预约演示

更新于：2025-05-07

ENPP3

更新于：2025-05-07

基本信息

别名

Alkaline phosphodiesterase I、B10、CD203c

+ [13]

简介

Hydrolase that metabolizes extracellular nucleotides, including ATP, GTP, UTP and CTP (PubMed:29717535, PubMed:9344668). Limits mast cells and basophils response during inflammation and during the chronic phases of allergic responses by eliminating extracellular ATP, a signaling molecule activating these cells in an autocrine manner. Metabolizes extracellular ATP in the lumen of the small intestine, and thereby prevents ATP-induced apoptosis of intestinal plasmacytoid dendritic cells (By similarity). Has a broad specificity and can also hydrolyze UDP-GlcNAc into UMP and GlcNAc-1-phosphate and potentially several other intracellular nucleotide sugars, including UDP-GalNAc, CMP-NeuAc, GDP-Fuc, and UDP-GlcA. Thereby, could modulate glycan biosynthesis and protein glycosylation (By similarity). Can hydrolyze extracellular dinucleoside polyphosphates, including the vasoactive adenosine polyphosphates as well (PubMed:12846830). In addition, displays an alkaline phosphodiesterase activity in vitro (PubMed:11342463).

关联

项与 ENPP3 相关的药物

XmAb-819

靶点

CD3 x ENPP3

作用机制

CD3刺激剂 [+3]

在研机构

Xencor, Inc.

原研机构

Xencor, Inc.

在研适应症

局部晚期透明细胞肾细胞癌 [+1]

非在研适应症-

最高研发阶段临床1期

首次获批国家/地区-

首次获批日期1800-01-20

JNJ-87890387

靶点

CD3 x ENPP3

作用机制

CD3刺激剂 [+1]

在研机构

Janssen Research & Development LLC

原研机构

Janssen Research & Development LLC

在研适应症

晚期恶性实体瘤

非在研适应症-

最高研发阶段临床1期

首次获批国家/地区-

首次获批日期1800-01-20

SIM0680

靶点

ENPP3

作用机制

ENPP3抑制剂

在研机构

先聲藥業集團有限公司

原研机构

先聲藥業集團有限公司

在研适应症

实体瘤

非在研适应症-

最高研发阶段临床前

首次获批国家/地区-

首次获批日期1800-01-20

项与 ENPP3 相关的临床试验

NCT06178614

/ Recruiting临床1期

A Phase 1 Study of JNJ-87890387, an Ectonucleotide Pyrophosphatase/Phosphodiesterase Family Member 3 (ENPP3) x CD3 Bispecific Antibody, for Advanced Solid Tumors

The purpose of this study is to determine recommended phase 2 dose(s) (RP2Ds) of JNJ-87890387 and to determine the safety of JNJ-87890387 at the RP2D(s).

开始日期2023-12-14

申办/合作机构

Janssen Research & Development LLC

NCT05433142

/ Recruiting临床1期

A Phase 1 Multiple Dose Study to Evaluate the Safety and Tolerability of XmAb819 in Subjects With Relapsed or Refractory Clear Cell Renal Cell Carcinoma

The purpose of this study is to assess the safety and tolerability of XmAb®819 administered intravenous (IV) or subcutaneous (SC) in subjects with relapsed or refractory clear cell renal cell carcinoma and to identify the minimum safe and biologically active dose and the recommended dose (RD).

开始日期2022-06-13

申办/合作机构

Xencor, Inc.

NCT02639182

/ Completed临床2期

A Multi-Center, Open Label, Randomized Phase 2 Study of AGS-16C3F vs. Axitinib in Metastatic Renal Cell Carcinoma

The purpose of this study was to evaluate the progression free survival (PFS), based on investigator radiologic review, of AGS-16C3F compared to axitinib in subjects with metastatic renal cell carcinoma.

开始日期2016-05-03

申办/合作机构

Astellas Pharma Global Development, Inc.

