Current medicinal chemistry最新文献

{"title":"Anticancer and Cyclooxygenase Inhibitory Activity of Benzylidene Derivatives of Fenobam and its Thio Analogues.","authors":"Wafa Hourani, Pran Kishore Deb, Maysa Alhawamdeh, Nizar Al-Shari, Pobitra Borah, Lina A Dahabiyeh, Abdulmuttaleb Yousef Jaber, Nefisath P, Shashiprabha S, Jagadeesh Prasad Dasappa, Katharigatta N Venugopala","doi":"10.2174/0109298673345068241120045638","DOIUrl":"https://doi.org/10.2174/0109298673345068241120045638","url":null,"abstract":"<p><strong>Introduction: </strong>A series of benzylidene derivatives of fenobam and its thio analogues (1-22) have been evaluated for their cytotoxicity against breast cancer (MCF-7, MDA-MB-231), ovarian cancer (A2780, SKOV-3) and cervical cancer (HELA) cell lines.</p><p><strong>Method: </strong>These compounds (1-22) exhibited 72-83% inhibition of Erk activity against the ovarian cancer cell line (A2780). Compounds 3 and 20 showed the highest DNA damage effect in Comet Assay against the A2780 cancer cell line as compared to the other tested analogues (4, 8, 11, 12, and 13) by using % Tail DNA and OTM. Compounds 3, 4, and 11 showed significant activities and selectivity towards COX-2 with 78%, 97%, and 89% inhibition, as compared to 17%, 57%, and 26% inhibition against COX-1 isoenzyme, respectively.</p><p><strong>Results: </strong>Interestingly, molecular docking scores were also in very good agreement with the experimental results regarding discriminating the selectivity index of the tested compounds against COX-1 & COX-2 enzymes. Further molecular dynamics (MD) simulation study revealed that the most selective compound, 13, binds with the COX-2 enzyme in a similar fashion to that of Rofecoxib, which was further supported by their MD-based free binding energies (MM-GBSA) of -49.76 ± 4.27 kcal/mol, and -44.84 ±3.78 kcal/mol, respectively.</p><p><strong>Conclusion: </strong>Moreover, in silico ADMET predictions showed adequate properties for these compounds, making them promising leads worthy of further optimization.</p>","PeriodicalId":10984,"journal":{"name":"Current medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.5,"publicationDate":"2024-12-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142834393","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"An Updated Review Deciphering Apigenin Nanostructures as Promising Therapeutic Efficiency in Human Carcinomas.","authors":"Fahad Khan, Mir Waqas Alam, Seema Ramniwas, Indra Rautela, Sorabh Lakhanpal, Pratibha Pandey","doi":"10.2174/0109298673339611241031031946","DOIUrl":"https://doi.org/10.2174/0109298673339611241031031946","url":null,"abstract":"<p><p>Apigenin (APG) is being investigated for its potential in treating different forms of cancer. It can regulate many cellular processes, such as cell proliferation, apoptosis, cell cycle arrest, invasion, metastasis, and autophagy, via controlling multiple cellular signaling pathways. In addition, this chemical demonstrates a significant preference for cancer cells over healthy cells. This is a crucial factor when compared to other treatments for cancer. However, apigenin is distinguished by its limited ability to dissolve in water, sluggish absorption when taken orally, rapid metabolism, and strong affinity for binding to plasma proteins. Therefore, oral dosing generally results in low plasma concentrations. Nanotechnology is being developed to address the constraints of pharmacokinetics and physicochemical properties. It offers a precise and regulated method for delivering drugs, enhancing oral absorption, improving their solubility in water, and reducing side effects. The mechanism of action of apigenin has persuaded the scientific community to acknowledge it as an anticancer drug, hence supporting the utility of apigenin nano formulations as a contemporary therapeutic tool. Nonetheless, diverse nanocarriers for apigenin have effectively addressed inadequate water solubility and non-specificity towards target tissues. This review summarizes diverse biological aspects of apigenin and elaborates on the issues associated with using apigenin nanocarriers to enhance its efficacy in human carcinomas. Subsequent in vivo tests showed its capacity to decrease tumor size, prompting further experimentation with human subjects.</p>","PeriodicalId":10984,"journal":{"name":"Current medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.5,"publicationDate":"2024-12-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142834391","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"FHL1 Inhibition by Mir-1301-3p Promotes Uterine Corpus Endometrial Carcinoma Cell Proliferation and Migration: A Prognostic Insight.","authors":"Mengna Zhu, Buze Chen, Lu Miao, Jieyun Sun, Yuanyuan Li, Pei Zhang, Xiaoyuan Lu","doi":"10.2174/0109298673341564241031063856","DOIUrl":"https://doi.org/10.2174/0109298673341564241031063856","url":null,"abstract":"<p><strong>Background: </strong>The impact of microRNA-1301-3p (miR-1301-3p) on various cancer subtypes is noteworthy. However, its specific role within the framework of uterine corpus endometrial carcinoma (UCEC) is yet to be clearly defined.