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靶向GPCR藥物發(fā)現(xiàn)

Targeted GPCR Drug Discovery

靶向GPCR藥物發(fā)現(xiàn)

GPCR簡介

GPCR(G蛋白偶連受體)是藥物研發(fā)領(lǐng)域的明星靶標，目前有超700種獲批藥物靶向GPCR，約占目前所有獲批藥物的1/3GPCR在信號轉(zhuǎn)導(dǎo)中發(fā)揮著核心作用:癌癥、心臟病、糖尿病、阿爾茨海默病等危害人類健康的重大疾病均與GPCR密切相關(guān)。然而，在GPCR家族的800多個GPCR成員中，只有大約90個是已知的藥物靶點，包括孤兒受體在內(nèi)的近300個成員在新藥開發(fā)方面具有重要的價值與潛力。

01

GPCR蛋白表達純化

康體生命采用尖端的重組蛋白功能表達和純化技術(shù)，在昆蟲和哺乳動物細胞表達系統(tǒng)方面積累了豐富的經(jīng)驗，能夠制備高活性、高純度的藥物靶點(GPCR蛋白)，用于下游功能鑒定、結(jié)構(gòu)分析等定制化服務(wù)。

02

基于冷凍電鏡的GPCR結(jié)構(gòu)解析

康體生命依托世界一流的冷凍電子顯微鏡平臺，分析GPCR與藥物候選分子復(fù)合物的高分辨率結(jié)構(gòu)，為下游AI藥物篩選和基于結(jié)構(gòu)的藥物分子發(fā)現(xiàn)提供豐富且關(guān)鍵的結(jié)構(gòu)生物學(xué)信息。

03

靶向GPCR的納米抗體藥物發(fā)現(xiàn)

康體生命擁有成熟的納米抗體藥物發(fā)現(xiàn)平臺和羊駝養(yǎng)殖基地，可使用天然庫或免疫庫篩選能夠調(diào)節(jié)GPCR靶點活性的新功能納米抗體候選藥物。

康體生命一一助力靶向GPCR的新藥研發(fā)

康體生命以世界領(lǐng)先的納米抗體發(fā)現(xiàn)平臺為基礎(chǔ)，結(jié)合計算生物學(xué)、結(jié)構(gòu)生物學(xué)和分子藥理學(xué)等前沿技術(shù)，創(chuàng)建了靶向GPCR的藥物發(fā)現(xiàn)平臺，并致力于提供高效的靶向GPCR納米抗體篩選等CRO服務(wù)，為GPCR結(jié)構(gòu)解析及新藥研發(fā)再添助力。

  • 提供一站式高活性GPCR表達、純化及結(jié)構(gòu)鑒定服務(wù)

  • GPCR功能驗證服務(wù)

  • 冷凍電鏡中心

  • 基于GPCR結(jié)構(gòu)的藥物發(fā)現(xiàn)

  • 我們將在項目的每一階段生成項目進度報告

GPCR蛋白產(chǎn)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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創(chuàng)意小鎮(zhèn)康體生命研究院

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