Ferroptosis and hearing loss: from molecular mechanisms to therapeutic interventions [0.03%]
铁死亡与听力损失：从分子机制到治疗干预
Xingyi Lv,Chenyi Yang,Xianying Li et al.
Xingyi Lv et al.
Hearing loss profoundly affects social engagement, mental health, cognition, and brain development, with sensorineural hearing loss (SNHL) being a major concern. Linked to ototoxic medications, ageing, and noise exposure, SNHL presents sign...
Identification of a novel pyrrolo[2,3- b]pyridine compound as a potent glycogen synthase kinase 3β inhibitor for treating Alzheimer's disease [0.03%]
新型吡咯并[2,3-b]吡啶化合物作为治疗阿尔茨海默病的糖原合酶激酶3β抑制剂的鉴定
Qing-Qing Xun,Jing Zhang,Lei Feng et al.
Qing-Qing Xun et al.
Herein, a novel pyrrolo[2,3-b]pyridine-based glycogen synthase kinase 3β (GSK-3β) inhibitor, S01, was rationally designed and synthesised to target Alzheimer's disease (AD). S01 inhibited GSK-3β, with an IC50 of 0.35 ± 0.06 nM, and had ...
Discovery of a selective and reversible LSD1 inhibitor with potent anticancer effects in vitro and in vivo [0.03%]
具有显著的体内和体外抗癌效果的选择性可逆LSD1抑制剂的发现
Xiao-Song Zhang,Jin-Zhan Liu,Ying-Ying Mei et al.
Xiao-Song Zhang et al.
Lysine-specific demethylase 1 (LSD1) is abnormally overexpressed in various tumour tissues of patients and has been an attractive anticancer target. In this work, a potent LSD1 inhibitor (compound 14) was designed and synthesised by the mol...
Development of ketobenzothiazole-based peptidomimetic TMPRSS13 inhibitors with low nanomolar potency [0.03%]
具有低纳米摩尔效力的酮苯并噻唑基肽模拟物TMPRSS13抑制剂的发展
Alexandre Joushomme,Antoine Désilets,William Champagne et al.
Alexandre Joushomme et al.
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,...
Myeloperoxidase as a therapeutic target for oxidative damage in Alzheimer's disease [0.03%]
髓过氧化物酶作为治疗阿尔茨海默病氧化损伤的治疗靶点
Astrid Mayleth Rivera Antonio,Itzia Irene Padilla Martínez,Mónica A Torres-Ramos et al.
Astrid Mayleth Rivera Antonio et al.
Alzheimer's disease (AD) is a major neurodegenerative disorder more common in older adults. One of the leading AD hypotheses involves the amyloid beta (A) production, it is associated to oxidative stress, neuroinflammation, and neurovascula...
Tomasz M Wróbel,Angelika Grudzińska,Jibira Yakubu et al.
Tomasz M Wróbel et al.
Prostate cancer (PCa) is one of the most prevalent malignancies affecting men worldwide, and androgen deprivation therapy (ADT) is a primary treatment approach. CYP17A1 inhibitors like abiraterone target the steroidogenic pathway to reduce ...
Identification of novel inhibitors of dengue viral NS5 RNA-dependent RNA polymerase through molecular docking, biological activity evaluation and molecular dynamics simulations [0.03%]
基于分子对接、生物活性评价和分子动力学模拟的登革病毒NS5依赖RNA的RNA聚合酶抑制剂的研究
Keli Zong,Chaochun Wei,Wei Li et al.
Keli Zong et al.
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)...
Selisistat, a SIRT1 inhibitor, enhances paclitaxel activity in luminal and triple-negative breast cancer: in silico, in vitro, and in vivo studies [0.03%]
塞利西司塔（Sirt1抑制剂）通过体内和体外研究增强紫杉醇在腔面型及三阴性乳腺癌中的活性
Anna Wawruszak,Jarogniew Luszczki,Damian Bartuzi et al.
Anna Wawruszak et al.
Sirtuins (SIRTs) are NAD+-dependent histone deacetylases, which play a key role in cancer progression; however, their prognostic values in breast cancer (BC) remain a subject of debate and controversy. Accumulative evidence suggests that ea...
Discovery of novel biphenyl compounds bearing hydroxamic acid moiety as the first PD-L1/class I HDACs dual inhibitors [0.03%]
一类新型含羟胺基 biphenyl 衍生物的发现及其作为 PD-L1/组蛋白去乙酰酶复合抑制剂的研究
Dandan Yuan,Yali Gao,Lin Xia et al.
Dandan Yuan et al.
Herein, we firstly reported a series of biphenyl compounds bearing hydroxamic acid moiety as PD-L1/class I HDACs dual inhibitors. Among them, compound 14 displayed the strongest inhibitory activity in vitro against HDAC2 and HDAC3 with IC50...
Exploring covalent inhibitors of SARS-CoV-2 main protease: from peptidomimetics to novel scaffolds [0.03%]
用于探索SARS-CoV-2主要蛋白酶共价抑制剂：从肽模拟物到新骨架分子
Noor Atatreh,Radwa E Mahgoub,Mohammad A Ghattas
Noor Atatreh
Peptidomimetic inhibitors mimic natural peptide substrates, employing electrophilic warheads to covalently interact with the catalytic Cys145 of Mpro. Examples include aldehydes, α-ketoamides, and aza-peptides, with discussions on their me...