Journal of Enzyme Inhibition and Medicinal Chemistry最新文献_第4页

Rational design, synthesis, and molecular modelling insights of dual DNA binders/DHFR inhibitors bearing arylidene-hydrazinyl-1,3-thiazole scaffold with apoptotic and anti-migratory potential in breast MCF-7 cancer cells. 具有乳腺癌MCF-7细胞凋亡和抗迁移潜力的芳基烯-肼基-1,3-噻唑支架双DNA结合物/DHFR抑制剂的合理设计、合成和分子建模见解

IF 5.6 2区医学

Journal of Enzyme Inhibition and Medicinal Chemistry Pub Date : 2025-12-01 Epub Date: 2025-03-04 DOI: 10.1080/14756366.2025.2468353

Marwa H El-Wakil, Rasha A Ghazala, Hadeel A El-Dershaby, Danuta Drozdowska, Agnieszka Wróbel-Tałałaj, Cezary Parzych, Artur Ratkiewicz, Beata Kolesińska, Heba A Abd El-Razik, Farid S G Soliman

{"title":"Rational design, synthesis, and molecular modelling insights of dual DNA binders/DHFR inhibitors bearing arylidene-hydrazinyl-1,3-thiazole scaffold with apoptotic and anti-migratory potential in breast MCF-7 cancer cells.","authors":"Marwa H El-Wakil, Rasha A Ghazala, Hadeel A El-Dershaby, Danuta Drozdowska, Agnieszka Wróbel-Tałałaj, Cezary Parzych, Artur Ratkiewicz, Beata Kolesińska, Heba A Abd El-Razik, Farid S G Soliman","doi":"10.1080/14756366.2025.2468353","DOIUrl":"10.1080/14756366.2025.2468353","url":null,"abstract":"In light of searching for new breast cancer therapies, DNA-targeted small molecules were rationally designed to simultaneously bind DNA and inhibit human dihydrofolate reductase (hDHFR). Fourteen new arylidene-hydrazinyl-1,3-thiazoles (5-18) were synthesised and their dual DNA groove binding potential and in vitro hDHFR inhibition were performed. Two compounds, 5 and 11, proved their dual efficacy. Molecular docking and molecular dynamics simulations were performed for those active derivatives to explore their mode of binding and stability of interactions inside DHFR active site. Anti-breast cancer activity was assessed for 5 and 11 on MCF-7 cells using MTX as reference. IC50 measurements revealed that both compounds were more potent and selective than MTX. Cytotoxicity was examined against normal skin fibroblasts to examine safety and selectivity Moreover, mechanistic studies including apoptosis induction and wound healing were performed. Further in silico ADMET assessment was conducted to determine their eligibility as drug leads suitable for future optimisation and development.","PeriodicalId":15769,"journal":{"name":"Journal of Enzyme Inhibition and Medicinal Chemistry","volume":"40 1","pages":"2468353"},"PeriodicalIF":5.6,"publicationDate":"2025-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11881662/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143542164","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 PLK1 inhibitor with high inhibitory potency using a combined virtual screening strategy. 使用联合虚拟筛选策略发现一种具有高抑制效力的新型PLK1抑制剂。

IF 5.6 2区医学

Journal of Enzyme Inhibition and Medicinal Chemistry Pub Date : 2025-12-01 Epub Date: 2025-03-07 DOI: 10.1080/14756366.2025.2467798

Zhen Xu, Lixia Guan, Yuting Wang, Miao-Miao Niu, Yashi Ruan, Cen Xu, Li Yang

引用次数: 0

Production and functional characteristics of a novel hirudin variant with better anticoagulant activities than bivalirudin. 一种抗凝血活性优于比伐鲁定的水蛭素新变体的制备及其功能特征。

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: 10.1080/14756366.2025.2554899