100 项与 ENPP3 相关的临床结果

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100 项与 ENPP3 相关的转化医学

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0 项与 ENPP3 相关的专利（医药）

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746

项与 ENPP3 相关的文献（医药）

2025-04-01·Allergology International

Establishment of a novel human basophil cell line for functional analysis and in vitro allergy testing

Article

作者: Abe, Takaaki ; Maebara, Kanako ; Miyata, Shigeki ; Satake, Masahiro ; Kurita, Ryo ; Takahashi, Daisuke ; Tani, Yoshihiko

BACKGROUNDBasophils are the rarest granulocytes and play diverse roles, e.g., in protective immunity and allergic inflammatory reactions. However, the underlying molecules and mechanisms involved in basophil differentiation and functions, particularly in humans, remain largely unknown. This may be due to the lack of high-quality research tools.METHODSWe established a novel, immortalized, human basophil cell line by introducing human papillomavirus 16-E6/E7, c-MYC, and BCL-xL gene expression systems into cultured basophils, and evaluated whether this cell line is useful as a research tool, compared with KU812, which is the most commonly-used human basophil cell line.RESULTSThis cell line expressed various basophil markers, including CD123, CD203c, and the high-affinity immunoglobulin (Ig)E receptor α-chain and can mature into more differentiated cells under specific culture conditions. The differentiated cells stimulated with anti-IgE antibodies showed increased CD203c expression in a dose-dependent manner, whereas the differentiated KU812 cells showed little activation after the stimulation. The established cell line also demonstrated increased sensitivity to allergic activation when stimulated with an allergen (NP-BSA) and allergen-specific IgE (anti-NP-IgE). Furthermore, histamine- and interleukin-4-releasing abilities were also confirmed. These allergic activation profiles were similar to those of basophils from healthy individuals, although the activation levels of the established cells were lower than those of basophils from highly-sensitive individuals.CONCLUSIONSThese findings suggest that the established basophil cell line has substantially different characteristics from a conventional cell line and could serve as a new tool for investigating basophil differentiation and functions, as well as for testing allergic reactions.

2025-04-01·Journal of Allergy and Clinical Immunology

Baseline basophil activation and early suppression is associated with clinical outcome after peanut sublingual immunotherapy

Article

作者: Burks, A Wesley ; Virkud, Yamini V ; Smeekens, Johanna M ; Kulis, Michael D ; Yue, Xiaohong ; Keet, Corrine A ; Bird, J Andrew ; Guo, Rishu ; Humphrey, Jessica R ; Kim, Edwin H

BACKGROUNDSublingual immunotherapy (SLIT) was recently shown to safely induce desensitization and remission of peanut allergy in 1-to 4-year-old children.OBJECTIVEBasophil activation has been shown to be suppressed in allergen-specific immunotherapy. We aimed to evaluate the timing of basophil suppression during peanut SLIT and its impact on clinical outcomes.METHODSFifty peanut-allergic children were enrolled in a peanut SLIT trial and randomized to active peanut or placebo SLIT for 36 months followed by a three-month avoidance period to evaluate remission. Blood was collected at baseline, 12, 24, 36, and 39 months to measure basophil activation by CD63 and CD203c.RESULTSFor participants on peanut SLIT, basophil activation based on CD63 expression was significantly reduced by 12 months and continued to decrease throughout peanut SLIT, whereas CD63 activation in participants receiving placebo remained unchanged from 0-36 months. CD203c expression remained unchanged for both peanut SLIT and placebo participants throughout the trial. Actively treated participants who achieved remission had lower CD63 expression at baseline and significant suppression of CD63 expression by 12 months, while treatment failures had higher CD63 expression at baseline and lack of suppression by 12 months. Lower basophil activation in those achieving remission, compared to those that failed treatment, remained present for up to 3 years.CONCLUSIONSFollowing peanut SLIT, participants who achieved remission had significantly suppressed basophils by 12 months, compared to unsuccessful participants that were not desensitized, suggesting that early suppression of basophils may be indicative of peanut SLIT efficacy.

