1. GPCR 靶点价值与研究挑战

G蛋白偶联受体(GPCR)是人体内规模最大、功能最为多样的受体家族,广泛参与神经传递、免疫调控、内分泌信号及代谢稳态等关键生理过程。当前,超过30%的上市药物以GPCR为直接或间接作用靶点。随着代谢性疾病、肿瘤免疫及神经系统疾病研究的不断深入,越来越多孤儿GPCR被证实与疾病密切相关,使GPCR持续成为极具潜力的药物开发核心靶点。

然而,GPCR的结构特性为研究与药物开发带来了显著挑战。作为高度疏水的多跨膜蛋白,GPCR只有在完整脂质膜环境中才能维持天然构象,一旦脱离细胞膜极易发生构象改变甚至失活。这使得基于变性或固定条件的传统检测方法(如Western blot、ELISA或免疫组化)难以真实反映GPCR在活细胞表面的表达状态及其生理相关性,从而限制了受体识别、信号机制解析及候选药物筛选的准确性。

2. 为什么 GPCR 研究必须依赖流式抗体

要真正理解GPCR的生物学功能并推动其药物开发,关键在于能否在活细胞水平直接检测并定量天然构象的细胞表面受体。GPCR流式细胞术抗体通过在完整膜环境中进行检测,已成为目前评估GPCR表达、抗体结合能力及靶点可及性的关键技术手段。

围绕GPCR的构象依赖性与活细胞检测需求,流式抗体在研究与药物开发中体现出以下核心价值:

01

天然构象识别

在活细胞膜环境中直接识别GPCR天然构象,真实反映生理状态下的受体表达。

02

单细胞定量分析

基于流式细胞术实现单细胞分辨率的定量检测,精准比较不同条件下的GPCR表达差异。

03

高门槛流式验证

仅筛选可在活细胞表面稳定结合GPCR的抗体,确保流式信号可靠、结果可
重复。

04

支撑药物研发决策

用于评估靶点可及性与抗体开发潜力,降低GPCR靶向药物早期研发风险。       

3. GPCR流式抗体应用

基于活细胞流式细胞术对 GPCR 的直接检测能力,GPCR 流式抗体在实际研究与开发中展现出显著优势。通过保留天然构象识别、实现单细胞水平的定量分析、与多种功能实验高度联用,并适配多种细胞类型,流式抗体为 GPCR 表达验证、抗体筛选及功能研究提供了更接近真实生理状态的技术支撑。下图概述了 GPCR 流式抗体在关键应用场景中的核心优势。

保留天然构象识别能力

抗体识别活细胞膜上的天然受体,不依赖变性或固定过程,更接近生理状
态。

与功能实验联用

可与Ca2+流实验、信号转导分析、内吞实验等结合,形成完整的GPCR研究
体系。

定量检测表达水平

流式可实现单细胞分辨率下的精确定量,便于比较不同处理组之间的GPCR表达差异。                        

适用于多种细胞类型

无论是原代细胞、转染细胞系还是免疫细胞群体,均可快速检测受体分布。    

4. 缔码GPCR流式抗体的技术优势

GPCR作为典型的七次跨膜膜蛋白,天然构象极其复杂。传统GPCR抗体在应用中往往需要破膜处理才能结合受体内部表位,这不仅破坏了膜结构,也会导致信号丢失和假阳性问题。缔码的GPCR流式抗体则完全不同——依托Nanodisc全长膜蛋白平台制备的天然构象抗原,筛选出的抗体能够特异识别活细胞膜表面GPCR表位,实现无需破膜、直接检测。这意味着研究者可以在最接近生理状态的条件下,定量分析GPCR的表达与构象变化,从而获得更可靠、更有生物学意义的数据。

缔码拥有丰富的GPCR流式抗体靶点库,涵盖免疫、神经、代谢、肿瘤等多个研究方向: 

