Next Issue
Volume 3, September
Previous Issue
Volume 3, March
 
 

Targets, Volume 3, Issue 2 (June 2025) – 11 articles

  • Issues are regarded as officially published after their release is announced to the table of contents alert mailing list.
  • You may sign up for e-mail alerts to receive table of contents of newly released issues.
  • PDF is the official format for papers published in both, html and pdf forms. To view the papers in pdf format, click on the "PDF Full-text" link, and use the free Adobe Reader to open them.
Order results
Result details
Select all
Export citation of selected articles as:
13 pages, 1763 KiB  
Article
A Report on the Antidepressant-like Activity of Paullinia pinnata Methanol Leaf Extract in Mice and Possible Involvement of Monoaminergic Mechanisms
by Raymond I. Ozolua, Muideen A. Ajibade, Dickson O. Uwaya, Abigail M. Akhigbemen and Israel O. Bolanle
Targets 2025, 3(2), 22; https://doi.org/10.3390/targets3020022 - 16 Jun 2025
Viewed by 202
Abstract
In West Africa, Paullinia pinnata (P. pinnata) alcohol leaf extracts are used to treat disorders such as depression and anxiety with no documented scientific justification. We have therefore evaluated the potential anxiolytic and antidepressant effects of Paullinia pinnata methanol leaf extract [...] Read more.
In West Africa, Paullinia pinnata (P. pinnata) alcohol leaf extracts are used to treat disorders such as depression and anxiety with no documented scientific justification. We have therefore evaluated the potential anxiolytic and antidepressant effects of Paullinia pinnata methanol leaf extract (PPME) in mice, along with probable underlying mechanisms. Adult Swiss albino mice were administered 100, 200, and 400 mg/kg of PPME orally before subjecting them through elevated plus maze (EPM) and hole-board tests to assess the anxiolytic effect. The tail suspension test (TST) and the forced swim test (FST) were used to assess the antidepressant-like effects. Reserpine, labetalol, and risperidone were used to investigate probable mechanisms of action. In both FST and TST, the duration of immobility was considerably reduced by PPME. Conversely, PPME had no significant effect on the number of mice who dipped their heads into the hole-board or entered the EPM’s open arm. Mechanistic analysis revealed that in mice given labetalol or risperidone beforehand, PPME dramatically reduced the length of immobility and reversed ptosis and akinesia caused by reserpine. Our findings suggest that PPME possesses antidepressant-like, but not anxiolytic-like, effects in mice, and antidepressant action may involve enhancing noradrenergic and serotonergic mechanisms. Full article
Show Figures

Figure 1

17 pages, 2758 KiB  
Review
Targeted Treatment Approaches for Gastrointestinal Metastases of Malignant Melanoma: Clinical Insights and Overcoming Drug Resistance
by Tsvetelina Velikova, Marina Konaktchieva and Milena Peruhova
Targets 2025, 3(2), 21; https://doi.org/10.3390/targets3020021 - 11 Jun 2025
Viewed by 239
Abstract
Gastrointestinal metastases of malignant melanoma are relatively common and pose significant challenges to clinical management due to their complex presentation and resistance to therapy. Early detection and a multidisciplinary treatment approach are critical to improve outcomes. This review highlights targeted treatment strategies for [...] Read more.
Gastrointestinal metastases of malignant melanoma are relatively common and pose significant challenges to clinical management due to their complex presentation and resistance to therapy. Early detection and a multidisciplinary treatment approach are critical to improve outcomes. This review highlights targeted treatment strategies for gastrointestinal melanoma metastases, focusing on current therapeutic options and the mechanisms underlying drug resistance. Advances in immune checkpoint inhibitors (ICIs) and targeted therapies, such as BRAF and MEK inhibitors, have revolutionized melanoma treatment, yet their efficacy is often limited by the emergence of resistance mechanisms, including genetic mutations, tumor microenvironment factors, and immune escape. Herein, we explore potential resistance biomarkers for resistance and emerging targeting treatments targeting these pathways. Understanding the molecular and cellular mechanisms driving drug resistance remains critical to overcoming therapeutic limitations, emphasizing the importance of collaborative efforts in research and clinical practice to refine therapeutic approaches and improve survival rates for patients with metastatic melanoma involving the gastrointestinal tract. Future directions include optimizing combination therapies and leveraging precision medicine to address resistance and disease progression. Full article
Show Figures

