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 siRNA...
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. High...
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 that could help...
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 selective serotonin...
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 the G...
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...
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 if sufficiently selective...
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...
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 an...
08:00 , Mar 5, 2007 |  BioCentury  |  Tools & Techniques

Relaxing the hyper heart

Blocking a receptor-regulating protein present in the adrenals prevents a failing heart from going into overdrive and allows it to relax and heal, according to a report in Nature Medicine by researchers at the Center...