</p><p><strong>Objective: </strong>The objective of this research was to investigate and clarify the function of miR-1301-3p in relation to UCEC.</p><p><strong>Methods: </strong>Sample data for our study were sourced from The Cancer Genome Atlas (TCGA). Using various statistical techniques, we assessed the potential of miR-1301-3p as a diagnostic and prognostic indicator, as well as its association with clinical characteristics. Additionally, we conducted an analysis of the genes targeted by miR-1301-3p. The expression levels of miR-1301-3p in uterine corpus endometrial carcinoma (UCEC) cell lines were determined by quantitative real-time PCR (qRT-PCR). Cellular viability and migratory capacity were measured using the CCK8 assay and Transwell migration assays, respectively. Moreover, the expression levels of genes and proteins targeted by miR-1301-3p were identified through dual-luciferase reporter gene assays and Western blot analysis.</p><p><strong>Results: </strong>Expression patterns of miR-1301-3p varied across cancer subtypes, which were significantly linked to specific histological classifications, achieving statistical significance (p < 0.001). In UCEC, higher miR-1301-3p levels correlated with reduced overall survival (p = 0.012) and progression-free survival (p = 0.016), and it emerged as an independent prognostic marker for UCEC. A comparative analysis revealed significantly higher miR-1301-3p levels in UCEC cell lines compared to normal endometrial epithelial cells. Four and a half LIM domains 1 (FHL1) exhibited a negative correlation with miR-1301-3p levels within UCEC tissue samples. miR-1301-3p was shown to promote UCEC cell proliferation and migration through its binding to the 3'-untranslated region (UTR) of the FHL1 gene, thereby repressing FHL1 expression. Additionally, augmenting FHL1 levels was observed to counteract the enhancing impact of miR-1301-3p on UCEC cells.</p><p><strong>Conclusion: </strong>miR-1301-3p regulates the proliferation and migration of UCEC cells by interacting with the FHL1 gene. miR-1301-3p may serve as a promising prognostic biomarker in UCEC.</p>","PeriodicalId":10984,"journal":{"name":"Current medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.5,"publicationDate":"2024-12-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142812667","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"ORG-317 Repurposing as a Potential Agonist Targeting TMEM236 in Colorectal Cancer Treatment: Insights from Molecular Dynamics Simulation, Principal Component Analysis, and Free Energy Landscape Study.","authors":"Neha Shree Maurya, Shikha Kushwah, Amit Chaudhary, Kavita Patel, Shruti Shukla, Ashutosh Mani","doi":"10.2174/0109298673322888240718104833","DOIUrl":"https://doi.org/10.2174/0109298673322888240718104833","url":null,"abstract":"<p><p><p> Background and objective: Colorectal Cancer (CRC) affects the colon and rectum part of the digestive system and is a significant global health concern, with approximately 1.1 million new cases annually. It ranks second in cancer-related deaths. Studies have shown future projections of CRC cases to enhance at a worrisome rate, estimating 3.2 million new cases and 1.6 million deaths worldwide by 2040. Studies have shown the downregulation of TMEM236 in CRC, and this study aimed to find the agonist to restore the function of TMEM236 via the drug repurposing method. </p><p> Methods: The different molecular and structural level analyses were performed to understand how the TMEM236 expression can be restored. To obtain the molecular level data, the following analyses were employed to understand the binding affinity and agonistic behaviour of the screened drugs: molecular docking, oral toxicity prediction, Molecular Dynamics (MD) simulation, Free Energy Landscape (FEL) analysis, and g_mmpbsa. </p><p> Results: The molecular docking, oral toxicity, and molecular interaction analyses have identified db06435, db05423, and db15197 drugs from the DrugBank database to either belong to an approved or investigational class of drugs as a potential agonist for TMEM236. The MD simulation and PCA analysis had shown db05423 (ORG-317) to exhibit stable interaction with TMEM236 protein. Similar results were obtained through FEL analysis. </p><p> Conclusion: The downregulation of TMEM236 expression and its constant binding affinity with db05423 during MD simulation suggest that this drug may restore the diminished function and expression of TMEM236. Additionally, it could function as an agonist and can be used for CRC treatment.</p>.