Current Drug Targets[JOURNAL]
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200 papers
Emerging Combinatorial Drug Delivery Strategies for Breast Cancer: A Comprehensive Review.
Singhai H, Raikwar S, Rathee S … +1 more , Jain SK
Curr Drug Targets · 2025 · PMID 39791149 · Publisher ↗
Breast cancer remains the second most prevalent cancer among women in the United States. Despite advancements in surgical, radiological, and chemotherapeutic techniques, multidrug resistance continues to pose significant...
Breast cancer remains the second most prevalent cancer among women in the United States. Despite advancements in surgical, radiological, and chemotherapeutic techniques, multidrug resistance continues to pose significant challenges in effective treatment. Combination chemotherapy has emerged as a promising approach to address these limitations, allowing multiple drugs to target malignancies via distinct mechanisms of action. Increasingly, the use of phytoconstituents alongside chemotherapeutic agents has shown promise in enhancing treatment outcomes. This combination therapy acts on key signaling pathways such as Hedgehog, Notch, Wnt/β- catenin, tyrosine kinases, and phosphatidylinositol 3-kinase (PI3K), which play critical roles in cellular proliferation, apoptosis, angiogenesis, differentiation, invasion, and metastasis. This review explores various signaling pathways involved in breast cancer progression, discusses conventional treatment methods like surgery, adjuvant radiotherapy, hormonal therapy, and chemotherapy, and highlights emerging nanocarrier-based drug delivery systems (DDS). Liposomes, dendrimers, exosomes, polymeric micelles, and nanoparticles (organic, inorganic, gold, magnetic, carbon-based, and quantum dots) are examined as innovative strategies for enhancing drug delivery efficacy. Furthermore, stimuli-responsive DDSs, including reactive oxygen species (ROS), enzyme-, and hypoxia- responsive systems, are presented as cutting-edge approaches to overcoming drug resistance. Special emphasis is placed on the co-delivery of chemotherapeutic agents and plant-based compounds, particularly in estrogen receptor-positive (ER+) breast cancer. This review aims to provide a comprehensive overview of novel combinatorial strategies and advanced nanocarriers for the effective and targeted treatment of breast cancer.
Diabetic Wound Healing: Factors, Mechanisms, and Treatment Strategies Using Herbal Components.
Porwal S, Malviya R, Sundram S … +2 more , Sridhar SB, Shareef J
Curr Drug Targets · 2025 · PMID 39791148 · Publisher ↗
Managing diabetic wounds is a significant challenge for healthcare professionals since severe complications and delayed recovery greatly impact the patients' quality of life. This article aimed to explore various factors...
Managing diabetic wounds is a significant challenge for healthcare professionals since severe complications and delayed recovery greatly impact the patients' quality of life. This article aimed to explore various factors affecting diabetic wound healing, the mechanism of wound healing, and potential natural products having wound healing capability. It focuses on mechanisms of action and the therapeutic effectiveness of the compounds employed in the management of diabetic wounds. The review discusses the function of nutrition in wound healing, emphasizing the significance of consuming adequate amounts of protein, energy, lipids, amino acids, vitamins, minerals, and water to promote healing. Several herbs, including , and , are being tested for wound healing qualities in diabetes circumstances. These plants have a variety of modes of action, including antioxidant, anti-inflammatory, antibacterial, and immunomodulatory activities that help to speed up wound healing, stimulate collagen formation, and promote tissue regeneration. The variety of action mechanisms seen in natural products, especially in plants, offers hope for the treatment of diabetic wounds. It may also be possible to improve healing results and the quality of life of diabetes individuals with chronic wounds by including these herbal treatments in wound care programs.
Signaling Dynamics in Osteogenesis: Unraveling Therapeutic Targets for Bone Generation.
Yang XD, Haga CL, Phinney DG
Curr Drug Targets · 2025 · PMID 39791147 · Publisher ↗
Diseases affecting bone encompass a spectrum of disorders, from prevalent conditions such as osteoporosis and Paget's disease, collectively impacting millions, to rare genetic disorders including Fibrodysplasia Ossifican...
