17:33 , Jan 9, 2019 |  BC Innovations  |  Distillery Therapeutics

Cardiovascular

INDICATION: Heart failure; ischemia/reperfusion injury Cell culture and mouse studies suggest inhibiting GRK2 localization to the mitochondria could help treat heart failure following cardiac ischemia/reperfusion injury. In a mouse model of heart failure following ischemia/reperfusion...
15:19 , Sep 20, 2018 |  BC Innovations  |  Distillery Therapeutics

Infectious disease

INDICATION: Influenza virus Cell culture and mouse studies suggest inhibiting GRK2 could help treat influenza A infection. In a human alveolar basal epithelium cell line infected with human or avian strains of influenza A, an...
22:06 , Jul 25, 2017 |  BC Innovations  |  Distillery Therapeutics

Cardiovascular

INDICATION: Heart failure In vitro and cell culture studies identified a methyltriazole-based GRK2 inhibitor that could help treat heart failure. Previous studies have shown GRK2 levels are elevated in cardiac tissue of heart failure patients....
00:36 , Jul 20, 2017 |  BC Extra  |  Preclinical News

Paper: GRK2 inhibitors could treat heart failure

In a paper published in the Journal of Medicinal Chemistry , researchers with Takeda Pharmaceutical Co. Ltd. (Tokyo:4502) described a new class of small molecule G protein-coupled receptor kinase 2 ( GRK2 ; GPRK2) inhibitors...
19:14 , Mar 29, 2017 |  BC Innovations  |  Distillery Therapeutics

Cardiovascular

INDICATION: Heart failure In vitro and cell culture studies identified a GRK2 -inhibiting analog of Paxil paroxetine that could help treat heart failure. Structure-based design, chemical synthesis and in vitro testing of analogs of the...
07:00 , Mar 31, 2016 |  BC Innovations  |  Distillery Therapeutics

Therapeutics: G protein-coupled receptor kinase 2 (GRK2; GPRK2)

Cardiovascular disease INDICATION: Heart failure Mouse studies suggest a peptide derived from GRK2 could help treat heart failure. In a mouse model of chronic pressure overload-induced heart failure, transgenic cardiac-specific expression of a peptide from...
07:00 , Jun 30, 2011 |  BC Innovations  |  Distillery Therapeutics

Indication: Cancer

Indication Target/marker/pathway Summary Licensing status Publication and contact information Cancer Cancer G protein-coupled receptor kinase 2 (GRK2; GPRK2); casein kinase 1a (CSNK1A; CKI-a) Cell culture studies suggest antagonizing GRK2 and CSNK1A could help treat cancers...
07:00 , Jun 30, 2011 |  BC Innovations  |  Targets & Mechanisms

Smoother tumor targets

Texas researchers have identified two kinases- GRK2 and CKI-a-that are responsible for phosphorylating smoothened , the central player in the hedgehog signaling pathway. 1 The findings could open a new front against the tumor-promoting pathway...
08:00 , Feb 18, 2010 |  BC Innovations  |  Distillery Therapeutics

Indication: Indication

Indication Target/marker/pathway Summary Licensing status Publication and contact information Neurology Pain G protein-coupled receptor kinase 2 (GRK2; GPRK2); macrophage inflammatory protein-1a (CCL3; MIP1A) In vitro and rodent studies suggest that preventing inflammation-induced loss of GRK2...
07:00 , Aug 21, 2008 |  BC Innovations  |  Targets & Mechanisms

GRK5: Big-hearted Target

A team of U.S. and U.K. researchers has uncovered a new role for G protein-coupled receptor kinase 5 in pathological cardiac hypertrophy, providing a first mechanistic target for this indication. 1 It behaves more like...