Target Cat.No. Product Name Applications
ADGRE2 DMC100370 Anti-ADGRE2 antibody(DMC370); IgG1 Chimeric mAb Flow Cyt
C5AR2 DMC100482 Anti-GPR77 antibody(DMC482); IgG1 Chimeric mAb Flow Cyt
CCR1 DMC100465 Anti-CCR1 antibody(DMC465); IgG1 Chimeric mAb Flow Cyt; WB
CCR2 DMC100447 Anti-CCR2 antibody(DMC447); IgG1 Chimeric mAb Flow Cyt
CCR4 DMC100297 Anti-CCR4 antibody(DMC297); IgG1 Chimeric mAb Flow Cyt
CCR5 DMC101003 Anti-CCR5 antibody(4F6); IgG1 Chimeric mAb Flow Cyt
CCR6 DMC100477 Anti-CCR6 antibody(DMC477); IgG1 Chimeric mAb Flow Cyt
CCR8 DME100180 Anti-CCR8 antibody(DM180); Rabbit mAb ELISA; Flow Cyt
  DME100196 Anti-CCR8 antibody(DM196); Rabbit mAb ELISA; Flow Cyt
CXCR1 DMC100470 Anti-CXCR1 antibody(DMC470); IgG1 Chimeric mAb Flow Cyt
CXCR2 DMC100681 Anti-CXCR2 antibody(DMC681); IgG1 Chimeric mAb Flow Cyt
CXCR3 DME100208 Anti-CXCR3 antibody(DM208); Rabbit mAb ELISA; Flow Cyt
CXCR4 DMC100680 Anti-CXCR4 antibody(DMC680), IgG1 Chimeric mAb Flow Cyt
CXCR5 DMC100679 Anti-CXCR5 antibody(DMC679), IgG1 Chimeric mAb Flow Cyt; IHC
  DMC100679P PE-conjugated Anti-CXCR5 antibody(DMC679), IgG1 Chimeric mAb Flow Cyt
CXCR7 DMC100443 Anti-CXCR7 antibody(DMC443); IgG1 Chimeric mAb Flow Cyt
Target Cat.No. Product Name Applications
CB1 DME100144 Anti-CB1 antibody(DM144); Rabbit mAb ELISA; Flow Cyt
GIPR DMC101001 Anti-GIPR antibody(3G5); IgG1 Chimeric mAb Flow Cyt
GLP1R DME101291 Anti-GLP1R antibody(1A4), Rabbit mAb Flow Cyt
GPR75 DMC100368 Anti-GPR75 antibody(DMC368); IgG1 Chimeric mAb Flow Cyt
  DMC100492 Anti-GPR75 antibody(DMC492); IgG1 Chimeric mAb Flow Cyt
  DMC100368B Biotinylated Anti-GPR75 antibody(DMC368); IgG1 Chimeric mAb Flow Cyt
  DMC100492B Biotinylated Anti-GPR75 antibody(DMC492); IgG1 Chimeric mAb Flow Cyt
  DME101136 Anti-GPR75 antibody(12B6), Rabbit mAb Flow Cyt
  DME101136B Biotinylated Anti-GPR75 antibody(12B6), Rabbit mAb Flow Cyt
  DMC100368P PE-conjugated Anti-GPR75 antibody(DMC368); IgG1 Chimeric mAb Flow Cyt
LGR4 DME101188 Anti-LGR4 antibody(1D9), Rabbit mAb Flow Cyt
MC4R DME101294 Anti-MC4R antibody(2H10), Rabbit mAb Flow Cyt
TSHR DMC101228 Anti-TSHR antibody(1C8), IgG1 Chimeric mAb Flow Cyt
Target Cat.No. Product Name Applications
CB1 DME100144 Anti-CB1 antibody(DM144); Rabbit mAb ELISA; Flow Cyt
GPR20 DME101292 Anti-GPR20 antibody(1E10), Rabbit mAb Flow Cyt
GRPR DME101290 Anti-GRPR antibody(3B12), Rabbit mAb Flow Cyt
MC4R DME101294 Anti-MC4R antibody(2H10), Rabbit mAb Flow Cyt
SSTR2 DMC100428 Anti-SSTR2 antibody(DMC428); IgG1 Chimeric mAb Flow Cyt
Target Cat.No. Product Name Applications
ADGRE2 DMC100370 Anti-ADGRE2 antibody(DMC370); IgG1 Chimeric mAb Flow Cyt
CXCR4 DMC100680 Anti-CXCR4 antibody(DMC680), IgG1 Chimeric mAb Flow Cyt
CXCR7 DMC100443 Anti-CXCR7 antibody(DMC443); IgG1 Chimeric mAb Flow Cyt
FZD10 DMC100487 Anti-FZD10 antibody(DMC487); IgG1 Chimeric mAb Flow Cyt
FZD4 DMC101111 Anti-FZD4 antibody(10E10), IgG1 Chimeric mAb Flow Cyt
GPR75 DMC100368 Anti-GPR75 antibody(DMC368); IgG1 Chimeric mAb Flow Cyt
  DMC100492 Anti-GPR75 antibody(DMC492); IgG1 Chimeric mAb Flow Cyt
  DMC100368B Biotinylated Anti-GPR75 antibody(DMC368); IgG1 Chimeric mAb Flow Cyt
  DMC100492B Biotinylated Anti-GPR75 antibody(DMC492); IgG1 Chimeric mAb Flow Cyt
  DME101136 Anti-GPR75 antibody(12B6), Rabbit mAb Flow Cyt
  DME101136B Biotinylated Anti-GPR75 antibody(12B6), Rabbit mAb Flow Cyt
  DMC100368P PE-conjugated Anti-GPR75 antibody(DMC368); IgG1 Chimeric mAb Flow Cyt
GPR87 DMC100478 Anti-GPR87 antibody(DMC478); IgG1 Chimeric mAb Flow Cyt
  DMC100478B Biotinylated Anti-GPR87 antibody(DMC478); IgG1 Chimeric mAb Flow Cyt
GPRC5D DME100091 Anti-GPRC5D antibody(DM91); Rabbit mAb ELISA; Flow Cyt
  DME100091B Biotinylated Anti-GPRC5D antibody(DM91); Rabbit mAb ELISA; Flow Cyt
  DME100091P PE-conjugated Anti-GPRC5D antibody(DM91); Rabbit mAb Flow Cyt
GRPR DME101290 Anti-GRPR antibody(3B12), Rabbit mAb Flow Cyt
LGR4 DME101188 Anti-LGR4 antibody(1D9), Rabbit mAb Flow Cyt
SSTR2 DMC100428 Anti-SSTR2 antibody(DMC428); IgG1 Chimeric mAb Flow Cyt