Diseases affecting bone encompass a spectrum of disorders, from prevalent conditions such as osteoporosis and Paget's disease, collectively impacting millions, to rare genetic disorders including Fibrodysplasia Ossificans Progressiva (FOP). While several classes of drugs, such as bisphosphonates, synthetic hormones, and antibodies, are utilized in the treatment of bone diseases, their efficacy is often curtailed by issues of tolerability and high incidence of adverse effects. Developing therapeutic agents for bone diseases is hampered by the fact that numerous pathways regulating bone metabolism also perform pivotal functions in other organ systems. Consequently, the selection of an appropriate target is a complicated process despite the significant demand for novel medications to address bone diseases. Research has shown the role of various cell signaling pathways, including Wnt, PTHR1, CASR, BMPRs, OSCAR, and TWIST1, in the regulation of osteogenesis, bone remodeling, and homeostasis. Disruptions in bone homeostasis can result in decreased bone density and the onset of osteoporosis. There remains a need for the development of drugs that can enhance bone remodeling with improved side effects profiles. The exploration of promising targets to stimulate bone formation has the potential to significantly advance the field of bone-related medical care, thereby improving the quality of life for millions. Additionally, a deeper understanding of anabolic and catabolic pathway mechanisms could enable future studies to explore synergistic effects between unrelated pathways. Herein, we explore potential drug targets that may be exploited therapeutically using small molecule agonists or antagonists to promote bone remodeling and discuss their advantages and limitations.
Repurposing Nano Curcumin: Unveiling its Therapeutic Potential in Diabetic Nephropathy.
Sharma R, Mali Y, Agrawal YO … +2 more , Agnihotri VV, Goyal SN
Curr Drug Targets · 2025 · PMID 39779572 · Publisher ↗
Currently, Diabetic Nephropathy (DN) stands as the predominant global cause of endstage renal disease. Many scientists believe that diabetes will eventually spread to pandemic levels due to the rising prevalence of the d...
Currently, Diabetic Nephropathy (DN) stands as the predominant global cause of endstage renal disease. Many scientists believe that diabetes will eventually spread to pandemic levels due to the rising prevalence of the disease. While the primary factor leading to diabetic nephropathy is vascular dysfunction induced by hyperglycemia, several other pathological elements, such as fibrosis, inflammation, and oxidative stress, also contribute to the progression of the disease. The primary targets of current DN therapy approaches are the underlying abnormalities of hypertension and glucose. With several targets and fewer side effects, curcumin is a commonly utilized antioxidant in DN. The present study emphasizes the critical role of oxidative stress and inflammation in the development of diabetic nephropathy. It reveals how these factors induce damage in key kidney cell types, highlighting their potential as therapeutic targets for this disease. In addition, by concentrating on Nrf2, SIRT1, HMGB1, NF-κB, and NLRP3 of curcumin, has strong anti- inflammatory and antioxidant characteristics. This review describes the role of curcumin in the therapeutic application of diabetic nephropathy. In this attempt, we tried to elaborate on the bench-to-bedside aspects of curcumin in DN, including clinical and preclinical investigations. The rationales of curcumin's mechanisms in alleviating symptoms of the DN were discussed. Curcumin could serve as the potential therapeutic agent for the patient seeking to recover from DN.
Pharmacological and Therapeutic Potential of a Natural Flavonoid Icariside II in Human Complication.
Singh D, Singh R
Curr Drug Targets · 2025 · PMID 39757637 · Publisher ↗
Emerging challenges to human health necessitate a coordinated effort to find both preventative and therapeutic techniques, with natural products at the forefront of attempts to gain novel medicines and minimize disease t...
Emerging challenges to human health necessitate a coordinated effort to find both preventative and therapeutic techniques, with natural products at the forefront of attempts to gain novel medicines and minimize disease transmission and related death. The medicinal potential of chemicals contained in plants has been known for centuries, leading to its use in homes and clinics for the treatment of numerous disorders. Despite global advancements, plant-based medicines continue to be utilized to treat various pathological illnesses or as alternatives to contemporary pharmaceuticals. The safety and low toxicity of natural products have led to their increasing acceptability for the prevention or treatment of many ailments. Flavonoids are biologically active compounds that are classified as polyphenols, which are a type of secondary metabolite found in all plants. Icariside II (ICA-II) is one of the secondary metabolites that belong to the flavonoid category of phytochemicals and is present in Maxim. In recent years, ICA-II has been discovered to show anti-inflammatory, antioxidant, anticancer, renal protecting, and cardiac protective effects, as well as several other biological characteristics. This review is focused on the exploration of the pharmacological activities of ICA-II. ICA-II is considered a prospective candidate for future clinical investigations due to a number of therapeutic properties.
