更新于：2024-11-01

Nal-Glu

更新于：2024-11-01

概要

研发状态

概要

基本信息

药物类型

化学药

别名-

靶点

GnRHR

作用机制

GnRHR拮抗剂(促性腺激素释放激素受体拮抗剂)

治疗领域-

在研适应症-

非在研适应症-

原研机构

The Salk Institute for Biological Studies

在研机构-

非在研机构

The Salk Institute for Biological Studies

最高研发阶段终止临床1期

首次获批日期-

最高研发阶段(中国)-

特殊审评-

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结构

分子式C73H97ClN18O14

InChIKeyUFOMLGCSEHLELA-YKJOSNDESA-N

CAS号103733-02-4

序列信息

Sequence Code 530309436

关联

100 项与 Nal-Glu 相关的临床结果

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100 项与 Nal-Glu 相关的转化医学

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100 项与 Nal-Glu 相关的专利（医药）

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134

项与 Nal-Glu 相关的文献（医药）

2024-10-01·Food Chemistry

Enhancing bread anti-staling with glucose-derived Maillard reaction products: In-depth analysis of starches, gluten networks, and moisture status

Article

作者: Liu, Shuyun ; Nagassa, Merga ; Pei, Hui ; He, Xinzhou ; Sun, Hanju ; Gao, Lingyan ; He, Shudong ; Li, Xiao

In this study, six types of amino acids (Ala, Phe, Glu, Gly, Ser, and Lys) were combined with glucose to produce Maillard reaction products (MRPs) named G-Ala, G-Phe, G-Glu, G-Gly, G-Ser and G-Lys. The effect of MRPs on bread staling was evaluated through texture and sensory analyses during storage. Furthermore, the study comprehensively analyzed the anti-staling mechanisms of MRPs by examining moisture content, starches, and gluten network changes. The results indicated that G-Gly and G-Glu delayed bread staling, with G-Gly showing the most significant effect. Compared with control, the staling rate and starch crystallinity of G-Gly bread decreased by 24.07% and 7.70%, respectively. Moreover, G-Gly increased the moisture content (3.48%), weakly bound water mobility (0.77%), and α-helix content (1.00%) of bread. Component identification and partial least squares regression further confirmed the aldonic acid, heterocyclic acids and heterocyclic ketones in MRPs inhibit water evaporation, gluten network loosening, and starch degradation, thereby delaying bread staling.

2023-12-01·Journal of Controlled Release

Supramolecular nanofiber of indomethacin derivative confers highly cyclooxygenase-2 (COX-2) selectivity and boosts anti-inflammatory efficacy

Article

作者: Li, Xingyi ; Deng, Jie ; Chen, Jinrun ; Xu, Xiaoning ; Deng, Mengyun ; Lei, Lei ; Wang, Jiaqing ; Chen, Lei ; Ren, Zhibin ; Lin, Deqing ; Chen, Lin

Herein, we report a facile method for converting carboxylate-containing indomethacin (Idm) into a cyclooxygenase-2 (COX-2) selective inhibitor via the amidation of an unnatural peptide sequence (Nal-Nal-Asp). The resulting indomethacin amides (i.e., Idm-Nal-Nal-Asp) have high selectivity for COX-2, and can self-assemble into a one-component supramolecular hydrogel that acts as a 'self-delivery' system for boosting anti-inflammatory efficacy. Self-assembled Idm-Nal-Nal-Asp hydrogel robustly inhibits COX-2 expression in lipopolysaccharide (LPS)-activated Raw 264.7 macrophages while also exhibits superior anti-inflammatory and antioxidant activities via reactive oxygen species (ROS)-related NF-κB and Nrf2/HO-1 pathways. Moreover, a rabbit model of endotoxin-induced uveitis (EIU) reveals that the Idm-Nal-Nal-Asp hydrogel outperforms clinically used 0.1 wt% diclofenac sodium eye drops in terms of in vivo anti-inflammatory efficacy via topical instillation route. As a rational approach to designing and applying COX-2 selective inhibitors, this work presents a simple method for converting non-selective nonsteriodal anti-inflammatory drugs (NSAIDs) into highly selective COX-2 inhibitors that can self-assemble into supramolecular hydrogel for anti-inflammation applications.

2023-12-01·Bioorganic Chemistry

γ-Glutamyltranspeptidase-Activated Near-Infrared fluorescent probe for visualization of Drug-Induced liver injury

Article

作者: Luo, Jianguang ; Zhu, Jiangmin ; Zhu, Dongrong ; Li, Yalin ; Liu, Feiyan ; Kong, Lingyi ; Li, Yin

Drug-induced liver injury (DILI), induced by overdose or chronic administration of drugs, has become the leading cause of acute liver failure. Therefore, an accurate diagnostic method for DILI is critical to improve treatment efficiency. The production of γ-glutamyltranspeptidase (GGT) is closely related to the progression of drug-induced hepatotoxicity. KL-Glu exhibits a prominent GGT-activated NIR fluorescence (734 nm) with a large Stokes shift (137 nm) and good sensitivity/selectivity, making it favorable for real-time detection of endogenous GGT activity. Using this probe, we evaluated the GGT up-regulation under the acetaminophen-induced liver injury model. Moreover, KL-Glu was successfully used to assess liver injury induced by the natural active ingredient triptolide and the effective amelioration upon treatment with N-acetyl cysteine (NAC) or Glutathione (GSH) in cells and in vivo by fluorescent trapping the fluctuation of GGT for the first time. Therefore, the fluorescent probe KL-Glu can be used as a potential tool to explore the function of GGT in the progression of DILI and for the early diagnosis and prognostic evaluation of DILI.

100 项与 Nal-Glu 相关的药物交易

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