286 research outputs found
Orchestrating Cytosolic Access: The Partnership of Cationic Lytic Peptide L17E and Potassium Channel KCa3.1
No full textIn this issue of Molecular Therapy, the study by Kuriyama et al.1 represents an advance in the field of intracellular delivery systems by elucidating a novel mechanism for cytosolic delivery mediated by a cationic amphiphilic lytic peptide L17E (IWLTALKFLGKHAAKHEAKQQLSKL-amide). The investigators demonstrate that the peptide achieves cytosolic delivery primarily through transient plasma membrane disruption, bypassing some of the endocytic pathways, and highlight the pivotal role of the calcium-activated potassium channel KCa3.1, encoded by the gene KCNN4, in facilitating this process. These findings offer a deeper understanding of peptide-mediated delivery using a potassium channel and raise intriguing questions about the broader implications for drug delivery strategies
The Role of Peptides in Combatting HIV Infection: Applications and Insights
Get PDFPeptide-based inhibitors represent a promising approach for the treatment of HIV-1, offering a range of potential advantages, including specificity, low toxicity, and the ability to target various stages of the viral lifecycle. This review outlines the current state of research on peptide-based anti-HIV therapies, highlighting key advancements and identifying future research directions. Over the past few years, there has been significant progress in developing synthetic peptide-based drugs that target various stages of the viral life cycle, including entry and replication. These approaches aim to create effective anti-HIV therapies. Additionally, peptides have proven valuable in the development of anti-HIV vaccines. In the quest for effective HIV vaccines, discovering potent antigens and designing suitable vaccine strategies are crucial for overcoming challenges such as low immunogenicity, safety concerns, and increased viral load. Innovative strategies for vaccine development through peptide research are, therefore, a key focus area for achieving effective HIV prevention. This review aims to explore the strategies for designing peptides with anti-HIV activity and to highlight their role in advancing both therapeutic and preventive measures against HIV
Protein Kinase Inhibitors in Drug Discovery
No full textThis chapter explores the ways in which protein kinase inhibitors perform.https://digitalcommons.chapman.edu/pharmacy_books/1001/thumbnail.jp
ALIH WAHANA DAN RANCANGAN DRAMATURGI NASKAH RANDAI PARANG KAMANG DENGAN GAYA REALISME SOSIAL
No full textNaskah randai Parang Kamang dialih wahana menjadi Naskah Siti Asiah. Pada naskah Siti Asiah berlatar belakang kebudayaan minangkabau pada saat zaman penjajahan Belanda, khususnya pada nagari Kamang. Pihak Belanda mewajibkan rakyat untuk membayar blasting. Masyarakat tidak mau membayar blasting, maka masyarakat melakukan perlawanan. Masyarakat setempat menamai dengan parang kamang. Dari peristiwa tersebut diangkat kembali delam bentuk pertunjukan teater dengan gaya realisme sosial. Yang menjadi pijakan bagi penulis dalam pengalih wahana naskah, setelah naskah randai Parang Kamang dialih wahana menjadi naskah Siti asiah. penulis menganalisis struktur dan teakstur dari naskah Siti Asiah dan membuat rancangan dramaturgi. Randai script “Parang Kamang” is mode-switched into the script of Siti Asiah. The background of Siti Asiah script is Minangkabau culture in Dutch colonial era, particularly in Kamang country. Netherlands required people to pay blasting. People did not want to pay blasting so they rebelled. Local people named this rebellion as Parang Kamang. That event is rewritten into a theater performance with social realism style that becomes the author’s foothold in modeswitching the script after randai script of Parang Kamang is mode-switched into script of Siti Asiah. Author analyzes the structure and texture of Siti Asiah script and make dramaturgy design.