Emerging Threats and Challenges of Monkeypox Virus: Exploration and Sensitivity.
Porwal S, Malviya R, Sridhar SB … +1 more , Kaur M
Curr Drug Targets · 2025 · PMID 39754774 · Publisher ↗
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Tachykinin Receptors and their Antagonists: Unraveling Their Role in Metabolic Disorders and Therapeutic Innovations.
Ahsan W, Javed SA, Najmi A … +1 more , Zoghebi K
Curr Drug Targets · 2025 · PMID 41668462 · Publisher ↗
INTRODUCTION: Metabolic disorders are major global health concerns with increasing prevalence worldwide. Experimental evidence suggests the role of tachykinins and their receptors in metabolic regulation, neuroendocrine...
INTRODUCTION: Metabolic disorders are major global health concerns with increasing prevalence worldwide. Experimental evidence suggests the role of tachykinins and their receptors in metabolic regulation, neuroendocrine control, and inflammatory responses. This review aims to explore the implications of tachykinin receptors and their antagonists in the management of metabolic disorders. METHODS: A comprehensive literature search was performed across major scientific databases to identify and analyze preclinical and clinical studies on tachykinin receptors and their antagonists in the context of metabolic disorders. The key mechanisms of action of drugs, important therapeutic outcomes, and challenges associated with drug development were covered. RESULTS: The reported experimental and clinical studies suggest that the antagonists of NK1R, NK2R, and NK3R could influence glucose metabolism, lipid homeostasis, and appetite regulation. While NK1R antagonists, such as aprepitant, demonstrated anti-inflammatory and neuroprotective effects, NK3R antagonists, including fezolinetant, showed promise in modulating energy balance and thermoregulation. DISCUSSION: These studies emphasized the emerging potential of tachykinin receptors and their antagonists in the management of metabolic dysfunctions. However, the challenges associated with its clinical translation, including receptor redundancy, limited biomarker-based patient stratification, and variations in receptor expression across species, are still relevant and need to be addressed to improve therapeutic outcomes. CONCLUSION: Tachykinin receptor antagonists hold significant potential as therapeutic agents in the management of metabolic disorders. Further studies are warranted to overcome translational barriers, address safety issues, validate biomarkers, and refine receptor selectivity to achieve maximum therapeutic benefits.
Novel Glitazones Protect Rotenone-induced Parkinsonism in Mouse Models by Targeting PGC1α.
Ayachit S, Ramesha GB, Krishna KL … +5 more , Pesaladinne UR, Ravanappa PB, Babu DD, Mehdi S, Pathak S
Curr Drug Targets · 2025 · PMID 41668456 · Publisher ↗
INTRODUCTION: Parkinson's disease (PD) is a persistent neurodegenerative condition marked by rising global rates of disability and mortality, warranting the need for new treatment options. The present investigation evalu...
INTRODUCTION: Parkinson's disease (PD) is a persistent neurodegenerative condition marked by rising global rates of disability and mortality, warranting the need for new treatment options. The present investigation evaluated the protective effects of novel glitazones C7 and C25 against rotenone-induced PD in a mouse model. METHODS: Molecular docking using Discovery Studio and molecular dynamics simulations were employed to evaluate the binding ability of C7 and C25 to the PGC-1α target protein. Pharmacokinetic evaluations of C7 and C25 were performed against the standard pioglitazone in the rats model, and acute toxicity assessments were conducted following OECD guidelines 423. The neuroprotective effects of C7 were tested in a rotenone-induced mouse model of PD at doses of 10, 20, and 30 mg/kg body weight. Behavioral studies, including locomotor activity, grip strength, and catalepsy, as well as biochemical analyses such as endogenous antioxidant levels and AChE levels, were assessed. RESULTS: The novel compound C7 demonstrated good binding and simulation at the PGC-1α target protein. The kinetic profile of C7 was found to be good when compared to C25. Both the novel glitazones were safe at 300 mg/kg body weight when tested for oral acute toxicity. The novel compound C7 effectively alleviated symptoms related to rotenone-induced PD, demonstrating its promise as a therapeutic candidate. DISCUSSION: In the rotenone-induced mouse model, compound C7 exhibited a promising anti-PD effect by attenuating oxidative stress and increasing muscular activity, which merits further investigations. CONCLUSION: Additional research using various induction models, along with further investigation of cellular and molecular markers in larger animal studies, is needed to validate these findings.
