靶向GPCR药物发现
Targeted GPCR Drug Discovery
靶向GPCR药物发现
GPCR简介
GPCR(G蛋白偶连受体)是药物研发领域的明星靶标，目前有超700种获批药物靶向GPCR，约占目前所有获批药物的1/3GPCR在信号转导中发挥着核心作用:癌症、心脏病、糖尿病、阿尔茨海默病等危害人类健康的重大疾病均与GPCR密切相关。然而，在GPCR家族的800多个GPCR成员中，只有大约90个是已知的药物靶点，包括孤儿受体在内的近300个成员在新药开发方面具有重要的价值与潜力。
01
GPCR蛋白表达纯化
康体生命采用尖端的重组蛋白功能表达和纯化技术，在昆虫和哺乳动物细胞表达系统方面积累了丰富的经验，能够制备高活性、高纯度的药物靶点(GPCR蛋白)，用于下游功能鉴定、结构分析等定制化服务。
02
基于冷冻电镜的GPCR结构解析
康体生命依托世界一流的冷冻电子显微镜平台，分析GPCR与药物候选分子复合物的高分辨率结构，为下游AI药物筛选和基于结构的药物分子发现提供丰富且关键的结构生物学信息。
03
靶向GPCR的纳米抗体药物发现
康体生命拥有成熟的纳米抗体药物发现平台和羊驼养殖基地，可使用天然库或免疫库筛选能够调节GPCR靶点活性的新功能纳米抗体候选药物。
康体生命一一助力靶向GPCR的新药研发
康体生命以世界领先的纳米抗体发现平台为基础，结合计算生物学、结构生物学和分子药理学等前沿技术，创建了靶向GPCR的药物发现平台，并致力于提供高效的靶向GPCR纳米抗体筛选等CRO服务，为GPCR结构解析及新药研发再添助力。
提供一站式高活性GPCR表达、纯化及结构鉴定服务
GPCR功能验证服务
冷冻电镜中心
基于GPCR结构的药物发现
我们将在项目的每一阶段生成项目进度报告
GPCR蛋白产品列表
| Class A GPCR (Rhodopsin-like family) | ||||
|---|---|---|---|---|
| Receptor | Receptor family | Species | Expression system | Description |
| 0PRM1 | opioid receptor | human | HEK293/Sf9 | full length |
| 0PRL1 | opioid receptor | human | HEK293/Sf9 | full length |
| 0PRK1 | opioid receptor | human | HEK293/Sf9 | full length |
| 0PRD1 | opioid receptor | human | HEK293/Sf9 | full length |
| CCR2 | Chemokine Receptor | human | HEK293/Sf9 | full length |
| CCR4 | Chemokine Receptor | human | HEK293/Sf9 | full length |
| CCR5 | Chemokine Receptor | human | HEK293/Sf9 | full length |
| CCR6 | Chemokine Receptor | human | HEK293/Sf9 | full length |
| CCR7 | Chemokine Receptor | human | HEK293/Sf9 | full length |
| CCR9 | Chemokine Receptor | human | HEK293/Sf9 | full length |
| Class A GPCR (Rhodopsin-like family) | ||||
|---|---|---|---|---|
| Receptor | Receptor family | Species | Expression system | Description |
| V2R | Vasopressin receptor | human | HEK293/Sf9 | full length |
| 5-HT 1A | Serotonin receptor | human | HEK293/5f9 | full length |
| 5-HT1B | Serotonin receptor | human | HEK293/Sf9 | full length |
| MTR1A | Melatonin receptor | human | HEK293/Sf9 | full length |
| MTR1B | Melatonin receptor | human | HEK293/Sf9 | full length |
| ADAZA | Adrenergic receptol | human | HEK293/5f9 | full length |
| ADA2B | Adrenergic receptol | human | HEK293/Sf9 | full length |
| ADA2C | Adrenergic receptol | human | HEK293/5f9 | full length |
| ADRB1 | Adrenergic receptol | human | HEK293/Sf9 | full length |
| ADRB2 | Adrenergic receptol | human | HEK293/Sf9 | full length |
| Class A GPCR (Rhodopsin-like family) | ||||
|---|---|---|---|---|
| Receptor | Receptor family | Species | Expression system | Description |
| CXCR1 | Chemokine Receptor | human | HEK293/Sf9 | full length |
| CXCR2 | Chemokine Receptor | human | HEK293/5f9 | full length |
| CXCR3 | Chemokine Receptor | human | HEK293/Sf9 | full length |
| CXCR4 | Chemokine Receptor | human | HEK293/5f9 | full length |
| CXCR5 | Chemokine Receptor | human | HEK293/Sf9 | full length |
| DRD1 | Dopamine receptor | human | HEK293/Sf9 | full length |
| DRD2 | Dopamine receptor | human | HEK293/Sf9 | full length |
| DRD3 | Dopamine receptor | human | HEK293/5f9 | full length |
| MC3R | Melanocortin receptor | human | HEK293/Sf9 | full length |
| MC4R | Melanocortin receptor | human | HEK293/Sf9 | full length |
| Class A GPCR (Rhodopsin-like family) | ||||
|---|---|---|---|---|
| Receptor | Receptor family | Species | Expression system | Description |
| OXTR | Oxytocin receptor | human | HEK293/Sf9 | full length |
| GHSR | Ghrelin receptor | human | HEK293/Sf9 | full length |
| CB1 | Cannabinoid receptor | human | HEK293/Sf9 | full length |
| CB2 | Cannabinoid receptor | human | HEK293/Sf9 | full length |
| CCKAR | Cholecystokinin receptor | human | HEK293/Sf9 | full length |
| CCKBR | Cholecystokinin receptor | human | HEK293/Sf9 | full length |
| 0X1R | Orexin receptor | human | HEK293/Sf9 | full length |
| 0X2R | Orexin receptor | human | HEK293/Sf9 | full length |
