Current drug targets最新文献

Several fibroblast growth factors are expressed in the developmental stage, while others are present in adults. They are vital in maintaining cellular homeostasis and signaling important cellular functions, such as regeneration and growth. Over the years, a spike of interest has been observed in clinical applications of the different members of this family, especially for their implications in glucose and lipid homeostasis, cancer, and regeneration. Yet, the extent of this vast family's roles in different cellular activities and their mechanism of action remain unclear. Furthermore, they are structurally unstable molecules, making clinical applications more difficult. This work reviews the mechanism of action of FGFs and offers valuable insights into their therapeutic potential.

Introduction: Despite their hazardous nature, snake venoms hold immense potential for the development of novel therapies. This summary delves into the key aspects of snake venom research, focusing on their significance as targets for neutralization, their utility as novel drugs, the application of in silico studies, and future prospects with nanotechnology. Significance of Snake Venom: Snake venom harbors a rich diversity of toxic proteins with a wide range of biological activities. Its importance lies in the possibility of neutralizing its detrimental effects and exploring its therapeutic potential for diverse ailments. Venom Neutralization: The development of more effective and specific antivenoms is crucial for treating snakebites, particularly in regions with a high prevalence of accidents. Molecular-level venom studies are essential for identifying novel targets for the development of more efficacious antivenoms. Venom as a Source of Novel Drugs: Proteins present in snake venom exhibit diverse pharmacological activities, including antithrombotic, anti-inflammatory, analgesic, and antimicrobial properties. Investigating these proteins can lead to the development of novel medications for various diseases. In silico Studies: Bioinformatics tools and molecular modelling can aid in the discovery of novel molecular targets in snake venom, accelerating the process of developing new drugs and therapies. Nanotechnology for Drug Delivery: Nanotechnology offers new possibilities for developing more efficient and targeted drug delivery systems, enhancing the safety and effectiveness of snake venom-based treatments.

Conclusion: Snake venom research represents a promising area of inquiry with immense potential for the development of novel drugs and therapies. The integration of traditional and innovative techniques, such as in silico studies and nanotechnology, can accelerate this process and contribute to the advancement of public health.

Globally, high mortality is brought on by RNA viruses, which are linked to chronic human disorders. Viruses dominate the WHO's current ranking of the top 10 global health hazards, especially RNA viruses. RNA viruses, like HIV, SARS-CoV-2, and influenza, which are among the most prevalent and frequently encountered RNA viruses, use RNA as their genetic material, making them prone to quick changes. They adapt rapidly, complicating the body's immune responses. HIV, a significant retrovirus, infiltrates the immune system, causing AIDS by compromising defenses against infections. SARS-CoV-2, which led to COVID-19, sparked a worldwide pandemic with respiratory symptoms, emphasizing the need for research and therapeutic innovations. The COVID-19 pandemic has demonstrated the insufficiency of available resources in effectively addressing emerging viral infections. Influenza, a seasonal RNA virus, triggers flu outbreaks, impacting public health. Research is crucial to understanding how these viruses interact with hosts, aiding the development of effective treatments and strengthening our ability to face new viral threats. The most effective defenses against viral illnesses are virus-specific vaccinations and antiviral drugs. The present review emphasizes the prevalence of the three most pathogenic and widespread RNA viruses, namely HIV, influenza, and SARS-CoV2, their pathophysiology, and the current treatment with FDA-approved drugs. It also incorporates novel analogs that are under clinical trials as there is an urgent need for innovative antiviral medications, and enormous global efforts are required to find secure and efficient cures for these viral infections.