Emerging Role of NAT10 as ac4C Writer in Inflammatory Diseases: Mechanisms and Therapeutic Applications.
Zhang W, Lu W, Wang M … +4 more , Yao D, Ma J, Hu X, Tao M
Curr Drug Targets · 2025 · PMID 39633518 · Publisher ↗
The incidence of inflammatory diseases, including infections, autoimmune disorders, and tumors, is consistently increasing year by year, posing a significant and growing threat to human health on a global scale. Recent r...
The incidence of inflammatory diseases, including infections, autoimmune disorders, and tumors, is consistently increasing year by year, posing a significant and growing threat to human health on a global scale. Recent research has indicated that RNA acetylation modification, a specific type of post-transcriptional modification, may play a critical role in the pathogenesis of these diseases. Among the various mechanisms of RNA modification, N-acetyltransferase 10 (NAT10) has been identified as the sole cytidine acetyltransferase in eukaryotes. NAT10 is responsible for acetylating mRNA cytosine, which leads to the formation of N4-acetylcytidine (ac4C), a modification that subsequently influences mRNA stability and translation efficiency. Despite these insights, the specific roles and underlying mechanisms by which RNA acetylation contributes to the onset and progression of inflammatory diseases remain largely unclear. This review aimed to elucidate the alterations in NAT10 expression, the modifications it induces in target genes, and its overall contribution to the pathogenesis of various inflammatory conditions. It has been observed that NAT10 expression tends to increase in most inflammatory conditions, thereby affecting the expression and function of target genes through the formation of ac4C. Furthermore, inhibitors targeting NAT10 present promising therapeutic avenues for treating inflammatory diseases by selectively blocking NAT10 activity, thereby preventing the modification of target genes and suppressing immune cell activation and inflammatory responses. This potential for therapeutic intervention underscores the critical importance of further research on NAT10's role in inflammatory disease pathogenesis, as understanding these mechanisms could lead to significant advancements in treatment strategies, potentially transforming the therapeutic landscape for these conditions.
Unraveling Neurological Drug Delivery: Polymeric Nanocarriers for Enhanced Blood-Brain Barrier Penetration.
Inamdar A, Gurupadayya B, Halagali P … +4 more , Tippavajhala VK, Khan F, Pathak R, Sharma H
Curr Drug Targets · 2025 · PMID 39513304 · Publisher ↗
Treating neurological illnesses is challenging because the blood-brain barrier hinders therapeutic medications from reaching the brain. Recent advances in polymeric nanocarriers (PNCs), which improve medication permeabil...
Treating neurological illnesses is challenging because the blood-brain barrier hinders therapeutic medications from reaching the brain. Recent advances in polymeric nanocarriers (PNCs), which improve medication permeability across the blood-brain barrier, may influence therapy strategies for neurological diseases. PNCs have several ways to deliver medications to the nervous system. This review article provides a summary of the parts and manufacturing methods involved in making PNCs. Additionally, it highlights the elements that result in PNCs having enhanced blood-brain barrier penetration. A combination of passive and active targeting strategies is used by PNCs intended to overcome the blood-brain barrier. Among these are micellar structures, nanogels, nanoparticles, cubosomes, and dendrimers. These nanocarriers, which are functionalized with certain ligands that target BBB transporters, enable the direct delivery of drugs to the brain. Mainly, the BBB prevents medications from entering the brain. Understanding the BBB's physiological and anatomical characteristics is necessary to get over this obstacle. Preclinical and clinical research demonstrates the safety and effectiveness of these PNCs, and their potential use in the treatment of neurological illnesses, including brain tumors, Parkinson's disease, and Alzheimer's disease, is discussed. Concerns that PNCs may have about their biocompatibility and possible toxicity are also covered in this review article. This study examines the revolutionary potential of PNCs in CNS drug delivery, potential roadblocks, ongoing research, and future opportunities for PNC design progress. PNCs open the door to more focused and efficient treatment for neurological illnesses by comprehending the subtleties of BBB penetration.