| PTGDR2 | prostaglandin receptor | human | HEK293/Sf9 | full length |
| PTGDR3 | prostaglandin receptor | human | HEK293/Sf9 | full length |
| PTGDR4 | prostaglandin receptor | human | HEK293/Sf9 | full length |
| Class B GPCR (Rhodopsin-like family) | ||||
|---|---|---|---|---|
| Receptor | Receptor family | Species | Expression system | Description |
| VIP2R | Vasoactive intestinal polypeptide rece ptor | human | HEK293/Sf9 | full length |
| VIP1R | Vasoactive intestinal polypeptide rece ptor | human | HEK293/Sf9 | full length |
| AMY3R | Amylin receptor | human | HEK293/Sf9 | full length |
| AMY2R | Amylin receptor | human | HEK293/Sf9 | full length |
| AMY1R | Amylin receptor | human | HEK293/Sf9 | full length |
| CRF2R | Corticotropinreleasing hormone receptor | human | HEK293/Sf9 | full length |
| CRF1R | Corticotropinreleasing hormone receptor | human | HEK293/Sf9 | full length |
| AM2R | Adrenomedullin receptor | human | HEK293/Sf9 | full length |
| AMIR | Adrenomedullin receptor | human | HEK293/Sf9 | full length |
| PTH2R | Parathyroid hormone receptor | human | HEK293/Sf9 | full length |
| Class B GPCR (Rhodopsin-like family) | ||||
|---|---|---|---|---|
| Receptor | Receptor family | Species | Expression system | Description |
| PTH1R | Parathyroid hormone receptor | human | HEK293/Sf9 | full length |
| CRHR2 | Corticotropin releasing hormone rece ptor | human | HEK293/Sf9 | full length |
| CRHR1 | Corticotropin releasing hormone rece ptor | human | HEK293/Sf9 | full length |
| CALCR | Calcitonin receptor | human | HEK293/Sf9 | full length |
| GHRHR | Glucagon receptor | human | HEK293/Sf9 | full length |
| GIPR | Glucagon receptor | human | HEK293/Sf9 | |
| GLP2R | Glucagon receptor | human | HEK293/Sf9 | full length |
| GLP1R | Glucagon receptor | human | HEK293/Sf9 | full length |
| GCGR | Glucagon receptor | human | HEK293/Sf9 | full length |
| SCTR | Secretin receptor | human | HEK293/Sf9 | full length |
| Class C GPCR (Rhodopsin-like family) | ||||
|---|---|---|---|---|
| Receptor | Receptor family | Species | Expression system | Description |
| CASR | Calcium-sensing receptor | human | HEK293/Sf9 | full length |
| GPRC6A | opioid receptor | human | HEK293/Sf9 | full length |
| GPRC5D | Glucagon receptor | human | HEK293/Sf9 | full length |
| GPRC5C | Chemokine Receptor | human | HEK293/Sf9 | full length |
| GPRC5B | Glucagon receptor | human | HEK293/Sf9 | full length |
| GPRC5A | Glucagon receptor | human | HEK293/Sf9 | full length |
| GPR179 | opioid receptor | human | HEK293/Sf9 | full length |
| GPR158 | opioid receptor | human | HEK293/Sf9 | full length |
| GPR156 | opioid receptor | human | HEK293/Sf9 | full length |
| TAS1R3 | Taste receptor | human | HEK293/Sf9 | full length |
| TAS1R2 | Taste receptor | human | HEK293/Sf9 | full length |
| Class C GPCR (Rhodopsin-like family) | ||||
|---|---|---|---|---|
| Receptor | Receptor family | Species | Expression system | Description |
| TAS1R1 | Taste receptor | human | HEK293/Sf9 | full length |
| mGluR7 | Metabotropic glutamate receptor | human | HEK293/Sf9 | full length |
| mGluR6 | Metabotropic glutamate receptor | human | HEK293/Sf9 | full length |
| mGluR5 | Metabotropic glutamate receptor | human | HEK293/Sf9 | full length |
| mGluR4 | Metabotropic glutamate receptor | human | HEK293/Sf9 | full length |
| mGluR3 | Metabotropic glutamate receptor | human | HEK293/Sf9 | full length |
| mGluR2 | Metabotropic glutamate receptor | human | HEK293/Sf9 | full length |
| mGluRI | Metabotropic glutamate receptor | human | HEK293/Sf9 | full length |
| GABBR2 | Gamma-aminobutyric acid receptor | human | HEK293/Sf9 | full length |
| GABBR1 | Gamma-aminobutyric acid receptor | human | HEK293/Sf9 | full length |
| CASR | Calcium-sensing receptor | human | HEK293/Sf9 | full length |
