预约演示

更新于：2025-05-07

APB

更新于：2025-05-07

基本信息

别名

Aminopeptidase B、AP-B、APB

+ [4]

简介

Exopeptidase which selectively removes arginine and/or lysine residues from the N-terminus of several peptide substrates including Arg(0)-Leu-enkephalin, Arg(0)-Met-enkephalin and Arg(-1)-Lys(0)-somatostatin-14. Can hydrolyze leukotriene A4 (LTA-4) into leukotriene B4 (LTB-4) (By similarity).

关联

项与 APB 相关的药物

Ubenimex

乌苯美司

靶点

APB x LTA4H

作用机制

APB抑制剂 [+2]

在研机构

Nippon Kayaku Co., Ltd. [+2]

原研机构

Nippon Kayaku Co., Ltd.

在研适应症

造血干细胞移植 [+6]

非在研适应症

淋巴水肿 [+1]

最高研发阶段批准上市

首次获批国家/地区

日本

首次获批日期1987-03-01

HAB-439

靶点

APB

作用机制

APB抑制剂 [+1]

在研机构-

原研机构

Hoechst AG

在研适应症-

非在研适应症

免疫缺陷综合征

最高研发阶段无进展

首次获批国家/地区-

首次获批日期1800-01-20

项与 APB 相关的临床试验

JPRN-jRCT2061230111

/ Recruiting临床3期IIT

Phase III Study of DFP-14323 plus Afatinib in Patients with NSCLC Harboring Uncommon EGFR mutations

开始日期2024-07-03

申办/合作机构-

CTR20232970

/ CompletedN/A

乌苯美司胶囊（30mg）在中国健康受试者中空腹和餐后给药条件下、单中心、随机、开放、单剂量、两序列、两周期、双交叉生物等效性试验

主要研究目的：按有关生物等效性试验的规定，选择Nippon Kayaku Co., Ltd.为持证商的乌苯美司胶囊（商品名：Bestatin，规格：30mg）为参比制剂，对西安万隆制药股份有限公司生产并提供的受试制剂乌苯美司胶囊（规格：30mg）进行空腹和餐后给药人体生物等效性试验，比较受试制剂中药物的吸收速度和吸收程度与参比制剂的差异是否在可接受的范围内，评估两种制剂在空腹和餐后给药条件下的生物等效性。次要研究目的：观察健康志愿受试者口服受试制剂乌苯美司胶囊（规格：30mg）和参比制剂乌苯美司胶囊（商品名：Bestatin，规格：30mg）的安全性。

开始日期2023-10-11

申办/合作机构

西安万隆制药股份有限公司

CTR20232253

/ CompletedN/A

乌苯美司胶囊在中国健康志愿者空腹及餐后给药条件下生物等效性试验

主要研究目的本研究以成都苑东生物制药股份有限公司研制的乌苯美司胶囊（10mg/粒）为受试制剂，原研厂家日本化药株式会社生产的乌苯美司胶囊（10mg/粒，商品名：Bestatin®）为参比制剂，评估受试制剂和参比制剂在空腹和餐后给药状态下的生物等效性，为该药注册申报及临床用药提供参考依据。次要研究目的评价中国健康志愿者空腹和餐后条件下受试制剂乌苯美司胶囊（10mg/粒）和参比制剂Bestatin®（10mg/粒）安全性。

开始日期2023-08-13

申办/合作机构

成都苑东生物制药股份有限公司

100 项与 APB 相关的临床结果

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100 项与 APB 相关的转化医学

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0 项与 APB 相关的专利（医药）

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440

项与 APB 相关的文献（医药）

2025-05-01·Plant, Cell & Environment

OsPIL15‐Induced Delay in Rice Heading Date via Direct Binding to the OsLF Promoter is Dependent on Functional Phytochrome B

Article

作者: Li, Yaping ; Xie, Xianzhi ; Xie, Lixia ; Zhou, Jinjun ; Peng, Yongbin ; Xu, Xiaohui ; He, Yanan ; Jiang, Conghui ; Sun, Wei ; Pu, Menglin ; Zheng, Chongke

ABSTRACTHeading date of rice (Oryza sativa) is a key factor determining rice production and regional adaptability. We analysed the molecular mechanism of OsPIL15, encoding phytochrome‐interacting factor‐like protein, in delaying rice heading date. Overexpression of OsPIL15 delayed rice heading date by upregulating Hd1 and inhibiting Hd3a and RFT1 expression. OsLF, encoding one rice heading repressor, was found to be the putative candidate regulated by OsPIL15 through a chromatin immunoprecipitation sequencing assay and a transcriptome sequencing assay. OsPIL15 could directly bind to the OsLF promoter and activated its expression. Knocking‐out OsLF in OsPIL15‐overexpressing lines resulted in flowering 2–3 days earlier, partially rescuing the delayed phenotype. This indicates that overexpression of OsPIL15 overexpression delays heading date partially through OsLF. Protein–protein interaction assay of OsPIL15 or OsPIL15‐∆APB (OsPIL15 lacking the active phytochrome B [phyB]‐binding [APB] motif) with PHYB showed that the APB motif was required for the interaction between OsPIL15 and PHYB. Furthermore, overexpression of either OsPIL15‐∆APB in the wild type or OsPIL15 in the phyB mutant did not delay rice heading date under natural long‐day conditions, suggesting that phyB influences OsPIL15‐mediated delay in rice heading date.