Figure 1

11 pages, 203 KiB  
Review
The Role of Osimertinib in Stage I–II Non-Small-Cell Lung Cancer with Activating EGFR Mutation
by Cesare Gridelli, Emanuela Nuccio and Francesca Casaluce
Targets 2025, 3(2), 20; https://doi.org/10.3390/targets3020020 - 11 Jun 2025
Viewed by 315
Abstract
Non-small-cell lung cancer (NSCLC) remains the leading cause of cancer-related deaths worldwide with only approximately 30% of new diagnoses manifesting with localized stages IA–IIA. Osimertinib is a third-generation inhibitor of the epidermal growth factor receptor (EGFR), which is used for treating metastatic, locally [...] Read more.
Non-small-cell lung cancer (NSCLC) remains the leading cause of cancer-related deaths worldwide with only approximately 30% of new diagnoses manifesting with localized stages IA–IIA. Osimertinib is a third-generation inhibitor of the epidermal growth factor receptor (EGFR), which is used for treating metastatic, locally advanced, and early-stage NSCLC expressing common EGFR mutations. Two phase III clinical trials supported yresectable locally advanced disease, consisting of the ADAURA and LAURA studies, respectively. On the other hand, conflicting data on neoadjuvant efficacy led to the design of the ongoing Neo-ADAURA trial. In this review, we describe the pivotal trials that led to the approval of osimertinib use as an adjuvant treatment in radically resected NSCLC patients and as maintenance therapy after chemoradiotherapy. We also summarize the principal ongoing clinical trials in the neoadjuvant and adjuvant settings. Finally, we analyze several issues about the use of osimertinib in those different early settings while also depicting future perspectives and the potential evolution of treatment strategies. Full article
15 pages, 1205 KiB  
Article
Anti-Inflammatory, Analgesic, and Anxiolytic Effects of Crude Extracts and Isolated Bioactive Fractional Compounds from Pouzolzia sanguinea
by Md. Qamrul Ahsan, Rateep Nasim, Md. Talat Nasim and S. M. Shahinul Islam
Targets 2025, 3(2), 19; https://doi.org/10.3390/targets3020019 - 10 Jun 2025
Viewed by 268
Abstract
Pharmacological relevance: Ethnic people residing in the Chittagong Hill Tracts (CHTs) of Bangladesh use Pouzolzia sanguinea to alleviate flatulence, for menstruation, inflammation, insomnia, and analgesia. However, there is no scientific evidence regarding the bioactivity of these plants. Aim: This study aimed to isolate [...] Read more.
Pharmacological relevance: Ethnic people residing in the Chittagong Hill Tracts (CHTs) of Bangladesh use Pouzolzia sanguinea to alleviate flatulence, for menstruation, inflammation, insomnia, and analgesia. However, there is no scientific evidence regarding the bioactivity of these plants. Aim: This study aimed to isolate bioactive fractional compounds from Pouzolzia sanguinea (IFCPS) crude extract to assess the anti-inflammatory, analgesic, and anxiolytic activities. Materials and Methods: Preparative TLC-bioautography and silica gel two-stage column chromatography were used to isolate bioactive fractional compounds from P. sanguinea methanol crude extracts. The anti-inflammatory, analgesic, and anxiolytic activities of extracts and IFCPS were studied by inhibiting protein denaturation, acetic acid-induced writhing, Eddy’s hot plate, field cross, and hole cross methods. Results: The dried crude extract’s chemical analysis revealed alkaloids, flavonoids, terpenoids, saponins, vitamin C, and tannins. Nine single isolated fractional compounds (IFC1PS to IFC9PS) were isolated through TLC. Among these, IFC2PS exhibited (p ˂ 0.01) the most potent anti-inflammatory activity in the inhibition of protein denaturation studies (70.51%), which was slightly lower than acetyl salicylic acid (82.29%), at160 µg/mL. This inhibitory effect occurred in a dose-dependent manner. IFC2PS exhibited the most potent peripheral analgesic and moderate central analgesic effects compared to the standard. In contrast, IFC1PS showed moderate effects in both areas. IFC8PS showed superior anxiolytic activities compared to crude extracts and other IFCPS. Conclusions: Out of the nine fractional compounds isolated, the IFC2PS reduced pain and inflammation, whilst IFC8PS exhibited anxiolytic activities. This is the first comprehensive study demonstrating the anti-inflammatory, analgesic, and anxiolytic effects of crude extracts and isolated fractional compounds from the whole plant of P. sanguinea, which may have immediate experimental and clinical applications. Full article
Show Figures