</p>","PeriodicalId":10984,"journal":{"name":"Current medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.5,"publicationDate":"2024-12-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142767328","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Development and Validation of a Diagnostic Model for AKI Based on the Analysis of Ferroptosis-related Genes.","authors":"Hengyue Zhu, Xuejia Yang, Ziwei Yuan, Zujian Hu, Yangyang Guo, Yongheng Bai, Jingzong Zhou","doi":"10.2174/0109298673296300240829075534","DOIUrl":"https://doi.org/10.2174/0109298673296300240829075534","url":null,"abstract":"<p><strong>Background: </strong>Acute kidney injury (AKI) is a common renal condition associated with various factors, including pre-renal, post-renal, and renal causes, with ischemia- reperfusion being a frequent contributor leading to tubular injury. Early identification of AKI is crucial but remains challenging.</p><p><strong>Methods: </strong>This study explored the molecular signature of AKI using gene microarray data from the GEO dataset, focusing on identifying ferroptosis-related features through three machine-learning algorithms. We also validated potential biomarkers through a hypoxia/ reoxygenation model.</p><p><strong>Results: </strong>ROC curves, expression differences, and associations with immune cells were analyzed for the three markers to confirm their potential as AKI biomarkers, each demonstrating strong diagnostic ability. Combining these markers proved more effective.</p><p><strong>Conclusion: </strong>The combination of AEBP2, MDM2, and NR4A1 as diagnostic biomarkers for AKI not only enhances detection capability but also holds promise as a significant tool in clinical practice, providing patients with diagnostic and therapeutic guidance.</p>","PeriodicalId":10984,"journal":{"name":"Current medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.5,"publicationDate":"2024-11-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142685999","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Fibroblast Heterogeneity in Hepatocellular Carcinoma and Identification of Prognostic Markers Based on Single-cell Transcriptome Analysis.","authors":"Junjun Jia, Xinyu Gu, Qingfei Chu","doi":"10.2174/0109298673348482241028074147","DOIUrl":"https://doi.org/10.2174/0109298673348482241028074147","url":null,"abstract":"<p><strong>Background: </strong>HCC is a malignant tumor with high morbidity and mortality. Fibroblasts play a key role in the tumor microenvironment (TME). However, the transcriptional regulatory mechanisms of fibroblasts remained unclear in HCC.</p><p><strong>Aim: </strong>The aim of this study was to explore the complex role of fibroblasts in hepatocellular carcinoma (HCC) and to reveal their transcriptional regulatory mechanisms.</p><p><strong>Objective: </strong>The goal of this study was to discover potential prognostic markers for HCC by analyzing the genetic variations and differentiation process of fibroblasts.</p><p><strong>Methods: </strong>Single-cell transcriptome data from the non-tumor liver site and primary tumor site of HCC were acquired from GSE149614, processed, and clustered using the Seurat pipeline. The inferCNV algorithm was applied to infer copy number variations (CNVs) in fibroblasts. Subsequently, the mechanism underlying the interaction between fibroblasts and other cells in the TME of HCC was analyzed using CellChat software. The trajectory of cellular differentiation of fibroblasts from normal state to malignant state was examined using Monocle 2. SCENIC analysis was performed to identify key transcription factors (TFs) in fibroblasts and assess their correlation with HCC prognosis. Finally, qRT-PCR and Transwell assays were carried out to analyze the mRNA expression and cell metastasis.</p><p><strong>Results: </strong>We identified a total of nine different cell types (B cells, cycling cells, endothelial cells, epithelial cells, fibroblasts, hepatocytes, macrophages, plasma cells, and T cells) based on the single-cell transcriptomic data of HCC. Among them, fibroblasts were highly enriched at the primary tumor site, and their number increased with advanced stages. In addition, significant deletions were detected on chromosome 6p of fibroblasts, and genes in this region were remarkably enriched in pathways associated with antigen processing and presentation. Intercellular communication showed that epithelial cells regulated fibroblasts the most. The differentiation of fibroblasts was mainly accompanied by a transition from normal to malignant state. Importantly, CEBPD and FOSB, the TFs most associated with the putative timing of fibroblasts, were under-expressed in human hepatocytes and showed a significant correlation with HCC prognosis. Overexpressed CEBPD inhibited HCC cell migration and invasion.