Application
Small molecule inhibitors of NOX4 signaling with a wide array of therapeutic potential.
Key Benefits
- Small molecule inhibitors of NOX4 signaling.
- Low cytotoxicity.
Market Summary
The NADPH oxidase 4 (NOX4) has gained considerable and growing attention during the past years because of its potential key involvement in a variety of diseases, some of which have high unmet medical needs. Currently the few known NOX4 inhibitors that are in clinical trials are non-specific molecules. Finding a new class of small molecule inhibitors has substantial advantages in drug development, as it provides opportunities for modifications to improve pharmacodynamics and/or pharmacokinetic properties.
Technical Summary
Emory researchers and colleagues from other universities have identified a new class of small molecules with promising inhibitory properties. NOX4 is an NADPH oxidase most abundantly expressed in the kidney and lung. The small molecules identified by our inventors inhibit NOX4-dependent intracellular signaling. Additionally, the compounds do not show any non-specific ROS scavenging activity, nor do they affect NOX4 expression. They were also shown to have low cytotoxic effects. These inhibitors are promising drug candidates in conditions such as idiopathic pulmonary fibrosis (IPF), pulmonary arterial hypertension (PAH), diabetic nephropathy, diabetic cardiomyopathy, diabetic neuropathy, and diabetic retinopathy, as well as cancers such as metastatic renal cell carcinoma (RCC).
Developmental Stage
Pre-clinical development.
Publication: Xu, Q. et al. (2018), Bioorg. Med. Chem., 26(5), 989-998.
