Journal of Enzyme Inhibition and Medicinal Chemistry最新文献_第2页

Synergistic optimizations of efficacy and membrane permeability of IRAK4 inhibitors: identifying new lead compounds for anti-inflammatory therapeutics. IRAK4抑制剂疗效和膜通透性的协同优化：确定抗炎治疗的新先导化合物

IF 5.6 2区医学

Journal of Enzyme Inhibition and Medicinal Chemistry Pub Date : 2025-12-01 Epub Date: 2025-06-19 DOI: 10.1080/14756366.2025.2518491

Kewon Kim, Ahyoung Jang, Hyeonsoo Han, Taeho Kim, Hwangseo Park, Sungwoo Hong

{"title":"Synergistic optimizations of efficacy and membrane permeability of IRAK4 inhibitors: identifying new lead compounds for anti-inflammatory therapeutics.","authors":"Kewon Kim, Ahyoung Jang, Hyeonsoo Han, Taeho Kim, Hwangseo Park, Sungwoo Hong","doi":"10.1080/14756366.2025.2518491","DOIUrl":"10.1080/14756366.2025.2518491","url":null,"abstract":"Interleukin-1 receptor-associated kinase 4 (IRAK4) is a serine/threonine kinase that plays a pivotal role in immune signalling and cytokine regulation, making it a compelling target for the treatment of inflammatory and autoimmune diseases. We initiated a drug discovery campaign based on the N2,N4-diphenylpyrimidine-2,4-diamine (DPDA) scaffold, employing an integrated strategy that combined structure-based de novo design, three-dimensional quantitative structure-activity relationship (3D-QSAR) modelling, and biochemical evaluation. This approach emphasised the optimisation of membrane permeability by controlling the 1-octanol/water partition coefficient (LogP), while also enforcing configurational constraints to enhance IRAK4-specific binding. Through iterative cycles of computational modelling and chemical synthesis, we identified 10 out of 17 newly synthesised compounds that exhibited potent IRAK4 inhibition at low-nanomolar concentrations in both enzymatic and cellular assays. Among these, compounds 10 and 13 stood out, demonstrating strong IRAK4 inhibitory activity, favourable membrane permeability, and minimal off-target kinase interactions.","PeriodicalId":15769,"journal":{"name":"Journal of Enzyme Inhibition and Medicinal Chemistry","volume":"40 1","pages":"2518491"},"PeriodicalIF":5.6,"publicationDate":"2025-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12180326/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144325934","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Discovery of a novel RSK2 inhibitor for the treatment of metastatic pancreatic cancer. 发现一种新的RSK2抑制剂用于治疗转移性胰腺癌。

IF 5.4 2区医学

Journal of Enzyme Inhibition and Medicinal Chemistry Pub Date : 2025-12-01 Epub Date: 2025-08-05 DOI: 10.1080/14756366.2025.2538673

Chi-Hsiu Chung, Kai-Cheng Hsu, Ming-Min Huang, Huang-Ju Tu, Shiow-Lin Pan, Min-Wu Chao

{"title":"Discovery of a novel RSK2 inhibitor for the treatment of metastatic pancreatic cancer.","authors":"Chi-Hsiu Chung, Kai-Cheng Hsu, Ming-Min Huang, Huang-Ju Tu, Shiow-Lin Pan, Min-Wu Chao","doi":"10.1080/14756366.2025.2538673","DOIUrl":"10.1080/14756366.2025.2538673","url":null,"abstract":"Pancreatic cancer is among the most lethal malignancies, with a five-year survival rate of only 6%. For patients with metastatic disease, current treatments extend median survival by merely four months. This study addresses the urgent need for targeted therapies, as no specific drugs are currently available. Clinical analyses revealed significantly elevated RSK2 expression in pancreatic cancer tissues, associated with shorter survival. We aimed to identify a novel RSK2 inhibitor for metastatic pancreatic cancer. Through structure-based virtual screening, we identified NSYSU-115 as a promising candidate with an IC50 of 45.5 nM. At low concentrations, NSYSU-115 significantly suppressed colony formation, while higher concentrations reduced cell viability and proliferation. It also inhibited phosphorylation of IκBα, a known RSK2 substrate, in a dose- and time-dependent manner. Furthermore, NSYSU-115 impaired cell migration and altered epithelial-mesenchymal transition (EMT) markers. These findings highlight NSYSU-115 as a potent kinase inhibitor with promising therapeutic potential for pancreatic cancer treatment.","PeriodicalId":15769,"journal":{"name":"Journal of Enzyme Inhibition and Medicinal Chemistry","volume":"40 1","pages":"2538673"},"PeriodicalIF":5.4,"publicationDate":"2025-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12326382/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144784409","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

