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Current Topics in Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 1568-0266
ISSN (Online): 1873-4294

Anthrax Lethal Factor Inhibitors as Potential Countermeasure of the Infection

Author(s): B.V.S. Suneel Kumar, Siddharth Malik, Pradeep Grandhi, Raveendra Dayam and J.A.R.P. Sarma

Volume 14, Issue 17, 2014

Page: [1977 - 1989] Pages: 13

DOI: 10.2174/1568026614666140929120231

Price: $65

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.

Graphical Abstract


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