Article
Biochemistry & Molecular Biology
Sampada S. Sawant, Satish Y. Gabhe, Kamalinder K. Singh
Summary: Malaria remains a serious health problem in tropical and subtropical regions, and there is an urgent need for new antimalarial drugs. A systematic investigation on the seeds of A. squamosa revealed that the oily fraction Annomaal has significant antimalarial activity both in vitro and in vivo, with a shorter treatment schedule compared to synthetic drugs. Further studies are needed to identify the active compounds in Annomaal responsible for its antimalarial properties.
Review
Chemistry, Medicinal
Christopher M. Woodley, Patricia S. M. Amado, Maria L. S. Cristiano, Paul M. O'Neill
Summary: Recent research has highlighted the need for fully synthetic endoperoxide-based antimalarials due to the rise of resistance to artemisinin in Southeast Asia and the synthetic limitations of the artemisinin scaffold. Various synthetic endoperoxide antimalarials utilizing different endoperoxide warheads have been explored, with two classes - 1,2,4-trioxolanes and 1,2,4,5-tetraoxanes - showing promise and still actively being developed.
MEDICINAL RESEARCH REVIEWS
(2021)
Article
Infectious Diseases
Navaporn Posayapisit, Jutharat Pengon, Philip J. Shaw, Chairat Uthaipibull, Darin Kongkasuriyachai, Aung Pyae Phyo, Francois Nosten, Yongyuth Yuthavong, Sumalee Kamchonwongpaisan
Summary: The effectiveness of antimalarial drug P218 against artemisinin-resistant Plasmodium falciparum is still uncertain, despite its efficacy against other drug-resistant parasites.
INTERNATIONAL JOURNAL OF ANTIMICROBIAL AGENTS
(2023)
Article
Infectious Diseases
Shaoqin Zheng, Yuan Liang, Zhaojia Wang, Min Liu, Yingyi Chen, Ying Ai, Wenfeng Guo, Guoming Li, Yueming Yuan, Zhiyong Xu, Wanting Wu, Xinan Huang, Zhibing Wu, Qin Xu, Jianping Song, Changsheng Deng
Summary: Artemisinin-based combination therapies (ACTs) are first-line antimalarial drugs. However, the emergence of resistance to ACTs in Plasmodium falciparum is a concern. This study successfully produced artemisinin-and piperaquine-resistant P. berghei K173 strains and explored the relationship between PfK13 and artemisinin resistance through DNA sequencing.
INFECTION AND DRUG RESISTANCE
(2022)
Review
Biochemistry & Molecular Biology
Benedito M. Dos Santos, Jude M. Przyborski, Celia R. S. Garcia
Summary: English Summary: The GPCR-like SR25 in Plasmodium falciparum, a species of apicomplexan parasites, is activated by a shift in potassium concentration, allowing the parasite to take advantage of its development by sensing different ionic concentrations in the external milieu. This pathway involves the activation of phospholipase C and an increase in cytosolic calcium. This report summarizes the role of potassium ions during parasite development based on available literature, contributing to our understanding of the cell cycle of Plasmodium spp.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Editorial Material
Biology
Colin Sutherland, Didier Menard
Summary: A tool that analyzes the genome of parasites in the blood of malaria patients can assist policymakers in making informed decisions on how to address the increase in drug-resistant infections.
Article
Microbiology
Amuza Byaruhanga Lucky, Chengqi Wang, Ahmad Rushdi Shakri, Mohammad Kalamuddin, Anongruk Chim-Ong, Xiaolian Li, Jun Miao
Summary: This study demonstrates the critical role of PfGCN5 gene in stress responses of Plasmodium falciparum, indicating its potential as a target for malaria intervention.
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY
(2023)
Article
Medicine, General & Internal
Harvie P. Portugaliza, H. Magloire Natama, Pieter Guetens, Eduard Rovira-Vallbona, Athanase M. Some, Aida Millogo, D. Florence Ouedraogo, Innocent Valea, Hermann Sorgho, Halidou Tinto, Nguyen Van Hong, Antonio Sitoe, Rosauro Varo, Quique Bassat, Alfred Cortes, Anna Rosanas-Urgell
Summary: The study found that in most infections from African cohorts, increased expression of pfap2-g and other sexual ring biomarkers was observed after treatment. The estimated parasite age at the time of treatment was negatively correlated with the increase in pfap2-g transcript levels, suggesting that younger parasites are less susceptible to stimulation of sexual conversion.
