface expression facilitating peptide useful for targeting integral plasma membrane proteins to the surface of a cell.

Abstract translation: 描述了在甜味转导途径中作为异寡聚复合物起作用的新鉴定的哺乳动物味细胞特异性G蛋白偶联受体，以及编码所述受体的基因和cDNA。 具体来说，描述了作为异寡聚复合物的甜味信号传导中起作用的T1R G蛋白偶联受体，以及编码相同基因和cDNA的方法，以及用于分离这些基因并分离和表达此类受体的方法。 还描述了使用这种异寡​​聚复合物鉴定推定的味觉调节化合物的方法，以及用于靶向细胞表面的整合质膜蛋白的新颖的表达表达促进肽。

公开(公告)号：US20120041078A1

公开(公告)日：2012-02-16

申请号：US13208594

申请日：2011-08-12

Applicant: Catherine TACHDJIAN ,  Donald S. Karanewsky ,  Xiao-Qing Tang ,  Hanghui Liu

Inventor： Catherine TACHDJIAN ,  Donald S. Karanewsky ,  Xiao-Qing Tang ,  Hanghui Liu

IPC: A61K47/22 ,  A23L1/236 ,  A61K47/30

CPC classification number: A23L1/22678 ,  A23L2/56 ,  A23L27/2054 ,  A23L27/88 ,  A23V2002/00 ,  A61K47/22 ,  A61K47/26

Abstract: The present invention includes methods of stabilizing one or more sweet enhancers when they are exposed to a light source as well as liquid compositions containing one or more sweet enhancers and one or more photostabilizers.

Abstract translation: 本发明包括当一种或多种增甜剂暴露于光源时稳定一种或多种甜味增强剂的方法以及含有一种或多种甜味增强剂和一种或多种光稳定剂的液体组合物。

公开(公告)号：US20110262937A1

公开(公告)日：2011-10-27

申请号：US13099327

申请日：2011-05-02

Applicant: Mark Zoller ,  Xiaodong Li ,  Lena Staszewski ,  Shawn O'Connell ,  Sergey Zozulya ,  Jon Elliot Adler ,  Hong Xu ,  Fernando Echeverri

Inventor： Mark Zoller ,  Xiaodong Li ,  Lena Staszewski ,  Shawn O'Connell ,  Sergey Zozulya ,  Jon Elliot Adler ,  Hong Xu ,  Fernando Echeverri

IPC: C07K14/705 ,  G01N33/554 ,  C12N5/071

CPC classification number: G01N33/5041 ,  A01K2217/05 ,  C07K14/705 ,  C07K2319/00 ,  C12Q1/6876 ,  C12Q2600/124 ,  C12Q2600/158 ,  G01N33/5008 ,  G01N33/566 ,  G01N2333/4719 ,  G01N2333/705 ,  G01N2333/726 ,  G01N2500/04

Abstract: The present invention relates to the discovery that the T1R receptors assemble to form functional taste receptors. Particularly, it has been discovered that co-expression of T1R1 and T1R3 results in a taste receptor that responds to umami taste stimuli, including monosodium glutamate. Also, it has been discovered that co-expression of the T1R2 and T1R3 receptors results in a taste receptor that responds to sweet taste stimuli including naturally occurring and artificial sweeteners.Also the present invention relates to the use of hetero-oligomeric taste receptors comprising T1R1/T1R3 and T1R2/T1R3 in assays to identify compounds that respectively respond to umami taste stimuli and sweet taste stimuli.Further, the invention relates to the constitutive of cell lines that stably or transiently co-express a combination of T1R1 and T1R3; or T1R2 and T1R3; under constitutive or inducible conditions. The use of these cells lines in cell-based assays to identify umami and sweet taste modulatory compounds is also provided, particularly high throughput screening assays that detect receptor activity by use of fluorometric imaging.Finally, the invention relates to the discovery that some compounds, e.g., lactisole, inhibit both the activities of human T1R2/T1R3 and T1R1/T1R3 receptors, and accordingly the sweet and umami taste, suggesting that these receptors may be the only sweet and umami receptors.