The structural basis of aldo-keto reductase 1C3 inhibition by 17α-picolyl and 17(E)-picolinylidene androstane derivatives. 17α-吡咯酰基和17(E)-吡咯酰基雄甾衍生物抑制醛酮还原酶1C3的结构基础。

IF 5.4 2区医学

Journal of Enzyme Inhibition and Medicinal Chemistry Pub Date : 2025-12-01 Epub Date: 2025-09-04 DOI: 10.1080/14756366.2025.2551979

Jovana J Plavša-Puž, Jiří Brynda, Jovana J Ajduković, Sofija Bekić, Andjelka Ćelić, Pavlína Řezáčová, Jana Škerlová, Edward Petri

{"title":"The structural basis of aldo-keto reductase 1C3 inhibition by 17α-picolyl and 17(E)-picolinylidene androstane derivatives.","authors":"Jovana J Plavša-Puž, Jiří Brynda, Jovana J Ajduković, Sofija Bekić, Andjelka Ćelić, Pavlína Řezáčová, Jana Škerlová, Edward Petri","doi":"10.1080/14756366.2025.2551979","DOIUrl":"10.1080/14756366.2025.2551979","url":null,"abstract":"Human aldo-keto reductase 1C3 (AKR1C3) is a steroid modifying enzyme involved in cancer progression. Here, A-ring modified 17α-picolyl and 17(E)-picolinylidene androstane derivatives are shown to inhibit AKR1C3 activity in vitro. None of the androstane derivatives have off-target affinity for the androgen receptor, based on a fluorescence assay in yeast cells. The X-ray structure of AKR1C3 in complex with the strongest inhibitor, a 17α-picolyl androstane with a C3-oxime modification, was determined at 1.7 Å resolution. Based on this crystal structure and molecular docking, inhibition of AKR1C3 by the 17α-picolyl or 17(E)-picolinylidene derivatives depends on interactions between the C3 modification and the NADP+ cofactor, while the C17α-picolyl or C17-picolinylidene group anchors the inhibitor to AKR1C3. Because one AKR1C3 inhibitor identified here was also previously reported to inhibit CYP17, it may be possible for future researchers to design dual AKR1C3/CYP17 inhibitors based on a steroid scaffold for potential treatment of advanced prostate cancers.","PeriodicalId":15769,"journal":{"name":"Journal of Enzyme Inhibition and Medicinal Chemistry","volume":"40 1","pages":"2551979"},"PeriodicalIF":5.4,"publicationDate":"2025-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12412325/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144992733","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Biotin-mediated drug delivery: does the biotin transporter mediate uptake of biotin conjugates? 生物素介导的药物递送：生物素转运体是否介导生物素偶联物的摄取？

IF 5.4 2区医学

Journal of Enzyme Inhibition and Medicinal Chemistry Pub Date : 2025-12-01 Epub Date: 2025-09-07 DOI: 10.1080/14756366.2025.2554896

Ravi Tripathi, Xiaoxiao Yang, Dongning Liu, Wen Lu, Binghe Wang

{"title":"Biotin-mediated drug delivery: does the biotin transporter mediate uptake of biotin conjugates?","authors":"Ravi Tripathi, Xiaoxiao Yang, Dongning Liu, Wen Lu, Binghe Wang","doi":"10.1080/14756366.2025.2554896","DOIUrl":"10.1080/14756366.2025.2554896","url":null,"abstract":"Sodium-dependent multivitamin transporter (SMVT) is a biotin transporter over-expressed in various types of cancer cells and is commonly studied for targeted drug delivery using biotin conjugates. However, such conjugates lack the carboxyl group needed for recognition by SMVT. Previously, we proposed that SMVT is unlikely the transporter of biotin conjugates. To experimentally assess this hypothesis, we examined intracellular enrichment and activation of the biotin-conjugated version of a well-established CO prodrug pair in cell culture. Although prodrug enrichment in SMVT-over-expressing cells was observed, this enrichment was not affected by excess biotin, indicating the lack of competition for SMVT. Additionally, two biotin analogs lacking the carboxyl group exhibited either augmentative or inhibitory effects depending on specific structural features. These findings support the notion that SMVT is not the transporter of biotin conjugates and underscore the need for further mechanistic studies of the transport mechanism(s) of biotin conjugates.","PeriodicalId":15769,"journal":{"name":"Journal of Enzyme Inhibition and Medicinal Chemistry","volume":"40 1","pages":"2554896"},"PeriodicalIF":5.4,"publicationDate":"2025-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12418800/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145015527","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Identification of novel potent peptide inhibitors targeting the polo-box domain of PLK1: structure-based pharmacophore modelling, virtual screening, molecular docking, molecular dynamics study and biological evaluation. 靶向PLK1 polo-box结构域的新型有效肽抑制剂的鉴定：基于结构的药效团建模、虚拟筛选、分子对接、分子动力学研究和生物学评价。