2025-03-01·Cancer Science

Tumor exosomal RNPEP promotes lung metastasis of liver cancer via inducing cancer‐associated fibroblast activation

Article

作者: Wu, Qiuping ; Li, Wenting ; Chen, Yuankun ; Gao, Yufeng ; Wu, Haifeng ; Weng, Minhua ; Yang, Yijun ; Pan, Gaofeng

AbstractCancer‐associated fibroblasts (CAFs) are essential players in the tumor microenvironment (TME) due to their roles in facilitating tumor progression and metastasis. It is worth noting that the high‐metastatic hepatocellular carcinoma (HCC) cell‐derived exosomes have exhibited the ability to transform normal fibroblasts into CAFs, which further fosters the lung metastasis of low‐metastatic HCC cells. Yet, the mechanisms underlying this tumor exosome‐induced metastatic niche formation are poorly explored. In this study, the secreted protein arginyl aminopeptidase (RNPEP) was highly expressed in the plasma of patients with HCC. In addition, high‐metastatic HCC cells showed augmented RNPEP expression levels in their exosomes. These exosomes induced obvious CAF‐like properties in the human fibroblast cell line MRC‐5, as evidenced by the increased CAF marker expression, and enhanced migratory ability. More strikingly, the secretions from high‐metastatic tumor exosome‐educated MRC‐5 cells increased tumor stemness and promoted epithelial–mesenchymal transition (EMT) in MHCC‐97L cells, a low‐metastatic HCC cell line. However, the knockdown of RNPEP in exosomes from high‐metastatic HCC cells abated the changes described above. Animal studies in vivo highlighted the pro‐tumor and pro‐metastatic effects of exosomal RNPEP on MHCC‐97L cells by inducing CAF activation. Furthermore, tumor‐derived exosomal RNPEP induced the activation of NF‐κB signaling in MRC‐5 cells, a critical pathway associated with CAF activation. Collectively, these results provide novel insight into tumor‐derived exosomal RNPEP for its crosstalk with CAFs during HCC lung metastasis.

2025-03-01·Brain Research

Asymmetric intra and inter-hemispheric subcellular rat brain correlation of arginyl-aminopeptidase activity during development and aging

Article

作者: Durán, Raquel ; Ramírez-Sánchez, Manuel ; Segarra, Ana Belén ; Vives, Francisco ; Banegas, Inmaculada ; Domínguez-Vías, Germán ; Prieto, Isabel ; Martínez-Cañamero, Magdalena

The functional significance of brain asymmetry is still largely unknown. Studying the level of correlation of neuropeptide-degrading activities between subcellular fractions such as synaptosomal, of the left and right hemispheres of male rats during development and aging could provide relevant data on their functional role during these periods. The present study analyzes the level of correlation of a enkephalin- or angiotensin III-degrading activity, such as membrane-bound arginyl-aminopeptidase activity (M-B ArgAP) between the left versus right homogenate and/or synaptosomal subcellular fractions obtained and processed independently from both brain hemispheres during development and aging. The tested ages were: fetuses, rats of one week, one month, five month and two year old. In homogenate, the results demonstrate high levels of positive correlations (left versus right homogenate) with high levels of significance, without differences among the ages analyzed. In synaptosomes the results demonstrate positive correlations with a level close to statistical significance (left versus right synaptosomes) in fetuses, significant correlations at one week, one month and five months, particularly at one week and five months, and a radical decrease in the level of left versus right correlation between synaptosomes of two-year-old animals, which could suggest a functional loss of the bilateral synaptic interaction that could be carried out at earlier ages by M-B ArgAP activity. The interaction between left or right synaptosomes versus left or right homogenates demonstrate decreasing levels of positive correlation from fetuses to five month old rats, without differences between correlations of the left synaptosomes with correlations of the right ones. However, in two year old rats the values of correlations of the left synaptosomes diverged significantly from the right ones. While left synaptosomal correlations exhibited positive values, the right correlations exhibited negative ones, showing. a clear asymmetry between both sides in aged rats suggesting a marked reduction with aging of the synaptic function in the right hemisphere.