Melatonin receptor 1 (MT1) is a class A GPCR that modulates neuronal firing, arterial vasoconstriction, cell proliferation in cancer cells, and reproductive and metabolic functions.  MT1 is a good therapeutic candidate for insomnia, circadian sleep disorders, depression, cardiovascular regulation, cancer, and neurodegenerative diseases.

CALIXAR’s MT1 Melatonin receptors aid in reliable fragment-based drug design (FBDD), structure-based drug discovery (SBDD) and antibody discovery against this specific target. 

Unlike Calixar’s MT1 Melatonin receptors, other alternative approaches have resulted in a Melatonin receptor that becomes mutated and truncated (96 amino-acids at the C-terminus). This truncation is unable to bind to its natural ligands. In addition, this mutated version becomes locked within an antagonist conformation.

As with all GPCRs, MT1 Melatonin receptors are unstable targets and inherently difficult to produce natively with conventional approaches. Traditionally, MT1 Melatonin receptors could only be locked in one specific conformation (e.g. antagonist) and were only ever developed in a solution that essentially cannot be pure, nor native (truncated, mutated), without PTMs, and consequently are unstable.

In contrast, CALIXAR’s MT1 Receptors are able to bind to agonists, antagonists, as well as allosteric modulators and preserve their structural and functional integrity. They are purified and stabilized to full length and wild-type (native) proteins.