IF 5.4 2区医学

Journal of Enzyme Inhibition and Medicinal Chemistry Pub Date : 2025-12-01 Epub Date: 2025-09-30 DOI: 10.1080/14756366.2025.2563601

Hong Zhou, Lixia Guan, Guoqiang Lin, Xiaotian Yang, Xingxia Zhang, Yejun Si, Yanming Zhang, Juan Chen

{"title":"Identification of novel potent peptide inhibitors targeting the polo-box domain of PLK1: structure-based pharmacophore modelling, virtual screening, molecular docking, molecular dynamics study and biological evaluation.","authors":"Hong Zhou, Lixia Guan, Guoqiang Lin, Xiaotian Yang, Xingxia Zhang, Yejun Si, Yanming Zhang, Juan Chen","doi":"10.1080/14756366.2025.2563601","DOIUrl":"10.1080/14756366.2025.2563601","url":null,"abstract":"Multiple myeloma, a hematological malignancy, shows PLK1 overexpression in cells correlates with poor prognosis, suggesting PLK1 as a potential therapeutic target. In this study, we discovered five peptides (PLs 1-5) targeting the polo box domain (PBD) of PLK1 through an integrated virtual screening strategy. MST assays confirmed that PLs 1-5 had strong binding affinity for PLK1, especially PL-1 (Kd = 3.11 ± 0.05 nM). Meanwhile, the kinase selectivity assay showed that the PL-1 had no significant inhibitory effects on a panel of other kinases. Molecular dynamics simulation further demonstrated the structural stability of PL-1 and PLK1 complex. Notably, PL-1 displayed potent antiproliferative efficacy against U266 multiple myeloma cells (IC50 = 0.09 ± 0.01 µM). PL-1 showed high intracellular uptake capacity. In addition, PL-1 exhibited good biostability in human serum and liver microsomes. Taken together, PL-1 is a potent and highly selective antitumor agent with considerable therapeutic promise for multiple myeloma.","PeriodicalId":15769,"journal":{"name":"Journal of Enzyme Inhibition and Medicinal Chemistry","volume":"40 1","pages":"2563601"},"PeriodicalIF":5.4,"publicationDate":"2025-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12486458/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145199595","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Identification of novel inhibitors of dengue viral NS5 RNA-dependent RNA polymerase through molecular docking, biological activity evaluation and molecular dynamics simulations. 通过分子对接、生物活性评价和分子动力学模拟鉴定登革病毒NS5 RNA依赖RNA聚合酶的新型抑制剂

IF 5.6 2区医学

Journal of Enzyme Inhibition and Medicinal Chemistry Pub Date : 2025-12-01 Epub Date: 2025-02-12 DOI: 10.1080/14756366.2025.2463006

Keli Zong, Chaochun Wei, Wei Li, Cong Wang, Jiajun Ruan, Xiaojing Liu, Susu Zhang, Hong Yan, Ruiyuan Cao, Xingzhou Li

{"title":"Identification of novel inhibitors of dengue viral NS5 RNA-dependent RNA polymerase through molecular docking, biological activity evaluation and molecular dynamics simulations.","authors":"Keli Zong, Chaochun Wei, Wei Li, Cong Wang, Jiajun Ruan, Xiaojing Liu, Susu Zhang, Hong Yan, Ruiyuan Cao, Xingzhou Li","doi":"10.1080/14756366.2025.2463006","DOIUrl":"10.1080/14756366.2025.2463006","url":null,"abstract":"The DENV-NS5 RNA-dependent RNA polymerase (RdRp) is essential for viral replication, and one of the targets of anti-virus. In this study, the Uni-VSW module was used to virtual screen 1.6 million compounds in the ChemDiv and TargetMol (USA) database, 27 candidates were obtained. Thereby 23 candidates were selected based on their binding free energies by 50 ns MD simulations. The biological activity of the candidates and the reference compounds (BCX4430 and Compound 27) were evaluated on their IC50 values against DENV-NGC, CC50 values, and selectivity index. Among these, the IC50 values of D1 and D8 were 13.06 ± 1.17 μM and 14.79 ± 7.76 μM, respectively, which were better than that of Compound 27 (IC50 =19.67 ± 1.12 μM). The comprehensive MD simulations were performed on the candidates to assess the stability behaviour and binding mechanisms. The density functional theory (DFT) analysis was also conducted to explore the structural and electronic properties.","PeriodicalId":15769,"journal":{"name":"Journal of Enzyme Inhibition and Medicinal Chemistry","volume":"40 1","pages":"2463006"},"PeriodicalIF":5.6,"publicationDate":"2025-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11823381/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143399453","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Ferroptosis and hearing loss: from molecular mechanisms to therapeutic interventions. 下垂铁与听力损失：从分子机制到治疗干预。

