靶向GPCR药物(wù)发现

Targeted GPCR Drug Discovery

靶向GPCR药物(wù)发现

GPCR简介

GPCR(G蛋白偶连受體(tǐ))是药物(wù)研发领域的明星靶标，目前有(yǒu)超700种获批药物(wù)靶向GPCR，约占目前所有(yǒu)获批药物(wù)的1/3GPCR在信号转导中发挥着核心作用(yòng):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(duō)个GPCR成员中，只有(yǒu)大约90个是已知的药物(wù)靶点，包括孤儿受體(tǐ)在内的近300个成员在新(xīn)药开发方面具有(yǒu)重要的价值与潜力。

01

GPCR蛋白表达纯化

康體(tǐ)生命采用(yòng)尖端的重组蛋白功能(néng)表达和纯化技术，在昆虫和哺乳动物(wù)细胞表达系统方面积累了丰富的经验，能(néng)够制备高活性、高纯度的药物(wù)靶点(GPCR蛋白)，用(yòng)于下游功能(néng)鉴定、结构分(fēn)析等定制化服務(wù)。

02

基于冷冻電(diàn)镜的GPCR结构解析

康體(tǐ)生命依托世界一流的冷冻電(diàn)子显微镜平台，分(fēn)析GPCR与药物(wù)候选分(fēn)子复合物(wù)的高分(fēn)辨率结构，為(wèi)下游AI药物(wù)筛选和基于结构的药物(wù)分(fēn)子发现提供丰富且关键的结构生物(wù)學(xué)信息。

03

靶向GPCR的纳米抗體(tǐ)药物(wù)发现

康體(tǐ)生命拥有(yǒu)成熟的纳米抗體(tǐ)药物(wù)发现平台和羊驼养殖基地，可(kě)使用(yòng)天然库或免疫库筛选能(néng)够调节GPCR靶点活性的新(xīn)功能(néng)纳米抗體(tǐ)候选药物(wù)。

康體(tǐ)生命一一助力靶向GPCR的新(xīn)药研发

康體(tǐ)生命以世界领先的纳米抗體(tǐ)发现平台為(wèi)基础，结合计算生物(wù)學(xué)、结构生物(wù)學(xué)和分(fēn)子药理(lǐ)學(xué)等前沿技术，创建了靶向GPCR的药物(wù)发现平台，并致力于提供高效的靶向GPCR纳米抗體(tǐ)筛选等CRO服務(wù)，為(wèi)GPCR结构解析及新(xīn)药研发再添助力。

  • 提供一站式高活性GPCR表达、纯化及结构鉴定服務(wù)

  • GPCR功能(néng)验证服務(wù)

  • 冷冻電(diàn)镜中心

  • 基于GPCR结构的药物(wù)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
0
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