Figure 1

34 pages, 7582 KiB  
Review
Recent Progress in Small Molecule Fluorescent Probes for Imaging and Diagnosis of Liver Injury
by Shuo Liu, Fei Huang, Xinyi Huang, Fuxin Zhang, Dong Pei, Jinlong Zhang and Jun Hai
Targets 2025, 3(2), 18; https://doi.org/10.3390/targets3020018 - 28 May 2025
Viewed by 319
Abstract
The liver is an essential metabolic organ that is involved in energy metabolism, protein synthesis, and detoxification. Many endogenous and exogenous factors can cause liver injury, a complex pathological condition. It poses a serious risk to human health due to its extremely varied [...] Read more.
The liver is an essential metabolic organ that is involved in energy metabolism, protein synthesis, and detoxification. Many endogenous and exogenous factors can cause liver injury, a complex pathological condition. It poses a serious risk to human health due to its extremely varied clinical manifestations, which range from mild fatty liver to liver fibrosis, cirrhosis, and even hepatocellular carcinoma. Because of their low specificity, lack of real-time monitoring, and invasiveness, traditional diagnostic techniques for liver injury, such as histopathological examination and serological analysis, have inherent limitations. Fluorescent probe technology, which offers high sensitivity, non-invasiveness, and real-time imaging capabilities, has become a potent tool in liver injury research and early diagnosis in recent years. The pathophysiology of liver injuries caused by alcohol, chemicals, drugs, and the immune system is methodically covered in this review, along with new developments in fluorescent probe development for their detection. The focused imaging properties of various fluorescent probes are highlighted, along with their possible uses in drug screening and early liver injury detection. This review attempts to offer theoretical insights to support the optimization of precision diagnostic and therapeutic approaches by summarizing these findings. Full article
(This article belongs to the Special Issue Recent Progress in Bioimaging and Targeted Therapy)
Show Figures

Figure 1

18 pages, 670 KiB  
Review
Targeting Obesity in Cardiovascular Disease Management: Cardiac Adipose Tissue Is a Real Biomarker!
by Saverio D’Elia, Ettore Luisi, Achille Solimene, Chiara Serpico, Mariarosaria Morello, Gisella Titolo, Valentina Maria Caso, Francesco S. Loffredo, Paolo Golino, Giovanni Cimmino and Francesco Natale
Targets 2025, 3(2), 17; https://doi.org/10.3390/targets3020017 - 23 May 2025
Viewed by 369
Abstract
Background: Obesity has been defined as a true worldwide “pandemic” by the World Health Organization and represents one of the major public health problems. It is associated with a reduction in life expectancy of about 7–8 years due to related cardiovascular diseases such [...] Read more.
Background: Obesity has been defined as a true worldwide “pandemic” by the World Health Organization and represents one of the major public health problems. It is associated with a reduction in life expectancy of about 7–8 years due to related cardiovascular diseases such as arterial hypertension, metabolic syndrome, insulin resistance, type 2 diabetes mellitus, and dyslipidemia. Adipose tissue is not merely a fat storage site but a true endocrine and immunologically active organ that secretes hormones and mediators (adipokines), influencing cardiovascular risk and host physiology. Objective: This review summarizes the current understanding of the role of epicardial adipose tissue (EAT) in cardiovascular disease pathophysiology and discusses its clinical diagnostic and therapeutic implications. Methods: A narrative non-systematic review was conducted focusing on recent literature concerning the biological and clinical aspects of cardiac adipose tissue, with particular emphasis on epicardial adipose tissue. The review examined its gene expression profile, secretory function, and interaction with cardiovascular structures and diseases. Findings: There are different types of adipose tissue, including cardiac adipose tissue, which comprises epicardial and pericardial (or paracardiac) fractions. Epicardial adipose tissue is unique due to its proximity to the heart and a distinct gene expression profile compared to other adipose depots such as visceral and subcutaneous fat. EAT plays a crucial role in the development and progression of cardiovascular diseases with high morbidity and mortality, acting both as a metabolic and inflammatory mediator. Conclusion: Cardiac adipose tissue, particularly EAT, is a key player in cardiometabolic disease. Understanding its pathophysiological role and incorporating imaging tools to evaluate EAT may enhance cardiovascular risk stratification and disease management. Full article
Show Figures