2025-02-05·Journal of Agricultural and Food Chemistry

Molecular and Immunological Characterization of Troponin C: An Allergen from Scylla paramamosain

Article

作者: Liu, Qingmei ; Luo, Lianzhong ; Li, Mengsi ; Chang, Chih-Jung ; Liu, Guangming ; Han, Xinyu ; Li, Fajie ; Liao, Yuni ; Liu, Yixiang ; Xia, Fei

Scylla paramamosain, a crustacean of substantial importance, is a frequent trigger of food allergies. This study examined the molecular and immunological properties of troponin C from S. paramamosain (Scy p TnC) as an allergen. The findings indicated that thermal stability of Scy p TnC comprised 150 amino acids and facilitated the induction of CD63/CD203c in basophils from crab allergy patients. Furthermore, treatment of Scy p TnC with chemical denaturants caused structural degradation, which resulted in diminished IgG binding capacity. Subsequently, 6 linear epitopes and 4 conformational epitope regions of TnC were predicted, with epitopes at the C-terminal being conserved throughout 9 discovered TnCs. Concurrently, mice sensitized with Scy p TnC exhibited markedly increased levels of IgE and IL-4 release, provoking a Th2 immune response. The results reveal crab allergens and enhance existing knowledge regarding allergenic components in crabs, thereby facilitating the advancement of molecular diagnostics and targeted therapeutic strategies.

项与 ENPP3 相关的新闻（医药）

2025-03-29

·医药笔记

中国企业引领ADC创新前沿

▎Armstrong2025年美国癌症研究协会年会（AACR）即将于4月25-30日在美国芝加哥举行，最近会议摘要已经公开，中国创新密集亮相。以ADC领域为例，绝大部分的报告来自中国药企，创新ADC接近100款，覆盖各种技术路线和靶点上的创新，真正开始引领ADC的创新前沿。双靶点ADC为ADC领域当前最热门的方向之一，百力司康、百奥赛图、博锐生物、橙帆医药、多禧生物、恒瑞医药、基石药业、金赛药业、康宁杰瑞、康源博创、联进生物、启德医药、石药集团、拓济生物、先声药业、信达生物、映恩生物、亲和力生物等多家企业布局。双毒素ADC也开始走到台前，康弘药业、亲和力生物系统布局双毒素ADC，康弘药业的KH815为全球首款进入临床阶段的双毒素ADC新药。两种payload分别为TOP1i和RAN POL2i，同时抑制RNA合成并诱导DNA双链断裂。康宁杰瑞进一步开发了双靶点双毒素ADC，即EGFR/HER3双毒素ADC新药JSKN021。传统ADC的理念是毒素经抗体结合受体介导内吞后释放，DXd-ADC则证明了旁观者效应的重要作用，宜联生物则进一步开发了非内吞ADC，靶向游离靶标VEGF，通过肿瘤微环境特异性酶来释放毒素，进一步打开了ADC药物的应用空间。维立志博开发了首款TCE的ADC，即DLL3/CD3 ADC新药LBL-058，由DLL3/CD3双抗偶联TOP1i而成，T细胞杀伤与payload细胞毒杀伤效应协同。虽然TCE在少数靶点已经开始突破实体瘤，但TCE-ADC的设计无疑为突破实体瘤提供了一种全新强化设计的思路。总结从此次AACR会议来看，中国ADC无论在数量上，还是在差异化设计上，毫无疑问都在真正引领ADC的创新前沿，新靶点ADC、新靶点组合双靶点ADC、双毒素ADC、PDC、TCE-ADC、非内吞ADC等等，以及AACR会议不涉及的自免ADC（映恩生物已经进入临床阶段）等。未来几年，国产ADC的临床突破和出海交易仍然是值得期待的行业焦点所在。Armstrong技术全梳理系列GPRC5D靶点全梳理；CD40靶点全梳理；CD47靶点全梳理；补体靶向药物技术全梳理；补体药物：眼科治疗的重要方向；Claudin 6靶点全梳理；Claudin 18.2靶点全梳理；靶点冷暖，行业自知；中国大分子新药研发格局；被炮轰的“me too”；佐剂百年史；胰岛素百年传奇；CUSBEA：风雨四十载；中国新药研发的焦虑；中国生物医药企业的研发竞争；中国双抗竞争格局；中国ADC竞争格局；中国双抗技术全梳理；中国ADC技术全梳理；Ambrx技术全梳理；Vir Biotech技术全梳理；Immune-Onc技术全梳理；亘喜生物技术全梳理；康哲药业技术全梳理；科济药业技术全梳理；恺佧生物技术全梳理；同宜医药技术全梳理；百奥赛图技术全梳理；腾盛博药技术全梳理；创胜集团技术全梳理；永泰生物技术全梳理；中国抗体技术全梳理；德琪医药技术全梳理；德琪医药技术全梳理2.0；和铂医药技术全梳理；荣昌生物技术全梳理；再鼎医药技术全梳理；药明生物技术全梳理；恒瑞医药技术全梳理；豪森药业技术全梳理；正大天晴技术全梳理；吉凯基因技术全梳理；基石药业技术全梳理；百济神州技术全梳理；百济神州技术全梳理第2版；信达生物技术全梳理；信达生物技术全梳理第2版；中山康方技术全梳理；复宏汉霖技术全梳理；先声药业技术全梳理；君实生物技术全梳理；嘉和生物技术全梳理；志道生物技术全梳理；道尔生物技术全梳理；尚健生物技术全梳理；康宁杰瑞技术全梳理；科望医药技术全梳理；科望医药技术全梳理2.0；岸迈生物技术全梳理；礼进生物技术全梳理；康桥资本技术全梳理；余国良的抗体药布局；荃信生物技术全梳理；安源医药技术全梳理；三生国健技术全梳理；仁会生物技术全梳理；乐普生物技术全梳理；同润生物技术全梳理；宜明昂科技术全梳理；派格生物技术全梳理；迈威生物技术全梳理；Momenta技术全梳理；NGM技术全梳理；普米斯生物技术全梳理；普米斯生物技术全梳理2.0；三叶草生物技术全梳理；贝达药业抗体药全梳理；泽璟制药抗体药全梳理；恒瑞医药抗体药全梳理；齐鲁制药抗体药全梳理；石药集团抗体药全梳理；豪森药业抗体药全梳理；华海药业抗体药全梳理；科伦药业抗体药全梳理；百奥泰技术全梳理；凡恩世技术全梳理。

