For Research Use Only Highly sensitive GPCR evaluation service.

Tanso Biosciences: GPCR functional profiling services

GPCRs are known to be extremely important therapeutic target molecules in many diseases. Almost 40% of currently approved medical products display clinical effects by acting against GPCRs. Although more than 300 GPCRs, excluding sensory receptors, have been annotated in humans, only a limited number of GPCRs have been used in medical drugs. The progress of new drug discovery for over 200 GPCRs is impeded by lack of assay methodology to evaluate candidate drug compounds and difficulty of pharmacological analysis.

Tanso Biosciences has developed a highly sensitive functional profiling platform for all human GPCRs, including GPCRs whose activity cannot be assessed by currently available methods, by combining proprietary reporter cell lines and Gα-proteins. We also offer GPCR Custom Profiling Services, which can be utilized for a variety of purposes including discovery of on-target molecules (ligands), validation of off-target effects on other receptors, and screening and optimization for specific GPCRs.

Advantages

  • High sensitivity, high signal-to-background ratio (Fig. 2) achieved with Tanso Biosciences proprietary assay method (Fig. 1)
  • Not only agonist and inverse agonist, but antagonist, PAM, and NAM can be assessed for ligand known GPCRs
  • A total of 313 human GPCRs (excluding sensory receptors) are covered.
  • High sensitivity assessment for G12/13 and Gi/o coreceptors, which are difficult to evaluate by conventional activity assays.
  • Compatibility with all Gα proteins allows assaying orphan receptors (agonist, inverse agonist mode)
  • Cost effective and short turn around time (Results will be delivered in 2 - 3 weeks after sample receipt).

Principle

Principle of GPCR Assay
Fig. 1 Principle of GPCR Assay

A GPCR activated by its ligand can activate multiple cellular signal transduction pathways through associated G proteins. In Tanso Biosciences' GPCR assay platform, we utilize proprietary reporter cell lines. In these cells, signals that have diverged into downstream cellular signal transduction pathways will be re-converged, and then amplified by accumulation effect. In this novel technology, sample-specific stimulation against target GPCR can be assessed with high sensitivity, using reporter Luciferase activity as an indicator.

Representative Results

Comparison between conventional assay.Tanso Biosciences custom assay.
Fig. 2 Comparison between conventional assay (left: J Biol Chem. 1995;270:12846-50.) and Tanso Biosciences custom assay (right).

Right: The agonist response for AGTR1 was assessed using Tanso Biosciences' assay. The results showed almost 100 fold higher sensitivity compared to conventional method, and achieved high S/B ratio.