Review
Chemistry, Medicinal
Neelima Shrivastava, Shah A. Khan, Saif Ahmad, Khalid Al-Balushi, Asif Husain
Summary: This review summarized the recent advances in the development of chemotherapeutic agents for malaria, focusing on the structure-activity relationship of potential antimalarial agents. The authors suggest that the multi-target conjugated hybrid approach is the best strategy for discovering and developing effective antimalarial agents.
MINI-REVIEWS IN MEDICINAL CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Jessica Correa Bezerra Bellei, Nicolas Glanzmann, Barbara Albuquerque Carpinter, Daniela Chaves Renhe, Carolina Brandi Marques, Marina Rocha Azevedo, Livia Maria Barreto, Vinicius Novaes Rocha, Isabelle Karine da Costa Nunes, Henrique Marcelo Gualberto Pereira, Elaine Soares Coimbra, Eduardo Antonio Ferraz Coelho, Adilson David da Silva, Fernando de Pilla Varotti, Kezia Katiani Gorza Scopel
Summary: Chloroquine remains the most effective drug for malaria treatment, although resistance to it has emerged. This study focuses on the synthesis of quinoline derivatives to develop new antimalarials. Compound 3 showed promising activity against malaria, inhibiting parasite growth and protecting against severe malaria development.
CHEMICO-BIOLOGICAL INTERACTIONS
(2022)
Article
Chemistry, Medicinal
Helenita C. Quadros, Aysun Capci, Lars Herrmann, Sarah D'Alessandro, Diana Fontinha, Raquel Azevedo, Wilmer Villarreal, Nicoletta Basilico, Miguel Prudencio, Svetlana B. Tsogoeva, Diogo R. M. Moreira
Summary: The artemisinin-quinoline hybrid compound 163A shows potent activity against the asexual blood stage of Plasmodium, with low cytotoxicity and high selectivity for mammalian cells. It suppresses hepatic infection and decreases gametocyte viability, potentially blocking malaria transmission. The bitopic ligand property of the hybrid enhances inhibition of beta-hematin and is essential for arresting the growth of asexual blood parasites.
Article
Pharmacology & Pharmacy
Jerome Dormoi, Remy Amalvict, Mathieu Gendrot, Bruno Pradines
Summary: The untreated malaria can quickly progress to severe forms, and drug resistance poses a threat to malaria protection efforts worldwide. Therefore, the development of new chemotherapy is necessary. This study contributes new data on the use of methylene blue (MB) in combination with common antimalarial drugs for the treatment of malaria and cerebral malaria. The results show that the combination of MB and AQ is a good candidate for preventing cerebral malaria.
Article
Microbiology
Lucien Platon, David A. Baker, Didier Menard
Summary: The ring-stage survival assay is the reference assay to measure in vitro Plasmodium falciparum artemisinin partial resistance. The main challenge of the standard protocol is to generate 0-to-3-h postinvasion ring stages (the stage least susceptible to artemisinin) from schizonts obtained by sorbitol treatment and Percoll gradient.
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY
(2023)
Article
Pharmacology & Pharmacy
Nanang Rudianto Ariefta, Baldorj Pagmadulam, Coh-ichi Nihei, Yoshifumi Nishikawa
Summary: This study evaluated the growth-inhibitory effects of the antimalarial agent sparsomycin against drug-resistant malaria parasites. The results showed that sparsomycin had inhibitory effects on both sensitive and resistant strains of the parasites. This study suggests that sparsomycin has potential as an alternative treatment for malaria.
Article
Genetics & Heredity
Veronica Feijoli Santiago, Jamille Gregorio Dombrowski, Rebeca Kawahara, Livia Rosa-Fernandes, Simon Ngao Mule, Oscar Murillo, Thais Viggiani Santana, Joao Victor Paccini Coutinho, Janaina Macedo-da-Silva, Lucas Cardoso Lazari, Erika Paula Machado Peixoto, Marcel Ivan Ramirez, Martin R. Larsen, Claudio Romero Farias Marinho, Giuseppe Palmisano
Summary: Malaria in pregnancy (MiP) is a significant issue in malaria-endemic areas, leading to adverse effects for both mother and fetus. This study identified the proteome signature of a mouse model and pregnant women infected with Plasmodium falciparum using mass spectrometry-based proteomics. The results showed the activation of the complement system during malaria in pregnancy, which was correlated with poor newborn outcomes.