IF 5.6 2区医学

Journal of Enzyme Inhibition and Medicinal Chemistry Pub Date : 2025-12-01 Epub Date: 2025-02-24 DOI: 10.1080/14756366.2025.2468853

Xingyi Lv, Chenyi Yang, Xianying Li, Yun Liu, Yu Yang, Tongyan Jin, Zhijian Chen, Jinjing Jia, Min Wang, Li Li

引用次数: 0

Bioactivity profiling of Sanghuangporus lonicerinus: antioxidant, hypoglycaemic, and anticancer potential via in-vitro and in-silico approaches. 桑黄孢的生物活性分析：通过体外和计算机方法的抗氧化、降糖和抗癌潜力。

IF 5.6 2区医学

Journal of Enzyme Inhibition and Medicinal Chemistry Pub Date : 2025-12-01 Epub Date: 2025-02-24 DOI: 10.1080/14756366.2025.2461185

Yusufjon Gafforov, Sofija Bekić, Manzura Yarasheva, Jovana Mišković, Nemanja Živanović, Jia Jia Chen, Edward Petri, Bekhzod Abdullaev, Sylvie Rapior, Young Won Lim, Ikram Abdullaev, Arshad Mehmood Abbasi, Soumya Ghosh, Wan Abd Al Qadr Imad Wan-Mohtar, Milena Rašeta

{"title":"Bioactivity profiling of Sanghuangporus lonicerinus: antioxidant, hypoglycaemic, and anticancer potential via in-vitro and in-silico approaches.","authors":"Yusufjon Gafforov, Sofija Bekić, Manzura Yarasheva, Jovana Mišković, Nemanja Živanović, Jia Jia Chen, Edward Petri, Bekhzod Abdullaev, Sylvie Rapior, Young Won Lim, Ikram Abdullaev, Arshad Mehmood Abbasi, Soumya Ghosh, Wan Abd Al Qadr Imad Wan-Mohtar, Milena Rašeta","doi":"10.1080/14756366.2025.2461185","DOIUrl":"10.1080/14756366.2025.2461185","url":null,"abstract":"This study investigates the mycochemical profile and biological activities of hydroethanolic (EtOH), chloroform (CHCl3), and hot water (H2O) extracts of Sanghuangporus lonicerinus from Uzbekistan. Antioxidant capacity was assessed using 2,2-diphenyl-1-picrylhydrazyl (DPPH), 2,2'-azino-bis-3-ethylbenzothiazoline-6-sulfonic acid (ABTS), NO, and FRAP assays, and in vitro hypoglycaemic effects were evaluated through α-amylase and α-glucosidase inhibition. Antiproliferative potential was explored by analysing the binding affinities of EtOH and H2O extracts to estrogen receptor α (ERα), ERβ, androgen receptor (AR), and glucocorticoid receptor (GR), with molecular docking providing structural insights. LC-MS/MS analysis revealed solvent-dependent phenolic profiles, with the EtOH extract containing the highest total phenolic content (143.15 ± 6.70 mg GAE/g d.w.) and the best antioxidant capacity. The EtOH extract showed significant hypoglycaemic effects, with 85.29 ± 5.58% inhibition of α-glucosidase and 41.21 ± 0.79% inhibition of α-amylase. Moderate ERβ binding suggests potential for estrogen-mediated cancer therapy, while strong AKR1C3 inhibition by the EtOH extract supports its therapeutic potential.","PeriodicalId":15769,"journal":{"name":"Journal of Enzyme Inhibition and Medicinal Chemistry","volume":"40 1","pages":"2461185"},"PeriodicalIF":5.6,"publicationDate":"2025-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11852365/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143483233","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Development of ketobenzothiazole-based peptidomimetic TMPRSS13 inhibitors with low nanomolar potency. 低纳摩尔效度酮苯并噻唑类肽类TMPRSS13抑制剂的研制。

