更新于：2024-11-01

XPNPEP2

更新于：2024-11-01

基本信息

别名

Aminoacylproline aminopeptidase、mAmP、Membrane-bound aminopeptidase P

+ [7]

简介

Membrane-bound metalloprotease which catalyzes the removal of a penultimate prolyl residue from the N-termini of peptides, such as Arg-Pro-Pro. May play a role in the metabolism of the vasodilator bradykinin.

关联

项与 XPNPEP2 相关的药物

ST-115

靶点

XPNPEP2

作用机制

XPNPEP2 inhibitors

在研机构

Loyola University of Chicago

原研机构

Loyola University of Chicago

在研适应症

缺血性卒中 [+1]

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

100 项与 XPNPEP2 相关的临床结果

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100 项与 XPNPEP2 相关的转化医学

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0 项与 XPNPEP2 相关的专利（医药）

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149

项与 XPNPEP2 相关的文献（医药）

2024-09-01·Bioorganic & Medicinal Chemistry Letters

[1,2,4]Triazolo[1,5-a]pyrimidine derivatives: Structure-activity relationship study leading to highly selective ENPP1 inhibitors

Article

作者: Kawaguchi, Mitsuyasu ; Minami, Shohei ; Ieda, Naoya ; Nakagawa, Hidehiko

The STING (stimulator of interferon genes) pathway is one of the pathways that regulate innate immunity, and the extracellular hydrolytic enzyme ecto-nucleotide pyrophosphatase/phosphodiesterase 1 (ENPP1) has been identified as its dominant negative regulator. Since activation of the innate immune system is a promising strategy for the treatment of various infectious diseases and cancers, ENPP1 inhibitors have attracted great attention as candidate drugs. We have previously identified small-molecule ENPP1 inhibitors having a [1,2,4]triazolo[1,5-a]pyrimidine scaffold by means of chemical screening using a fluorescence probe, TG-mAMP. In this study, we evaluated the structure-activity relationships of the hit and lead compounds in detail, and succeeded in developing compounds that strongly and selectively inhibit ENPP1 not only in vitro, but also in cellular systems.

2024-03-15·Science Advances

S -nitrosylation of a receptor-like cytoplasmic kinase regulates plant immunity

Article

作者: Pan, Qiaona ; Cui, Wenqiang ; Wang, Yiqin ; Liu, Fengquan ; Loake, Verity I P ; Yuan, Shuguang ; Loake, Gary J ; Cui, Beimi

Perception of pathogen/microbial-associated molecular patterns (P/MAMPs) by plant cell surface receptors leads to a sustained burst of reactive oxygen species (ROS), a key feature of P/MAMP-triggered immunity (PTI). Here we report that P/MAMP recognition leads to a rapid nitrosative burst, initiating the accumulation of nitric oxide (NO), subsequently leading to S -nitrosylation of the receptor-like cytoplasmic kinase (RLCK), botrytis-induced kinase 1 (BIK1), at Cys 80 . This redox-based, posttranslational modification, promotes the phosphorylation of BIK1, subsequently resulting in BIK1 activation and stabilization. Further, BIK1 S -nitrosylation increases its physical interaction with RBOHD, the source of the apoplastic oxidative burst, promoting ROS formation. Our data identify mechanistic links between rapid NO accumulation and the expression of PTI, providing insights into plant immunity.

2024-01-16·Langmuir

Development of a Sustainable Biobased Flame-Retardant Microcapsule and Its Flame-Retarding Mechanism on Asphalt Combustion

Article

作者: Xia, Wenjing ; Xu, Tao ; Dong, Ming

To develop an efficient, sustainable, and eco-friendly biobased flame-retardant microcapsule suitable for the working environments of tunnel asphalt pavement and reveal its flame-retarding mechanism on asphalt combustion, microencapsulated amylopectin (MAMP) was first prepared using an in situ polymerization method. Changes in the basic properties of amylopectin (AMP) and its compatibility with asphalt after microencapsulation were studied. Then, the flame retarding efficiency and improvement effects of MAMP on the flame retardancy of asphalt were investigated. Results show that melamine formaldehyde (MF) resin is evenly coated on the AMP surface without changing the chemical composition of AMP, increasing the thermal stability of AMP and the compatibility between AMP and asphalt. MAMP reacts with ammonium polyphosphate (APP) to release a number of incombustible gases to delay asphalt combustion at early stages and subsequently dehydrates to form a stable starch-based charring layer to suppress heat and mass transfer during asphalt combustion, improving the fire safety of asphalt materials. The added 3% MAMP can reduce the total enthalpy value of all exothermic peaks of the 10% APP-modified asphalt by 43.6%. As a carbonization agent, MAMP produces a charring layer with higher heat capacity during asphalt combustion, exerting an excellent inhibition effect on heat release. This study provides a reference for the application of biobased materials in flame-retarded asphalt pavements.