LncRNA HAGLROS: A Vital Oncogenic Propellant in Various Human Cancers.
Yang J, He H, Chen L … +4 more , Wei Y, Liu Y, Li X, Yuan C
Curr Drug Targets · 2025 · PMID 39484770 · Publisher ↗
HAGLR Opposite Strand lncRNA (HAGLROS) is a long non-coding RNA (lncRNA) located on the long arm of human chromosome 2 at locus 2q31.1. Emerging evidence highlights HAGLROS as a pivotal player in human cancers, character...
HAGLR Opposite Strand lncRNA (HAGLROS) is a long non-coding RNA (lncRNA) located on the long arm of human chromosome 2 at locus 2q31.1. Emerging evidence highlights HAGLROS as a pivotal player in human cancers, characterized by its significant upregulation across multiple malignancies where it functions as an oncogenic driver. Its aberrant expression is closely linked to the initiation and progression of 13 distinct cancer types, notably correlating with adverse clinical outcomes and reduced overall survival rates in 9 of these cancer types. Mechanistically, HAGLROS is under the regulatory influence of the transcription factor STAT3, exerts competitive binding to 9 miRNAs, activates 5 signaling pathways pivotal for cancer cell proliferation and metastasis, as well as intricately modulates gene expression profiles. Given its multifaceted roles, HAGLROS emerges as a promising candidate for cancer diagnostics and prognostics. Moreover, its potential as a therapeutic target holds considerable promise for novel treatment strategies in oncology. This review synthesizes current research on HAGLROS, covering its expression patterns, biological roles, and clinical significance in cancer. By shedding light on these aspects, this review aims to contribute new perspectives that advance our understanding of cancer biology, enhance diagnostic accuracy, refine prognostic assessments, and pave the way for targeted therapeutic interventions.
Trends of Artificial Intelligence (AI) Use in Drug Targets, Discovery and Development: Current Status and Future Perspectives.
Mohapatra M, Sahu C, Mohapatra S
Curr Drug Targets · 2025 · PMID 39473198 · Publisher ↗
The applications of artificial intelligence (AI) in pharmaceutical sectors have advanced drug discovery and development methods. AI has been applied in virtual drug design, molecule synthesis, advanced research, various...
The applications of artificial intelligence (AI) in pharmaceutical sectors have advanced drug discovery and development methods. AI has been applied in virtual drug design, molecule synthesis, advanced research, various screening methods, and decision-making processes. In the fourth industrial revolution, when medical discoveries are happening swiftly, AI technology is essential to reduce the costs, effort, and time in the pharmaceutical industry. Further, it will aid "genome-based medicine" and "drug discovery." AI may prepare proactive databases according to diseases, disorders, and appropriate usage of drugs which will facilitate the required data for the process of drug development. The application of AI has improved clinical trials on patient selection in a population, stratification, and sample assessment such as biomarkers, effectiveness measures, dosage selection, and trial length. Various studies suggest AI could be perform better compared to conventional techniques in drug discovery. The present review focused on the positive impact of AI in drug discovery and development processes in the pharmaceutical industry and beneficial usage in health sectors as well.
Current Updates on Pathogenesis, Systemic Therapy, and Treatment of Invasive Fungal Infections.
Singh SK, Pancholi SS
Curr Drug Targets · 2025 · PMID 39421988 · Publisher ↗
Numerous health hazards are associated with fungal infections, ranging from asymptomatic cases to potentially fatal invasive diseases that are especially dangerous for those with impaired immune systems. The main causes...
Numerous health hazards are associated with fungal infections, ranging from asymptomatic cases to potentially fatal invasive diseases that are especially dangerous for those with impaired immune systems. The main causes behind these diseases are opportunistic fungi, namely , and . Invasive fungal infections (IFIs) require a global response that includes the development of vaccines, standardized protocols for diagnosis, potent antifungal medications, and strategies to stop drug-resistant strains. Improving high-risk group diagnosis and treatment is essential to lowering death rates. This review highlights the substantial health concerns associated with fungal infections, especially in immunocompromised individuals, and identifies , and as the main pathogens. It highlights the necessity of international efforts, such as the development of novel diagnostic instruments, imaging methods, and antifungal drugs, to combat these invasive infections. The review also addresses the increasing need for novel treatment approaches in light of the developing resistance to widely used antifungal medications. Furthermore, the significance of secretory proteins in fungal pathogenicity and the potential of combination therapy are investigated. It is also suggested that a multimodal strategy be used to fight these illnesses, given the promise of multivalent vaccinations. Overall, this study emphasizes how critical it is to develop better diagnostic and treatment strategies in order to successfully control and lessen the impact of invasive fungal diseases on the health of the world.
