BioCentury | Jan 9, 2019
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...
BioCentury | Sep 20, 2018
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...
BioCentury | Jul 25, 2017
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....
BioCentury | Jul 20, 2017
Preclinical News

Paper: GRK2 inhibitors could treat heart failure

...kinase activity, then produced a lead compound that bound to GRK2 and the closely related GRK3...
BioCentury | Mar 29, 2017
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...
BioCentury | Mar 31, 2016
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...
BioCentury | Feb 13, 2014
Distillery Therapeutics

Indication: Cancer

...contact information Cancer Prostate cancer G protein-coupled receptor kinase 3 (GRK3; ADRBK2) Mouse and human sample studies suggest inhibiting ADRBK2...
...cells, shRNA against ADRBK2 decreased primary tumor growth compared with control shRNA, whereas overexpression of ADRBK2...
...proliferation. Next steps include investigating ADRBK2's mechanism of action and identifying small molecule inhibitors of ADRBK2...
BioCentury | Jun 30, 2011
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...
BioCentury | Jun 30, 2011
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...
BioCentury | Apr 28, 2011
Distillery Techniques

Technology: Disease models

This week in techniques Approach Summary Licensing status Publication and contact information Disease models Genetic mouse model of attention deficit hyperactivity disorder (ADHD) Mice lacking a gene linked to ADHD could be used to help...
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