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Last update 23 Jan 2025

APB

Last update 23 Jan 2025

Basic Info

Synonyms

Aminopeptidase B, AP-B, APB

+ [4]

Introduction

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).

Drugs associated with APB

Ubenimex

Target

APB x LTA4H

Mechanism

APB inhibitors [+2]

Active Org.

Nippon Kayaku Co., Ltd. [+2]

Originator Org.

Nippon Kayaku Co., Ltd.

Active Indication

Hematopoietic stem cell transplantation [+6]

Inactive Indication

Lymphedema [+1]

Drug Highest PhaseApproved

First Approval Ctry. / Loc.

First Approval Date01 Mar 1987

Clinical Trials associated with APB

JPRN-jRCT2061230111

/ RecruitingPhase 3IIT

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

Start Date03 Jul 2024

Sponsor / Collaborator-

CTR20232970

/ CompletedNot Applicable

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

[Translation] A single-center, randomized, open-label, single-dose, two-sequence, two-period, double-crossover bioequivalence study of ubenimex capsules (30 mg) in Chinese healthy subjects under fasting and fed conditions

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。

[Translation]

Main purpose of study: According to the relevant provisions of bioequivalence test, Nippon Kayaku Co., Ltd. is the licensee of Ubenimex Capsules (trade name: Bestatin, specification: 30mg) as the reference preparation, and the test preparation Ubenimex Capsules (specification: 30mg) produced and provided by Xi'an Wanlong Pharmaceutical Co., Ltd. are conducted on fasting and postprandial human bioequivalence tests to compare whether the absorption rate and degree of the drug in the test preparation are within the acceptable range with the reference preparation, and to evaluate the bioequivalence of the two preparations under fasting and postprandial administration conditions. Secondary purpose of study: To observe the safety of oral administration of the test preparation Ubenimex Capsules (specification: 30mg) and the reference preparation Ubenimex Capsules (trade name: Bestatin, specification: 30mg) by healthy volunteers.

Start Date11 Oct 2023

Sponsor / Collaborator

Xian Wanlong Pharmaceutical Co. Ltd.

CTR20232253

/ CompletedNot Applicable

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

[Translation] Bioequivalence study of ubenimex capsules in Chinese healthy volunteers under fasting and fed conditions

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。

[Translation]

Main research purpose This study uses Ubenimex Capsules (10 mg/capsule) developed by Chengdu Yuandong Biopharmaceutical Co., Ltd. as the test preparation, and Ubenimex Capsules (10 mg/capsule, trade name: Bestatin®) produced by the original manufacturer Nippon Kayaku Co., Ltd. as the reference preparation to evaluate the bioequivalence of the test preparation and the reference preparation under fasting and postprandial administration conditions, and provide a reference basis for the registration application and clinical use of the drug. Secondary research purpose Evaluate the safety of the test preparation Ubenimex Capsules (10 mg/capsule) and the reference preparation Bestatin® (10 mg/capsule) under fasting and postprandial conditions in healthy Chinese volunteers.

Start Date13 Aug 2023

Sponsor / Collaborator

Chengdu Easton Biopharmaceuticals Co., Ltd.

100 Clinical Results associated with APB

100 Translational Medicine associated with APB

0 Patents (Medical) associated with APB

465

Literatures (Medical) associated with APB

01 Mar 2025·Brain Research

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

Article

Author: 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.

01 Dec 2024·Photosynthesis Research

Structural comparison of allophycocyanin variants reveals the molecular basis for their spectral differences

Article

Author: Gisriel, Christopher J ; Croce, Roberta ; Shen, Gaozhong ; Brudvig, Gary W ; Elias, Eduard ; Bryant, Donald A ; Soulier, Nathan T

AbstractAllophycocyanins are phycobiliproteins that absorb red light and transfer the energy to the reaction centers of oxygenic photosynthesis in cyanobacteria and red algae. Recently, it was shown that some allophycocyanins absorb far-red light and that one subset of these allophycocyanins, comprising subunits from the ApcD4 and ApcB3 subfamilies (FRL-AP), form helical nanotubes. The lowest energy absorbance maximum of the oligomeric ApcD4-ApcB3 complexes occurs at 709 nm, which is unlike allophycocyanin (AP; ApcA-ApcB) and allophycocyanin B (AP-B; ApcD-ApcB) trimers that absorb maximally at ~ 650 nm and ~ 670 nm, respectively. The molecular bases of the different spectra of AP variants are presently unclear. To address this, we structurally compared FRL-AP with AP and AP-B, performed spectroscopic analyses on FRL-AP, and leveraged computational approaches. We show that among AP variants, the α-subunit constrains pyrrole ring A of its phycocyanobilin chromophore to different extents, and the coplanarity of ring A with rings B and C sets a baseline for the absorbance maximum of the chromophore. Upon oligomerization, the α-chromophores of all AP variants exhibit a red shift of the absorbance maximum of ~ 25 to 30 nm and band narrowing. We exclude excitonic coupling in FRL-AP as the basis for this red shift and extend the results to discuss AP and AP-B. Instead, we attribute these spectral changes to a conformational alteration of pyrrole ring D, which becomes more coplanar with rings B and C upon oligomerization. This study expands the molecular understanding of light-harvesting attributes of phycobiliproteins and will aid in designing phycobiliproteins for biotechnological applications.

28 Oct 2024·Nucleic Acids Research

Polyubiquitinated PCNA triggers SLX4-mediated break-induced replication in alternative lengthening of telomeres (ALT) cancer cells

Article

Author: Park, Su Hyung ; Myung, Kyungjae ; Kim, Sangin ; Kang, Nalae ; Ra, Jae Sun ; Lee, Kyoo-young

AbstractReplication stresses are the major source of break-induced replication (BIR). Here, we show that in alternative lengthening of telomeres (ALT) cells, replication stress-induced polyubiquitinated proliferating cell nuclear antigen (PCNA) (polyUb-PCNA) triggers BIR at telomeres and the common fragile site (CFS). Consistently, depleting RAD18, a PCNA ubiquitinating enzyme, reduces the occurrence of ALT-associated promyelocytic leukemia (PML) bodies (APBs) and mitotic DNA synthesis at telomeres and CFS, both of which are mediated by BIR. In contrast, inhibiting ubiquitin-specific protease 1 (USP1), an Ub-PCNA deubiquitinating enzyme, results in an increase in the above phenotypes in a RAD18- and UBE2N (the PCNA polyubiquitinating enzyme)-dependent manner. Furthermore, deficiency of ATAD5, which facilitates USP1 activity and unloads PCNAs, augments recombination-associated phenotypes. Mechanistically, telomeric polyUb-PCNA accumulates SLX4, a nuclease scaffold, at telomeres through its ubiquitin-binding domain and increases telomere damage. Consistently, APB increase induced by Ub-PCNA depends on SLX4 and structure-specific endonucleases. Taken together, our results identified the polyUb-PCNA-SLX4 axis as a trigger for directing BIR.

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