List of Targets

  Symbol Nomenclature Family
1 HTR1A 5-HT1A receptor 5-Hydroxytryptamine receptors
2 HTR1B 5-HT1B receptor 5-Hydroxytryptamine receptors
3 HTR1D 5-HT1D receptor 5-Hydroxytryptamine receptors
4 HTR1E 5-ht1e receptor 5-Hydroxytryptamine receptors
5 HTR1F 5-HT1F receptor 5-Hydroxytryptamine receptors
6 HTR2A 5-HT2A receptor 5-Hydroxytryptamine receptors
7 HTR2B 5-HT2B receptor 5-Hydroxytryptamine receptors
8 HTR2C 5-HT2C receptor 5-Hydroxytryptamine receptors
9 HTR4 5-HT4 receptor 5-Hydroxytryptamine receptors
10 HTR5A 5-HT5A receptor 5-Hydroxytryptamine receptors
11 HTR6 5-HT6 receptor 5-Hydroxytryptamine receptors
12 HTR7 5-HT7 receptor 5-Hydroxytryptamine receptors
13 CHRM1 M1 receptor Acetylcholine receptors (muscarinic)
14 CHRM2 M2 receptor Acetylcholine receptors (muscarinic)
15 CHRM3 M3 receptor Acetylcholine receptors (muscarinic)
16 CHRM4 M4 receptor Acetylcholine receptors (muscarinic)
17 CHRM5 M5 receptor Acetylcholine receptors (muscarinic)
18 ADORA1 A1 receptor Adenosine receptors
19 ADORA2A A2A receptor Adenosine receptors
20 ADORA2B A2B receptor Adenosine receptors
21 ADORA3 A3 receptor Adenosine receptors
22 ADRA1A α1A-adrenoceptor Adrenoceptors
23 ADRA1B α1B-adrenoceptor Adrenoceptors
24 ADRA1D α1D-adrenoceptor Adrenoceptors
25 ADRA2A α2A-adrenoceptor Adrenoceptors
26 ADRA2B α2B-adrenoceptor Adrenoceptors
27 ADRA2C α2C-adrenoceptor Adrenoceptors
28 ADRB1 β1-adrenoceptor Adrenoceptors
29 ADRB2 β2-adrenoceptor Adrenoceptors
30 ADRB3 β3-adrenoceptor Adrenoceptors
31 AGTR1 AT1 receptor Angiotensin receptors
32 APLNR apelin receptor Apelin receptor
33 GPBAR1(TGR5) GPBA receptor Bile acid receptor
34 BRS3 BB3 receptor Bombesin receptors
35 GRPR BB2 receptor Bombesin receptors
36 NMBR BB1 receptor Bombesin receptors
37 CALCR CT receptor Calcitonin receptors
38 CALCRL calcitonin receptor-like receptor Calcitonin receptors
39 CASR CaS receptor Calcium-sensing receptor
40 CNR1 CB1 receptor Cannabinoid receptors
41 CNR2 CB2 receptor Cannabinoid receptors
42 GPR119 GPR119 Cannabinoid receptors
43 GPR55 GPR55 Cannabinoid receptors
44 CMKLR1 chemerin receptor 1 Chemerin receptors
45 CCR1 CCR1 Chemokine receptors
46 CCR10 CCR10 Chemokine receptors
47 CCR2 CCR2 Chemokine receptors
48 CCR4 CCR4 Chemokine receptors
49 CCR5 CCR5 Chemokine receptors
50 CCR6 CCR6 Chemokine receptors
51 CCR7 CCR7 Chemokine receptors
52 CCR8 CCR8 Chemokine receptors
53 CCR9 CCR9 Chemokine receptors
54 CX3CR1 CX3CR1 Chemokine receptors
55 CXCR1 CXCR1 Chemokine receptors
56 CXCR2 CXCR2 Chemokine receptors
57 CXCR3 CXCR3 Chemokine receptors
58 CXCR5 CXCR5 Chemokine receptors
59 CXCR6 CXCR6 Chemokine receptors
60 XCR1 XCR1 Chemokine receptors
61 CCKAR CCK1 receptor Cholecystokinin receptors
62 CCKBR CCK2 receptor Cholecystokinin receptors
63 C3AR1 C3a receptor Complement peptide receptors
64 C5AR1 C5a1 receptor Complement peptide receptors
65 CRHR1 CRF1 receptor Corticotropin-releasing factor receptors
66 CRHR2 CRF2 receptor Corticotropin-releasing factor receptors
67 DRD1 D1 receptor Dopamine receptors
68 DRD2 D2 receptor Dopamine receptors
69 DRD3 D3 receptor Dopamine receptors
70 DRD4 D4 receptor Dopamine receptors
71 DRD5 D5 receptor Dopamine receptors
