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更新于：2025-05-07

WF-11605

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

LTRs

作用方式

拮抗剂

作用机制

LTRs拮抗剂(白三烯受体家族拮抗剂)

治疗领域-

在研适应症-

非在研适应症-

原研机构

Astellas Pharma, Inc.

在研机构-

非在研机构

Astellas Pharma, Inc.

权益机构-

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/序列

分子式C38H60O11

InChIKeyFBAPXRMZLULGNA-TVJNVOSNSA-N

CAS号127475-47-2

关联

100 项与 WF-11605 相关的临床结果

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100 项与 WF-11605 相关的转化医学

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100 项与 WF-11605 相关的专利（医药）

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项与 WF-11605 相关的文献（医药）

2024-05-08·Journal of the American Chemical Society

Biosynthesis of Enfumafungin-type Antibiotic Reveals an Unusual Enzymatic Fusion Pattern and Unprecedented C–C Bond Cleavage

Article

作者: Luo, Rui ; Yao, Xin-Sheng ; Chen, Guo-Dong ; Gao, Yao-Hui ; Hu, Dan ; Gao, Hao ; Bao, Xue-Feng ; Cao, Zhi-Qin ; Awakawa, Takayoshi ; Lv, Jian-Ming ; Mei, Qing-Hua ; Wang, Gao-Qian ; Qin, Sheng-Ying ; Abe, Ikuro

Enfumafungin-type antibiotics, represented by enfumafungin and fuscoatroside, belong to a distinct group of triterpenoids derived from fungi. These compounds exhibit significant antifungal properties with ibrexafungerp, a semisynthetic derivative of enfumafungin, recently gaining FDA's approval as the first oral antifungal drug for treating invasive vulvar candidiasis. Enfumafungin-type antibiotics possess a cleaved E-ring with an oxidized carboxyl group and a reduced methyl group at the break site, suggesting unprecedented C-C bond cleavage chemistry involved in their biosynthesis. Here, we show that a 4-gene (fsoA, fsoD, fsoE, fsoF) biosynthetic gene cluster is sufficient to yield fuscoatroside by heterologous expression in Aspergillus oryzae. Notably, FsoA is an unheard-of terpene cyclase-glycosyltransferase fusion enzyme, affording a triterpene glycoside product that relies on enzymatic fusion. FsoE is a P450 enzyme that catalyzes successive oxidation reactions at C19 to facilitate a C-C bond cleavage, producing an oxidized carboxyl group and a reduced methyl group that have never been observed in known P450 enzymes. Our study thus sets the important foundation for the manufacture of enfumafungin-type antibiotics using biosynthetic approaches.

2015-12-01·Tetrahedron

Bioactive oxygen-bridged cyclooctadienes from endophytic fungus Phomopsis sp. BCC 45011

作者: Chawanee Thongpanchang ; Wiwat Somyong ; Jittra Kornsakulkarn ; Nattawut Boonyuen ; Sumalee Supothina

Three new oxygen-bridged cyclooctadiene containing compounds, phomoxydienes A-C, and two new dothiorelones I and J, together with 10 known compounds were isolated from endophytic fungus, Phomopsis sp. BCC 45011.Structures were determined by NMR spectroscopic and MS spectrometric analyses.Mycoepoxydiene, deacetylmycoepoxydiene, phomoxydienes A and C, and cytosporone E displayed antimalarial and cytotoxic activities while 1893 A and cytosporone P showed only cytotoxic and antimalarial activity, resp.

1992-01-01·The Journal of Antibiotics4区 · 医学

WF11605, an antagonist of leukotriene B4 produced by a fungus. II. Structure determination.

4区 · 医学

Article

作者: Takase, Shigehiro ; Kayakiri, Natsuko ; Shigematsu, Nobuharu ; Tanaka, Hirokazu ; Tsujii, Eisaku

The structure of WF11605, a novel tetracyclic triterpene glucoside, was determined to be 1. The plane structure of deacetyl-WF11605 aglycone was elucidated as 2 through the concerted application of a series of 2D NMR techniques. The relative configurations were established by X-ray crystallographic analysis of bis(p-bromobenzoyl) derivative 3 and absolute stereochemistry by CD exciton chirality method.

100 项与 WF-11605 相关的药物交易

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