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
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