72 EDNRA ETA receptor Endothelin receptors
73 EDNRB ETB receptor Endothelin receptors
74 FPR1 FPR1 Formylpeptide receptors
75 FPR2 FPR2/ALX Formylpeptide receptors
76 FPR3 FPR3 Formylpeptide receptors
77 GPR120 FFA4 receptor Free fatty acid receptors
78 GPR40 FFA1 receptor Free fatty acid receptors
79 GPR41 FFA3 receptor Free fatty acid receptors
80 GPR43 FFA2 receptor Free fatty acid receptors
81 GPR84 GPR84 Free fatty acid receptors
82 GABBR1 GABAB1 GABAB receptors
83 GABBR2 GABAB2 GABAB receptors
84 GALR1 GAL1 receptor Galanin receptors
85 GALR2 GAL2 receptor Galanin receptors
86 GALR3 GAL3 receptor Galanin receptors
87 GHSR ghrelin receptor Ghrelin receptor
88 GCGR glucagon receptor Glucagon receptor family
89 GHRHR GHRH receptor Glucagon receptor family
90 GIPR GIP receptor Glucagon receptor family
91 GLP1R GLP-1 receptor Glucagon receptor family
92 GLP2R GLP-2 receptor Glucagon receptor family
93 SCTR secretin receptor Glucagon receptor family
94 FSHR FSH receptor Glycoprotein hormone receptors
95 LHCGR LH receptor Glycoprotein hormone receptors
96 TSHR TSH receptor Glycoprotein hormone receptors
97 GNRHR GnRH1 receptor Gonadotrophin-releasing hormone receptors
98 HRH1 H1 receptor Histamine receptors
99 HRH2 H2 receptor Histamine receptors
100 HRH3 H3 receptor Histamine receptors
101 HRH4 H4 receptor Histamine receptors
102 GPR109A HCA2 receptor Hydroxycarboxylic acid receptors
103 GPR109B HCA3 receptor Hydroxycarboxylic acid receptors
104 GPR81 HCA1 receptor Hydroxycarboxylic acid receptors
105 KISS1R kisspeptin receptor Kisspeptin receptor
106 CYSLTR1 CysLT1 receptor Leukotriene receptors
107 CYSLTR2 CysLT2 receptor Leukotriene receptors
108 LTB4R BLT1 receptor Leukotriene receptors
109 LTB4R2 BLT2 receptor Leukotriene receptors
110 OXER1(GPR170) OXE receptor Leukotriene receptors
111 LPAR1 LPA1 receptor Lysophospholipid (LPA) receptors
112 LPAR2 LPA2 receptor Lysophospholipid (LPA) receptors
113 LPAR3 LPA3 receptor Lysophospholipid (LPA) receptors
114 LPAR4 LPA4 receptor Lysophospholipid (LPA) receptors
115 LPAR5 LPA5 receptor Lysophospholipid (LPA) receptors
116 LPAR6 LPA6 receptor Lysophospholipid (LPA) receptors
117 MCHR1 MCH1 receptor Melanin-concentrating hormone receptors
118 MCHR2 MCH2 receptor Melanin-concentrating hormone receptors
119 MC1R MC1 receptor Melanocortin receptors
120 MC2R MC2 receptor Melanocortin receptors
121 MC3R MC3 receptor Melanocortin receptors
122 MC4R MC4 receptor Melanocortin receptors
123 MC5R MC5 receptor Melanocortin receptors
124 MTNR1A MT1 receptor Melatonin receptors
125 MTNR1B MT2 receptor Melatonin receptors
126 GRM1 mGlu1 receptor Metabotropic glutamate receptors
127 GRM2 mGlu2 receptor Metabotropic glutamate receptors
128 GRM4 mGlu4 receptor Metabotropic glutamate receptors
129 GRM5 mGlu5 receptor Metabotropic glutamate receptors
130 GRM6 mGlu6 receptor Metabotropic glutamate receptors
131 GRM8 mGlu8 receptor Metabotropic glutamate receptors
132 MLNR motilin receptor Motilin receptor
133 NMUR1 NMU1 receptor Neuromedin U receptors
134 NMUR2 NMU2 receptor Neuromedin U receptors
135 NPFFR1 NPFF1 receptor Neuropeptide FF/neuropeptide AF receptors
136 NPFFR2 NPFF2 receptor Neuropeptide FF/neuropeptide AF receptors