Molecular Insight into Obesity-Associated Nephropathy: Clinical Implications and Possible Strategies for its Management.
Gupta H, Bhandari U
Curr Drug Targets · 2025 · PMID 39411934 · Publisher ↗
Obesity is a significant health concern due to its rapid increase worldwide. It has been linked to the pathogenic factors of renal diseases, cancer, cardiovascular diseases, hypertension, dyslipidemia, and type 2 diabete...
Obesity is a significant health concern due to its rapid increase worldwide. It has been linked to the pathogenic factors of renal diseases, cancer, cardiovascular diseases, hypertension, dyslipidemia, and type 2 diabetes. Notably, obesity raises the likelihood of developing chronic kidney disease (CKD), leading to higher adult mortality and morbidity rates. This study explores the molecular mechanisms that underlie obesity-associated nephropathy and its clinical implications. Obesity-Associated Nephropathy (OAN) develops and worsens due to insulin resistance and hyperinsulinemia, which promote renal sodium reabsorption, glomerular hyperfiltration, and hypertension, leading to progressive kidney damage. Renal damage is further aggravated by persistent inflammation and redox damage, mediated by adipokines and proinflammatory cytokines, such as TNF-α and IL-6. Furthermore, stimulation of the sympathetic nervous system and the renin-angiotensin- aldosterone system (RAAS) intensifies glomerular hypertension and fibrosis. These elements cause glomerular hyperfiltration, renal hypertrophy, and progressive kidney damage. Clinical manifestations of obesity-associated nephropathy include proteinuria, reduced glomerular filtration rate (GFR), and ultimately, CKD. Management strategies currently focus on lifestyle modifications, such as weight loss through diet and exercise, which have been effective in reducing proteinuria and improving GFR. Pharmacological treatments targeting metabolic pathways, including GLP-1 receptor agonists and SGLT2 inhibitors, have shown renoprotective properties. Additionally, traditional RAAS inhibitors offer therapeutic benefits. Early detection and comprehensive management of OAN are essential to prevent its progression and lessen the burden of CKD.
A Review on Nanotechnologically Derived Phytomedicines for the Treatment of Hepatocellular Carcinoma: Recent Advances in Molecular Mechanism and Drug Targeting.
Sahu C, Sahu RK, Roy A
Curr Drug Targets · 2025 · PMID 39385414 · Publisher ↗
The second largest cause of cancer-related death worldwide, Hepatocellular Carcinoma (HCC) is also the most common primary liver cancer. HCC typically arises in patients with liver cirrhosis. Existing synthetic medicines...
The second largest cause of cancer-related death worldwide, Hepatocellular Carcinoma (HCC) is also the most common primary liver cancer. HCC typically arises in patients with liver cirrhosis. Existing synthetic medicines for treating chronic liver disease are ineffective and come with undesirable side effects. Although herbal remedies have widespread popularity, there is still a long road ahead before they are fully accepted by the scientific community. Secondary metabolites and phytochemicals found in plants are abundant in both the human diet and the non-human environment. Natural plant chemicals have been shown to be beneficial as therapeutic and chemopreventive treatments for a wide variety of chronic disorders. Many diseases, including HCC, can be effectively treated with the help of phytochemicals found in food. Resveratrol, curcumin, urolithin A, silibinin, quercetin, N-trans-feruloyl octopamine, emodin, lycopene, caffeine, and phloretin are all examples. Approximately, 60% of all anticancer medications are determined to be derived from natural substances, according to recent studies. Plant derivatives have played an important role in cancer due to their capacity to scavenge free radicals, limit cell proliferation, and set off apoptosis. The progression of HCC is linked to inflammatory signaling pathways, and this study sought to look at how novel approaches, such as phytomedicines, are being used to fight cancer. Recent advancements in molecular mechanisms and drug targeting for HCC have been discussed in this review.
