更新于：2024-11-01

Shikimate激酶

更新于：2024-11-01

基本信息

别名-

简介-

关联

项与 Shikimate激酶相关的药物

Shikimate kinase inhibitors 3i(University of Santiago de Compostela)

靶点

Shikimate激酶

作用机制

Shikimate激酶抑制剂

在研机构

University of Santiago de Compostela

原研机构

University of Santiago de Compostela

在研适应症

幽门螺杆菌感染

非在研适应症-

最高研发阶段药物发现

首次获批国家/地区-

首次获批日期1800-01-20

Shikimate kinase inhibitors 3e(University of Santiago de Compostela)

靶点

Shikimate激酶

作用机制

Shikimate激酶抑制剂

在研机构

University of Santiago de Compostela

原研机构

University of Santiago de Compostela

在研适应症

幽门螺杆菌感染

非在研适应症-

最高研发阶段药物发现

首次获批国家/地区-

首次获批日期1800-01-20

AA-002

靶点

Shikimate激酶

作用机制

Shikimate激酶抑制剂

在研机构-

原研机构

A2a Pharmaceuticals, Inc.初创企业

在研适应症-

非在研适应症

革兰氏阴性菌感染

最高研发阶段无进展

首次获批国家/地区-

首次获批日期1800-01-20

100 项与 Shikimate激酶相关的临床结果

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100 项与 Shikimate激酶相关的转化医学

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0 项与 Shikimate激酶相关的专利（医药）

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380

项与 Shikimate激酶相关的文献（医药）

2025-01-01·Food Chemistry

Preharvest methyl jasmonate application delays cell wall degradation and upregulates phenolic metabolism and antioxidant activities in cold stored raspberries

Article

作者: Woodward, Andrew ; Afrifa-Yamoah, Eben ; Hasan, Mahmood Ul ; Shah, Hafiz Muhammad Shoaib ; Singh, Zora

The effects of preharvest methyl jasmonate (MeJA) spray application on the physicochemical quality, metabolism of phenolics, and cell wall components in raspberries were investigated during a 10-day cold storage period. MeJA spray reduced firmness loss, decay incidence, and weight loss, while maintained higher levels of soluble solids content, ascorbic acid, anthocyanins and flavonoids in raspberries. Furthermore, MeJA application resulted in increased total pectin and protopectin levels, as well as lowered water-soluble pectin, and activities of pectin methyl esterase, polygalacturonase and cellulase enzymes. Additionally, MeJA treatment upregulated the phenylpropanoid pathway, leading to higher endogenous phenolics and activities of phenylalanine-ammonia lyase and shikimate dehydrogenase. In conclusion, preharvest MeJA spray application could be adopted to enhance the storage potential of cold-stored raspberries for 10 days by maintaining higher firmness, assuring better physicochemical quality, and increasing phenolic metabolism, while reducing cell wall hydrolysis.

2024-12-31·Journal of Enzyme Inhibition and Medicinal Chemistry

Identification of potential inhibitors against Staphylococcus aureus shikimate dehydrogenase through virtual screening and susceptibility test

Article

作者: Deng, Qi ; Zhu, Mengfan ; Qu, Jinfeng

Staphylococcus aureus shikimate dehydrogenase (SaSDH) plays a crucial role in the growth of Staphylococcus aureus (S. aureus), but absent in mammals and therefore a potential target for antibacterial drugs to treat drug-resistant S. aureus infection. In this study, a 3D model of SaSDH was constructed by homology modelling and inhibitors of SaSDH were screened through virtual screening. (-)-Gallocatechin gallate and rhodiosin were identified as inhibitors with K_is of 2.47 μM and 73.38 μM, respectively. Molecular docking and isothermal titration calorimetry showed that both inhibitors interact with SaSDH with a K_D of 44.65 μM for (-)-gallocatechin gallate and 16.45 μM for rhodiosin. Both inhibitors had antibacterial activity, showing MICs of 50 μg/mL for (-)-gallocatechin gallate and 250 μg/mL for rhodiosin against S. aureus. The current findings have the potential for identification of drugs to treat S. aureus infections by targeting SaSDH.

2024-11-01·Planta

Histochemical and molecular analyses reveal an insight into the scent volatiles synthesis and emission in ephemeral flowers of Murraya paniculata (L.) Jack

Article

作者: Datta, Sinjini ; Ballabh, Lopamudra ; Paul, Shobhon ; Mitra, Adinpunya

MAIN CONCLUSIONTemporal histolocalization of floral volatiles in the petal epidermis of Murraya paniculata was found to be linked with the coordinated expression of candidate genes and successive accumulation of an internal pool of volatiles. Murraya paniculata (Rutaceae) is known for its highly fragrant ephemeral flowers that emit volatiles to attract nocturnal pollinators. To unfold the patterns of volatile emission in relation to floral life-span, we studied time-course accumulation and emission rate of scent volatiles at six timepoints of floral maturation, at an interval of 4 h starting from the bud stage to the senescence stage on the next day. This study revealed the maximum emission rate of scent volatiles at the anthesis stage at 18:00 h. This finding correlates well with the maximum accumulation of volatiles in the internal pool of the flowers at this stage. The key volatiles detected in both emitted and internal pools were benzaldehyde, benzeneacetaldehyde, linalool, caryophyllene, germacrene-D and α-farnesene. In addition, the internal pool also contained substantial amounts of indole, scopoletin, caffeine and osthole. To histochemically localize the temporal accumulation of major volatile groups in the epidermal cells, petal cross sections were stained with NaDi and ferric chloride to visualize terpenes and phenolics, respectively, under light microscope. Histolocalization studies showed a higher accumulation of terpenes at 14:00 h and 18:00 h, which subsequently was reduced as senescence approached. Significant phenolics in the abaxial and adaxial layers of the petal epidermis accumulated at 18:00 h and at the early senescence (06:00 h) stages. Furthermore, temporal localization of active shikimate dehydrogenase (SKDH) protein through in-gel activity assay demonstrated higher enzymatic activities at anthesis (18:00 h) and fully bloomed (02:00 h) stages, supporting the findings of higher accumulation of phenolic volatiles at 18:00 h and 06:00 h stages. Expression analysis of major candidate genes of floral scent volatiles pathway supported the hypothesis that the emission rate of floral fragrance reached its maximum at the anthesis (18:00 h) stage. In contrast, biosynthesis of scent compounds started at the bud (14:00 h) stage itself as indicated by the RT-PCR semi-quantitative estimation. As flowers of M. paniculata attract multiple pollinator species, this study could also serve as a springboard for pollination biology in Rutaceae, which includes important fruit crops.