Peijuan Ge, Min Jin, Zimo Li, Licheng Zhu

{"title":"Production and functional characteristics of a novel hirudin variant with better anticoagulant activities than bivalirudin.","authors":"Peijuan Ge, Min Jin, Zimo Li, Licheng Zhu","doi":"10.1080/14756366.2025.2554899","DOIUrl":"10.1080/14756366.2025.2554899","url":null,"abstract":"Current antithrombotic therapies face dual constraints of bleeding complications and monitoring requirements. Although natural hirudin provides targeted thrombin inhibition, its clinical adoption is hindered by sourcing limitations. This study developed a recombinant hirudin variant HMg (rHMg) with enhanced anticoagulant activity through genetic engineering and established cost-effective large-scale production methods. The synthesised HMg gene was expressed in E. coli BL21 via a pET vector plasmid, followed by nickel-affinity purification. Systematic evaluations demonstrated rHMg's antithrombin activity of 9573 ATU/mg, dose-dependent prolongation of APTT/PT/TT. It has superior thrombin inhibition with the IC50 and Ki values were 2.8 and 0.323 nM respectively compared to FDA approved drug bivalirudin (p < 0.001). The high-yield prokaryotic expression of rHMg with enhanced anticoagulant efficacy provides a novel strategy for developing affordable antithrombotic drugs, showing significant potential for cardiovascular disease management.","PeriodicalId":15769,"journal":{"name":"Journal of Enzyme Inhibition and Medicinal Chemistry","volume":"40 1","pages":"2554899"},"PeriodicalIF":5.4,"publicationDate":"2025-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12416005/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145015546","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

High-throughput virtual screening, identification and in vitro biological evaluation of novel inhibitors of PLK1 and NRP1. 新型PLK1和NRP1抑制剂的高通量虚拟筛选、鉴定及体外生物学评价

IF 5.4 2区医学

Journal of Enzyme Inhibition and Medicinal Chemistry Pub Date : 2025-12-01 Epub Date: 2025-08-18 DOI: 10.1080/14756366.2025.2514677

Yang Xia, Yuting Chang, Lixia Guan, Yifei Geng, Qi Zhang, Xiaozhou Shen, Qian Bu, Miao-Miao Niu, Gaohua Han

{"title":"High-throughput virtual screening, identification and in vitro biological evaluation of novel inhibitors of PLK1 and NRP1.","authors":"Yang Xia, Yuting Chang, Lixia Guan, Yifei Geng, Qi Zhang, Xiaozhou Shen, Qian Bu, Miao-Miao Niu, Gaohua Han","doi":"10.1080/14756366.2025.2514677","DOIUrl":"10.1080/14756366.2025.2514677","url":null,"abstract":"Overexpression of PLK1 and NRP1 correlate with enhanced proliferative activity in lung cancer cells, thus the development of dual-target PLK1/NRP1 inhibitors holds great therapeutic promise. In this study, five compounds (PLN 1-5) targeting both PLK1 and NRP1 were identified using a multi-step virtual screening approach. PLN-5 showed nanomolar inhibitory potency against PLK1 (IC50 = 2.07 ± 0.13 nM) and NRP1 (IC50 = 5.15 ± 0.24 nM), exceeding the positive controls onvansertib and EG00229 by approximately 9-fold and 124-fold, respectively. Molecular dynamics (MD) simulations revealed that PLN-5 maintained a stable binding to the active sites of PLK1 and NRP1. Importantly, MTT assays showed that PLN-5 had significant antiproliferative activity (IC50 = 0.27 ± 0.02 μM) against human lung cancer cells, with no significant inhibitory effect on normal lung cells. In conclusion, these results demonstrate the therapeutic potential of PLN-5 as a dual-targeting antitumor agent that warrants further development.","PeriodicalId":15769,"journal":{"name":"Journal of Enzyme Inhibition and Medicinal Chemistry","volume":"40 1","pages":"2514677"},"PeriodicalIF":5.4,"publicationDate":"2025-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12364115/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144873484","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

27-Hydroxycholesterol in cancer development and drug resistance. 27-羟基胆固醇在癌症发展和耐药中的作用。

IF 5.6 2区医学

Journal of Enzyme Inhibition and Medicinal Chemistry Pub Date : 2025-12-01 Epub Date: 2025-05-22 DOI: 10.1080/14756366.2025.2507670