Precision Targeting of BET Proteins - Navigating Disease Pathways, Inhibitor Insights, and Shaping Therapeutic Frontiers: A Comprehensive Review.
Amrutkar RD, Amesar MV, Chavan LB … +2 more , Baviskar NS, Bhamare VG
Curr Drug Targets · 2025 · PMID 39385413 · Publisher ↗
The family of proteins known as Bromodomain and Extra-Terminal (BET) proteins has become a key participant in the control of gene expression, having a significant impact on numerous physiological and pathological mechani...
The family of proteins known as Bromodomain and Extra-Terminal (BET) proteins has become a key participant in the control of gene expression, having a significant impact on numerous physiological and pathological mechanisms. This review offers a thorough investigation of the BET protein family, clarifying its various roles in essential cellular processes and its connection to a variety of illnesses, from inflammatory disorders to cancer. The article explores the structural and functional features of BET proteins, emphasizing their special bromodomain modules that control chromatin dynamics by identifying acetylated histones. BET proteins' complex roles in the development of cardiovascular, neurodegenerative, and cancer diseases are carefully investigated, providing insight into possible treatment avenues. In addition, the review carefully examines the history and relevance of BET inhibitors, demonstrating their capacity to modify gene expression profiles and specifically target BET proteins. The encouraging outcomes of preclinical and clinical research highlight BET inhibitors' therapeutic potential across a range of disease contexts. The article summarizes the state of BET inhibitors today and makes predictions about the challenges and future directions of the field. This article provides insights into the changing field of BET protein-targeted interventions by discussing the potential of personalized medicine and combination therapies involving BET inhibitors. This thorough analysis combines many aspects of BET proteins, such as their physiological roles and their roles in pathophysiological conditions. As such, it is an invaluable tool for scientists and medical professionals who are trying to figure out how to treat patients by using this fascinating protein family.
Envisioning Glucose Transporters (GLUTs and SGLTs) as Novel Intervention against Cancer: Drug Discovery Perspective and Targeting Approach.
Shafi S, Khan MA, Ahmad J … +3 more , Rabbani SA, Singh S, Najmi AK
Curr Drug Targets · 2025 · PMID 39377414 · Publisher ↗
Metabolic reprogramming and altered cellular energetics have been recently established as an important cancer hallmark. The modulation of glucose metabolism is one of the important characteristic features of metabolic re...
Metabolic reprogramming and altered cellular energetics have been recently established as an important cancer hallmark. The modulation of glucose metabolism is one of the important characteristic features of metabolic reprogramming in cancer. It contributes to oncogenic progression by supporting the increased biosynthetic and bio-energetic demands of tumor cells. This oncogenic transformation consequently results in elevated expression of glucose transporters in these cells. Moreover, various cancers exhibit abnormal transporter expression patterns compared to normal tissues. Recent investigations have underlined the significance of glucose transporters in regulating cancer cell survival, proliferation, and metastasis. Abnormal regulation of these transporters, which exhibit varying affinities for hexoses, could enable cancer cells to efficiently manage their energy supply, offering a crucial edge for proliferation. Exploiting the upregulated expression of glucose transporters, GLUTs, and Sodium Linked Glucose Transporters (SGLTs), could serve as a novel therapeutic intervention for anti-cancer drug discovery as well as provide a unique targeting approach for drug delivery to specific tumor tissues. This review aims to discussthe previous and emerging research on the expression of various types of glucose transporters in tumor tissues, the role of glucose transport inhibitors as a cancer therapy intervention as well as emerging GLUT/SGLT-mediated drug delivery strategies that can be therapeutically employed to target various cancers.
An Overview of Research Advances in Oncology Regarding the Transcription Factor ATF4.
Chen Y, Gao Q, Wang D … +4 more , Zou X, Li X, Ji J, Liu B
Curr Drug Targets · 2025 · PMID 39350552 · Publisher ↗
This review provides a comprehensive overview of the recent advancements in research on ATF4 (Activating Transcription Factor 4) within the field of oncology. As a crucial transcription factor, ATF4 has garnered increasi...
