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Melatonin receptor type 1A
Target name: Melatonin receptor type 1A (MTR1A)
Gene: MTNR1A
Uniprot Accession: P48039
Origin: Human (Homo sapiens)
Class: Class A GPCR
Sequence: Full-length, wildtype sequence, with a N-terminus Strep tag II, 8xHis-tag, and TEV protease cleavage site
Affinity Tag: Strepx2/His (both N-terminal)
Catalogue number: PP2
Theor. MW: 44,8kDa
Shipment temperature: Dry Ice
Storage conditions: Store at -80°C
Expression system: Sf9 insect cells (baculovirus)
Purity: >90%
Purification: Metal Affinity Chromatography in presence of Sarkosyl/CHS
Activity: Confirmed by radiobinding assay and activation of Gi
Concentration: Up to 5mg/ml
Sample buffer: 25mM Na2HPO4 pH 8.0, 150mM NaCl, 0.86%/0.18% Sarkosyl/CHS
Available quantity: From 10µg up to mg scale
Melatonin receptor type 1A: We apply a unique & custom-built program to give you an edge
Melatonin receptor type 1A (MTR1A) modulates neuronal firing, arterial vasoconstriction, cell proliferation in cancer cells, and reproductive and metabolic functions. MTR1A is a good therapeutic candidate for insomnia, circadian sleep disorders, depression, cardiovascular regulation, cancer, and neurodegenerative diseases.
CALIXAR’s Melatonin receptor type 1A aids in reliable fragment-based drug design (FBDD), structure-based drug discovery (SBDD) and antibody discovery against this specific target.
Unlike Calixar’s MTR1A, 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, MTR1A is unstable target and inherently difficult to produce natively with conventional approaches. Traditionally, Melatonin receptor type 1A 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 MTR1A is 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.
CALIXAR’s MTR1A is the first native full-length and operative target on the market. Other existing MTR1A targets are either mutated and or truncated. Our Melatonin receptor type 1A is produced in a eukaryotic arrangement with the precise post-translational adjustments (glycosylation).
CALIXAR’s MTNR1A Melatonin receptors are high-quality membrane proteins utilized in (bio)drug discovery projects and are adapted for use in pharmaceutical firms, biotechnology companies, as well as for academic teams that are committed to the life science fields.
- Capacity to adapt the buffer condition
- Antibodies (including nanobodies, scaffold proteins, aptamers)
- Small molecules
- 3D Structures (classical X-ray or XFEL, Cryo-EM, NMR)
- Medicine discovery (Screening: HTS, FBDD, SBDD; Hit and lead validation)
- Antibody discovery (Immunization and display technology)
- Clinical stage (drug validation on reliable native MT1)