</p><p><strong>Conclusion: </strong>In conclusion, our study revealed that fibroblast recruitment and differentiation, as well as copy number loss at chromosome 6p, were associated with a higher degree of malignancy and immune dysfunction in HCC. The current discoveries provided new insights into the clinical treatment and diagnosis of HCC.</p>","PeriodicalId":10984,"journal":{"name":"Current medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.5,"publicationDate":"2024-11-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142616438","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Stimuli-Responsive Nano/Biomaterials for Smart Drug Delivery in Cardiovascular Diseases: Promises, Challenges and Outlooks.","authors":"Pegah Vosoughi, Seyed Morteza Naghib, M R Mozafari","doi":"10.2174/0109298673319981241021063524","DOIUrl":"https://doi.org/10.2174/0109298673319981241021063524","url":null,"abstract":"<p><p>Cardiovascular Diseases (CVDs) are responsible for the highest number of deaths and disabilities globally. Although numerous therapeutic options exist for treating CVDs, most traditional strategies have proven ineffective in halting or significantly slowing disease progression, often leading to unfavorable side effects. Using nanocarriers represents an innovative strategy for treating CVD, enabling the personalized delivery of medications to precise locations within the cardiovascular system. Despite significant advancements in pharmacological treatments, challenges persist in effectively administering drugs to the CV system. Employing nanocarriers represents an innovative strategy for treating CVD, enabling the tailored administration of medications to precise locations within the cardiovascular system. Various studies have determined the future outlook of nanomedicines for clinical applications as nanocarrier design continues to improve, leading to enhanced drug delivery and treatment outcomes. The article focuses on the delivery systems of drugs that are effective strategies for treating cardiovascular diseases. This manuscript also seeks to explore new possibilities for how the emerging concept of nanotherapeutics could revolutionize our traditional diagnostic and treatment methods in the coming years.</p>","PeriodicalId":10984,"journal":{"name":"Current medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.5,"publicationDate":"2024-11-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142603541","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"The Risk Genes S1PR5, CMC1, and ASAH1 as Potential Targets for the Diagnosis, Immunotherapy, and Treatment of Colon Adenocarcinoma by Single-Cell and Bulk RNA Sequencing Analysis","authors":"Zipeng Xu, Jiantao Gong, Weidong Hu, Chen Ge, Genxi Tong, Fengjun Cai, Zhenghai Zhu, Yihang Yuan, Chaobo Chen","doi":"10.2174/0109298673331144241009082052","DOIUrl":"10.2174/0109298673331144241009082052","url":null,"abstract":"<p><strong>Objective: </strong>Globally, one of the main causes of cancer-related mortality is Colon Adenocarcinoma (COAD). In this study, a new special Immune Cell Functions (ICF) risk model was constructed using single-cell and bulk RNA sequencing data to develop a new understanding and clinical applications for COAD.</p><p><strong>Methods: </strong>The immune function gene sets were downloaded from a literature reference, and the\u0000COAD single-cell dataset GSE146771 was downloaded from the Tumour Immune Single Cell\u0000Hub database. Using Lasso analysis, a multiple gene signature was made from the enrichment\u0000scores of immune function gene sets that were enriched in different ways. Robust validation of\u0000the signature was then performed in multiple independent cohorts. After that, we built the model\u0000using a 10-fold cross-test and evaluated its independence for clinical usage using a nomogram.\u0000We also investigated the connection between signature and immune function, genetic variation,\u0000immunotherapy, and the cancer immunological microenvironment. Lastly, we used qPCR and\u0000immunohistochemistry to examine the expression of the unreported model genes. To find the\u0000regulatory functions of unreported model genes, an EdU assay was employed.</p><p><strong>Results: </strong>First, 20 differentially enriched immune function gene sets were identified. Ten genes can be used as a risk profile to assess the prognosis of colon cancer, according to Lasso regression analysis. Signature performance was stable in both the training cohort and two independent GEO external cohorts, and risk scores were confirmed as independent prognostic factors. At the same time, our risk model continued to be highly predictive across various clinical clusters and clinical characteristics, such as immune checkpoints, tumour genome mutations, and chemotherapeutic drug resistance. Patients in the low-risk group have exhibited a higher chance of benefiting from immunotherapy, according to immunotherapy response research. qPCR and immunohistochemistry analysis have revealed S1PR5 expression as high in COAD tissues, while CMC1 and ASAH1 expression has been found to be low. According to the findings of the functional experiment, S1PR5, CMC1, and ASAH1 may control the ability of CRC cells to proliferate.