Robert H. Oakley - Durham NC, US Christine C. Hudson - Durham NC, US
Assignee:
Molecular Devices Corporation - Sunnyvale CA
International Classification:
G01N 33/566
US Classification:
435 72, 435 721, 435 76, 436501
Abstract:
The present invention relates to agonist-independent methods of screening for compounds that alter GPCR desensitization. Included in the present invention are cell lines containing GRKs, in which GPCRs are desensitized in the absence of agonist; the GRKs may be modified. The present invention relates to methods to determine if a GPCR is expressed at the plasma membrane, and if the GPCR has an affinity for arrestin. Modified GPCRs which have increased arrestin affinity are included in the present invention. These modified GPCRs are useful in methods to screen for compounds that alter desensitization, including both the agonist-independent methods and agonist-dependent methods described herein.
Mitchell A. deLong - Raleigh NC, US Marcos L. Sznaidman - Durham NC, US Robert H. Oakley - Durham NC, US Allen E. Eckhardt - Durham NC, US Christine Hudson - Durham NC, US Jeffrey D. Yingling - Apex NC, US Michael Peel - Chapel Hill NC, US Thomas E. Richardson - Durham NC, US Claire Louise Murray - Chapel Hill NC, US Brian H. Heasley - Wake Forest NC, US Paresma R. Patel - San Diego CA, US
Assignee:
Aerie Pharmaceuticals, Inc. - Research Triangle Park NC
International Classification:
C07D 217/00 C07D 401/00 C07D 215/00
US Classification:
546146, 546148, 546152
Abstract:
Isoquinoline compounds with G are provided that influence, inhibit or reduce the action of a G-protein receptor kinase. Pharmaceutical compositions including therapeutically effective amounts of the isoquinoline compounds and pharmaceutically acceptable carriers are also provided. Various methods using the compounds and/or compositions to affect disease states or conditions such as cancer, osteoporosis and glaucoma are also provided.
Methods Of Screening Compounds For Grk6 Modulating Activity
Robert Oakley - Durham NC, US Christine Hudson - Durham NC, US Marc Caron - Hillsborough NC, US Raul Gainetdinov - Durham NC, US Robert Lefkowitz - Durham NC, US Richard Premont - Durham NC, US
International Classification:
G01N 33/567 G01N 33/53
US Classification:
435007200
Abstract:
The present invention relates to methods of treating disease by altering G protein coupled receptor kinase (GRK) 6. This may be done by altering the expression or activity of the protein, for example. The present invention may be used for disease diagnosis, by detecting the expression or activity of GRK6. The present invention relates to a GRK6 deficient mouse, GRK6 splice variants, and methods of use. The present invention also relates to methods of identifying compounds that alter GRK6 activity. The present invention relates to disease treatment by altering GRK6 expression or activity.
Mitchell deLong - Raleigh NC, US Marcos Sznaidman - Durham NC, US Robert Oakley - Durham NC, US Allen Eckhardt - Durham NC, US Christine Hudson - Durham NC, US Jeffrey Yingling - Apex NC, US Michael Peel - Chapel Hill NC, US Thomas Richardson - Durham NC, US Clare Murray - Chapel Hill NC, US Brian Heasley - Wake Forest NC, US Paresma Patel - San Diego CA, US
Assignee:
Aerie Pharmaceuticals, Inc. - Research Triangle Park NC
International Classification:
A61K 31/44
US Classification:
514357000, 546332000
Abstract:
Hydrazide compounds with GPCR desensitization inhibitory activity are provided that may be used to influence, inhibit or reduce the action of a G-protein receptor kinase. Pharmaceutical compositions including therapeutically effective amounts of the hydrazide compounds and pharmaceutically acceptable carriers are also provided. Various methods using the compounds and/or compositions to affect disease states or conditions controlled or influenced by GPCRs are also provided. Various methods using the compounds and/or compositions to affect disease states or conditions such as cancer, osteoporosis and glaucoma are also provided.
Mitchell A. deLong - Raleigh NC, US Marcos L. Sznaidman - Durham NC, US Robert H. Oakley - Durham NC, US Allen E. Eckhardt - Durham NC, US Christine Hudson - Durham NC, US Jeffrey D. Yingling - Apex NC, US Michael Peel - Chapel Hill NC, US Thomas E. Richardson - Durham NC, US Clare Louise Murray - Chapel Hill NC, US Brian H. Heasley - Wake Forest NC, US Paresma R. Patel - San Diego CA, US
Assignee:
Aerie Pharmaceuticals, Inc. - Research Triangle Park NC
Isoquinoline compounds with G are provided that influence, inhibit or reduce the action of a G-protein receptor kinase. Pharmaceutical compositions including therapeutically effective amounts of the isoquinoline compounds and pharmaceutically acceptable carriers are also provided. Various methods using the compounds and/or compositions to affect disease states or conditions such as cancer, osteoporosis and glaucoma are also provided.
Robert H. Oakley - Durham NC, US Christine C. Hudson - Durham NC, US
Assignee:
Molecular Devices Corporation - Sunnyvale CA
International Classification:
C12Q 1/68 C12N 5/10 C07H 21/00
US Classification:
435 6, 435325, 536 221
Abstract:
The present invention relates to agonist-independent methods of screening for compounds that alter GPCR desensitization. Included in the present invention are cell lines containing GRKs, in which GPCRs are desensitized in the absence of agonist; the GRKs may be modified. The present invention relates to methods to determine if a GPCR is expressed at the plasma membrane, and if the GPCR has an affinity for arrestin. Modified GPCRs which have increased arrestin affinity are included in the present invention. These modified GPCRs are useful in methods to screen for compounds that alter desensitization, including both the agonist-independent methods and agonist-dependent methods described herein.
The present invention relates to agonist-independent methods of screening for compounds that alter GPCR desensitization. Included in the present invention are cell lines containing GRKs, in which GPCRs are desensitized in the absence of agonist; the GRKs may be modified. The present invention relates to methods to determine if a GPCR is expressed at the plasma membrane, and if the GPCR has an affinity for arrestin. Modified GPCRs which have increased arrestin affinity are included in the present invention. These modified GPCRs are useful in methods to screen for compounds that alter desensitization, including both the agonist-independent methods and agonist-dependent methods described herein.
Mitchell A. deLong - Raleigh NC, US Marcos L. Sznaidman - Durham NC, US Robert H. Oakley - Durham NC, US Allen E. Eckhardt - Durham NC, US Christine Hudson - Durham NC, US Jeffrey D. Yingling - Apex NC, US Michael Peel - Chapel Hill NC, US Thomas E. Richardson - Durham NC, US Clare Louise Murray - Chapel Hill NC, US Brian H. Heasley - Wake Forest NC, US Paresma R. Patel - San Diego CA, US
Assignee:
AERIE PHARMACEUTICALS, INC. - Research Triangle Park NC
Isoquinoline compounds with G are provided that influence, inhibit or reduce the action of a G-protein receptor kinase. Pharmaceutical compositions including therapeutically effective amounts of the isoquinoline compounds and pharmaceutically acceptable carriers are also provided. Various methods using the compounds and/or compositions to affect disease states or conditions such as cancer, osteoporosis and glaucoma are also provided.