Proteases, once thought to degrade proteins solely, are now recognized as key signaling molecules central to numerous physiological processes, including bone remodeling. Dysregulated protease contributes to various pathological diseases, including cardiovascular diseases, cancer, inflammation, osteoporosis, and neurological disorders. Protease targeting is now quite far along; some small molecules are already on the market, and others are in development. Despite drugs having been successfully developed to inhibit well-defined proteases, including angiotensin-converting enzyme and HIV protease, designing selective inhibitors for the newly identified protease targets is still difficult owing to problems like poor target selectivity. This review covers principles guiding the discovery of protease drugs with a focus on recent approaches, including the use of allosteric sites. In bone remodeling, proteases are involved in the regulation of cell surface properties and extracellular matrix in the degradation process that is fundamental to bone mineral density and quality. In particular, cathepsins, dipeptidyl peptidases, and caspases have become attractive targets for the therapy of osteoporosis. Selective inhibitors are different from other drugs in the way that they selectively inhibit bone resorption processes and do not bear on osteoblast survival factors or bone formation. However, some inhibitors proved to be effective in increasing bone density in osteoporotic patients, but due to side effects, they were withdrawn, highlighting the necessity of selective inhibitors. Newer generations of selective allosteric inhibitors aiming at protease activity would be safer and give an unexplored therapeutic angle to tackle osteoporosis without interfering with other physiological processes.

Neuron loss is the main feature of neurodegenerative diseases. The two most prevalent neurodegenerative illnesses are Parkinson's and Alzheimer's diseases. While several medications are currently approved to treat neurodegenerative disorders, most of them only address the symp-toms that are related to the disorders. Owing to their severity and complex multifactorial patho-physiology, the approved medications currently in clinical use have not demonstrated sufficient efficacy and have limited therapeutic options. Enhancing medicine quality can be achieved using highly efficient conjugate chemistry methods, necessitating ongoing discovery efforts on hybrid drugs in academia and industry. The present review illustrates hybrid compounds and the design strategies that helped to create them. Developing multi-target directed ligands (MTDLs) is a more advantageous and sensible strategy for treating long-term complex illnesses like neurodegenera-tive diseases. Compared to classic treatments, hybrid drugs can deliver combination therapies in a single multifunctional agent, making them more potent and specific. Three main objectives are being initiated by using hybridization techniques in drug design: (i) increasing selectivity, (ii) im-proving activity, and (iii) reducing toxicity. The development of hybrid medications may offer a valuable method for producing compounds that are less likely to develop resistance and more likely to be effective. Hybrid drugs hold great promise, but a few technical and regulatory obsta-cles must be overcome before they can be successfully used in clinical settings.

Delayed diagnosis and limited treatment options make ovarian cancer difficult to treat. This paper examines the growing role of Carbon Dots (CDs) in ovarian cancer diagnosis and treatment. Photoluminescence and biocompatibility make CDs ideal for biomedical use. We emphasize their ability to improve fluorescence and molecular imaging in imaging and diagnostics. We also demonstrate the efficacy of carbon dots in targeted drug delivery systems in overcoming drug resistance and improving therapeutic outcomes. Photodynamic and photothermal therapies are used to show that CDs can treat hypoxic ovarian cancer tumours. We also discuss CD safety issues and constraints, emphasising the need for thorough assessments and fine-tuning. Future research focuses on personalised medicine and CD integration with other therapies. This text concludes by discussing CDs' clinical use and the challenges of production and regulatory approval. CDs can improve ovarian cancer diagnosis and treatment, improving patient outcomes and survival.

Acne vulgaris is the 8th most commonly prevailing skin disorder worldwide. Its pervasiveness has been predominant in juveniles, especially males, during adolescence and in females during adulthood. The lifestyle and nutrition adopted have been significantly reported to impact the occurrence and frequency of acne. It typically occurs over the regions of the forehead, upper chest, and back of the body, which are regions with high proportions of active sebaceous follicles. The market today is flooded with the pool of anti-acne medications (oral, topical/systemic) that contain either a single therapeutic agent or a blend targeting multiple pathological pathways. However, the clinical applicability of these preparations is limited due to formulation stability, drug penetrability, and targeting, the incidence of secondary effects, antibiotic resistance, etc. Moreover, the effectiveness of the former therapies varies as per the type and severity of acne. Therefore, it is necessary to extensively research skin physiology under normal and diseased conditions so that newer, safer, and more effective medications can be devised. Moreover, their safety and efficacy should be validated by employing various acne models, and their comparative profiling should be done with standard marketed anti-acne preparations. Acne models assist to uncover the complex disease pathogenesis and identify the potential targets for therapeutic interventions. This review is an attempt to highlight varied in-vitro, ex-vivo, and in-vivo testing procedures done to assess drug efficacy, track disease progression, and compare test substances with existing treatments. By presenting a unified approach to acne modeling, this review will assist researchers in selecting the most appropriate model for their specific research goals, helping them to generate valuable and reproducible data to support the development of effective acne therapies.

