Inhibition of Glutamine Synthetase: A Potential Drug Target in Mycobacterium tuberculosis

被引：50

作者：

Mowbray, Sherry L. ^{[1
]}

Kathiravan, Muthu K. ^{[2
]}

Pandey, Abhishek A. ^{[3
]}

Odell, Luke R. ^{[4
]}

机构：

[1] Uppsala Univ, Sci Life Lab, Dept Cell & Mol Biol, Biomed Ctr, SE-75124 Uppsala, Sweden

[2] Seven Hills Coll Pharm, Tirupati 517561, Andhra Pradesh, India

[3] Sinhgad Coll Pharm, Dept Pharmaceut Chem, Pune 411041, Maharashtra, India

[4] Uppsala Univ, Dept Med Chem, Biomed Ctr, SE-75123 Uppsala, Sweden

来源：

MOLECULES | 2014年 / 19卷 / 09期

关键词：

tuberculosis; glutamine synthetase; drug discovery; structure-activity relationship; Mycobacterium tuberculosis; GAMMA-SUBSTITUTED PHOSPHINOTHRICINS; METHIONINE SULFOXIMINE; MECHANISM; DERIVATIVES; ANALOGS; DESIGN; ACID; ENZYME; EXPRESSION; RESISTANT;

D O I：

10.3390/molecules190913161

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Tuberculosis is an infectious disease caused by Mycobacterium tuberculosis. Globally, tuberculosis is second only to AIDS in mortality and the disease is responsible for over 1.3 million deaths each year. The impractically long treatment schedules (generally 6-9 months) and unpleasant side effects of the current drugs often lead to poor patient compliance, which in turn has resulted in the emergence of multi-, extensively-and totally-drug resistant strains. The development of new classes of anti-tuberculosis drugs and new drug targets is of global importance, since attacking the bacterium using multiple strategies provides the best means to prevent resistance. This review presents an overview of the various strategies and compounds utilized to inhibit glutamine synthetase, a promising target for the development of drugs for TB therapy.

引用

页码：13161 / 13176

页数：16

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