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).
Export Options
About this article
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 |
Call for Papers in Thematic Issues
AlphaFold in Medicinal Chemistry: Opportunities and Challenges
AlphaFold, a groundbreaking AI tool for protein structure prediction, is revolutionizing drug discovery. Its near-atomic accuracy unlocks new avenues for designing targeted drugs and performing efficient virtual screening. However, AlphaFold's static predictions lack the dynamic nature of proteins, crucial for understanding drug action. This is especially true for multi-domain proteins, ...read more
Artificial intelligence for Natural Products Discovery and Development
Our approach involves using computational methods to predict the potential therapeutic benefits of natural products by considering factors such as drug structure, targets, and interactions. We also employ multitarget analysis to understand the role of drug targets in disease pathways. We advocate for the use of artificial intelligence in predicting ...read more
Chemistry Based on Natural Products for Therapeutic Purposes
The development of new pharmaceuticals for a wide range of medical conditions has long relied on the identification of promising natural products (NPs). There are over sixty percent of cancer, infectious illness, and CNS disease medications that include an NP pharmacophore, according to the Food and Drug Administration. Since NP ...read more
Current Trends in Drug Discovery Based on Artificial Intelligence and Computer-Aided Drug Design
Drug development discovery has faced several challenges over the years. In fact, the evolution of classical approaches to modern methods using computational methods, or Computer-Aided Drug Design (CADD), has shown promising and essential results in any drug discovery campaign. Among these methods, molecular docking is one of the most notable ...read more
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
- Announcements
Related Articles
-
Recent Development of Functionalized N-heterocyclic Carbene Ligands:Coordination Chemistry and Catalytic Applications
Current Organic Chemistry Synthesis and Biological Activity of Chiral Dihydropyrazole: Potential Lead for Drug Design
Mini-Reviews in Medicinal Chemistry The Course of COVID-19 in Four Patients with HIV During the Pandemic
Current HIV Research Improving Brain MR Image Classification for Tumor Segmentation using Phase Congruency
Current Medical Imaging A Further Step Toward an Optimal Ensemble of Classifiers for Peptide Classification, a Case Study: HIV Protease
Protein & Peptide Letters COVID-19 Outbreak and Emerging Management through Pharmaceutical Therapeutic Strategy
Current Pharmaceutical Design Going 3D – Cell Culture Approaches for Stem Cell Research and Therapy
Current Tissue Engineering (Discontinued) Classes of Sigma2 (σ2) Receptor Ligands: Structure Affinity Relationship (SAfiR) Studies and Antiproliferative Activity
Current Pharmaceutical Design Withdrawal Notice: Mucoadhesive Microspheres: An Emerging Trends in Therapy of Diabetes Mellitus
Current Diabetes Reviews Impact of Metaheuristic Techniques in Pandemic of COVID-19
Coronaviruses Novel Triazolyl Berberine Derivatives Prepared via CuAAC Click Chemistry: Synthesis, Anticancer Activity and Structure-Activity Relationships
Anti-Cancer Agents in Medicinal Chemistry Hydroxamic Acids, Recent Breakthroughs in Stereoselective Synthesis and Biological Evaluations
Current Organic Synthesis Brief Psychotic Disorder during COVID-19 Infection: Marked Stressor or Neuropsychiatric Symptoms?
Current Psychiatry Research and Reviews Large Compound Databases for Structure-Activity Relationships Studies in Drug Discovery
Mini-Reviews in Medicinal Chemistry Chromone, A Privileged Scaffold in Drug Discovery: Developments in the Synthesis and Bioactivity
Mini-Reviews in Medicinal Chemistry COVID-19, Angiotensin-Converting Enzyme 2 and Renin-Angiotensin System Inhibition: Implications for Practice
Current Hypertension Reviews Recent Progress in the Discovery of New CCR5 and CXCR4 Chemokine Receptor Antagonists as Inhibitors of HIV-1 Entry. Part 2*
Current Medicinal Chemistry - Anti-Infective Agents Selective Serotonin Re-Uptake Inhibitors and Hyponatremia in Acutely Medically-Ill Inpatients
Current Drug Safety Visual and Quantitative Assessment of COVID-19 Pneumonia on Chest CT: The Relationship with Disease Severity and Clinical Findings
Current Medical Imaging Synthesis and Antimalarial Activity of Novel Side Chain Modified Antimalarial Agents Derived from 4-Aminoquinoline
Medicinal Chemistry