摘要
背景:恶性疟原虫半胱氨酸蛋白酶(又称恶性疟原虫)参与疟原虫不同的红细胞周期过程,如宿主血红蛋白水解,红细胞侵入和红细胞破裂。迄今为止,对4种结瘤蛋白进行生化鉴定后,属于类木瓜蛋白酶cc1家族的fp-2和fp-3是必需的血红蛋白酶。因此,在寻找新的治疗方法时,它们可以被称为潜在的抗疟疾药物靶点,这可以减轻抗药性的增加所带来的负担。e到目前的抗疟药物。 目的:本综述总结了最重要的结果,重点介绍了药物设计方法,以了解抑制作用的机制和发现抑制作用的机制。来自P的抗半胱氨酸蛋白酶的受体。 恶性疟原虫。 结果:本文介绍了一种合理的计算机辅助药物发现方法来设计有前途的鹰枕抑制剂,重点介绍了各种基于结构和配体的药物发现方法。玲来了。此外,还强调了配体识别的关键特征。 结论:本综述将对从事开发药物设计策略以靶向半胱氨酸蛋白酶、FP-2和FP-3的科学家感兴趣。
关键词: 半胱氨酸蛋白酶,计算机辅助药物发现,镰蛋白,血红蛋白降解,疟疾,恶性疟原虫。
图形摘要
Current Drug Targets
Title:Targeting Cysteine Proteases from Plasmodium falciparum: A General Overview, Rational Drug Design and Computational Approaches for Drug Discovery
Volume: 19 Issue: 5
关键词: 半胱氨酸蛋白酶,计算机辅助药物发现,镰蛋白,血红蛋白降解,疟疾,恶性疟原虫。
摘要: Background: The Plasmodium falciparum cysteine proteases, also known as falcipains, are involved in different erythrocytic cycle processes of the malaria parasite, e.g. hydrolysis of host haemoglobin, erythrocyte invasion, and erythrocyte rupture. With the biochemical characterization of four falcipains so far, FP-2 (falcipain-2) and FP-3 (falcipain-3), members of the papain-like CAC1 family, are essential haemoglobinases. They could therefore be referred to as potential anti-malarial drug targets in the search for novel therapies, which could ease the burden caused by the increasing resistance to current antimalarial drugs.
Objectives: This review provides a summary of the most important results, highlighting the drug design approaches essential for the understanding of the mechanism of inhibition and discovery of inhibitors against cysteine proteases from P. falciparum.
Results: Rational and computer-aided drug discovery approaches for the design of promising falcipain inhibitors are described herein, with a focus on a variety of structure-based and ligand-based modeling approaches. Moreover, the key features of ligand recognition against these targets are emphasized.
Conclusion: This review would be of interest to scientists engaged in the development of drug design strategies to target the cysteine proteases, FP-2 and FP-3.
Export Options
About this article
Cite this article as:
Targeting Cysteine Proteases from Plasmodium falciparum: A General Overview, Rational Drug Design and Computational Approaches for Drug Discovery, Current Drug Targets 2018; 19 (5) . https://dx.doi.org/10.2174/1389450117666161221122432
DOI https://dx.doi.org/10.2174/1389450117666161221122432 |
Print ISSN 1389-4501 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-5592 |
Related Books

- Author Guidelines
- Bentham Author Support Services (BASS)
- 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
Related Articles
-
Structure and Function of RNase AS: A Novel Virulence Factor From Mycobacterium tuberculosis
Current Medicinal Chemistry Carnitine Metabolism and Deficit - When Supplementation is Necessary?
Current Pharmaceutical Biotechnology Pharmacogenetics and Inflammatory Bowel Disease
Current Pharmacogenomics and Personalized Medicine Synthesis of Substituted -N-(5-((7-Methyl-2-Oxo-2H-Chromen-4-yl)- Methyl)-1,3,4-Thiadiazol-2-yl)-Benzamide Derivatives Using TBTU as Coupling Agent and their Evaluation for Anti Tubercular Activity
Letters in Organic Chemistry Lyn Regulates Cytotoxicity in Respiratory Epithelial Cells Challenged by Cigarette Smoke Extracts
Current Molecular Medicine Factors Affecting Sexual Transmission of HIV-1: Current Evidence and Implications for Prevention
Current HIV Research Do You See What I See: Recognition of Protozoan Parasites by Toll-Like Receptors
Current Immunology Reviews (Discontinued) IO Nation: The Rise of Immuno-Oncology
Current Pharmacogenomics and Personalized Medicine 3-Phenyl-1H-Indole-5-Sulfonamides: Structure-Based Drug Design of a Promising Class of Carbonic Anhydrase Inhibitors
Current Pharmaceutical Design Nanoparticles vs Cancer: A Multifuncional Tool
Current Topics in Medicinal Chemistry Conjugated Diyne Chemistry: Synthesis, Natural Existence and Applications
Current Organocatalysis Melatonin, Autophagy and Intestinal Bowel Disease
Current Pharmaceutical Design Immunological Mechanism and Clinical Application of PAMP Adjuvants
Recent Patents on Anti-Cancer Drug Discovery New Strategies and Paradigm for Drug Target Discovery: A Special Focus on Infectious Diseases Tuberculosis, Malaria, Leishmaniasis, Trypanosomiasis and Gastritis
Infectious Disorders - Drug Targets The Protein Folding Problem: A Biophysical Enigma
Current Pharmaceutical Biotechnology Revision of the Regioselectivity of the Beirut Reaction of Monosubstituted Benzofuroxans with Benzoylacetonitrile. 6-Substituted quinoxaline-2-carbonitrile 1,4- dioxides: Structural Characterization and Estimation of Anticancer Activity and Hypoxia Selectivity
Current Organic Synthesis Synthesis of Novel Azetidinone Derivatives as Antitubercular Agents
Letters in Drug Design & Discovery Targeting Bacterial RNA Polymerase: Promises for Future Antisense Antibiotics Development
Infectious Disorders - Drug Targets HIV-Specific T Cells: Strategies for Fighting a Moving Target
Current HIV Research Honey as a Source of Dietary Antioxidants: Structures, Bioavailability and Evidence of Protective Effects Against Human Chronic Diseases
Current Medicinal Chemistry