Duke University

Temple University

Research Triangle Institute

Molecular Devices Corporation

Sanford-burnham Medical Research Institute

Lawrence S Barak

Marc G Caron

Jie Zhang

Stephen S Ferguson

Robert H Oakley

Stephane Alain Laporte

Robert Anthony Mook

Herbert H Seltzman

Jiangbo Wang

Wei Chen

Mary E Abood

Pingwei Zhao

Anthony B Pinkerton

David Needham

Herbert K Lyerly

Paul M Hershberger

Patrick R Maloney

Satyamaheshwar Peddibhotla

Michael P Hedrick

Xiu-rong Ren

Robert A Mook

Anthony Angelo Ribeiro

H Kim Lyerly

Michael A Shetzline

Minyong Chen

Xiu-Rong Ren

Herbert Kim Lyerly

Described are methods of treating a disease associated with dysregulation of the Wnt/Frizzled signaling pathway. The methods include identifying subjects in need of therapy, administering inhibitors of the Wnt/Frizzled signaling pathway, pharmaceutical compositions including the inhibitors, and methods of using the compounds and compositions for treating cancer, bacterial and viral infection, lupus, type II diabetes, nonalcoholic steatohepatitis (NASH) and nonalcoholic fatty liver disease (NAFLD) in a subject.

Chemical modulators of signaling pathways and therapeutic use

Provided herein are small molecule neurotensin receptor agonists, compositions comprising the compounds, and methods of using the compounds and compositions comprising the compounds.

Small molecule agonists of neurotensin receptor 1

Compounds are provided having agonistic activity against G protein-coupled receptor 35 (GPR35). The compounds are useful for providing antinociception, providing neuroprotection in case of stroke or ischemia, or treating gastric inflammation.

Treatment of disorders associated with G protein-coupled receptor 35 (GPR35)

Compounds of general Formulas (I), (IA), (IB) are described, along with compositions containing the same and methods of use thereof, inhibiting the hedgehog pathway in a cell or inhibiting unwanted proliferation of a cell.

Smoothened modulators and methods of use thereof

Described are methods of detecting G-protein coupled receptor (GPCR) activity in vivo and in vitro; methods of assaying GPCR activity; and methods of screening for GPCR ligands, G protein-coupled receptor kinase (GRK) activity, and compounds that interact with components of the GPCR regulatory process. Constructs useful in such methods are described.

Methods of assaying receptor activity and constructs useful in such methods

The present invention is related to the detection of GPCR ligands in a test sample by using a single cell biosensor expressing a GPCR. Preferably, the test sample is derived from a biological or environmental sample. This invention may be used to detect the presence of a disease or to detect the presence of a harmful agent in the environment. Included in the present invention is an array of biosensors that detect ligands of various GPCRs.

Single-cell biosensor for the measurement of GPCR ligands in a test sample

The present invention relates to modified G-protein coupled receptors (GPCRs). The modified GPCRs of the present invention include GPCRs that have been modified to have carboxyl terminal tails comprising one or more sites of phosphorylation, preferably one or more clusters of phosphorylation sites. The modified GPCRs of the present invention may comprise a retained portion of a carboxyl-terminus region from a first GPCR fused to a polypeptide, wherein the polypeptide comprises the one or more clusters of phosphorylation. The present invention also relates to methods of screening compounds and sample solutions for GPCR activity using the modified GPCRs.

Modified G-protein coupled receptors

The methods of the present invention allow the screening of a test composition for non-receptor-specific GPCR desensitization inhibitory activity. The methods involve screening a test composition for an indication of GPCR desensitization inhibitory activity against two or more GPCRs that are different from each other. When there is an indication that a particular test composition has GPCR desensitization inhibitory activity with respect to each of the two or more GPCRs that are different from one another, then, according to the present invention, there is an indication that the test composition has non-receptor-specific GPCR desensitization inhibitory activity.

Methods of screening compositions for G protein-coupled receptor desensitization inhibitory activity

Described are methods of detecting G-protein coupled receptor (GPCR) activity in vivo and in vitro; methods of assaying GPCR activity; and methods of screening for GPCR ligands, G Protein-coupled receptor kinase (GRK) activity, and compounds that interact with components of the GPCR regulatory process.

Methods of assaying receptor activity

Described are methods of detecting G-protein coupled receptor (GPCR) activity in vivo and in vitro; methods of assaying GPCR activity; and methods of screening for GPCR ligands, G Protein-coupled receptor kinase (GRK) activity, and compounds that interact with components of the GPCR regulatory process. Constructs useful in such methods are described.

Methods of assaying receptor activity and constructs useful in such

Growing community of inventors

Durham, NC, United States of America

Lawrence S Barak