</p><p><strong>Conclusion: </strong>In this study, using scRNA-seq and bulk RNA-seq data, we created a risk model to predict the prognosis and effectiveness of immunotherapy in patients with COAD. In addition, we have discovered three model genes (S1PR5, CMC1, and ASAH1) that have not been reported before. These genes have the potential to be novel therapeutic targets in Colorectal Cancer (CRC). These findings suggest that this model could be used to evaluate the prognostic risk and identify potential targets for COAD patient treatment.</p>","PeriodicalId":10984,"journal":{"name":"Current medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.5,"publicationDate":"2024-11-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142603542","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"C-Reactive Protein Biosensor for Diagnosing Infections Caused by Orthopedic Trauma.","authors":"Xiancui Liu, Cunhua Wang, Honglong Fu, Xudong Li, Subash C B Gopinath, Sreeramanan Subramaniam","doi":"10.2174/0109298673322598241021111322","DOIUrl":"https://doi.org/10.2174/0109298673322598241021111322","url":null,"abstract":"<p><strong>Introduction: </strong>Infections linked to orthopedic trauma are common complications that place a significant strain on the healthcare system. Immediate identification of the infection and its severity is essential for providing effective treatment.</p><p><strong>Method: </strong>C-reactive Protein (CRP) is a commonly used inflammatory marker in orthopedic surgery and has proven to be a valuable biomarker for diagnosing and monitoring infections. Specifically, CRP aids in the early identification of postoperative infections. This research work has focused on developing a highly sensitive CRP biosensor using iron oxide nanomaterial-modified dielectric sensors.</p><p><strong>Result: </strong>Gold Urchin (GU)-conjugated aptamers and antibodies were used as probes and attached to the electrode via amine linkers. The aptamer-GU-antibody-modified electrode detected CRP at concentrations as low as 1 pg/mL, with an R2 value of 0.9942. Furthermore, CRP-spiked serum exhibited an increase in current response at all concentrations of CRP, indicating selective detection of CRP. Additionally, control experiments using complementary sequences of the aptamer, relevant proteins, and non-immune antibodies did not enhance the current responses, confirming the specific identification of CRP.</p><p><strong>Conclusion: </strong>The sensing strategy has enabled the detection of CRP at its lowest levels, facilitating the identification of infections during orthopedic surgery and subsequent treatment.</p>","PeriodicalId":10984,"journal":{"name":"Current medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.5,"publicationDate":"2024-11-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142603540","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Advances in Discovery and Design of Anti-influenza Virus Peptides.","authors":"Shixin Li, Xi Xie, Shaofen Zhou, Jian He","doi":"10.2174/0109298673325318241004100506","DOIUrl":"https://doi.org/10.2174/0109298673325318241004100506","url":null,"abstract":"<p><p>The influenza virus, a well-known pathogen that causes respiratory illness, remains an important global health threat because of the significant morbidity and mortality rates of people infected with the virus annually. The influenza virus undergoes frequent antigenic variation, and with the increasing frequency of resistant influenza strains against existing antiviral drugs, there is an urgent need for the development of new anti- influenza treatment strategies. Peptides have the potential to offer high potency, selectivity, and relatively low drug resistance. As such, the design and screening of novel anti- influenza virus peptides with high potency have become increasingly important in an effort to fight global influenza epidemics. Herein, we introduce three approaches to developing anti-influenza virus peptides: discovery from natural products, library construction for antiviral peptide screening, and rational design based on functional regions of influenza viral proteins. This review summarizes recent progress in the discovery and design of anti-influenza virus peptides over the past 20 years.</p>","PeriodicalId":10984,"journal":{"name":"Current medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.5,"publicationDate":"2024-11-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142603539","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}