……更多GPCR靶点持续更新中。

凭借DiProTM Nanodisc全长膜蛋白平台的支撑,缔码正不断推出识别天然构象的新GPCR流式抗体,让研究者能够轻松实现高特异性活细胞检测与定量分析,全面赋能GPCR药物研发。

5. 案例展示

Anti-CCR1 antibody(DMC465); IgG1 Chimeric mAb

antibody-dmc100465 ccr1 fc2

(A) DMC100465 does not bind to CHO-S cells that do not express CCR1.
(B) A clear peak shift of DMC100465 was seen compared to the control when incubated with CCR1-expressing 8226 cells, indicating strong binding of DMC100465 to CCR1. Antibodies were incubated at 5 μg/ml.

Anti-CCR6 antibody(DMC477); IgG1 Chimeric mAb

antibody-dmc100477 ccr6 fc2

(A) DMC100477 does not bind to CHO-S cells that do not express CCR6.
(B) A clear peak shift of DMC100477 was seen compared to the control when incubated with CCR6-expressing Huh7 cells, indicating strong binding of DMC100477 to CCR6. Antibodies were incubated at 5 μg/mL.

Anti-GPRC5D antibody(DM91); Rabbit mAb

antibody-dme100091 gprc5d fc1

(A) DME100091 does not bind to Jurkat cells that do not express GPRC5D.

(B) A clear peak shift of DME100091 was seen compared to the control when incubated with GPRC5D-expressing MM.1S cells, indicating strong binding of DME100091 to GPRC5D. Antibodies were incubated at 5 µg/mL.

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