上海达吉特药业科技有限公司——筛靶就找达吉特（官网）

以直接结合筛选为核心，兼顾广度与深度：HuProt™ 20K人类蛋白组芯片给出靶点筛选的更优解

分类：科学前沿发布时间：2026-06-24 17:01:11

凭借高通量、高覆盖度、直接结合筛选及结果可重复等优势，HuProt™ 20K人类蛋白组芯片已成为药物研发与机制研究领域的重要靶点筛选技术。

HuProt™ 20K人类蛋白组芯片简介：

HuProt™人类蛋白质组微阵列，又称20K人类蛋白组芯片，是目前全球通量最高、覆盖最全面的蛋白质芯片。芯片上点制了超过两万种高质量全长重组人源蛋白，覆盖81%的人类基因组ORF区。目前，HuProt™ 20K人类蛋白组芯片已经在研究领域得到广泛的应用，如小分子靶点鉴定、蛋白质相互作用、自身抗体标志物谱、抗体特异性、DNA/RNA与蛋白互作研究等。在药物靶点发现领域，HuProt™ 20K芯片凭借其独特优势成为小分子药物直接靶点鉴定的明星技术。

HuProt™ 20K人类蛋白组芯片

HuProt™ 20K人类蛋白组芯片所包含蛋白概述

蛋白覆盖广：

HuProt™ 20K人类蛋白组芯片共收录超过21,000种独特的全长人类蛋白质、异构体变体及蛋白片段，可覆盖16,794个独立的人类基因。凭借极高的蛋白覆盖度与优异的蛋白质量，HuProt™ 20K芯片是目前全球范围内覆盖最广的人类蛋白集合产品。

HuProt™ 20K人类蛋白质组芯片所覆盖的蛋白种类及数量

蛋白质量高：

1.优质表达系统：HuProt™ 20K芯片上的蛋白质采用真核酵母表达系统逐一表达，酵母表达系统不仅提供利于复杂蛋白正确折叠的真核分子伴侣环境，还具备完善的蛋白折叠和翻译后修饰能力（如糖基化、磷酸化）。相比于原核系统（如大肠杆菌）表达的蛋白，能够确保其呈现生理相关的构象表位，经尿素/DTT变性实验证实其互作活性高度依赖于正确折叠。

HuProt™ 20K人类蛋白质组芯片上蛋白质纯化流程，特异性富集折叠态蛋白

2.标签设计与纯化工艺：HuProt™ 20K芯片上的蛋白质通过N端GST-His6双标签进行纯化，在天然条件下利用谷胱甘肽（GSH）琼脂糖树脂特异性捕获折叠态的GST融合蛋白，该流程能有效筛除未折叠或错误折叠的蛋白聚集体，特异性地保留正确折叠的蛋白。

3.多重严格的质控措施：每个蛋白均经过Sanger测序确证ORF插入正确性、凝胶电泳验证纯度与预期分子量，并在点制后通过抗-GST染色进行严格的批次质控（要求>95%的点为GST阳性），确保了芯片上蛋白质的高保真度与实验重现性。

HuProt™ 20K人类蛋白质芯片构建全流程

HuProt™ 20K人类蛋白组芯片的应用场景

HuProt™ 20K芯片对于这些高质量的单体蛋白直接固定于芯片表面，使得20K芯片在靶点筛选中能够精准锁定样本的直接结合靶点蛋白，彻底规避细胞内蛋白复合物与间接信号级联的干扰。这不仅能高效捕捉弱结合与瞬时互作、降低假阳性与靶点遗漏风险，更实现了全蛋白组级别的无偏筛选，为小分子药物（尤其是天然产物与多靶点分子）的直接靶点鉴定与机制解析提供了高通量、高可靠性的核心技术支撑。此外，HuProt™ 20K芯片上的蛋白均设有两个重复蛋白位点，通过评估两个重复蛋白位点信号，能够直观判断实验批次内重现性，有效降低因蛋白点样差异或实验随机漂移产生的偶然误差，为芯片数据的可靠性和重现性提供了内在支撑。

