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Exploration of Drug Science
ISSN 2836-7677 · Open Exploration · 179 artikel di indeks
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Harnessing nanomaterials to overcome antimicrobial resistance in Gram-positive bacteria: a systematic review
Background: Antimicrobial resistance (AMR) among Gram-positive bacteria has emerged as a significant global health threat, with pathogens such as methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant Enterococcus faecium (VRE) exhibiting increasing resistance to conventional…
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Small molecule and fragment-based phenotypic screening for novel building blocks with antimycobacterial activity
Aim: To design, synthesize, and test small molecules and fragment-based compounds with putative selective anti-mycobacterial activity. Methods: Standard chemosynthetic processes were used to synthesize 42 compounds. A cell-based phenotypic screen for inhibitors of mycobacterial growth was used to…
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A case series of CBT-inspired behavioral and medical interventions for uncontrolled type 2 diabetes
Type 2 diabetes mellitus (T2DM) is a global health challenge often complicated by poor treatment adherence, suboptimal lifestyle habits, and progressive metabolic deterioration. Cognitive behavioral therapy (CBT) has been shown to improve adherence and psychological outcomes, yet its integration…
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Prophylactic metoclopramide for preventing opioid-induced nausea and vomiting in cancer pain: a retrospective cohort study
Aim: To evaluate the real-world effectiveness of prophylactic metoclopramide in preventing opioid-induced nausea and vomiting (OINV) during the initial phase of strong opioid therapy in opioid-naïve patients with cancer-related pain. Methods: This retrospective, single-center observational cohort…
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Vinyl sulfones: selective and tunable covalent warheads against challenging enzyme targets
Over the past several decades there has been a growing recognition of the role that covalent drug candidates have played in the drug development process. With this recognition, compounds that are capable of selectively and irreversibly inactivating their targets through covalent bond formation are…
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Updates on intranasal nanomedicine design for central nervous system disease treatment
Intranasal drug delivery exhibits therapeutic potential for the treatment of central nervous system (CNS) diseases, as it allows pharmaceuticals to bypass the blood-brain barrier (BBB) via the olfactory and trigeminal pathways. The primary advantage of this method lies in its non-invasiveness and…
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Exploring s-triazine derivatives as anticancer agents
The s-triazine scaffold has emerged as a privileged heterocyclic nucleus/moiety in pharmaceutical discovery and development, owing to its presence in several natural products and clinically relevant therapeutic agents, including enasidenib, gedatolisib, bimiralisib, atrazine, indaziflam, and…
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Flagellar pocket receptors as entry point for protein-based drugs against kinetoplastid parasites
Aim: Kinetoplastids are flagellated protozoa encompassing multiple parasitic species responsible for severe neglected diseases. Although treatments exist, therapeutic failure and toxic side effects underscore the need for innovative drug development. Recent advances in protein design have…
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Anti-inflammatory activity and secondary metabolite profiling of Eucalyptus camaldulensis (Myrtaceae)
Aim: This study investigated the anti-inflammatory effect of the extract and fractions of Eucalyptus camaldulensis and also profiled the secondary metabolites of its most active fraction. Methods: The leaves of E. camaldulensis were collected, authenticated and extracted with methanol. The extract…
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AI-driven discovery of antimicrobial peptides and derivatives: database and tools
The global rise of antimicrobial resistance (AMR) has emerged as one of the most pressing threats to public health. This crisis calls for the urgent development of alternative therapeutic agents against antibiotic-resistant pathogens. Antimicrobial peptides (AMPs) are widely present in nature, with…
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Advanced Therapy Medicinal Products (ATMPs): fundamental concepts, classification, and translational challenges
Advanced Therapy Medicinal Products (ATMPs) represent a transformative class of innovative therapies based on genes, cells, or engineered tissues that aim to modify, repair, or replace biological functions at a fundamental level. This review provides a foundational overview of ATMPs, addressing…
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Medicinal plants for skin and wound-healing in Brazil: an ethnobotanical and antibacterial review
Brazil harbors remarkable biological and cultural diversity, reflected in a rich body of traditional knowledge regarding the medicinal use of plants. This study synthesized ethnobotanical evidence on plants traditionally used for skin and wound healing in Brazil and examined their convergence with…
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Bacteriophage therapy in the antibiotic resistance era: mechanistic promise, clinical evidence, and system-level barriers
Antimicrobial resistance (AMR) poses a growing global health threat, progressively undermining the clinical effectiveness of conventional antibiotic therapies. Despite their proven efficacy and standardized clinical frameworks, antibiotics exert strong selective pressures that accelerate…
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Prediction of absolute bioavailability of medicines in adults and children from oral clearance
Aim: Two empirical methods were used to predict the absolute bioavailability (F) of medicines in adults and children following oral administration in the absence of intravenous (IV) dosing. This study systematically evaluates the predictive performance of Equation 1 to predict F in adults and…
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Synchronizing obesity management with survodutide
The therapeutic landscape for obesity is changing rapidly, driven by the recognition of obesity as a chronic, biologically heterogeneous disease, with clinically relevant organ consequences. In this context, the phase 3 SYNCHRONIZE™-1 trial of survodutide, a once-weekly dual agonist of glucagon…
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Cannabinoid therapeutics in the 21st century: from molecular mechanisms to equitable clinical integration
Cannabis sativa has a long history in ethnomedicine, but advances in molecular biology and regulatory shifts have reignited global interest in its therapeutic potential. Cannabinoid research in the 21st century spans molecular pharmacology, clinical applications, and public health integration. This…
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Acid-hydrolyzed nanocrystalline starch excipients for direct-compression tableting: a systematic review
Background: Acid-hydrolyzed nanocrystalline starch has attracted interest as a sustainable pharmaceutical excipient because of its crystallinity, compactibility, and potential suitability for direct compression tableting. However, the available evidence on its fabrication methods, material…
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Synergistic attack of “old drugs for new uses”: repositioning strategies in cancer combination therapy
Cancer treatment faces severe challenges such as drug resistance, side effects, and high costs. The “repurposing old drugs” strategy, which involves repositioning approved drugs for non-oncology indications for cancer treatment, has opened up new avenues for developing efficient, low-toxicity, and…
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Adapting the plant defense systems’ toolbox of Michael acceptors to electrophilic drug development
Plant metabolites are an invaluable source of bioactive molecules, and a high percentage of them can react covalently with their targets. Lipid-derived α,β-unsaturated systems (Michael acceptors), which are present in all plants, regulate signaling pathways in cells. In addition, they potentially…