公开(公告)号：US08030008B2

公开(公告)日：2011-10-04

申请号：US11555617

申请日：2006-11-01

Applicant: Xiaodong Li ,  Hong Xu ,  Qing Li ,  Huixian Tang ,  Alexey Pronin

Inventor： Xiaodong Li ,  Hong Xu ,  Qing Li ,  Huixian Tang ,  Alexey Pronin

IPC: G01N33/567 ,  C07K14/705

CPC classification number: G01N33/566 ,  G01N2333/726 ,  G01N2500/02 ,  G01N2500/04 ,  G01N2500/10

Abstract: The present invention relates to the discovery that specific human taste receptors in the T2R taste receptor family respond to particular bitter compounds. The invention further relates to the use of these receptors in assays for identifying ligands that modulate the activation of these taste receptors by these bitter ligands and related compounds and which may be used as additives and/or removed from foods, beverages, cosmetics and medicinals in order to modify (block) T2R-associated bitter taste.

Abstract translation: 本发明涉及T2R味觉受体家族中的特定人味受体对特定苦味化合物的反应的发现。 本发明还涉及这些受体在测定中用于鉴定通过这些苦味配体和相关化合物调节这些味觉受体的活化的配体的用途，并且可以用作添加剂和/或从食品，饮料，化妆品和药物中去除 订单修改（阻断）T2R相关苦味。

公开(公告)号：US20110230502A1

公开(公告)日：2011-09-22

申请号：US13051586

申请日：2011-03-18

Applicant: Catherine TACHDJIAN ,  Xiao-Qing Tang ,  Sara Werner ,  Marketa Rinnova ,  Qing Chen ,  Guy Servant ,  Xiaodong Li ,  Feng Zhang ,  Haitian Liu ,  Albert Zlotnik ,  Mark Zoller ,  Boris Klebansky ,  Richard Fine ,  Xinshan Kang

Inventor： Catherine TACHDJIAN ,  Xiao-Qing Tang ,  Sara Werner ,  Marketa Rinnova ,  Qing Chen ,  Guy Servant ,  Xiaodong Li ,  Feng Zhang ,  Haitian Liu ,  Albert Zlotnik ,  Mark Zoller ,  Boris Klebansky ,  Richard Fine ,  Xinshan Kang

IPC: A61K31/519 ,  A61K31/522 ,  A61K31/437 ,  A61K31/4355 ,  A61K31/4365 ,  A61P27/00

CPC classification number: C07D513/04 ,  A23L2/39 ,  A23L2/60 ,  A23L27/30 ,  A23L27/31 ,  A23L27/33 ,  A23L27/34 ,  A23L27/88 ,  C07D215/42 ,  C07D215/54 ,  C07D215/56 ,  C07D239/70 ,  C07D239/84 ,  C07D239/94 ,  C07D239/95 ,  C07D285/16 ,  C07D417/04 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04 ,  C07D491/04 ,  C07D491/056 ,  C07D493/04 ,  C07D495/04 ,  C07D495/14 ,  C07D513/20 ,  G01N33/566

Abstract: The present invention provides screening methods for identifying modifiers of chemosensory receptors and their ligands, e.g., by determining whether a test entity is suitable to interact with one or more interacting sites within the Venus flytrap domains of the chemosensory receptors as well as modifiers capable of modulating chemosensory receptors and their ligands.

Abstract translation: 本发明提供了用于鉴定化学感受器及其配体的调节剂的筛选方法，例如通过确定测试实体是否适合与化学感应受体的金星蝇捕获结构域内的一个或多个相互作用位点相互作用，以及能调节 化学感受器及其配体。

公开(公告)号：US07968693B2

公开(公告)日：2011-06-28

申请号：US12144097

申请日：2008-06-23

Applicant: Jon Elliot Adler

Inventor： Jon Elliot Adler

IPC: C12N15/12 ,  C07K14/705

CPC classification number: G01N33/74 ,  A01K2217/05 ,  A61K38/00 ,  C07H21/04 ,  C07K14/705 ,  C07K2319/00 ,  G01N33/566 ,  G01N33/582 ,  G01N2333/726 ,  G01N2500/00 ,  G01N2500/04

Abstract: Newly identified mammalian taste-cell-specific G Protein-Coupled Receptors and the genes encoding said receptors are described. Specifically, T2R taste G Protein-Coupled Receptors that are believed to be involved in bitter taste sensation, and the genes encoding the same, are described, along with methods for isolating such genes and for isolating and expressing such receptors. Methods for representing taste perception of a particular tastant in a mammal are also described, as are methods for generating a novel molecules or combinations of molecules that elicit a predetermined taste perception in a mammal, and methods for simulating one or more tastes.