Figure 1

25 pages, 2921 KiB  
Review
The Design and Prospects of Influenza Virus Vaccines Based on Conserved Epitopes and Adjuvant Optimization
by Meng-Qian Zhang, Jin-Wei Bu, Zhi-Gang Wang and Shu-Lin Liu
Targets 2025, 3(2), 16; https://doi.org/10.3390/targets3020016 - 19 May 2025
Viewed by 693
Abstract
Influenza viruses pose a significant threat to human health, and vaccination remains the most cost-effective and efficient strategy for controlling outbreaks. This review first introduces the molecular characteristics of influenza A virus (IAV) and examines how conserved epitopes contribute to overcoming its high [...] Read more.
Influenza viruses pose a significant threat to human health, and vaccination remains the most cost-effective and efficient strategy for controlling outbreaks. This review first introduces the molecular characteristics of influenza A virus (IAV) and examines how conserved epitopes contribute to overcoming its high variability, laying the foundation for broadly protective vaccine design. Different vaccine platforms are then categorized and analyzed through representative examples to highlight their research significance and application potential. The discussion further extends to the role of adjuvants in modulating immune responses, with a focus on how their optimization enhances vaccine efficacy. We explore future directions in vaccine design, highlighting the synergistic potential of conserved epitope targeting and adjuvant improvement in advancing the next generation of influenza vaccines. Full article
(This article belongs to the Special Issue Recent Progress in Bioimaging and Targeted Therapy)
Show Figures

Figure 1

14 pages, 6493 KiB  
Case Report
A Case Report on Magnetic Resonance-Guided Surveillance of a Giant Hydatid Cyst: Implications for Therapeutic Management and Other Modalities
by Florian Stephan Bienenfeld, Marija Zubčić, Alessio Sciacqua, Giacomo Fascia, Manuela Montatore, Gianmichele Muscatella and Giuseppe Guglielmi
Targets 2025, 3(2), 15; https://doi.org/10.3390/targets3020015 - 1 May 2025
Viewed by 337
Abstract
Background and Clinical Significance: Cystic echinococcosis (CE), also known as hydatid disease, is a zoonosis in whose life cycle humans can be an accidental intermediate host. The liver is the most commonly affected organ, with complications like cyst rupture, hematogenous spread, and [...] Read more.
Background and Clinical Significance: Cystic echinococcosis (CE), also known as hydatid disease, is a zoonosis in whose life cycle humans can be an accidental intermediate host. The liver is the most commonly affected organ, with complications like cyst rupture, hematogenous spread, and infection. Imaging techniques, such as ultrasound, CT, and MRI scans, play a vital role in diagnosing and classifying the disease, facilitating the appropriate therapeutic approach. Treatment options include albendazole for early stage cysts, with more invasive procedures like PAIR, MoCAT, and surgery for advanced cases. This article highlights the importance of imaging modalities in the diagnosis and therapeutic management of CE. Case Presentation: We report a case of a 23-year-old female patient presenting with nausea, fatigue, and loss of appetite to the emergency department, who was diagnosed with a giant echinococcosis lesion. The patient received ultrasound, MR, and CT diagnostics initially. The surveillance included ultrasound and MRI, as well as an anthelmintic therapy, and eventually led to an open resection. Conclusions: This case highlights the importance of imaging modalities in diagnosing and therapeutically managing CE. It explains the key features of each WHO classification stage of the disease for each modality, emphasizing the value of an MRI scan as a possibility for surveillance and a bridge to surgery. Full article
Show Figures

Figure 1

19 pages, 1598 KiB  
Review
Molecular and Immunological Mechanisms Associated with Diesel Exhaust Exposure
by Naresh Singh and Samantha Sharma
Targets 2025, 3(2), 14; https://doi.org/10.3390/targets3020014 - 21 Apr 2025
Viewed by 614
Abstract
Air pollution, particularly from vehicular emissions, has emerged as a critical environmental health concern, contributing to a global estimated 7 million premature deaths annually. Diesel exhaust, a major component of urban air pollution, contains fine particulate matter and gases that evade respiratory filtration, [...] Read more.
Air pollution, particularly from vehicular emissions, has emerged as a critical environmental health concern, contributing to a global estimated 7 million premature deaths annually. Diesel exhaust, a major component of urban air pollution, contains fine particulate matter and gases that evade respiratory filtration, penetrating deep into the lungs and triggering oxidative stress, inflammation, and immune dysregulation. Epidemiological and in vitro studies have linked diesel exhaust exposure to respiratory diseases such as asthma, chronic obstructive pulmonary disease, pulmonary fibrosis, and lung cancer, with immunological mechanisms playing a central role. Diesel exhaust particles induce oxidative stress, impair macrophage phagocytosis, and skew T-cell polarization toward pro-inflammatory Th2 and Th17 responses, exacerbating chronic inflammation and tissue damage. Despite these insights, significant gaps remain in understanding the precise immunomodulatory pathways and long-term systemic effects of diesel exhaust exposure. While animal models and in vitro studies provide valuable data, they often fail to capture the complexity of human exposure and immune responses. Further research is needed to elucidate the mechanisms underlying diesel exhaust-induced immune dysregulation, particularly in vulnerable populations with pre-existing respiratory conditions. This review focuses on summarizing the current knowledge and identifying gaps that are essential for developing targeted interventions and policies to mitigate the adverse health impacts of diesel exhaust and improve respiratory health outcomes globally. Full article
Show Figures