137 NPSR1 NPS receptor Neuropeptide S receptor
138 NPBWR1 NPBW1 receptor Neuropeptide W/neuropeptide B receptors
139 NPBWR2 NPBW2 receptor Neuropeptide W/neuropeptide B receptors
140 NPY1R Y1 receptor Neuropeptide Y receptors
141 NPY2R Y2 receptor Neuropeptide Y receptors
142 NPY4R Y4 receptor Neuropeptide Y receptors
143 NPY5R Y5 receptor Neuropeptide Y receptors
144 NTSR1 NTS1 receptor Neurotensin receptors
145 NTSR2 NTS2 receptor Neurotensin receptors
146 OPRD1 δ receptor Opioid receptors
147 OPRK1 κ receptor Opioid receptors
148 OPRL1 NOP receptor Opioid receptors
149 OPRM1 μ receptor Opioid receptors
150 HCRTR1 OX1 receptor Orexin receptors
151 HCRTR2 OX2 receptor Orexin receptors
152 ACKR1(CCBP1) ACKR1 Orphan receptors
153 ACKR2(CCBP2) ACKR2 Orphan receptors
154 ACKR3(CXCR7) ACKR3 Orphan receptors
155 ACKR4(CCR11) ACKR4 Orphan receptors
156 AGTR2 AT2 receptor Orphan receptors
157 CCRL2 CCRL2 Orphan receptors
158 GPR1 chemerin receptor 2 Orphan receptors
159 GPR101 GPR101 Orphan receptors
160 GPR107 GPR107 Orphan receptors
161 GPR12 GPR12 Orphan receptors
162 GPR132(G2A) GPR132 Orphan receptors
163 GPR135 GPR135 Orphan receptors
164 GPR137 GPR137 Orphan receptors
165 GPR139 GPR139 Orphan receptors
166 GPR141 GPR141 Orphan receptors
167 GPR142 GPR142 Orphan receptors
168 GPR143 GPR143 Orphan receptors
169 GPR146 GPR146 Orphan receptors
170 GPR148 GPR148 Orphan receptors
171 GPR149 GPR149 Orphan receptors
172 GPR15 GPR15 Orphan receptors
173 GPR150 GPR150 Orphan receptors
174 GPR151(GALR4) GPR151 Orphan receptors
175 GPR152 GPR152 Orphan receptors
176 GPR153 GPR153 Orphan receptors
177 GPR156 GPR156 Orphan receptors
178 GPR157 GPR157 Orphan receptors
179 GPR158 GPR158 Orphan receptors
180 GPR160 GPR160 Orphan receptors
181 GPR161 GPR161 Orphan receptors
182 GPR162 GPR162 Orphan receptors
183 GPR17 GPR17 Orphan receptors
184 GPR171 GPR171 Orphan receptors
185 GPR173 GPR173 Orphan receptors
186 GPR174 GPR174 Orphan receptors
187 GPR175 TPRA1 Orphan receptors
188 GPR176 GPR176 Orphan receptors
189 GPR18 GPR18 Orphan receptors
190 GPR182 GPR182 Orphan receptors
191 GPR19 GPR19 Orphan receptors
192 GPR20 GPR20 Orphan receptors
193 GPR21 GPR21 Orphan receptors
194 GPR22 GPR22 Orphan receptors
195 GPR25 GPR25 Orphan receptors
196 GPR26 GPR26 Orphan receptors
197 GPR27 GPR27 Orphan receptors
198 GPR3 GPR3 Orphan receptors
199 GPR30 GPER Orphan receptors
200 GPR31 GPR31 Orphan receptors
201 GPR32 GPR32 Orphan receptors
202 GPR34 GPR34 Orphan receptors
203 GPR35 GPR35 Orphan receptors
204 GPR37 GPR37 Orphan receptors
205 GPR37L1 GPR37L1 Orphan receptors
206 GPR39 GPR39 Orphan receptors
207 GPR4 GPR4 Orphan receptors
208 GPR45 GPR45 Orphan receptors
209 GPR50 GPR50 Orphan receptors
210 GPR52 GPR52 Orphan receptors
211 GPR6 GPR6 Orphan receptors
212 GPR61 GPR61 Orphan receptors
213 GPR62 GPR62 Orphan receptors
214 GPR63 GPR63 Orphan receptors
215 GPR65 GPR65 Orphan receptors
216 GPR68 GPR68 Orphan receptors
217 GPR75 GPR75 Orphan receptors
218 GPR78 GPR78 Orphan receptors
219 GPR82 GPR82 Orphan receptors
220 GPR83 GPR83 Orphan receptors
221 GPR85 GPR85 Orphan receptors
222 GPR87 GPR87 Orphan receptors
223 GPR88 GPR88 Orphan receptors
224 GPRC5A GPRC5A Orphan receptors