抗体药物偶联物AACR会议

2025-03-27

·摩熵医药

2025年AACR，超200款中国创新药闪耀亮相！

注：本文不构成任何投资意见和建议，以官方/公司公告为准；本文仅作医疗健康相关药物介绍，非治疗方案推荐（若涉及），不代表平台立场。任何文章转载需要得到授权。 2025年美国癌症研究协会年会（AACR）即将于4月25-30日在美国芝加哥举行，最近会议摘要已经公开，据不完全统计，今年有 95 家中国药企亮相 AACR 会议，带来了超 200 项新药研究结果，其中包括 60 项 ADC 研究、31 项双抗研究和 11 项单抗研究，其他药物类型还有多肽偶联药物、分子胶、细胞疗法、三抗、PROTAC 等。 ADC药物中，有几个重要的趋势，新靶点ADC、双抗ADC、双毒素ADC大量涌现。布局双抗ADC的有百力司康、百奥赛图、博锐生物、橙帆医药、多禧生物、恒瑞医药、基石药业、金赛药业、康宁杰瑞、康源博创、联进生物、启德医药、石药集团、拓济生物、先声药业、信达生物、映恩生物、亲和力生物等。布局双毒素ADC的有多禧生物、康弘药业、康宁杰瑞、亲和力生物等。从靶点来看，消化道肿瘤的CDH17最为热门，有11款，分别来自博奥信、博锐生物、橙帆医药（CDH17/Claudin18.2）、华东医药、乐普生物、礼新医药、迈威生物、拓创生物、维立志博、先声药业、宜联生物。百济神州首次披露了 4-1BB/GPC3 双抗 BGB-B2033，EGFR/MET 三抗 BG-T187、PRMT5 抑制剂 BGB-58067 等产品的临床前研究数据。先声药业公布了多款差异化布局的 ADC 最新研究结果，靶点涉及 CDH17、ENPP3、EGFR/cMet、cMET/B7H3 等。信达生物则首次披露了 IBI3010 的靶点为 FRα 。此外，恒瑞、翰森、齐鲁、石药等也在此次 AACR 会议上发布了重要研究数据。2025年AACR会议摘要：中国药企将披露的超 200 项新药研究结果列表小结近年来，中国创新药在 AACR 会议上的影响力持续攀升，吸引了越来越多目光。也越来越多的项目出海达成合作，中国创新药研发实力不容小觑。 END 近期热门资源获取 CGT产业现状与未来趋势蓝皮书-202406 中药行业现状与未来趋势白皮书-202407 2023年医药企业综合实力排行榜-202408 跨越国界，引领创新：中国药企出海的布局实践-202408 专利即将到期五大重磅小分子药品，国内仿制药“战况”几何?-202409 中国放射性药物市场现状分析报告-202410 合成生物产业发展前景及中国合成生物产业链上中下游企业分析-202410 中国合成生物学创投市场分析报告-202410 中国糖尿病临床诊疗与药物多渠道市场数据分析-202411 基于剂型改良的复杂注射剂分析--微球篇-202411 2024医美注射材料市场发展分析报告-20241213 国家药品集采跟踪报告-前9批次集采回顾与展望-202411 近期更多摩熵咨询热门报告，识别下方二维码领取联系我们，体验摩熵医药更多专业服务会议合作园区服务数据库咨询定制服务媒体合作 👆👆👆点击上方图片，即可开启摩熵化学数据查询点击阅读原文，申请摩熵医药企业版免费试用！

