Protease-Activated Receptor Type 2 Modulators and InhibitorsTechnology #ua14-181
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Invention: UA14-181 is a novel and highly potent PAR2 modulator. Because PAR2 activation plays a pivotal role in a variety of inflammatory diseases, high affinity and potent ligands of the PAR2 receptor like those found in UA14-181 represent a novel approach to the prevention and treatment of inflammatory diseases.
Background: PAR2 is a well-known cell surface receptor that is involved in the physiology of acute and chronic inflammatory diseases like asthma, inflammatory bowel disease, chronic pain, cancer, and vascular disorders, as well as playing a critical role in angiogenesis and tumor growth. A number of compounds have been explored for use as a drug candidate for the modulation of PAR2, though none have emerged with the potency and selectivity necessary to serve as a leading candidate in vitro.
Application: UA14-181 has been shown to increase ligand efficacy and potency greater than 200-fold. This novel PAR2 antagonist may allow for the development of important and, so far missing, compounds to control PAR2 activation in vitro and in vivo. UA14-181 represents a promising drug development candidate that could promote beneficial anti-inflammatory health effects while limiting the detrimental effects of PAR2 activation and inhibition during disease.
Advantages: UA14-181 is the most potent and efficacious PAR2 agonist known to date. Preliminary research offers a strong preclinical rationale for further development and testing of UA14-181 for the treatment of asthma and other disorders associated with PAR2 activation.