Abstract
Anthrax Lethal Factor (LF) is a zinc-dependent metalloprotease, one of the virulence factor of anthrax infection. Three forms of the anthrax infection have been identified: cutaneous (through skin), gastrointestinal (through alimentary tract), and pulmonary (by inhalation of spores). Anthrax toxin is composed of protective antigen (PA), lethal factor (LF), and edema factor (EF). Protective antigen mediates the entry of Lethal Factor/Edema Factor into the cytosol of host cells. Lethal factor (LF) inactivates mitogen-activated protein kinase kinase inducing cell death, and EF is an adenylyl cyclase impairing host defenses. In the past few years, extensive studies are undertaken to design inhibitors targeting LF. The current review focuses on the small molecule inhibitors targeting LF activity and its structure activity relationships (SAR).
Keywords: Anthrax, bacillus anthracis, lethal factor, LF inhibitor, metalloprotease.
Current Topics in Medicinal Chemistry
Title:Anthrax Lethal Factor Inhibitors as Potential Countermeasure of the Infection
Volume: 14 Issue: 17
Author(s): B.V.S. Suneel Kumar, Siddharth Malik, Pradeep Grandhi, Raveendra Dayam and J.A.R.P. Sarma
Affiliation:
Keywords: Anthrax, bacillus anthracis, lethal factor, LF inhibitor, metalloprotease.
Abstract: Anthrax Lethal Factor (LF) is a zinc-dependent metalloprotease, one of the virulence factor of anthrax infection. Three forms of the anthrax infection have been identified: cutaneous (through skin), gastrointestinal (through alimentary tract), and pulmonary (by inhalation of spores). Anthrax toxin is composed of protective antigen (PA), lethal factor (LF), and edema factor (EF). Protective antigen mediates the entry of Lethal Factor/Edema Factor into the cytosol of host cells. Lethal factor (LF) inactivates mitogen-activated protein kinase kinase inducing cell death, and EF is an adenylyl cyclase impairing host defenses. In the past few years, extensive studies are undertaken to design inhibitors targeting LF. The current review focuses on the small molecule inhibitors targeting LF activity and its structure activity relationships (SAR).
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Cite this article as:
Kumar Suneel B.V.S., Malik Siddharth, Grandhi Pradeep, Dayam Raveendra and Sarma J.A.R.P., Anthrax Lethal Factor Inhibitors as Potential Countermeasure of the Infection, Current Topics in Medicinal Chemistry 2014; 14 (17) . https://dx.doi.org/10.2174/1568026614666140929120231
DOI https://dx.doi.org/10.2174/1568026614666140929120231 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
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