Delving into the Latest Updates on 青岛利福特生物医学研究所 with Synapse

概览

疾病领域	数量

肿瘤	1

排名前五的药物类型	数量

小分子化药	2

排名前五的靶点	数量

Tubulin(微管蛋白)	1

关联

3

项与青岛利福特生物医学研究所相关的药物

BG-136

靶点-

作用机制-

在研机构

青岛利福特生物医学研究所 [+3]

原研机构

青岛利福特生物医学研究所

在研适应症

晚期恶性实体瘤 [+1]

非在研适应症-

最高研发阶段临床1期

首次获批国家/地区-

首次获批日期-

Deuterated Plinabulin (Marine Biomedical Research Institute of Qingdao)

靶点

Tubulin

作用机制

微管蛋白抑制剂

在研机构

青岛利福特生物医学研究所

原研机构

青岛利福特生物医学研究所

在研适应症

肿瘤

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-

MBRI-003

靶点-

作用机制-

在研机构

青岛利福特生物医学研究所

原研机构

青岛利福特生物医学研究所

在研适应症

炎症性肠病

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-

100 项与青岛利福特生物医学研究所相关的临床结果

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0 项与青岛利福特生物医学研究所相关的专利（医药）

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140

项与青岛利福特生物医学研究所相关的文献（医药）

2024-12-01·European Journal of Medicinal Chemistry

Discovery of novel nitrofuran PROTAC-like compounds as dual inhibitors and degraders targeting STING

Article

作者: Xue, Liang ; Liu, Lu ; Jiang, Tao ; Qiu, Tingting ; Yin, Ruijuan ; Liu, Ruixue ; Zhang, Lican

Aberrant activation of the innate immune molecule STING can initiate inflammation and autoimmune diseases. Small molecule inhibitors targeting STING have demonstrated therapeutic efficacy against these conditions. Moreover, employing degradants to target STING represents a novel approach to drug design strategy. Consequently, we have designed and synthesized a series of covalent degradants targeting STING. Among them, compound P8 exhibited the highest degradation capacity, with a 24-h DC₅₀ of 2.58 μM in THP-1 cells. In THP-1 cells, P8 specifically degraded STING proteins through the lysosomal pathway, acting as dual a degrader and inhibitor to manifest anti-inflammatory effects. Conversely, in RAW264.7 cells, P8 solely acted as an inhibitor without exhibiting degradative capacity towards the STING protein level. Additionally, P8 displayed renal-protective properties in a cisplatin-induced acute kidney injury model. These results highlight the significant potential of further investigating compound P8.

2024-11-01·Bioorganic & Medicinal Chemistry

Design, synthesis and biological evaluation of novel diphenylamine analogues as NLRP3 inflammasome inhibitors

Article

作者: Wang, Huimin ; Liu, Jinyu ; Jiang, Yuqi ; Kang, Tongtong ; Li, Xiaoyang ; Sun, Simin

The aberrant activation of the NLRP3 inflammasome has been implicated in the pathogenesis of numerous inflammation-related diseases. Development of NLRP3 inflammasome inhibitors is expected to provide a new strategy for the treatment of these diseases. Herein, a novel series of diphenylamine derivatives were designed based on the lead compounds H20 and H28, and the preliminary structure-activity relationship was studied. The representative compound 19 displayed significantly higher inhibitory activity against NLRP3 inflammasome compared to lead compounds H20 and H28, with an IC₅₀ of 0.34 μM. Mechanistic studies indicated that compound 19 directly targets the NLRP3 protein (K_D: 0.45 μM), blocking the assembly and activation of the NLRP3 inflammasome, leading to anti-inflammatory effects and inhibition of cellular pyroptosis. Our findings indicated that compound 19 is a promising NLRP3 inhibitor and could potentially serve as a lead compound for further optimization.

2024-11-01·International Journal of Biological Macromolecules

Propylene glycol alginate sodium sulfate suppressed lung metastasis by blocking P-selectin to recruit CD4 regulatory T cells

Article

作者: Zhang, Lei ; Qiu, Peiju ; Ma, He ; Cai, Kaiyu ; Li, Chunxia ; Yang, Jinbo ; Bi, Shijie ; Li, Yannan ; Wu, Lijuan ; Xu, Huixin ; Guan, Huashi

P-selectin has been shown to enhance growth and metastasis of mouse tumors by promoting regulatory T cell (Treg) infiltration into the tumors. Theoretically, a P-selectin antagonist could suppress the process. Popylene glycol alginate sodium sulfate (PSS) is a heparin-like marine drug, which was originally approved to treat cardiovascular disease in China. Previously, we reported that PSS was an effective P-selectin antagonist in vitro. However, it is unknown whether PSS can regulate Treg infiltration and its effect on lung metastasis in vivo. Our results showed that PSS at 30 mg/kg significantly suppressed lung metastasis and improved overall survival, with potency comparable to the positive control LMWH. Mechanistic study indicated that PSS blocked tumor cells adhesion and activated platelets by directly binding with activated platelet's P-selectin. Compared to the model group, PSS decreased the percent of Tregs by 63 % in lungs after treating for 21 days while increasing CD8+ T cells (1.59-fold) and Granzyme B+ CD8 T cells (2.08-fold)' percentage for generating an adaptive response for systemic tumor suppression. The study indicated that the P-selectin antagonist, PSS, suppressed lung metastasis by inhibiting the infiltration of regulatory T cells (Treg) into the tumors.

100 项与青岛利福特生物医学研究所相关的药物交易

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100 项与青岛利福特生物医学研究所相关的转化医学

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管线布局

2024年11月05日管线快照

管线布局中药物为当前组织机构及其子机构作为药物机构进行统计，早期临床1期并入临床1期，临床1/2期并入临床2期，临床2/3期并入临床3期

临床前

2

1

临床申请批准

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当前项目

药物(靶点)	适应症	全球最高研发状态

BG-136	实体瘤更多	临床申请批准
MBRI-003	炎症性肠病更多	临床前
Deuterated Plinabulin (Marine Biomedical Research Institute of Qingdao) ( Tubulin )	肿瘤更多	临床前