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

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...
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

This week in therapeutics Indication Target/marker/pathway Summary Licensing status Publication and contact information Cancer Prostate cancer G protein-coupled receptor kinase 3 (GRK3; ADRBK2) Mouse and human sample studies suggest inhibiting ADRBK2 could help suppress prostate...
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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