scholarly journals Targeting the Plasmodium falciparum Proteome and Organelles for Potential Antimalarial Drug Candidates

2021 ◽  
Author(s):  
James Abugri
Keyword(s):  
Antimalarial Drug ◽  
Malaria Parasite ◽  
Treatment Options ◽  
Mortality Data ◽  
Antimalarial Drug Resistance ◽  
Drug Candidates ◽  
Parasite Biology ◽  
Almost All ◽  
Druggable Targets ◽  
Emergence Of Resistance

There is an overarching need to find alternative treatment options for malaria and this quest is more pressing in current times due to the morbidity and mortality data arising from most endemic countries and partially owing to the fact that the SARS-Cov-2 pandemic has diverted much public health attention. Additionally, the therapeutic options available for malaria has been severely threatened with the emergence of resistance to almost all existing drugs by the human malaria parasite. The Artemisinin Combination Therapies (ACTs) which hitherto have been the mainstay for malaria have encountered resistance in South East Asia, a notorious ground zero for the emergence of antimalarial drug resistance. This review analyses few key druggable targets of the parasite and the potential to leverage strategic inhibitors to mitigate the scourge of malaria by providing a concise assessment of the essential proteins of the malaria parasite that could serve as targets. Furthermore, this work provides a summary of the advances made in malaria parasite biology and the potential to leverage such findings for antimalarial drug production.

scholarly journals Inhibitors of the Plasmodium falciparum Hsp90 towards Selective Antimalarial Drug Design: The Past, Present and Future

Cells ◽  
2021 ◽  
Vol 10 (11) ◽  
pp. 2849
Author(s):  
Melissa Stofberg ◽  
Celine Caillet ◽  
Marianne Villiers ◽  
Tawanda Zininga
Keyword(s):  
Drug Resistance ◽  
Antimalarial Drug ◽  
Protein Quality ◽  
Unmet Need ◽  
Heat Shock Protein 90 ◽  
Complex Life Cycle ◽  
Antimalarial Drug Resistance ◽  
Resistance Development ◽  
Almost All ◽  
New Strategies

Malaria is still one of the major killer parasitic diseases in tropical settings, posing a public health threat. The development of antimalarial drug resistance is reversing the gains made in attempts to control the disease. The parasite leads a complex life cycle that has adapted to outwit almost all known antimalarial drugs to date, including the first line of treatment, artesunate. There is a high unmet need to develop new strategies and identify novel therapeutics to reverse antimalarial drug resistance development. Among the strategies, here we focus and discuss the merits of the development of antimalarials targeting the Heat shock protein 90 (Hsp90) due to the central role it plays in protein quality control.

scholarly journals The impact of HIV-1 on the malaria parasite biomass in adults in sub-Saharan Africa contributes to the emergence of antimalarial drug resistance

2008 ◽  
Vol 7 (1) ◽  
Author(s):  
Jean-Pierre Van geertruyden ◽  
Joris Menten ◽  
Robert Colebunders ◽  
Eline Korenromp ◽  
Umberto D'Alessandro
Keyword(s):  
Drug Resistance ◽  
Antimalarial Drug ◽  
Malaria Parasite ◽  
Sub Saharan Africa ◽  
Antimalarial Drug Resistance ◽  
Sub Saharan ◽  
The Impact ◽  
Hiv 1

scholarly journals Chloroquine and Sulfadoxine–Pyrimethamine Resistance in Sub-Saharan Africa—A Review

2021 ◽  
Vol 12 ◽  
Author(s):  
Alexandra T. Roux ◽  
Leah Maharaj ◽  
Olukunle Oyegoke ◽  
Oluwasegun P. Akoniyon ◽  
Matthew Adekunle Adeleke ◽  
...  
Keyword(s):  
Drug Resistance ◽  
Antimalarial Drug ◽  
Indoor Residual Spraying ◽  
Sub Saharan Africa ◽  
Bed Nets ◽  
African Countries ◽  
Antimalarial Drug Resistance ◽  
Sub Saharan ◽  
Insecticide Treated Bed Nets ◽  
Emergence Of Resistance

Malaria is a great concern for global health and accounts for a large amount of morbidity and mortality, particularly in Africa, with sub-Saharan Africa carrying the greatest burden of the disease. Malaria control tools such as insecticide-treated bed nets, indoor residual spraying, and antimalarial drugs have been relatively successful in reducing the burden of malaria; however, sub-Saharan African countries encounter great challenges, the greatest being antimalarial drug resistance. Chloroquine (CQ) was the first-line drug in the 20th century until it was replaced by sulfadoxine–pyrimethamine (SP) as a consequence of resistance. The extensive use of these antimalarials intensified the spread of resistance throughout sub-Saharan Africa, thus resulting in a loss of efficacy for the treatment of malaria. SP was replaced by artemisinin-based combination therapy (ACT) after the emergence of resistance toward SP; however, the use of ACTs is now threatened by the emergence of resistant parasites. The decreased selective pressure on CQ and SP allowed for the reintroduction of sensitivity toward those antimalarials in regions of sub-Saharan Africa where they were not the primary drug for treatment. Therefore, the emergence and spread of antimalarial drug resistance should be tracked to prevent further spread of the resistant parasites, and the re-emergence of sensitivity should be monitored to detect the possible reappearance of sensitivity in sub-Saharan Africa.

