DR. MICHAEL RUSH LERNER, M.D
Dermatology at 4 Ave, San Diego, CA

2003000, Jan 9, 2003

Aug 28, 2002

10/229973

Michael Lerner - Rancho Santa Fe CA, US

G01N033/567, C12M001/34

435/007210, 435/287200

The invention exploits the evolutionary principles responsible for the development of the broad spectrum general odorant detector system, to create a G-protein coupled receptor (GPCR) based system capable of detecting and discriminating between thousands of chemicals. The means is to subject a defined set of receptors such as G-protein coupled receptors, tyrosine kinase receptors, and/or ion channels, to the types of evolutionary forces that have created the array of approximately 1,000 natural receptors used in general olfaction by higher animals. This goal is accomplished by ‘directed evolution-in-a-test-tube’ by imposing very high rates of mutation and extremely strict selection criteria to create a sensor. The novel sensor is selected using a sensitive melanophore-based functional bioassay. Stimulation of the sensor upon interaction with chemical signatures derived from ordinances will result in a calcium ion flux rapidly detectable as a fluorescent signal.

2004014, Jul 22, 2004

Dec 6, 2002

10/314048

David Unett - San Diego CA, US
Ruoping Chen - San Diego CA, US
Jeremy Richman - San Diego CA, US
Daniel Connolly - Carlsbad CA, US
Huong Dang - San Diego CA, US
Bryan Choi - Bonita CA, US
James Leonard - San Diego CA, US
Yaron Hakak - San Diego CA, US
Chen Liaw - San Diego CA, US
Dominic Behan - San Diego CA, US
Derek Chalmers - Cardiff CA, US
Michael Lerner - Rancho Santa Fe CA, US
Kevin Lowitz - Somerset NJ, US

Arena Pharmaceuticals, Inc. - San Diego CA

G01N033/53, A61K031/4439

435/007100, 514/341000

The present invention relates to methods of identifying whether a candidate compound is a modulator of a G protein-coupled receptor (GPCR). In preferred embodiments, the GPCR is human. In other preferred embodiments, the GPCR is coupled to Gi and lowers the level of intracellular cAMP. In other preferred embodiments, the GPCR is expressed endogenously by adipocytes. In further preferred embodiments, the GPCR inhibits intracellular lipolysis. In other further preferred embodiments, the GPCR is a nicotinic acid receptor. The present invention also relates to methods of using a modulator of said GPCR. Preferred modulator is agonist. Agonists of the invention are useful as therapeutic agents for the prevention or treatment of metabolic-related disorders, including dyslipidemia, atherosclerosis, coronary heart disease, stroke, insulin resistance, and type 2 diabetes.

2005000, Jan 6, 2005

Jul 23, 2004

10/897815

David Unett - San Diego CA, US
Ruoping Chen - San Diego CA, US
Jeremy Richman - San Diego CA, US
Daniel Connolly - Carlsbad CA, US
Chen Liaw - San Diego CA, US
Dominic Behan - San Diego CA, US
Derek Chalmers - Cardiff CA, US
Michael Lerner - Rancho Santa Fe CA, US
Huong Dang - San Diego CA, US
Bryan Choi - Bonita CA, US
James Leonard - San Diego CA, US
Yaron Hakak - San Diego CA, US
Kevin Lowitz - Sunnyvale CA, US

Arena Pharmaceuticals, Inc. - San Diego CA

A61K031/4439, G01N033/53

514341000, 435007100

The present invention relates to methods of identifying whether a candidate compound is a modulator of a G protein-coupled receptor (GPCR). In preferred embodiments, the GPCR is human. In other preferred embodiments, the GPCR is coupled to Gi and lowers the level of intracellular cAMP. In other preferred embodiments, the GPCR is expressed endogenously by adipocytes. In further preferred embodiments, the GPCR inhibits intracellular lipolysis. In other further preferred embodiments, the GPCR is a nicotinic acid receptor. The present invention also relates to methods of using a modulator of said GPCR. Preferred modulator is agonist. Agonists of the invention are useful as therapeutic agents for the prevention or treatment of metabolic-related disorders, including dyslipidemia, atherosclerosis, coronary heart disease, stroke, insulin resistance, and type 2 diabetes.

2007007, Apr 5, 2007

Nov 22, 2006

11/603625

Chen Liaw - San Diego CA, US
Dominic Behan - San Diego CA, US
Derek Chalmers - Cardiff CA, US
Michael Lerner - Rancho Santa Fe CA, US
Huong Dang - San Diego CA, US
Bryan Choi - Bonita CA, US
James Leonard - San Diego CA, US
Yaron Hakak - San Diego CA, US
Kevin Lowitz - Sunnyvale CA, US
David Unett - San Diego CA, US
Ruoping Chen - San Diego CA, US
Jeremy Richman - San Diego CA, US
Daniel Connolly - Carlsbad CA, US

Arena Pharmaceuticals, Inc. - San Diego CA

A01K 67/027, G01N 33/53, C12P 21/06, C07D 403/02, C07K 14/705

800014000, 435007100, 800018000, 435069100, 435320100, 435325000, 546268100, 514341000

The present invention relates to methods of identifying whether a candidate compound is a modulator of a G protein-coupled receptor (GPCR). In preferred embodiments, the GPCR is human. In other preferred embodiments, the GPCR is coupled to Gi and lowers the level of intracellular cAMP. In other preferred embodiments, the GPCR is expressed endogenously by adipocytes. In further preferred embodiments, the GPCR inhibits intracellular lipolysis. In other further preferred embodiments, the GPCR is a nicotinic acid receptor. The present invention also relates to methods of using a modulator of said GPCR. Preferred modulator is agonist. Agonists of the invention are useful as therapeutic agents for the prevention or treatment of metabolic-related disorders, including dyslipidemia, atherosclerosis, coronary heart disease, stroke, insulin resistance, and type 2 diabetes.

7829298, Nov 9, 2010

Aug 31, 2004

10/930662

David J. Unett - San Diego CA, US
Ruoping Chen - San Diego CA, US
Jeremy G. Richman - San Diego CA, US
Daniel T. Connolly - Solana Beach CA, US
Huong T. Dang - San Diego CA, US
Bryan J. Choi - Bonita CA, US
James N. Leonard - San Diego CA, US
Yaron Hakak - San Diego CA, US
Chen W. Liaw - San Diego CA, US
Dominic P. Behan - San Diego CA, US
Derek T. Chalmers - Cardiff CA, US
Michael R. Lerner - Rancho Santa Fe CA, US
Kevin P. Lowitz - Sunnyvale CA, US

Arena Pharmaceuticals, Inc. - San Diego CA

G01N 33/53

435 72

The present invention relates to methods of identifying whether a candidate compound is a modulator of a G protein-coupled receptor (GPCR). In preferred embodiments, the GPCR is human. In other preferred embodiments, the GPCR is coupled to Gi and lowers the level of intracellular cAMP. In other preferred embodiments, the GPCR is expressed endogenously by adipocytes. In further preferred embodiments, the GPCR inhibits intracellular lipolysis. In other further preferred embodiments, the GPCR is a nicotinic acid receptor. The present invention also relates to methods of using a modulator of said GPCR. Preferred modulator is agonist. Agonists of the invention are useful as therapeutic agents for the prevention or treatment of metabolic-related disorders, including dyslipidemia, atherosclerosis, coronary heart disease, stroke, insulin resistance, and type 2 diabetes.