Bryan D Moyer, 5312413 Willow Hill Dr, Moorpark, CA 93021

7932058, Apr 26, 2011

Jun 6, 2008

12/134302

Bryan Moyer - San Diego CA, US
Albert Zlotnik - San Diego CA, US
Peter Hevezi - Encinitas CA, US
Hortensia Soto - San Diego CA, US
Dalia Kalabat - El Cajon CA, US
Min Lu - San Diego CA, US
Na Gao - San Diego CA, US
Evan Carl White - Fair Oaks CA, US

Senomyx, Inc. - San Diego CA

C12N 15/10
C07K 14/705

435 911, 435 78

This invention relates to novel rationale and methods for identifying human and primate taste-specific genes, including genes involved in salty taste perception, especially human salty taste perception, but also genes involved in sweet, bitter, umami, and sour taste perception, and genes involved in other taste cell or taste receptor related activities such as digestive function and digestive related diseases, taste cell turnover, immunoregulation of the oral and digestive tract, and metabolic regulation such as in diabetes and obesity, the genes identified using these methods, and assays for identifying taste modulators (enhancers or blockers) and potential therapeutics using these genes. These compounds have potential application in modulating (enhancing or blocking) taste perception, especially salty taste perception and as potential therapeutics. In addition, this invention relates to novel methods for identifying taste-specific genes that can be used as markers for different taste cell types, including sweet, bitter, umami, sour, salty, and other taste cells in mammals as well as assays that measure the activity of the sweet, bitter, umami, or sour receptor in the presence of these genes to identify modulators of sweet, bitter, umami, and sour taste and to identify therapeutics especially for treating digestive or metabolic disorders, taste loss, and oral infections. Particularly, the genes identified herein and antibodies or oligos thereto can be used as markers to identify and/or purify specific taste cells e. g.

8105792, Jan 31, 2012

Jul 9, 2004

10/887233

Guy Servant - San Diego CA, US
Hong Chang - San Diego CA, US
Cyril Redcrow - San Diego CA, US
Sumita Ray - San Diego CA, US
Imran Clark - Carlsbad CA, US
Bryan Moyer - Thousand Oaks CA, US

Senomyx, Inc. - San Diego CA

G01N 33/53

435 72

In one aspect, the present invention relates to a mammalian cell-based high-throughput assay for the profiling and screening of human epithelial sodium channel (hENaC) cloned from a human kidney c-DNA library and is also expressed in other tissues including human taste tissue. The present invention further relates to amphibian oocyte-based medium-throughput electrophysiological assays for identifying human ENaC modulators, preferably ENaC enhancers. Compounds that modulate ENaC function in a cell-based ENaC assay are expected to affect salty taste in humans. The assays described herein have advantages over existing cellular expression systems. In the case of mammalian cells, such assays can be run in standard 96 or 384 well culture plates in high-throughput mode with enhanced assay results being achieved by the use of a compound that inhibits ENaC function, preferably an amiloride derivative such as Phenamil. In the case of the inventive oocyte electrophysiological assays (two-electrode voltage-clamp technique), these assays facilitate the identification of compounds which specifically modulate human ENaC. The assays of the invention provide a robust screen useful to detect compounds that facilitate (enhance) or inhibit hENaC function.

8357499, Jan 22, 2013

Jan 6, 2006

11/326441

Mark Zoller - La Jolla CA, US
Hong Xu - San Diego CA, US
Lena Staszewski - San Diego CA, US
Bryan Moyer - Thousand Oaks CA, US
Alexey Pronin - San Diego CA, US
Jon Elliot Adler - Sherwood OR, US
Guy Servant - San Diego CA, US
Nicholas Callamaras - San Diego CA, US

Senomyx, Inc. - San Diego CA

G01N 33/567
C07K 14/705
C12N 15/12

435 721, 435 71, 435 72, 436501

The present invention relates to isolated nucleic acid sequences that encode human olfactory cyclic nucleotide gated (CNG) channel subunits, and the corresponding polypeptides. The invention further relates to the use of human CNG channels to profile, screen for, and identify compounds that modulate the human olfactory CNG channel. More specifically, the invention relates to the expression of the human olfactory CNG channel in cells, preferably mammalian cells, and the use of these cells in high throughput cell-based assays to identify compounds that enhance or block human olfactory CNG function. Compounds that activate the olfactory CNG channel will enhance smell and can be used to make foods more palatable for individuals with attenuated olfactory function. Conversely, compounds that inhibit the olfactory CNG channel will inhibit smell and can be use to block malodors. Additionally, the invention relates to the use of cell-based olfactory CNG channel assays to identify modulates of G-protein coupled receptor (GPCRs) and other proteins that regulate cyclic nucleotide levels.

2003022, Dec 11, 2003

Jul 8, 2002

10/189507

Mark Zoller - San Diego CA, US
Hong Xu - San Diego CA, US
Lena Staszewski - San Diego CA, US
Bryan Moyer - San Diego CA, US
Alexy Pronin - San Diego CA, US
Jon Adler - San Diego CA, US
Guy Servant - San Diego CA, US
Nicholas Callamaras - San Diego CA, US

Senomyx, Inc. - La Jolla CA

G01N033/53
G01N033/567
C07H021/04
C12P021/02
C12N005/06
C07K014/47

435/007200, 435/069100, 435/320100, 435/325000, 530/350000, 536/023500

The present invention relates to isolated nucleic acid sequences that encode human olfactory cyclic nucleotide gated (CNG) channel subunits, and the corresponding polypeptides. The invention further relates to the use of human CNG channels to profile, screen for, and identify compounds that modulate the human olfactory CNG channel. More specifically, the invention relates to the expression of the human olfactory CNG channel in cells, preferably mammalian cells, and the use of these cells in high throughput cell-based assays to identify compounds that enhance or block human olfactory CNG function. Compounds that activate the olfactory CNG channel will enhance smell and can be used to make foods more palatable for individuals with attenuated olfactory function. Conversely, compounds that inhibit the olfactory CNG channel will inhibit smell and can be use to block malodors. Additionally, the invention relates to the use of cell-based olfactory CNG channel assays to identify modulates of G-protein coupled receptor (GPCRs) and other proteins that regulate cyclic nucleotide levels.