Yaxin Hou, Zhiguang Fu, Chenhui Wang, Paulina Kucharzewska, Yuan Guo, Sihe Zhang

{"title":"27-Hydroxycholesterol in cancer development and drug resistance.","authors":"Yaxin Hou, Zhiguang Fu, Chenhui Wang, Paulina Kucharzewska, Yuan Guo, Sihe Zhang","doi":"10.1080/14756366.2025.2507670","DOIUrl":"10.1080/14756366.2025.2507670","url":null,"abstract":"27-Hydroxycholesterol (27HC), a cholesterol metabolite, functions both as a selective oestrogen receptor (ER) modulator and a ligand for liver X receptors (LXRs). The discovery of 27HC involvement in carcinogenesis has unveiled new research avenues, yet its precise role remains controversial and context-dependent. In this review, we provide an overview of the biosynthesis and metabolism of 27HC and explore its cancer-associated signalling, with a particular focus on ER- and LXR-mediated pathways. Given the tissue-specific dual role of 27HC, we discuss its differential impact across various cancer types. Furthermore, we sort out 27HC-contributed drug resistance mechanisms from the perspectives of drug efflux, cellular proliferation, apoptosis, epithelial-mesenchymal transition (EMT), antioxidant defence, epigenetic modification, and metabolic reprogramming. Finally, we highlight the chemical inhibitors to mitigate 27HC-driven cancer progression and drug resistance. This review offers an updated role of 27HC in cancer biology, setting the stage for future research and the development of targeted therapeutics.","PeriodicalId":15769,"journal":{"name":"Journal of Enzyme Inhibition and Medicinal Chemistry","volume":"40 1","pages":"2507670"},"PeriodicalIF":5.6,"publicationDate":"2025-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12100970/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144119860","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 conformation constrained tetracyclic compounds as potent chitinase OfChi-h inhibitors with a novel binding mode. 发现构象受限的四环化合物作为有效的几丁质酶OfChi-h抑制剂，具有新的结合模式。

IF 5.6 2区医学

Journal of Enzyme Inhibition and Medicinal Chemistry Pub Date : 2025-12-01 Epub Date: 2025-07-07 DOI: 10.1080/14756366.2025.2528056

Pengtao Yuan, Xi Jiang, Xintong Ni, Xusheng Shao, Xuhong Qian, Qing Yang

{"title":"Discovery of conformation constrained tetracyclic compounds as potent chitinase OfChi-h inhibitors with a novel binding mode.","authors":"Pengtao Yuan, Xi Jiang, Xintong Ni, Xusheng Shao, Xuhong Qian, Qing Yang","doi":"10.1080/14756366.2025.2528056","DOIUrl":"10.1080/14756366.2025.2528056","url":null,"abstract":"Chitinase h (Chi-h) has been identified as a promising pesticide target due to its exclusive distribution in lepidopteran insects and its essential role in the moulting processes. In this study, we leverage OfChi-h from destructive agricultural pest Ostrinia furnacalis (Asian corn borer) as a model target to identify novel chitinase inhibitors. A conformational restriction approach was employed to design a series of novel OfChi-h inhibitors. Among these, compound 6a showed the highest inhibitory activity against OfChi-h, with a Ki value of 58 nM. Molecular docking analysis suggested that 6a tightly bound to three subsites (-3 to -1) of OfChi-h. The binding mode is further confirmed by the co-crystallization data of 6a with the SmChiA, a bacterial homologue of OfChi-h, at a resolution of 1.8 Å. This research presents a novel approach for the development of highly potent insect chitinase inhibitors, offering potential tools for effective pest control.","PeriodicalId":15769,"journal":{"name":"Journal of Enzyme Inhibition and Medicinal Chemistry","volume":"40 1","pages":"2528056"},"PeriodicalIF":5.6,"publicationDate":"2025-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12239106/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144575581","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 potent inhibitors of potential VEGFR2: a graph neural network-based virtual screening and in vitro study. 潜在VEGFR2的有效抑制剂的鉴定：基于图神经网络的虚拟筛选和体外研究。

IF 5.6 2区医学

Journal of Enzyme Inhibition and Medicinal Chemistry Pub Date : 2025-12-01 Epub Date: 2025-06-20 DOI: 10.1080/14756366.2025.2518192

