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(biāo),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(dá)純化
康體生命采用尖端的重組蛋白功能表達(dá)和純化技術(shù),在昆蟲和哺乳動物細(xì)胞表達(dá)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(dá)、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(jìn)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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