IF 5.6 2区医学

Journal of Enzyme Inhibition and Medicinal Chemistry Pub Date : 2025-12-01 Epub Date: 2025-02-20 DOI: 10.1080/14756366.2025.2466841

Alexandre Joushomme, Antoine Désilets, William Champagne, Malihe Hassanzadeh, Gabriel Lemieux, Alice Gravel-Trudeau, Matthieu Lepage, Sabrina Lafrenière, Ulrike Froehlich, Karin List, Pierre-Luc Boudreault, Richard Leduc

{"title":"Development of ketobenzothiazole-based peptidomimetic TMPRSS13 inhibitors with low nanomolar potency.","authors":"Alexandre Joushomme, Antoine Désilets, William Champagne, Malihe Hassanzadeh, Gabriel Lemieux, Alice Gravel-Trudeau, Matthieu Lepage, Sabrina Lafrenière, Ulrike Froehlich, Karin List, Pierre-Luc Boudreault, Richard Leduc","doi":"10.1080/14756366.2025.2466841","DOIUrl":"10.1080/14756366.2025.2466841","url":null,"abstract":"TMPRSS13, a member of the Type II Transmembrane Serine Proteases (TTSP) family, is involved in cancer progression and in respiratory virus cell entry. To date, no inhibitors have been specifically developed for this protease. In this study, a chemical library of 65 ketobenzothiazole-based peptidomimetic molecules was screened against a proteolytically active form of recombinant TMPRSS13 to identify novel inhibitors. Following an initial round of screening, subsequent synthesis of additional derivatives supported by molecular modelling revealed important molecular determinants involved in TMPRSS13 inhibition. One inhibitor, N-0430, achieved low nanomolar affinity towards TMPRSS13 activity in a cellular context. Using a SARS-CoV-2 pseudovirus cell entry model, we further demonstrated the ability of N-0430 to block TMPRSS13-dependent entry of the pseudovirus. The identified peptidomimetic inhibitors and the molecular insights into their potency gained from this study will aid in the development of specific TMPRSS13 inhibitors.","PeriodicalId":15769,"journal":{"name":"Journal of Enzyme Inhibition and Medicinal Chemistry","volume":"40 1","pages":"2466841"},"PeriodicalIF":5.6,"publicationDate":"2025-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11843629/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143458173","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Promoting collagen synthesis: a viable strategy to combat skin ageing. 促进胶原蛋白合成：对抗皮肤老化的可行策略。

IF 5.6 2区医学

Journal of Enzyme Inhibition and Medicinal Chemistry Pub Date : 2025-12-01 Epub Date: 2025-04-11 DOI: 10.1080/14756366.2025.2488821

Shan Wang, Feifan Li, Xilong Feng, Meiling Feng, Xiaotian Niu, Xiaoying Jiang, Wenchao Chen, Renren Bai

{"title":"Promoting collagen synthesis: a viable strategy to combat skin ageing.","authors":"Shan Wang, Feifan Li, Xilong Feng, Meiling Feng, Xiaotian Niu, Xiaoying Jiang, Wenchao Chen, Renren Bai","doi":"10.1080/14756366.2025.2488821","DOIUrl":"https://doi.org/10.1080/14756366.2025.2488821","url":null,"abstract":"Skin ageing is a complex physiological process primarily characterised by the deepening of wrinkles and the sagging of the skin. Collagen is essential for maintaining skin elasticity and firmness. As skin ages, it experiences structural and functional changes in collagen, including a decrease in collagen synthesis and an increase in collagen hydrolysis. Thus, promoting collagen synthesis represents a practical strategy for mitigating skin ageing. This review systematically described the functions, classifications and biosynthesis process of collagen, as well as its role in skin ageing. Additionally, the major signalling pathways and targets associated with collagen synthesis were also discussed. More importantly, the review provided a detailed summary of natural products with collagen synthesis-promoting effects and highlighted small molecule compounds with potential anti-ageing activity, especially PPARδ agonists. The relevant content offers potential targets and lead compounds for the development of anti-skin ageing therapies.","PeriodicalId":15769,"journal":{"name":"Journal of Enzyme Inhibition and Medicinal Chemistry","volume":"40 1","pages":"2488821"},"PeriodicalIF":5.6,"publicationDate":"2025-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11995770/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144012815","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0