Journal of Pharmacology and Experimental Therapeutics, 2013
Although the use of ET receptor antagonists has been useful in ameliorating disease pathology, there are certain draw- backs to consider. The use of ET antagonists has previously been associated with side effects, such as an increase in heart rate, facial flush, and/or facial edema (Fleisch et al., 2000). In addition, certain ET antagonists may interfere with anticoagulants, such as warfarin, and therefore pose a risk of thrombosis (Weber et al., 1999). These studies indicate the importance of only regulated antagonism of the ET receptor system as a therapeutic tool.
An alternative strategy for prevention of ET-1–induced pathology would be to target the actual elevated levels of ET-1 in pathologic conditions.
At ET-traps Limited, we have developed an Fc-based fusion protein that has a very high binding affinity; in the pico molar range, which is higher than ERAs that are already in clinical use.
Creating a Soluble Binder to Endothelin-1 Based on the Natural Ligand Binding Domains of the Endothelin-1 (G-Protein-Coupled) Receptor: Arjun Jain et al., International Journal of Peptide Research and Therapeutics, 2017
Our PoC work (both in vitro and in vivo) has shown that the ET-traps are non- toxic or cytotoxic at the working concentration, which gives an efficacious effect.
Endothelin-1 traps potently reduce pathologic markers back to basal levels in an in vitro model of diabetes; Arjun Jain et al., Journal of Diabetes & Metabolic Disorders, 2018
In vivo studies demonstrate that endothelin-1 traps are a potential therapy for type I diabetes; Arjun Jain et al., Journal of Diabetes & Metabolic Disorders, 2019 [Accepted, under Publication]
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To know more about Endothelin-1 being implicated in a host of different diseases and its effects, current treatment options, click the link below.