Recent advances in the discovery of Src kinase inhibitors
No full textSrc family kinases are involved in the regulation of a wide variety of normal cellular signal transduction pathways, such as cell growth, differentiation, survival, adhesion and migration. Considerable evidence implicates elevated expression and/or activity of Src kinases in many human cancers, osteoporosis, cardiovascular disorders and immune system dysfunction; thus, this family of protein tyrosine kinases now exists as intriguing targets for both basic research and drug discovery. Herein, a number of examples of currently developed Src family kinase inhibitors in selected patents from 2002 - 2005 will be described. Special attention will be made to the chemical diversity of ATP binding site inhibitors, potency, selectivity and therapeutic application of the compounds. © 2005 Ashley Publications Ltd
Cyclic Peptides with Antifungal Properties Derived from Bacteria, Fungi, Plants, and Synthetic Sources
Get PDFFungal infections remain a significant concern for human health. The emergence of microbial resistance, the improper use of antimicrobial drugs, and the need for fewer toxic antifungal treatments in immunocompromised patients have sparked substantial interest in antifungal research. Cyclic peptides, classified as antifungal peptides, have been in development as potential antifungal agents since 1948. In recent years, there has been growing attention from the scientific community to explore cyclic peptides as a promising strategy for combating antifungal infections caused by pathogenic fungi. The identification of antifungal cyclic peptides from various sources has been possible due to the widespread interest in peptide research in recent decades. It is increasingly important to evaluate narrow- to broad-spectrum antifungal activity and the mode of action of synthetic and natural cyclic peptides for both synthesized and extracted peptides. This short review aims to highlight some of the antifungal cyclic peptides isolated from bacteria, fungi, and plants. This brief review is not intended to present an exhaustive catalog of all known antifungal cyclic peptides but rather seeks to showcase selected cyclic peptides with antifungal properties that have been isolated from bacteria, fungi, plants, and synthetic sources. The addition of commercially available cyclic antifungal peptides serves to corroborate the notion that cyclic peptides can serve as a valuable source for the development of antifungal drugs. Additionally, this review discusses the potential future of utilizing combinations of antifungal peptides from different sources. The review underscores the need for the further exploration of the novel antifungal therapeutic applications of these abundant and diverse cyclic peptides
Development of Cytarabine Prodrugs and Delivery Systems for Leukemia Treatment
Get PDFImportance of the field: Cytarabine is a polar nucleoside drug used for the treatment of myeloid leukemia and non-Hodgkin’s lymphoma. The drug has a short plasma half-life, low stability, and limited bioavailability. Overdosing of patients with continuous infusions may lead to side effects. Thus, various prodrug strategies and delivery systems have been extensively explored to enhance the half-life, stability, and delivery of cytarabine. Among the recent cytarabine prodrugs, amino acid conjugate ValCytarabine and fatty acid derivative CP-4055 (in phase 3 trials) have been investigated for the treatment of leukemia and solid tumors, respectively. Alternatively, delivery systems of cytarabine have emerged for the treatment of different cancers. The liposomal-cytarabine formulation (DepoCyt®) has been approved for the treatment of lymphomatous meningitis.
Areas covered in this review: Various prodrug strategies evaluated for cytarabine are discussed. Then, the review summarizes the drug delivery systems that have been used for more effective cancer therapy. What reader will gain: This review provides in-depth discussion of the prodrug strategy and delivery systems of cytarabine derivatives for the treatment of cancer. The design of cytarabine prodrugs and delivery systems provide insights for designing the next generation of more effective anticancer agents with enhanced delivery and stability.
Take home message: Strategies on designing cytarabine prodrug and delivery formulations showed great promise in developing effective anticancer agents with better therapeutic profile. Similar studies with other anticancer nucleosides can be an alternative approach to gaining access to more effective anticancer agents
Inflammation and Detection: Rethinking the Biomarker Landscape in Gastric Cancer
Get PDFGastric carcinoma is a leading cause of cancer-related mortality worldwide, yet reliable noninvasive biomarkers for its early detection remain limited. As research continues to elucidate the inflammatory underpinnings of tumor initiation and progression, it has become increasingly clear that pro-inflammatory cytokines may hold promise as diagnostic adjuncts. Serum cytokines such as interleukin (IL)-1β, IL-6, IL-8, and interferon-gamma have been frequently reported as elevated in gastric cancer patients compared to healthy individuals. These molecules, known for their roles in modulating tumor-promoting inflammation, angiogenesis, and immune evasion, may serve as accessible indicators of disease presence or progression. Several studies have shown that individual cytokines, particularly IL-6 and IL-8, can achieve receiver operating characteristic curves and area under the curve values exceeding 0.70, suggesting reasonable diagnostic utility. We assess the comparative utility of individual cytokines versus multiplex panels, evaluate their roles in tumor biology and treatment resistance, and situate these findings within the broader inflammatory biomarker landscape. Limitations of the current literature, including small sample sizes, heterogeneity in study design, and lack of specificity, are critically discussed. We advocate for prospective, multicenter validation studies and highlight the promise of integrating inflammatory cytokine profiling into diagnostic algorithms. Composite cytokine panels may better reflect the complex immunobiology of tumor progression and offer a scalable, accessible adjunct to current gastric cancer screening strategies
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