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更新于：2025-05-07

NPC-15199

更新于：2025-05-07

概要

概要

基本信息

药物类型

小分子化药

别名

靶点-

作用方式-

作用机制

免疫抑制剂

治疗领域

心血管疾病免疫系统疾病消化系统疾病+ [2]

在研适应症-

非在研适应症

动脉粥样硬化溃疡性结肠炎变应性接触性皮炎+ [2]

原研机构

Scios, Inc.

在研机构-

非在研机构

Scios, Inc.Scios Pharma

权益机构-

最高研发阶段终止临床2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/序列

分子式C21H23NO4

InChIKeyCBPJQFCAFFNICX-IBGZPJMESA-N

CAS号35661-60-0

关联

100 项与 NPC-15199 相关的临床结果

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100 项与 NPC-15199 相关的转化医学

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100 项与 NPC-15199 相关的专利（医药）

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8,303

项与 NPC-15199 相关的文献（医药）

2025-07-01·Colloids and Surfaces B: Biointerfaces

Synergistic effects of hydrophilic residues in the transmembrane region on lipid scrambling activity of dimeric helices

Article

作者: Nakao, Hiroyuki ; Saito, Hiroaki ; Ikeda, Keisuke ; Nakano, Minoru ; Tsujii, Toshiki

Phospholipid scramblases promote lipid transbilayer movement (flip-flop) in the plasma membrane, which is involved in a wide range of cellular functions, such as phagocytosis and blood coagulation. One structural characteristic of scramblases and model lipid scrambling peptides is the presence of hydrophilic residues in their transmembrane domains. These hydrophilic regions are considered the active sites through which lipid polar headgroups pass during the translocation process. However, how the structural arrangement of hydrophilic residues results in strong lipid scrambling activities in scramblases needs to be investigated, because the effects of a single hydrophilic residue on lipid scrambling are much lower than the activity of natural scramblases. Here, we developed double-spanning transmembrane peptides containing varying numbers of Gln residues. A combination of lipid vesicle experiments and molecular dynamics simulations indicates that lipid scrambling activities are synergistically enhanced by the proximity between planes created by Gln residues aligned parallel to the helix and that interactions between Gln and Trp residues stabilize the strongly active structures. The contribution of Gln residues to lipid scrambling activity suggests that the alignment and proximity of hydrophilic residues in the transmembrane region is one of the mechanisms of lipid scrambling by natural scramblases. This study provides clues for the energetic and structural mechanisms of lipid scrambling and for the design of artificial phospholipid scramblases.

2025-06-05·Journal of Applied Polymer Science

Synthesis and Characterization of Polymer‐Drug Conjugates by Strain‐Promoted Azide‐Alkyne Cycloaddition‐Mediated Polymerization

作者: Adesina, Simeon K. ; Gbadegesin, Omotola D.

ABSTRACTPolymer‐drug conjugates (PDCs) modify the biodistribution of small‐molecule anticancer agents to prevent undesired off‐target adverse effects. Here, we report the preparation of two PDCs by strain‐promoted [3 + 2] azide‐alkyne cycloaddition‐mediated step‐growth polymerization. This method does not require the use of a catalyst or high temperatures, and it allows the rapid synthesis of high molecular‐weight PDCs containing gemcitabine (Mw ~ 40.18 kDa) and doxorubicin (Mw ~ 1800 kDa) with narrow molecular weight distribution and high drug loading (29.2 wt% gemcitabine and 10.3wt% doxorubicin). α‐ω‐bis‐azide‐terminated bifunctional gemcitabine‐coupled and doxorubicin‐coupled monomers, with drug linkage via Gly‐Phe‐Leu‐Gly (GFLG), a cathepsin B‐sensitive peptide linker, were separately synthesized and polymerized using a dibenzoazacyclooctyne bifunctional polyethylene glycol monomer. Preliminary in vitro evaluations of the PDCs showed cathepsin B‐catalyzed drug release at pH 5.0. The applied method for the syntheses of the PDCs enables the selective delivery of potent anticancer agents.

2025-05-01·European Journal of Medicinal Chemistry

The discovery of novel antimicrobial peptides against drug-resistant bacteria based on fragments fusion strategy

Article

作者: Tian, Long ; Meng, Qingbin ; Chen, Longming ; Ye, Weifeng ; Xu, Yijie ; Han, Jiaqi ; Wang, Taoran ; Ning, Ziyao ; Meng, Zhao ; Zeng, Chunlan ; Jing, Jie

Since the escalating prevalence of multidrug-resistant (MDR) bacterial infections posing global health challenges, novel antimicrobial agents are urgently needed. This study designed a series of antimicrobial peptides by fusing two fragments of antimicrobial peptides sC18_4b (1-9) and MSI-78 (10-16). Among these peptides, 13DK_allDab exhibited broad-spectrum antimicrobial efficacy against six different MDR bacterial strains with relatively low MICs. It exerted antibacterial effects through a membrane-disruption mechanism and maintained high stability in serum environment. Moreover, 13DK_allDab displayed low cytotoxicity and hemolysis in vitro, and significant therapeutic efficacy in a mouse acute peritonitis model. These findings demonstrate that 13DK_allDab is a promising antimicrobial agent in counteracting multidrug-resistant bacterial infections.

100 项与 NPC-15199 相关的药物交易

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研发状态

10 条进展最快的记录,

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适应症	最高研发状态	国家/地区	公司	日期
动脉粥样硬化	临床2期	-	Scios Pharma	-
动脉粥样硬化	临床2期	美国	Scios, Inc.	-
动脉粥样硬化	临床2期	-	Scios Pharma	-
动脉粥样硬化	临床2期	美国	Scios, Inc.	-
溃疡性结肠炎	临床2期	美国	Scios, Inc.	-
变应性接触性皮炎	临床2期	美国	Scios, Inc.	-
再灌注损伤	临床2期	美国	Scios, Inc.	-
类风湿关节炎	临床2期	美国	Scios, Inc.	-