Figure 1

15 pages, 2964 KiB  
Article
Semisynthetic Flavonoids as GSK-3β Inhibitors: Computational Methods and Enzymatic Assay
by Heberth de Paula, Fernanda Souza, Lara Ferreira, Jéssica A. B. Silva, Rayssa Ribeiro, Juliana Vilachã, Flávio S. Emery, Valdemar Lacerda, Jr. and Pedro A. B. Morais
Targets 2025, 3(2), 13; https://doi.org/10.3390/targets3020013 - 15 Apr 2025
Viewed by 377
Abstract
Glycogen synthase kinase-3 beta (GSK-3β) plays a crucial role in multiple cellular processes and is implicated in different types of cancers and neurological disorders, including Alzheimer’s disease. Despite extensive efforts to develop novel GSK-3β inhibitors, the discovery of potent and selective lead compounds [...] Read more.
Glycogen synthase kinase-3 beta (GSK-3β) plays a crucial role in multiple cellular processes and is implicated in different types of cancers and neurological disorders, including Alzheimer’s disease. Despite extensive efforts to develop novel GSK-3β inhibitors, the discovery of potent and selective lead compounds remains a challenge. In this study, we evaluated the GSK-3β inhibitory potential of semisynthetic flavonoid derivatives, which exhibited sub-micromolar activity. To gain further insights, we employed molecular docking, molecular dynamics simulations, and pharmacokinetic profile predictions. The docking studies revealed that the most potent inhibitor, compound 10, establishes key interactions with the ATP-binding site. Molecular dynamics simulations further confirmed that compound 10 maintains stable interactions with GSK-3β throughout the simulation. Additionally, pharmacokinetic predictions identified compound 3 as a promising candidate for Alzheimer’s disease therapy due to its ability to cross the blood–brain barrier. These findings suggest that, within the studied flavonoid derivatives, these compounds (particularly 10 and 3) hold potential as lead compounds for GSK-3β inhibition. The combination of strong enzymatic inhibition, stable binding interactions, and favorable pharmacokinetic properties highlights their promise for further development in cancer and neurodegenerative disease research. Full article
Show Figures

Figure 1

5 pages, 392 KiB  
Case Report
Rapid Response with Daratumumab for Pure Red Cell Aplasia in a Case of Aplastic Anemia with Mixed Chimerism After ABO-Mismatched Stem Cell Transplant
by Martina Canichella, Luca Cupelli, Mariagiovanna Cefalo, Cinzia Sparapani, Antonella Matteocci, Giuseppe Ausoni, Paola Zambardi, Flavia Cantoni, Vanessa Velotta, Giovanna Suppo and Paolo de Fabritiis
Targets 2025, 3(2), 12; https://doi.org/10.3390/targets3020012 - 3 Apr 2025
Viewed by 411
Abstract
Pure red cell aplasia (PRCA) following major ABO-mismatched allogeneic hematopoietic stem cell transplantation (HSCT) is a challenging complication, affecting 7–10% of patients and significantly impacts quality of life. Despite half of patients showing a resolution within three–six months after HSCT, PRCA might require [...] Read more.
Pure red cell aplasia (PRCA) following major ABO-mismatched allogeneic hematopoietic stem cell transplantation (HSCT) is a challenging complication, affecting 7–10% of patients and significantly impacts quality of life. Despite half of patients showing a resolution within three–six months after HSCT, PRCA might require treatment. Various therapeutic approaches have been investigated, including erythropoietin, plasmapheresis or immunomodulatory therapies (rituximab, bortezomib, corticosteroids, donor lymphocyte infusion (DLI), or the early tapering of immunosuppressive drugs), and TPO-mimetic agents, though responses have generally remained suboptimal. Recently, daratumumab has emerged as a promising, safe, and effective treatment for PRCA, documented by numerous case reports and series. We present a case of PRCA arising in a patient with mixed chimerism following a sibling HSCT for aplastic anemia (AA). In line with the literature, our findings highlight the effectiveness of daratumumab in PRCA from the first dose, although daratumumab administrations were delayed by the onset of infectious complications. Our case supports the earlier introduction of daratumumab in the treatment strategy of PRCA to avoid patient exposure to ineffective therapies that carry risks of increased immunosuppression and infections. Indeed, in our specific case, the early introduction of daratumumab may interrupt the immune hematologic mechanism underlying PRCA, which, in the context of mixed chimerism, could increase the risk of graft failure. Full article
Show Figures

Figure 1

Previous Issue
Next Issue
Back to TopTop