Review
Pharmacology & Pharmacy
Ilma Shakeel, Neha Basheer, Gulam Mustafa Hasan, Mohammad Afzal, Md. Imtaiyaz Hassan
Summary: PLK1, a conserved mitotic serine-threonine protein kinase, plays important roles in cell division and genome stability. Its expression is controlled by cell cycle stages and blocking PLK1 expression can inhibit tumor cell proliferation and induce apoptosis, making it an attractive target for drug development.
JOURNAL OF DRUG TARGETING
(2021)
Review
Pharmacology & Pharmacy
Indrakant K. Singh, Pratibha Kumari, Pooja Mittal, Amit Kumar, Bharti Singal, Gulam M. Hasan, Rajiv Aggarwal, Md. Amjad Kamal, Archana Singh, Md. Imtaiyaz Hassan
Summary: COVID-19, caused by SARS-CoV-2, can be treated with plant-based materials and other drugs. Vaccines and DNA/RNA therapy have shown high clinical significance, while various forms of vitamins, minerals, herbs, and phytonutrients can enhance immunity against the virus. However, these measures should be combined with social distancing and quarantine.
CURRENT PHARMACEUTICAL DESIGN
(2021)
Review
Biotechnology & Applied Microbiology
Sabeeha Ali, Manzar Alam, Gulam Mustafa Hasan, Md Imtaiyaz Hassan
Summary: The prolonged use of antibiotics has led to the development of multidrug resistance in many organisms, causing a global health crisis. Klebsiella pneumoniae is a causative organism for various infections and recently, both immunocompromised and healthy individuals are equally susceptible to K. pneumoniae infections due to the emergence of hypervirulent strains. This review discusses the pathophysiology of K. pneumoniae, including its virulence determinants, and explores potential drug targets for the discovery of novel drugs and effective treatment regimens.
BRIEFINGS IN FUNCTIONAL GENOMICS
(2022)
Review
Biochemistry & Molecular Biology
Manzar Alam, Md. Meraj Ansari, Saba Noor, Taj Mohammad, Gulam Mustafa Hasan, Syed Naqui Kazim, Md. Imtaiyaz Hassan
Summary: TBK1 plays a fundamental role in regulating cellular responses and controlling signaling cascades. Dysregulation of the TBK1 pathway is associated with various pathophysiological conditions. Inhibitors targeting TBK1 have potential therapeutic applications for diseases, including cancer.
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
(2022)
Review
Immunology
Monika Mariebernard, Abhinab Mohanty, Vinoth Rajendran
Summary: This review focuses on the classification of antimalarial agents based on their killing time and the appearance of organelles during the intraerythrocytic development of Plasmodium falciparum. The study reveals that different drugs have different killing kinetics and target different organelles at different stages of parasite development. Understanding the timing and mechanism of antimalarial action is crucial for designing effective combination therapies and evaluating clinical resistance.
PATHOGENS AND DISEASE
(2022)
Article
Biochemistry & Molecular Biology
Manzar Alam, Gulam Mustafa Hasan, Md Meraj Ansari, Rishi Sharma, Dharmendra Kumar Yadav, Md Imtaiyaz Hassan
Summary: Thymoquinone (TQ), a natural phytochemical found in Nigella sativa, has been proven to have anti-cancer, anti-oxidant, and anti-inflammatory properties, and exhibits antitumor activity by modulating multiple pathways and molecular targets.
Article
Pharmacology & Pharmacy
Yash Gupta, Neha Sharma, Snigdha Singh, Jesus G. Romero, Vinoth Rajendran, Reagan M. Mogire, Mohammad Kashif, Jordan Beach, Walter Jeske, Poonam, Bernhards R. Ogutu, Stefan M. Kanzok, Hoseah M. Akala, Jennifer Legac, Philip J. Rosenthal, David J. Rademacher, Ravi Durvasula, Agam P. Singh, Brijesh Rathi, Prakasha Kempaiah
Summary: A novel multistage antimalarial compound called Calxinin has been developed and exhibits potent inhibitory activity against drug-sensitive and drug-resistant strains of Plasmodium falciparum. It has a unique mechanism of action and shows potential therapeutic, prophylactic, and transmission-blocking properties against malaria parasites resistant to current antimalarials.
Review
Cell Biology
Saleha Anwar, Moyad Shahwan, Gulam Mustafa Hasan, Asimul Islam, Md. Imtaiyaz Hassan
Summary: The human genome encodes more than 500 protein kinases, many of which are associated with cancer. MARK4 is a protein kinase associated with various cancer types due to its important role in regulating microtubule dynamics and cell division. MARK4 is also linked to other pathologies such as Alzheimer's disease and obesity.