抗体药物偶联物AACR会议细胞疗法蛋白降解靶向嵌合体

2025-02-27

·Firstwordpharma

Xencor further shrinks oncology pipeline with pause on vudalimab

Xencor has paused further development of its PD-1xCTLA-4 bispecific antibody vudalimab, another sign the company appears to be pivoting away from oncology to concentrate more on autoimmune diseases. In the disclosure, tucked in Xencor's fourth-quarter financial results Thursday, the company states it "has prioritised resources to advance other pipeline programmes."Xencor noted that it completed enrollment in two studies of vudalimab in metastatic castration-resistant prostate cancer (mCRPC) and in Part 1 of a study in non–small-cell lung cancer. "Safety data from the three studies…remain consistent with prior data disclosures," it added.Disappointing prostate cancer studyThe move follows disappointing Phase II results reported for vudalimab last year, showing a 33% objective response rate in heavily pretreated mCRPC patients, but with only three confirmed partial responses. However, more concerning, was a fatal case of treatment-related autoimmune hepatitis that raised safety questions despite the company maintaining there were no general concerns of hepatitis based on data from over 240 patients.The company's seeming retreat from oncology had already begun last year when Johnson & Johnson terminated its rights to plamotamab, a CD20xCD3 bispecific T-cell engager that was being developed for blood cancers. Rather than abandoning the compound, however, Xencor has repurposed it for multi-drug resistant rheumatoid arthritis, with a Phase Ib/IIa proof-of-concept study planned for the first half of 2025.Its autoimmune portfolio also includes XmAb942, an anti-TL1A antibody with extended half-life, that is being developed for inflammatory bowel disease, with initial healthy volunteer data expected in the first half of 2025, and plans to enter Phase II in ulcerative colitis in the second half. Meanwhile, XmAb657, a preclinical CD19xCD3 bispecific T-cell engager for autoimmune disease, is slated to move into Phase I in the second half.Oncology still in playHowever, despite pruning its oncology pipeline, Xencor still appears to have ambitions in the space. The company continues to advance XmAb819, a T-cell engaging bispecific antibody targeting ENPP3 in clear cell renal cell carcinoma. Initial data will be presented at a medical conference during the second half of 2025.Other oncology assets include XmAb541, which targets CLDN6 in solid tumours, and XmAb808, a B7-H3xCD28 bispecific antibody being tested in Phase I with Merck & Co.'s Keytruda (pembrolizumab). "To date a maximum tolerated dose has not been reached, and data from the study (of XmAb808) are expected to inform future development decisions for the programme," Xencor said."In 2024, we began rebalancing our pipeline to focus on XmAb drug candidates that leverage our protein engineering strengths and reduce exposure to biological uncertainties… We are enthusiastic about ongoing advancement within our oncology portfolio of T-cell engager programmes that are nearing important clinical inflection points," stated CEO Bassil Dahiyat.

临床2期临床1期抗体药物偶联物蛋白降解靶向嵌合体