Recent Advances and Computational Approaches in Peptide Drug Discovery

2019 ◽  
Vol 25 (31) ◽  
pp. 3358-3366 ◽  
Author(s):  
Neha S. Maurya ◽  
Sandeep Kushwaha ◽  
Ashutosh Mani
Keyword(s):  
Docking Studies ◽  
Computational Approaches ◽  
Simulation Tools ◽  
Drug Candidates ◽  
Recent Advances ◽  
Long Duration ◽  
Stability Of Complexes ◽  
Therapeutic Peptides ◽  
Target Binding ◽  
Druggable Targets

Background: Drug design and development is a vast field that requires huge investment along with a long duration for providing approval to suitable drug candidates. With the advancement in the field of genomics, the information about druggable targets is being updated at a fast rate which is helpful in finding a cure for various diseases. Methods: There are certain biochemicals as well as physiological advantages of using peptide-based therapeutics. Additionally, the limitations of peptide-based drugs can be overcome by modulating the properties of peptide molecules through various biomolecular engineering techniques. Recent advances in computational approaches have been helpful in studying the effect of peptide drugs on the biomolecular targets. Receptor – ligand-based molecular docking studies have made it easy to screen compatible inhibitors against a target.Furthermore, there are simulation tools available to evaluate stability of complexes at the molecular level. Machine learning methods have added a new edge by enabling accurate prediction of therapeutic peptides. Results: Peptide-based drugs are expected to take over many popular drugs in the near future due to their biosafety, lower off-target binding chances and multifunctional properties. Conclusion: This article summarises the latest developments in the field of peptide-based therapeutics related to their usage, tools, and databases.

A Brief Review on Dual Target of PARP1 and STAT3 for Cancer Therapy: A Novel Perception

2020 ◽  
Vol 16 (2) ◽  
pp. 115-134
Author(s):  
Kaviarasan Lakshmanan ◽  
Gowramma Byran ◽  
Manal Mohammed
Keyword(s):  
Signaling Pathways ◽  
Single Molecule ◽  
Treatment Options ◽  
Poor Response ◽  
Cytotoxic Agents ◽  
Acquired Drug Resistance ◽  
Single Target ◽  
New Strategy ◽  
Cancer Multiple ◽  
Almost All

Background: Cancer is a disease characterized by the uncontrolled growth and spread of abnormal cells. Around the world, over 10 million cancer cases occur annually. Half of all men and one-third of all women will develop some form of cancer during their lifetime. It is one of the most feared diseases, primarily because half of those diagnosed with cancer die from it. There are several treatments available for cancer. Almost all traditional cytotoxic agents suffer from severe toxicities and other undesirable side effects. Objective: In recent years, the development of targeted medicines has made significant achievements. Unfortunately, though these agents can block key regulators of signaling pathways in cancer, multiple compensatory pathways always attenuate pharmacological effect of single-target drugs. In addition, poor response rates and acquired drug resistance also represent a significant barrier to widespread use of targeted medicines. More recently, a number of combinatorial therapies have expanded treatment options, which can directly block several key signaling pathways and create a synergistic effect. Conclusion: Therefore, in order to overcome these barriers, the present investigation aims to develop a new strategy for designing a single molecule with inhibition of two receptors (PARP1 and STAT3) simultaneously and producing enhanced anti-cancer activity with less and/or null toxicity.

scholarly journals Glioblastoma and MiRNAs

Cancers ◽  
2021 ◽  
Vol 13 (7) ◽  
pp. 1581
Author(s):  
Swalih P. Ahmed ◽  
Javier S. Castresana ◽  
Mehdi H. Shahi
Keyword(s):  
Brain Tumors ◽  
Human Body ◽  
Diagnostic Tool ◽  
Poor Prognosis ◽  
Treatment Options ◽  
Diagnosis And Treatment ◽  
Therapeutic Success ◽  
Knowing That ◽  
Almost All ◽  
Cell Signaling Pathways

Glioblastoma (GB) is one of the most common types of lethal brain tumors. Although several treatment options are available including surgery, along with adjuvant chemo and radiotherapy, the disease has a poor prognosis and patients generally die within 14 months of diagnosis. GB is chemo and radio resistant. Thus, there is a critical need for new insights into GB treatment to increase the chance of therapeutic success. This is why microRNA (miRNA) is being potentially considered in the diagnosis and treatment of glioblastoma. The objective of our review is to provide a holistic picture of GB up-regulated and down-regulated miRNA, in relationship with the expression of other genes, cell signaling pathways, and their role in GB diagnosis and treatment. MiRNA treatment is being considered to be used against GB together with radiotherapy and chemotherapy. Moreover, the use of miRNA as a diagnostic tool has also begun. Knowing that miRNAs are isolated in almost all human body fluids and that there are more than 3000 miRNAs in the human genome, plus the fact that each miRNA controls hundreds of different mRNAs, there is still much study needed to explore how miRNAs relate to GB for its proliferation, progression, and inhibition.

scholarly journals Synthesis, characterization and biological activity of organometallic derivatives of the antimalarial drug mefloquine as new antischistosomal drug candidates

MedChemComm ◽  
2018 ◽  
Vol 9 (11) ◽  
pp. 1905-1909 ◽  
Author(s):  
Faustine d'Orchymont ◽  
Jeannine Hess ◽  
Gordana Panic ◽  
Marta Jakubaszek ◽  
Lea Gemperle ◽  
...  
Keyword(s):  
Biological Activity ◽  
Antimalarial Drug ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
Drug Candidates ◽  
Derivatives Of

The design, synthesis, characterization and biological evaluation of new ferrocenyl and ruthenocenyl derivatives of the antimalarial mefloquine is described.

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