A range of heterocyclic compounds, including Isatin (oneH-indole-2, 3-dione) and its by-products, have been shown to represent potential unit blocks in the synthesis of potential medicinal agents. Numerous studies have been carried out on isatin, its synthesis, biological uses, and its chemical composition since when it was discovered. Functionally, these isatin-containing heterocycles have demonstrated antibacterial, antidiabetic, antiviral, antitubercular, and anticancer properties, among many others. In vitro and In vivo efficaciousness of several Isatin moieties has been assessed in recent years based on their antimicrobial qualities. Isatin has shown great promise as a flexible heterocycle in the realm of drug development in recent years. Many viruses have caused extensive epidemics during the last 50 years, which have had detrimental effects on social, economic, and health conditions. The current unprecedented SARS-CoV-2 epidemic necessitates intensive research into the development of potent antiviral medications. It has been shown that Isatin, a flexible heterocycle, has a great deal of potential for drug development. Appropriately functionalized Isatin compounds have shown noteworthy and extensive antiviral activities throughout the last fifty years. The goal of this study is to gather all known data on Isatin derivatives' antiviral activity, emphasizing their structure-activity correlations as well as research on mechanistic and molecular modelling. We think that the scientific community will find this review to be a useful tool in the development of more efficient and powerful antiviral treatments based on Isatin scaffolds.

Metallothionein 1J pseudogene (MT1JP) is a long non-coding RNA (lncRNA) that functions as a tumor suppressor in various malignancies. Reduced MT1JP expression is associated with increased tumor proliferation, migration, invasion, epithelial-mesenchymal transition (EMT), and treatment resistance in nine cancers, such as gastric cancer, intrahepatic cholangiocarcinoma, hepatocellular carcinoma, and breast cancer. Mechanistically, MT1JP acts as a competitive endogenous RNA (ceRNA) to regulate oncogenic microRNAs (miRNAs), including miR-92a-3p, miR-214-3p, and miR-24-3p. This regulation restores tumor suppressor genes, such as FBXW7, RUNX3, and PTEN, thereby disrupting oncogenic pathways, including PI3K/AKT, Wnt/βcatenin, and p53, promoting apoptosis, and inhibiting tumor progression. Clinically, MT1JP expression correlates with tumor grade, differentiation, TNM stage, lymph node metastasis, and patient prognosis, suggesting its potential as a diagnostic and prognostic biomarker. Furthermore, its therapeutic potential in RNA-based treatments has attracted significant attention. Despite these findings, questions remain regarding its role in epigenetic regulation, transcriptional control, and RNA delivery. This review explores the molecular mechanisms underlying MT1JP, highlighting its clinical relevance and potential as a therapeutic target. Future research should focus on elucidating its role in epigenetic regulation, overcoming challenges in therapeutic delivery, and validating its utility as a biomarker for different cancers. MT1JP holds promise for advancing precision oncology by providing innovative approaches for cancer diagnosis and treatment.

Background: Myopia is one of the most common eye diseases worldwide, with an increasing incidence observed in recent years. Globally, effective treatments for myopia have been extensively explored. In recent years, research on drugs for the treatment of myopia has become a popular topic in ophthalmology, with some breakthroughs having been achieved. Compared with surgical treatment, drug treatment is easier for people to accept. Although the efficacy of some drugs in delaying the development of myopia has been confirmed, the mechanism and site of action of some drugs are still not completely clear.

Objective: In this study, we review the recent related research on drug therapy for myopia at home and abroad, describe the mechanism of various drugs in treating myopia, evaluate their clinical application value, and identify existing problems.

Results: These drugs include atropine, a series of anticholinergic drugs, dopamine agonists, 7- methylxanthine, and intraocular pressure-lowering drugs.

Conclusion: Results highlight the efficacy of atropine in myopia treatment with minimal side effects. Anticholinergic medications, such as atropine, have demonstrated efficacy in managing the progression of myopia with a reduced incidence of adverse effects. The emphasis is placed on achieving better long-term effectiveness and minimizing the rebound effect after treatment is stopped. Furthermore, participating in outdoor activities and reducing eye strain are proven strategies for preventing myopia.