RNA-based ATTEC: an RNA-guided autophagy-lysosome platform for targeted protein degradation [0.03%]
基于RNA的ATTEC：一种用于靶向降解蛋白质的RNA引导的自噬溶酶体平台
Yunqiu Zhang,Wanting Yang,Yan Xu et al.
Yunqiu Zhang et al.
Targeted protein degradation (TPD) has emerged as a breakthrough in drug discovery and a global biomedical research hotspot. However, its reliance on traditional small-molecule ligands inherently restricts the scope of targetable proteins. ...
From rational design to mechanistic validation: A scaffold optimization strategy for antibacterial candidates with synergistic cytoprotective and pathogen-eradicating properties [0.03%]
从理性设计到机制验证：开发具有协同细胞保护和病原根除性质的抗菌候选药物支架优化策略
Yuanyuan Hu,Bingqian Zhang,Lujie Zhang et al.
Yuanyuan Hu et al.
The global prevalence of Staphylococcus aureus (S. aureus) in clinical settings represents a critical hazard to global public health security, highlighting the pressing demand for highly effective antibacterial compounds with novel molecula...
Discovery and biological evaluation of HS13 as a novel covalent ligand targeting the NSD2-PWWP1 domain [0.03%]
HS13的发现及其作为靶向NSD2-PWWP1的新共价配体的生物活性评价
Chang Liu,Qian Wang,Xinhua Xie et al.
Chang Liu et al.
The PWWP1 domain of NSD2 is an epigenetic reader essential for the subcellular localization of NSD2 and is frequently implicated in oncogenesis, making it an attractive therapeutic target. Our previous work has identified the C294 residue o...
Discovery of a mitochondria-targeted propranolol conjugate PL37 that induces mitophagy for potent anti-hemangioma activity [0.03%]
发现靶向线粒体的PL37（普萘洛尔衍生物），通过诱导自噬发挥强力治疗血管瘤作用
Mengge Zhang,Jian Chen,Liying Meng et al.
Mengge Zhang et al.
Propranolol is the first-line therapy for infantile hemangioma (IH), yet its clinical utility is limited by systemic adverse effects, variable patient response, and an incompletely defined mechanism of action. To develop a more effective an...
Design, synthesis, and biological evaluation of aryl urea derivatives as novel STING inhibitors based on SN-011 [0.03%]
基于SN-011设计合成芳基脲衍生物作为新型STING抑制剂及其活性评价研究
Chaoxin Wang,Runan Zheng,Qing Zhang et al.
Chaoxin Wang et al.
Abnormal activation of the cyclic GMP-AMP synthase (cGAS)-stimulator of the interferon genes (STING) pathway drives excessive inflammatory responses and plays a key role in the pathological process of various inflammatory diseases, and thus...
An update on DOT1LWT/MUT modulators as a promising anticancer strategy [0.03%]
DOT1L/WT/MUT调节剂作为有前景的抗癌策略研究进展
Xue Fan,Shuyu Liu,Luyao Wang et al.
Xue Fan et al.
Disruptor of telomeric silencing 1-like (DOT1L) is the only identified H3K79 methyltransferase and its dysregulation, mutations, or aberrant activity are closely implicated in the pathogenesis and progression of various diseases. Due to the...
Transport specificity of FpvA and FpvB for pyoverdine-antibiotic conjugates in Pseudomonas aeruginosa [0.03%]
铜绿假单胞菌中FpvA和FpvB对吡咯渡铁素-抗生素缀合物的转运特异性
Johan Revol-Tissot,Christine Cézard,Anne Forster et al.
Johan Revol-Tissot et al.
Pyoverdines (PVDs) are fluorescent siderophores produced by many Pseudomonas species. In P. aeruginosa, the TonB-dependent transporters (TBDT) FpvA and FpvB mediate PVD-dependent iron acquisition. PVDs have emerged as promising vectors for ...
Design and engineering of μO-conotoxin MfVIA mutants to enhance NaV1.8 inhibition and analgesic efficacy in inflammatory pain [0.03%]
设计和工程改造μO-康托克斯肽MfVIA突变体以增强对NaV1.8的抑制作用及在炎症痛中的镇痛功效
Xinyu Gao,Nan Wang,Leqing Zhan et al.
Xinyu Gao et al.
Voltage-gated sodium (NaV) channels are essential for action potential initiation and propagation and play key roles in pain signaling. NaV1.8 is predominantly expressed in nociceptors and drives persistent sodium currents that support repe...
Xianqiang Yu,Dingyan Yu,Ye Wang et al.
Xianqiang Yu et al.
Antibody-drug conjugates (ADCs) represent a major advance in precision cancer therapy by combining the high target specificity of monoclonal antibodies with the potent cytotoxicity of small-molecule payloads through chemical linkers. Among ...
CDK4/6-targeted therapy: From clinical inhibitors to emerging strategies to overcome resistance [0.03%]
CDK4/6靶向治疗：从临床抑制剂到克服耐药性的新兴策略
Wenjie Sha,Dijing Feng,Zitong Yan et al.
Wenjie Sha et al.
The Cyclin-dependent kinase 4/6 (CDK4/6) complex orchestrates the critical G1-to-S phase transition by phosphorylating the Retinoblastoma protein (Rb), establishing it as a validated therapeutic target in oncology. The clinical deployment o...