2006013, Jun 22, 2006

Dec 8, 2004

11/006802

Guy Servant - San Diego CA, US
Mark Ozeck - San Diego CA, US
Paul Brust - San Diego CA, US
Hong Xu - San Diego CA, US
Lena Staszewski - San Diego CA, US
Jon Adler - San Diego CA, US
Mark Zoller - La Jolla CA, US
Nicholas Callamaras - San Diego CA, US
Alexey Pronin - San Diego CA, US
Bryan Moyer - San Diego CA, US

G01N 33/53
C07K 14/705

435007100, 530350000

Screening assays, preferably high throughput, are provided that screen libraries of candidate compounds to identify agonists, antagonists, enhancers or modulators of taste receptors (bitter, sweet or savory (umami) taste receptor) using test cells that co-express at least one functional taste receptor and an olfactory cyclic nucleotide-gated channel (oCNGC). (The oCNGC preferably comprises at least one mutation in one or more subunits that renders the resultant oCNGC more sensitive to CAMP (which in turn enhances the sensitivity of assay using this oCNGC). These taste modulatory compounds are identified based on their effect on oCNGC activity, e.g., using fluorimetric assays that screen for changes in intracellular calcium or sodium concentration in test cells that co-express at least one taste receptor, oCNGC and a Gprotein.

2006022, Oct 5, 2006

Feb 2, 2006

11/345403

Bryan Moyer - San Diego CA, US
Fernando Echeverri - Chula Vista CA, US
Min Lu - San Diego CA, US
Bianca Laita - Oceanside CA, US

SENOMYX, INC. - LaJolla CA

G01N 33/53
C07H 21/04
C07K 14/705
C07K 16/28
C12P 21/06

435007100, 530350000, 530388220, 435320100, 435325000, 536023500, 435069100

Nucleic acid sequences encoding novel splice variants that encode subunits of an ENaC expressed in human taste tissue are provided. These splice variants when expressed in association with other ENaC subunits, i.e., α, β and γ subunits or α, β and Δ subunits may be used to produce amiloride-insensitive ENACs. The resultant amiloride-insensitive ENaCs are useful in in vitro assays for identifying ENaC modulators that modulate taste (enhance or inhibit), particularly human salty taste.

2007016, Jul 12, 2007

Oct 19, 2006

11/583086

Guy Servant - San Diego CA, US
Mark Williams - Carlsbad CA, US
Andrew Patron - San Marcos CA, US
Poonit Kamdar - San Diego CA, US
Qing Chen - San Diego CA, US
Bryan Moyer - San Diego CA, US
David Dahan - Oceanside CA, US
Tanya Ditschun - San Diego CA, US
Sumita Ray - San Diego CA, US
Amy Ligani - San Diego CA, US

SENOMYX, INC. - LaJolla CA

G01N 33/567

435007200

Robust cell based assays are provided that use cells that express wild-type or modified TRPM5 nucleic acid sequences in order to identify putative taste modulators, preferably sweet, bitter and umami taste modulators. The preferred assays use HEK-293 cells that express TRPM5, optionally at least one GPCR, preferably a taste specific GPCR, and a G protein that couples therewith. These assays detect TRPM5 modulators by use of membrane potential dyes that emit fluorescence on changes in TRPM5 activity based on changes in membrane potential and these changes in fluorescence are detectable using Fluorimetric Imaging Plate Readers (FLIPR).

2007025, Nov 8, 2007

Sep 28, 2006

11/536394

Guy Servant - San Diego CA, US
Paul Brust - San Diego CA, US
Bryan Moyer - San Diego CA, US
Min Lu - San Diego CA, US
Fernando Echeverri - Chula Vista CA, US
David Dahan - Oceanside CA, US
Mark Zoller - La Jolla CA, US
Mark Williams - Carlsbad CA, US
Rachel Kimmich - Carlsbad CA, US
Poonit Kamdar - San Diego CA, US
Tanya Ditschun - San Diego CA, US
Andrew Patron - San Marcos CA, US

Senomyx, Inc. - San Diego CA

C12Q 1/68
C07H 21/02
C07H 21/04
C12N 15/85
C12N 5/10

435006000, 435320100, 435358000, 435363000, 435365000, 435366000, 435367000, 536023100, 536024100

Modified human TRPM8 nucleic acid sequences which are efficiently expressed in human cells and cell-based assays and test kits containing same are provided. These assays identify TRPM8 modulators using cells that express a modified human TRPM8 nucleic acid sequence according to the invention, wherein said sequence has been modified relative to a wild-type human TRPM8 nucleic acid sequence in order to optimize ion channel expression in desired cells. Assays using these modified TRPM8 sequences have been shown to identify compounds that modulate the human TRPM8 ion channel better or comparably to known coolants such as menthol and icilin.