Shengzhen Hou, Shuning Diao, Yuxiang He, Taiying Li, Wenhui Meng, Jinping Zhang

{"title":"Identification of potent inhibitors of potential VEGFR2: a graph neural network-based virtual screening and in vitro study.","authors":"Shengzhen Hou, Shuning Diao, Yuxiang He, Taiying Li, Wenhui Meng, Jinping Zhang","doi":"10.1080/14756366.2025.2518192","DOIUrl":"10.1080/14756366.2025.2518192","url":null,"abstract":"VEGFR2 is a transmembrane tyrosine kinase receptor expressed on vascular endothelial cells and is closely associated with tumour cell growth. A comparison of traditional Chinese medicines and natural products with existing VEGFR2 inhibitors revealed that the former exhibited superior anticancer properties while concomitantly showing a reduced incidence of adverse effects. We proposed a novel strategy for screening potential candidates targeting VEGFR2 in a Chinese medicine monomer database using a combination of AI deep learning and structure-based drug design. The graph neural network served as the final predictive model to evaluate the molecular activities within the database, resulting in the selection of six candidate compounds. Kinase inhibition assays showed that the three compounds exhibited significant inhibition of VEGFR2. Molecular docking and molecular dynamics simulations further demonstrated the stability of their binding to VEGFR2. This study identified three compounds that effectively inhibited VEGFR2, making them promising candidates in cancer treatment.","PeriodicalId":15769,"journal":{"name":"Journal of Enzyme Inhibition and Medicinal Chemistry","volume":"40 1","pages":"2518192"},"PeriodicalIF":5.6,"publicationDate":"2025-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144333204","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Enzyme sequence optimisation via Gromov-Wasserstein Autoencoders integrating MSA techniques. 酶序列优化通过Gromov-Wasserstein自动编码器集成MSA技术。

IF 5.6 2区医学

Journal of Enzyme Inhibition and Medicinal Chemistry Pub Date : 2025-12-01 Epub Date: 2025-07-03 DOI: 10.1080/14756366.2025.2524742

Xuze Wang, Yangyang Li, Xiancong Hou, Hao Liu

{"title":"Enzyme sequence optimisation via Gromov-Wasserstein Autoencoders integrating MSA techniques.","authors":"Xuze Wang, Yangyang Li, Xiancong Hou, Hao Liu","doi":"10.1080/14756366.2025.2524742","DOIUrl":"10.1080/14756366.2025.2524742","url":null,"abstract":"Enzyme sequence design has always been a challenging task, particularly in optimising key properties such as enzyme solubility, stability, and activity. This study proposes an innovative approach by utilising a variational autoencoder (VAE) model integrated with the Gromov-Wasserstein (GW) distance for enzyme sequence optimisation. The GWAE model improves representation learning by using the GW distance, thereby generating functional variants with desired characteristics. We also introduce an innovative enzyme dataset construction method that incorporates multiple sequence alignment (MSA) techniques to address sequence length discrepancies, enhancing the accuracy of the optimisation process. Experimental results show that the GWAE model outperforms the traditional VAE on multiple metrics. The generated enzyme sequences demonstrate superior solubility, stability, and hydrophobicity. Additionally, by integrating AlphaFold3 for structural prediction, we verify the structural stability of the generated sequences, further enhancing their practical applicability.","PeriodicalId":15769,"journal":{"name":"Journal of Enzyme Inhibition and Medicinal Chemistry","volume":"40 1","pages":"2524742"},"PeriodicalIF":5.6,"publicationDate":"2025-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12231317/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144553709","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

Targeting MED8 enhances sorafenib sensitivity in hepatocellular carcinoma by disrupting epithelial-mesenchymal transition mechanisms. 靶向MED8通过破坏上皮-间质转化机制增强索拉非尼在肝癌中的敏感性。

IF 5.4 2区医学

Journal of Enzyme Inhibition and Medicinal Chemistry Pub Date : 2025-12-01 Epub Date: 2025-10-21 DOI: 10.1080/14756366.2025.2574988

Ming Li, Xiaoxiang You, Tinghao Yuan, Jun He, Zhiliang Xu, Siqin Liang, Lei Mao, Anan Jin, Xinwen Zhou, Bo Yi, Jingao Li, Qiang Tu