HuProt™ 20K人类蛋白组芯片的技术原理/实验流程：

1.首先利用封闭液对HuProt™ 20K芯片进行预处理，降低小分子探针与芯片基质之间的非特异性吸附。

2.随后将生物素标记的小分子探针与HuProt™ 20K芯片共同孵育，使其与芯片上的靶点蛋白发生结合。

3.经洗涤去除非特异性吸附的分子后，加入荧光-链霉亲和素溶液。

4.最后通过芯片扫描和数据分析，采集在通过检测芯片上的荧光信号，并结合数据分析筛选，确定小分子药物的直接结合靶点蛋白。

HuProt™ 20K人类蛋白质芯片筛选小分子靶蛋白流程

HuProt™ 20K人类蛋白组芯片的独特优势：

1.筛选直接结合，发现小分子的真实靶点：HuProt™ 20K芯片上的每种蛋白均以独立形式固定于芯片表面，可直接检测小分子与单一蛋白之间的结合情况，有效避免细胞内蛋白复合物及间接作用带来的干扰。

2.蛋白质量高，降低靶点遗漏风险：HuProt™ 20K芯片上的蛋白采用酵母表达纯化，丰度高、纯度高，可有效捕捉小分子与蛋白间的弱相互作用和瞬时相互作用。

3.筛选范围广，实现全蛋白组筛选：HuProt™ 20K芯片凭借超过20,000种人源蛋白的超高覆盖度，能够在单次实验中进行全蛋白组范围的结合靶点筛选。

4.高通量高性价比，适用复杂机制研究：尤其适用于天然产物、先导化合物、多靶点药物及作用机制未知分子的靶点挖掘，可一次性发现数十至数百个结合蛋白靶标，具有更高的筛靶效率和性价比。

HuProt™ 20K人类蛋白组芯片筛靶案例：

凭借高通量、高覆盖度、直接结合筛选及结果可重复等优势，HuProt™ 20K人类蛋白组芯片已成为药物研发与机制研究领域的重要靶点筛选技术，20K芯片的筛选结果能够为后续SPR、CETSA、DARTS、Pull-down、功能验证及信号通路研究提供明确方向，大幅提升靶点发现效率和机制研究深度。截止目前，达吉特已经有上百个交付的HuProt™ 20K芯片项目数据先后在各类国际知名刊物上发表，这些高水平论文正在为新时代中国药物研发事业的发展提供新的思路和新方向。

达吉特客户利用HuProt™ 20K人类蛋白组芯片筛靶案例

现列举部分达吉特客户利用HuProt™ 20K人类蛋白组芯片已经发表的文章案例：

达吉特客户案例1：南方医科大学珠江医院何肖龙教授团队在《Gut》（IF = 23.0）发表了题为“Gut microbial-derived N-acetylmuramic acid alleviates colorectal cancer via the AKT1 pathway”的文章。研究发现了一种特定的肽聚糖片段N-乙酰胞壁酸（NAM）对结直肠癌具有潜在的治疗作用。随后，基于HuProt™ 20K人类蛋白组芯片筛选NAM的直接靶点，进一步与结直肠癌相关蛋白进行联合分析，最终锁定了NAM的直接靶点是AKT1。深入研究发现，NAM靶向抑制AKT1的磷酸化水平，下调AKT1-FoxO3a信号通路的表达，抑制结直肠癌的发生与发展。

文章解读：Gut（IF：23.1）丨南方医科大学何肖龙团队揭示肠道菌群通过自身组分靶向调控结直肠癌细胞关键靶点的抗癌新机制

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达吉特客户案例2：中国人民解放军总医院（301医院）陈香美院士团队在《Advanced Science》（IF=14.3）发表了题为“Isoquercitrin Alleviates Diabetic Nephropathy by Inhibiting STAT3 Phosphorylation and Dimerization”的研究论文。研究首次揭示了天然产物异槲皮苷对糖尿病肾病的潜在治疗作用。采用HuProt™ 20K人类蛋白组芯片筛选其直接靶点，再通过靶点功能与调控通路的富集分析，层层递进最终锁定关键靶点。深入的机制研究证实，异槲皮苷靶向并阻碍内皮细胞和肾小管上皮细胞中STAT 3的磷酸化和二聚化，抑制其转录活性，从而发挥肾保护作用。

