BRD-7929(BRD-7929) - 药物靶点：FARSA_专利_临床

概要

基本信息

药物类型

化学药

别名

靶点

FARSA

作用机制

FARSA调节剂(phenylalanyl-tRNA synthetase subunit alpha modulators)

治疗领域

感染消化系统疾病

在研适应症-

非在研适应症

隐孢子虫病

原研机构

卫材（中国）药业有限公司

The Broad Institute, Inc.

University of Illinois At UrbanaChampaign

+ [2]

在研机构-

非在研机构

卫材（中国）药业有限公司

The Broad Institute, Inc.

University of Illinois At UrbanaChampaign

+ [2]

最高研发阶段无进展临床前

首次获批日期-

最高研发阶段(中国)无进展

特殊审评-

关联

100 项与 BRD-7929 相关的临床结果

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100 项与 BRD-7929 相关的转化医学

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100 项与 BRD-7929 相关的专利（医药）

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2

项与 BRD-7929 相关的文献（医药）

2022-07-01·Structure2区 · 生物学

Inhibition of Plasmodium falciparum phenylalanine tRNA synthetase provides opportunity for antimalarial drug development

2区 · 生物学

Article

作者: Tabassum, Heena ; Schreiber, Stuart L ; Sharma, Amit ; Harlos, Karl ; Manickam, Yogavel ; Comer, Eamon ; Parvez, Suhel ; Sharma, Manmohan ; Mutharasappan, Nachiappan ; Melillo, Bruno

Bicyclic azetidine compounds possess antimalarial activity via targeting of the cytoplasmic Plasmodium falciparum (Pf) protein translation enzyme phenylalanine-tRNA synthetase (cFRS). These drugs kill parasites both in vitro and in vivo, including the blood, liver, and transmission developmental stages. Here we present the co-crystal structure of PfcFRS with a potent inhibitor, the bicyclic azetidine BRD7929. Our studies reveal high-affinity binding of BRD7929 with PfcFRS along with exquisite specificity compared with the human enzyme, leading in turn to potent and selective inhibition of the parasite enzyme. Our co-crystal structure shows that BRD7929 binds in the active site in the α subunit of PfcFRS, where it occupies the amino acid site, an auxiliary site, and partially the ATP site. This structural snapshot of inhibitor-bound PfcFRS thus provides a platform for the structure-guided optimization of novel antimalarial compounds.

2016-11-01·Nature Reviews Drug Discovery

Novel antimalarial target identified

Article

作者: Crunkhorn, Sarah

This short article discusses the identification of a bicyclic azetidine BRD7929 which prevented disease transmission, ensured prophylaxis and displayed single low-dose cure, with activity against all Plasmodium parasite life stages.

100 项与 BRD-7929 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
隐孢子虫病	临床前	美国	The Broad Institute, Inc.	2020-09-30
隐孢子虫病	临床前	荷兰	TropIQ Health Sciences BV	2020-09-30
隐孢子虫病	临床前	美国	University of Illinois At UrbanaChampaign	2020-09-30
隐孢子虫病	临床前	中国	无锡药明康德新药开发股份有限公司	2020-09-30
隐孢子虫病	临床前	中国	卫材（中国）药业有限公司	2020-09-30