This review provides a comprehensive overview of the recent advancements in research on ATF4 (Activating Transcription Factor 4) within the field of oncology. As a crucial transcription factor, ATF4 has garnered increasing attention for its role in cancer research. The review begins with an exploration of the regulatory mechanisms of ATF4, including its transcriptional control, post-translational modifications, and interactions with other transcription factors. It then highlights key research findings on ATF4's involvement in various aspects of tumor biology, such as cell proliferation, differentiation, apoptosis and survival, invasion and metastasis, and the tumor microenvironment. Furthermore, the review discusses the potential of targeting ATF4 as a novel therapeutic strategy for cancer treatment. It also explores how ATF4's interactions with existing anticancer drugs could inform the development of more effective therapeutic agents. By elucidating the role of ATF4 in tumor biology and its potential clinical applications, this review aims to provide new insights and strategies for cancer treatment.
Enhancements in Parkinson's Disease Management: Leveraging Levodopa Optimization and Surgical Breakthroughs.
Sharma R, Kour A, Dewangan HK
Curr Drug Targets · 2025 · PMID 39350551 · Publisher ↗
Parkinson's disease (PD) is a complex neurological condition caused due to inheritance, environment, and behavior among various other parameters. The onset, diagnosis, course of therapy, and future of PD are thoroughly e...
Parkinson's disease (PD) is a complex neurological condition caused due to inheritance, environment, and behavior among various other parameters. The onset, diagnosis, course of therapy, and future of PD are thoroughly examined in this comprehensive review. This review also presents insights into pathogenic mechanisms of reactive microgliosis, Lewy bodies, and their functions in the evolution of PD. It addresses interaction complexity with genetic mutations, especially in genes such as UCH-L1, parkin, and α-synuclein, which illuminates changes in the manner dopaminergic cells handle proteins and use proteases. This raises the improved outcomes and life quality for those with PD. Potential treatments for severe PD include new surgical methods like Deep Brain Stimulation (DBS). Further, exploration of non-motor manifestations, such as cognitive impairment, autonomic dysfunction, and others, is covered in this review article. These symptoms have a significant impact on patients' quality of life. Furthermore, one of the emerging therapeutic routes that are being investigated is neuroprotective medicines that aim to prevent the aggregation of α-synuclein and interventions that modify the progression of diseases. The review concludes by stressing the dynamic nature of PD research and the potential game-changing impact of precision medicines on current approaches to therapy.
Advances in Cysteine Protease B Inhibitors for Leishmaniasis Treatment.
Gini ALR, João EE, Lopes JR … +5 more , Da Cunha PST, Velasquez AMA, Graminha MAS, Dos Santos JL, Scarim CB
Curr Drug Targets · 2025 · PMID 39350405 · Publisher ↗
The expression and release of cysteine proteases by spp. and their virulence factors significantly influence the modulation of host immune responses and metabolism, rendering cysteine proteases intriguing targets for dr...
The expression and release of cysteine proteases by spp. and their virulence factors significantly influence the modulation of host immune responses and metabolism, rendering cysteine proteases intriguing targets for drug development. This review article explores the substantial role of cysteine protease B (CPB) in medicinal chemistry from 2001 to 2024, particularly concerning combatting parasites. We delve into contemporary advancements and potential prospects associated with targeting cysteine proteases for therapeutic interventions against leishmaniasis, emphasizing drug discovery in this context. Computational analysis using the pkCSM tool assessed the physicochemical properties of compounds, providing valuable insights into their molecular characteristics and drug-like potential, enriching our understanding of the pharmacological profiles, and aiding rational inhibitor design. Our investigation highlights that while nonpeptidic compounds constitute the majority (69.2%, 36 compounds) of the dataset, peptidomimetic- based derivatives (30.8%, 16 compounds) also hold promise in medicinal chemistry. Evaluating the most promising compounds based on dissociation constant () and half maximal inhibitory concentration (IC) values revealed notable potency, with 41.7% and 80.0% of nonpeptidic compounds exhibiting values < 1 μM, respectively. On the other hand, all peptidic compounds evaluated for (43.8%) and IC (31.3%) obtained values < 1 μM, respectively. Further analysis identified specific compounds within both categories (nonpeptidic: 1, 2, and 4; peptidic: 48-52) as particularly promising, warranting deeper investigation into their structure-activity relationships. These findings underscore the diverse landscape of inhibitors in medicinal chemistry and highlight the potential of both nonpeptidic and peptide-based compounds as valuable assets in therapeutic development against leishmaniasis.
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