文章解读：Adv Sci（IF=14.3）| 301医院陈香美院士/李平/蔡广研团队发现异槲皮苷可通过调控STAT3缓解糖尿病肾病

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达吉特客户案例3：上海交通大学医学院孙宇教授团队在《Nature Communications》（IF=15.7）发表了题为“The natural flavonoid dihydromyricetin targets senescent cells via PRDX2 and alleviates age-related diseases”的研究论文。本研究通过功能筛选发现天然黄酮类化合物二氢杨梅素（Dihydromyricetin，DMY）具有多效的抗衰老作用。进一步，通过HuProt™ 20K人类蛋白组芯片结合Pull down+MS技术，全面筛选DMY的结合靶点。最终发现DMY通过靶向过氧化物还原蛋白2（PRDX2）调控其核转位或氧化还原活性，发挥双重抗衰老作用的分子机制。同为需要生物素标记小分子的筛靶技术，20K人类蛋白组芯片与Pull-down具有良好的结合筛靶优势。依托于20K芯片的高通量和高验证率优势，结合Pull down技术在更接近生理环境条件下的筛选，提高靶点的生理相关性。两技术联用，可兼顾筛选广度与验证深度，显著提高靶点筛选效率与结果准确性。

文章解读：Nat Commun丨上海交通大学医学院孙宇团队揭秘二氢杨梅素靶向PRDX2“双效抗衰”新机制

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HuProt™ 20K人类蛋白组芯片达吉特客户发文：

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19.Hu M, Xu Y, Wang Y, et al. Gut microbial-derived N-acetylmuramic acid alleviates colorectal cancer via the AKT1 pathway. Gut. Published online February 27, 2025. doi:10.1136/gutjnl-2024-332891(南方医科大学珠江医院) IF=23.1

20.Shao M, Zhang X, Sun J, et al. Saikosaponin b1 Attenuates Liver Fibrosis by Blocking STAT3/Gli1 Interaction and Inducing Gli1 Degradation. Exploration. 2766-8509.(浙江中医药大学) IF=22.5

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22.Xu X, Yan Y, Zheng M, et al. Emodin Alleviates Sepsis-Induced Multiorgan Damage by Inhibiting NETosis through Targeting Neutrophils BCL-10. Adv Sci (Weinh). 2025 Aug 8:e17129.(首都医科大学附属北京中医医院) IF=14.1

23.Xuan C, Chen D, Zhang S, et al. Isoquercitrin Alleviates Diabetic Nephropathy by Inhibiting STAT3 Phosphorylation and Dimerization. Adv Sci (Weinh). Published online April 4, 2025. doi:10.1002/advs.202414587(中国人民解放军总医院) IF=14.1

24.Chen L, Liu DH, Li YX, et al. Akebia Saponin D Targeting Ubiquitin Carboxyl-Terminal Hydrolase 4 Promotes Peroxisome Proliferator-Activated Receptor Gamma Deubiquitination and Activation of Brown Adipose Tissue Thermogenesis in Obesity. MedComm (2020). 2025;6(11):e70420. Published 2025 Oct 15. doi:10.1002/mco2.70420(中日友好医院) IF=10.7

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28.Lu H, Fan L, Zhang W, et al. The mitochondrial genome-encoded peptide MOTS-c interacts with Bcl-2 to alleviate nonalcoholic steatohepatitis progression. Cell Rep. 2024;43(1):113587. doi:10.1016/j.celrep.2023.113587(西安第四军医大学) IF=7.5

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34.Ma X, Hu Q, Jiang T, et al. Dehydroevodiamine Alleviates Ulcerative Colitis by Inhibiting the PI3K/AKT/NF-κB Signaling Pathway via Targeting AKT1 and Regulating Gut Microbes and Serum Metabolism. Molecules. 2024;29(17):4031. Published 2024 Aug 26. doi:10.3390/molecules29174031(成都中医药大学) IF=4.2

35.Li D, Wei R, Zhang X, et al. Gut commensal metabolite rhamnose promotes macrophages phagocytosis by activating SLC12A4 and protects against sepsis in mice. Acta Pharm Sin B. 2024;14(7):3068-3085. doi:10.1016/j.apsb.2024.03.025(南方医科大学) IF=14.6

36.Cui J, Chen Y, Yang Q, et al. Protosappanin A Protects DOX-Induced Myocardial Injury and Cardiac Dysfunction by Targeting ACSL4/FTH1 Axis-Dependent Ferroptosis. Adv Sci (Weinh). 2024;11(34):e2310227. doi:10.1002/advs.202310227(哈尔滨医科大学附属第二医院) IF=14.1

37.Zheng Y, Zhao L, Xiong Z, et al. Ursolic acid targets secreted phosphoprotein 1 to regulate Th17 cells against metabolic dysfunction-associated steatotic liver disease. Clin Mol Hepatol. 2024;30(3):449-467. doi:10.3350/cmh.2024.0047(上海中医药大学联合广州中医药大学) IF=14

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