{"title":"Targeting MED8 enhances sorafenib sensitivity in hepatocellular carcinoma by disrupting epithelial-mesenchymal transition mechanisms.","authors":"Ming Li, Xiaoxiang You, Tinghao Yuan, Jun He, Zhiliang Xu, Siqin Liang, Lei Mao, Anan Jin, Xinwen Zhou, Bo Yi, Jingao Li, Qiang Tu","doi":"10.1080/14756366.2025.2574988","DOIUrl":"10.1080/14756366.2025.2574988","url":null,"abstract":"HCC is a highly lethal cancer characterised by significant sorafenib resistance, leading to poor patient outcomes. Recent studies have suggested that MED8 plays a role in enhancing tumour resistance to drugs, but its role in drug resistance in HCC has not yet been reported. This study found significantly higher MED8 expression in HCC tissues compared to adjacent noncancerous tissues. Increased MED8 expression in HCC correlates with poorer overall survival. Functional assays demonstrated that reduced MED8 expression inhibited HCC cell proliferation and epithelial-mesenchymal transition, promoted apoptosis, and increased sensitivity to sorafenib. Overexpression of MED8 elevated TRIP4 protein levels. TRIP4 overexpression negated the effects of MED8 knockdown, whereas TRIP4 suppression inhibited MED8-driven EMT. Mechanistically, MED8 interacts with TRIP4, reducing its ubiquitination and stabilising TRIP4 protein levels. Our findings indicate that the MED8-TRIP4 axis plays a role in sorafenib resistance in HCC and could serve as a therapeutic target for HCC treatment.","PeriodicalId":15769,"journal":{"name":"Journal of Enzyme Inhibition and Medicinal Chemistry","volume":"40 1","pages":"2574988"},"PeriodicalIF":5.4,"publicationDate":"2025-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12541920/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145337019","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

Medicinal chemistry breakthroughs on ATM, ATR, and DNA-PK inhibitors as prospective cancer therapeutics. ATM， ATR和DNA-PK抑制剂作为前瞻性癌症治疗药物的药物化学突破。

IF 5.6 2区医学

Journal of Enzyme Inhibition and Medicinal Chemistry Pub Date : 2025-12-01 Epub Date: 2025-04-21 DOI: 10.1080/14756366.2025.2489720

Ram Sharma, Anshul Mishra, Monika Bhardwaj, Gurpreet Singh, Larasati Vanya Indira Harahap, Sakshi Vanjani, Chun Hsu Pan, Kunal Nepali

{"title":"Medicinal chemistry breakthroughs on ATM, ATR, and DNA-PK inhibitors as prospective cancer therapeutics.","authors":"Ram Sharma, Anshul Mishra, Monika Bhardwaj, Gurpreet Singh, Larasati Vanya Indira Harahap, Sakshi Vanjani, Chun Hsu Pan, Kunal Nepali","doi":"10.1080/14756366.2025.2489720","DOIUrl":"https://doi.org/10.1080/14756366.2025.2489720","url":null,"abstract":"This review discusses the critical roles of Ataxia Telangiectasia Mutated Kinase (ATM), ATM and Rad3-related Kinase (ATR), and DNA-dependent protein kinase (DNA-PK) in the DNA damage response (DDR) and their implications in cancer. Emphasis is placed on the intricate interplay between these kinases, highlighting their collaborative and distinct roles in maintaining genomic integrity and promoting tumour development under dysregulated conditions. Furthermore, the review covers ongoing clinical trials, patent literature, and medicinal chemistry campaigns on ATM/ATR/DNA-PK inhibitors as antitumor agents. Notably, the medicinal chemistry campaigns employed robust drug design strategies and aimed at assembling new structural templates with amplified DDR kinase inhibitory ability, as well as outwitting the pharmacokinetic liabilities of the existing DDR kinase inhibitors. Given the success attained through such endeavours, the clinical pipeline of DNA repair kinase inhibitors is anticipated to be supplemented by a reasonable number of tractable entries (DDR kinase inhibitors) soon.","PeriodicalId":15769,"journal":{"name":"Journal of Enzyme Inhibition and Medicinal Chemistry","volume":"40 1","pages":"2489720"},"PeriodicalIF":5.6,"publicationDate":"2025-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12013171/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144010874","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