225 GPRC5B GPRC5B Orphan receptors
226 GPRC5C GPRC5C Orphan receptors
227 GPRC5D GPRC5D Orphan receptors
228 GPRC6A GPRC6 receptor Orphan receptors
229 LGR4 LGR4 Orphan receptors
230 LGR5 LGR5 Orphan receptors
231 LGR6 LGR6 Orphan receptors
232 MAS1 MAS1 Orphan receptors
233 MAS1L MAS1L Orphan receptors
234 MRGPRD MRGPRD Orphan receptors
235 MRGPRE MRGPRE Orphan receptors
236 MRGPRF MRGPRF Orphan receptors
237 MRGPRG MRGPRG Orphan receptors
238 MRGPRX1 MRGPRX1 Orphan receptors
239 MRGPRX2 MRGPRX2 Orphan receptors
240 MRGPRX3 MRGPRX3 Orphan receptors
241 MRGPRX4 MRGPRX4 Orphan receptors
242 TAAR2 TAAR2 Orphan receptors
243 TAAR5 TAAR5 Orphan receptors
244 TAAR6 TAAR6 Orphan receptors
245 TAAR8 TAAR8 Orphan receptors
246 TAAR9 TAAR9 Orphan receptors
247 OXGR1(GPR80/99) oxoglutarate receptor Oxoglutarate receptors
248 PTH1R PTH1 receptor Parathyroid hormone receptors
249 PTH2R PTH2 receptor Parathyroid hormone receptors
250 PTAFR PAF receptor Platelet-activating factor receptor
251 PROKR1 PKR1 Prokineticin receptors
252 PROKR2 PKR2 Prokineticin receptors
253 PRLHR PrRP receptor Prolactin-releasing peptide receptor
254 PTGDR DP1 receptor Prostanoid receptors
255 PTGDR2 DP2 receptor Prostanoid receptors
256 PTGER1 EP1 receptor Prostanoid receptors
257 PTGER2 EP2 receptor Prostanoid receptors
258 PTGER3 EP3 receptor Prostanoid receptors
259 PTGER4 EP4 receptor Prostanoid receptors
260 PTGFR FP receptor Prostanoid receptors
261 PTGIR IP receptor Prostanoid receptors
262 F2R PAR1 Proteinase-activated receptors
263 F2RL1 PAR2 Proteinase-activated receptors
264 F2RL2 PAR3 Proteinase-activated receptors
265 F2RL3 PAR4 Proteinase-activated receptors
266 QRFPR QRFP receptor QRFP receptor
267 RXFP1 RXFP1 Relaxin family peptide receptors
268 RXFP2 RXFP2 Relaxin family peptide receptors
269 RXFP3 RXFP3 Relaxin family peptide receptors
270 RXFP4 RXFP4 Relaxin family peptide receptors
271 SSTR1 SST1 receptor Somatostatin receptors
272 SSTR2 SST2 receptor Somatostatin receptors
273 SSTR3 SST3 receptor Somatostatin receptors
274 SSTR4 SST4 receptor Somatostatin receptors
275 SSTR5 SST5 receptor Somatostatin receptors
276 GPR183 GPR183 Steroid receptors
277 GPR91 succinate receptor Succinate receptor
278 TACR1 NK1 receptor Tachykinin receptors
279 TACR2 NK2 receptor Tachykinin receptors
280 TACR3 NK3 receptor Tachykinin receptors
281 TRHR TRH1 receptor Thyrotropin-releasing hormone receptors
282 TAAR1 TA1 receptor Trace amine receptor
283 UTS2R UT receptor Urotensin receptor
284 AVPR1A V1A receptor Vasopressin and oxytocin receptors
285 AVPR1B V1B receptor Vasopressin and oxytocin receptors
286 AVPR2 V2 receptor Vasopressin and oxytocin receptors
287 OXTR OT receptor Vasopressin and oxytocin receptors
288 ADCYAP1R1 PAC1 receptor VIP and PACAP receptors
289 VIPR1 VPAC1 receptor VIP and PACAP receptors
290 VIPR2 VPAC2 receptor VIP and PACAP receptors

* The assay mode includes agonist/inverse agonist, antagonist, and PAM/NAM. For orphan receptors, we accept only agonist/inverse agonist.

This product is "Research reagent". It is prohibited to use against humans or animals in medical care, clinical diagnoses, or as food.

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