Abstract translation: 描述了新鉴定的哺乳动物味细胞特异性G蛋白偶联受体和编码所述受体的基因。 具体地，描述被认为涉及苦味感觉的T2R味道G蛋白偶联受体以及编码它们的基因，以及用于分离这些基因并分离和表达此类受体的方法。 还描述了用于表示哺乳动物中特定促味剂的味觉的方法，以及用于产生在哺乳动物中引发预定味觉的新分子或分子组合的方法，以及用于模拟一种或多种口味的方法。

公开(公告)号：US07906328B2

公开(公告)日：2011-03-15

申请号：US12270824

申请日：2008-11-13

Applicant: Mark Zoller ,  Xiaodong Li ,  Lena Staszewski ,  Shawn O'Connell ,  Sergey Zozulya ,  Jon Elliot Adler ,  Hong Xu ,  Fernando Echeverri

Inventor： Mark Zoller ,  Xiaodong Li ,  Lena Staszewski ,  Shawn O'Connell ,  Sergey Zozulya ,  Jon Elliot Adler ,  Hong Xu ,  Fernando Echeverri

IPC: C12N5/00 ,  C12N5/02 ,  C12N1/20 ,  C12N15/00 ,  C12N15/74 ,  C12P21/06 ,  C07K1/00 ,  C07K14/00 ,  C07K17/00

CPC classification number: G01N33/5041 ,  A01K2217/05 ,  C07K14/705 ,  C07K2319/00 ,  C12Q1/6876 ,  C12Q2600/124 ,  C12Q2600/158 ,  G01N33/5008 ,  G01N33/566 ,  G01N2333/4719 ,  G01N2333/705 ,  G01N2333/726 ,  G01N2500/04

Abstract: The present invention relates to the discovery that the T1R receptors assemble to form functional taste receptors. Particularly, it has been discovered that co-expression of T1R1 and T1R3 results in a taste receptor that responds to umami taste stimuli, including monosodium glutamate. Also, it has been discovered that co-expression of the T1R2 and T1R3 receptors results in a taste receptor that responds to sweet taste stimuli including naturally occurring and artificial sweeteners. Also the present invention relates to the use of hetero-oligomeric taste receptors comprising T1R1/T1R3 and T1R2/T1R3 in assays to identify compounds that respectively respond to umami taste stimuli and sweet taste stimuli. Further, the invention relates to the constitutive of cell lines that stably or transiently co-express a combination of T1R1 and T1R3; or T1R2 and T1R3; under constitutive or inducible conditions. The use of these cells lines in cell-based assays to identify umami and sweet taste modulatory compounds is also provided, particularly high throughput screening assays that detect receptor activity by use of fluorometric imaging.

Abstract translation: 本发明涉及T1R受体组装形成功能性味觉受体的发现。 特别地，已经发现，T1R1和T1R3的共表达导致对鲜味刺激（包括谷氨酸钠）起反应的味觉感受器。 此外，已经发现，T1R2和T1R3受体的共表达导致对包括天然存在的和人造甜味剂的甜味刺激有反应的味觉受体。 本发明还涉及在测定中使用包含T1R1 / T1R3和T1R2 / T1R3的异低聚味觉感受器来鉴定分别响应于鲜味刺激和甜味刺激的化合物。 此外，本发明涉及稳定或瞬时共表达T1R1和T1R3的组合的细胞系的组成; 或T1R2和T1R3; 在组成型或诱导性条件下。 还提供了在基于细胞的测定中使用这些细胞系以鉴定鲜味和甜味调节化合物，特别是通过使用荧光成像检测受体活性的高通量筛选测定。