CELLULAR SIGNALLING
(2022)
Review
Biochemistry & Molecular Biology
Mohd. Yousuf, Manzar Alam, Anas Shamsi, Parvez Khan, Gulam Mustafa Hasan, Qazi M. Rizwanul Haque, Md. Imtaiyaz Hassan
Summary: Cyclin-dependent kinase 6 (CDK6) plays a significant role in cancer and is considered an effective drug target for therapy. CDK4/6 inhibitors have shown promising anti-cancer activity by preventing tumor development through inhibiting Rb phosphorylation and E2F liberation. This article discusses the roles of CDK6 in cancer, the current status of CDK4/6 inhibitors in therapy, and emphasizes the potential of combining CDK4/6 inhibitors with other drugs for cancer treatment.
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
(2022)
Article
Biochemistry & Molecular Biology
Dhiraj Kumar, Gulam Mustafa Hasan, Asimul Islam, Md. Imtaiyaz Hassan
Summary: Huntington's disease is a common autosomal dominant disease that affects a large number of patients. Despite early genetic diagnostics, effective disease-modifying treatments are still lacking. Ongoing clinical trials are exploring potential drugs to alleviate symptoms by targeting the root cause at the molecular level. Although a major phase III trial was unexpectedly discontinued, there is still optimism about the potential of this technique.
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
(2023)
Article
Medicine, Research & Experimental
Manzar Alam, Gulam Mustafa Hasan, Sayed M. Eldin, Mohd Adnan, Muhammad Bilal Riaz, Asimul Islam, Ilyas Khan, Md. Imtaiyaz Hassan
Summary: Non-small cell lung carcinoma (NSCLC) is the most common malignancy worldwide. Genetic modifications in upstream signaling molecules stimulate signaling cascades, leading to cancer cell proliferation, cancer development, and drug resistance. Efforts have been made to understand the mechanisms of cancer development and develop effective therapeutic approaches for NSCLC by modifying transcription factors and targeting specific cellular signaling pathways in tumor progression. This comprehensive review provides deeper mechanistic insights into the molecular mechanism of action of various signaling molecules and their targeting in the clinical management of NSCLC.
BIOMEDICINE & PHARMACOTHERAPY
(2023)
Review
Biochemistry & Molecular Biology
Ashar Rais, Afzal Husain, Gulam Mustafa Hasan, Md. Imtaiyaz Hassan
Summary: The extracellular matrix (ECM) is a complex network that helps cells aggregate and form functional structures. It plays multiple roles in tissue structure and function, beyond its initial passive functions. The discovery of cellular receptors and their interaction with ECM components has opened new avenues for understanding the role of ECM in developmental programs, wound healing, and tumour progression. This review focuses on how ECM influences the progression of the somatic cell cycle and provides molecular insights into the communication between adhesion complex, signaling pathways, and cell cycle machinery.
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
(2023)
Article
Biochemistry & Molecular Biology
Saleha Anwar, Taj Mohammad, Md. Khabeer Azhar, Hera Fatima, Afsar Alam, Gulam Mustafa Hasan, Asimul Islam, Punit Kaur, Md. Imtaiyaz Hassan
Summary: MARK4 is a kinase known for phosphorylating tau protein and causing Alzheimer's disease. Bacopa monnieri extracts have neuroprotective roles and have been used to treat neurological disorders. Bacopaside II shows strong binding affinity for MARK4 and inhibits its kinase activity.
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
(2023)
Review
Nutrition & Dietetics
Md. Khabeer Azhar, Saleha Anwar, Gulam Mustafa Hasan, Anas Shamsi, Asimul Islam, Suhel Parvez, Md. Imtaiyaz Hassan
Summary: Rosmarinic acid (RA) is an abundant phytochemical with anti-inflammatory and antioxidant properties, playing significant roles in cancer, neuroprotection, and diabetes.
Review
Chemistry, Multidisciplinary
Gulam Mustafa Hasan, Md. Imtaiyaz Hassan, Sukhwinder Singh Sohal, Anas Shamsi, Manzar Alam
Summary: Non-small cell lung carcinoma (NSCLC) is the most common cancer globally, and phytochemicals and small molecule inhibitors have been found to effectively prevent NSCLC and other types of cancers by regulating signaling pathways. This review focuses on the bioactive compounds and small-molecule inhibitors, such as EGCG, Perifosine, ABT-737, Thymoquinine, Quercetin, Venetoclax, Gefitinib, and Genistein, and discusses their potential in NSCLC therapy.
