GLP1R is a hot target in the field of treating type 2 diabetes mellitus and a highly sought-after drug target. We invested heavily in the production of this G-protein-coupled receptor and accomplished the purification of the human full-length version of the protein in a copolymer/lipid nanodisc containing native lipids. This form of the protein represents the most native condition after purification that can be achieved - for the highest confidence in your drug discovery endeavors. We also validated the in vitro kinetics of a well-known GLP1R antagonist and cross-referenced them with in vivo literature values to ensure a high-quality product for our customers.

The Glucagon-like peptide 1 receptor is just one example of our new R&D target pipeline. In the table below you can see which proteins are currently under close examination as well. Are you tempted to get your hands on these highly relevant drug targets? Then reach out to our Service Team for this unique opportunity to bring your research to the next level!

#	Target	Class	Comment	Construct	Expression	Protein	Activity	Structure	Antibody	Drug
1	GLPR1	GPCR	GLP1 receptor agonists have been approved for clinical use to treat type 2 diabetes mellitus, inluding exenatide, liraglutide, albiglutide and lixisenatide.
2	P2X4	Ion Channel	P2X4 is involved in pathologies including neuropathic pain and inflammation, involved in autoimmune models.
3	hERG (ERG1, KCNH2)	Ion Channel	hERG1 mediates the repolarizing cardiac current. Blocking of hERG by drugs intended for other therapeutic targets can lead to arrhythmias and sudden death.
4	TGR5	GPCR	Historically identified as a metabolic regulator, more recently additional functions such as regulation of the inflammatory response, cancer and liver regeneration were discovered.
5	ß1 Adrenergic Receptor	GPCR	b1AR influences blood pressure homeostasis and cardiac output, medications treat these conditions by either potentiating or inhibiting the functions of the ADRB-1.
6	MC4R	GPCR	Receptor specific to the heptapeptide core common to adrenocorticotropic hormone and α-, β-, and γ-MSH. Central role in energy homeostasis and somatic growth. Mediated by G proteins that stimulate adenylate cyclase.
7	NTSR1	GPCR	Tridecapeptide neurotensin. Signaling effected via G proteins that activate a phosphatidylinositol-calcium 2nd messenger system. Activation of downstream MAP kinases & protection of cells against apoptosis.
8	OPRM1, MOR-1	GPCR	Receptor for natural and synthetic opioids including morphine, heroin, DAMGO, fentanyl, etorphine, buprenorphin and methadone.
9	SLC17A6, VGluT2	SLC Transporter	Multifunctional transporter that transports L-glutamate as well as multiple ions such as chloride, proton, potassium, sodium and phosphate.
10	TYROBP/DAP12	Receptor	Complex with TYROBP, Receptor for lipoprotein particles, microglia proliferation, Associated with Alzheimer disease
11	TREM2	Receptor	Receptor signaling complex with TYROBP, mediates microglial activation, proliferation, migration, apoptosis & expression of pro-inflammatory (IL6R/CCL3) & anti-inflammatory cytokines (ARG1)
12	CLDN18.2	Claudins	Antibody ligand, immunotherapy based drug development, cancer
13	P2RY10	GPCR	T-cell mediated diseases, orphan GPCR, natural ligand: sphigosine 1-phosphate
14	FAS	Receptor	Receptor for TNFSF6/FASLG. Homotrimer, solvent-exposed domains, aggregation prone
15	CCR8	GPCR	Receptor for the chemokine CCL1/SCYA1/I-309, CCL1 activated with unclear mechanism, Cancer, Alternative coreceptor with CD4 for HIV-1 infection.
16	GPR17	GPCR	Dual specificity receptor uracil nucleotides and cysteinyl leukotrienes (CysLTs), Signals through G(i) and inhibition of adenylyl cyclase, stroke, brain, spinal cord trauma, MS
17	P2RY11	GPCR	Receptor ATP/ADP coupled to G-proteins, Development of anti-inflammator/immunosuppresive therapeutics, anti-inflammatory effect in human dendritic cells
18	CCR7	GPCR	Receptor for the MIP-3-beta chemokine, Probable mediator of EBV effects on B-lymphocytes or of normal lymphocyte functions, Cancer, rheumatoid arthritis, ligand non-protein
19	ACKR2	GPCR	Inflammatory diseases, large variety of ligands, chemokine sequestration
20	DRD1	GPCR	Dopamine receptor, activity is mediated by G proteins which activate adenylyl cyclase, Ligand is non-protein (dopamine)
21	SLC52A3	SLC Transporter	Potential homodimer or requires chaperone, Disease related (Brown-Vialetto-Van Laere syndrome and Fazio-Londe disease)
22	KCNA3, Kv1.3	Ion Channel	Mediates the voltage-dependent potassium ion permeability of excitable membranes, Margatoxin (short peptide toxin) as ligand, poor stability in detergent
23	CD163	Receptor	Acute phase-regulated receptor involved in clearance and endocytosis of hemoglobin/haptoglobin complexes by macrophages, Disease marker in inflammatory conditions
24	SCN11A	Ion Channel	Na channel mediating voltage-dependent Na ion permeability of excitable membranes, electrical transmission of pain signals, ligand (tetrodotoxin), needs beta subunits, B1 and B2 from one vector
25	TLR5	Receptor	Pattern recognition receptor (PRR) located on the cell surface that participates in the activation of innate immunity and inflammatory response, Rheumatoid arthritis, osteoclastogenesis, and bone loss
26	SV2A	Receptor	Role in the control of regulated secretion in neural/endocrine cells, enhancing selectively low-frequency neurotransmission, target for anti epilepsy drugs
27	SLC2A1	SLC	Facilitative glucose transporter, which is responsible for constitutive or basal glucose uptake. Very broad substrate specificity; can transport wide range of aldoses incl. pentoses and hexoses
28	EGFR	Receptor	Homo/Heterodimer triggered by ligand, no structure of transmembrane or kinase region as detergent belt is blocking analysis of structures, very relevant drug target
29	TRPC1	Ion Channel	Thought to form a receptor-activated non-selective calcium permeant cation channel. Probably is operated by a phosphatidylinositol 2nd messenger system activated by receptor tyrosine kinases or GPCRs.