靶向GPCR藥物發(fā)現
Targeted GPCR Drug Discovery
靶向GPCR藥物發(fā)現
GPCR簡(jiǎn)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在信號轉導中發(fā)揮著(zhù)核心作用:癌癥、心臟病、糖尿病、阿爾茨海默病等危害人類(lèi)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(gè)GPCR成員中,只有大約90個(gè)是已知的藥物靶點(diǎn),包括孤兒受體在內的近300個(gè)成員在新藥開(kāi)發(fā)方面具有重要的價(jià)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(chóng)和哺乳動(dòng)物細胞表達系統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(diǎn)(GPCR蛋白),用于下游功能鑒定、結構分析等定制化服務(wù)。
                                            02
基于冷凍電鏡的GPCR結構解析
康體生命依托世界一流的冷凍電子顯微鏡平臺,分析GPCR與藥物候選分子復合物的高分辨率結構,為下游AI藥物篩選和基于結構的藥物分子發(fā)現提供豐富且關(guān)鍵的結構生物學(xué)信息。
                                            03
靶向GPCR的納米抗體藥物發(fā)現
康體生命擁有成熟的納米抗體藥物發(fā)現平臺和羊駝養殖基地,可使用天然庫或免疫庫篩選能夠調節GPCR靶點(diǎn)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)現平臺為基礎,結合計算生物學(xué)、結構生物學(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結構解析及新藥研發(fā)再添助力。
提供一站式高活性GPCR表達、純化及結構鑒定服務(wù)
                                    
                                GPCR功能驗證服務(wù)
                                    
                                冷凍電鏡中心
                                    
                                基于GPCR結構的藥物發(fā)現
                                    
                                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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