Evolving CRBN ligands enhance the drug-like properties of protein degraders [0.03%]
进化CRBN配体可增强蛋白质降解药物的类药性
Xin-Qian Ji,Lin Wang,Xing-Jie Dai
Xin-Qian Ji
Proteolysis-targeting chimaeras (PROTACs) enable event-driven degradation of disease-relevant proteins by hijacking the ubiquitin-proteasome system (UPS). Cereblon (CRBN) is the most widely exploited recruiter due to its well-characterised ...
Discovery of ALA-hydroxypyridinone hybrids: novel strategies for photodynamic therapy against superficial tumours [0.03%]
原卟啉IX衍生物在浅表性肿瘤光动力治疗中的应用研究新策略
Xiaoying Jiang,Meiling Feng,Xiaotian Niu et al.
Xiaoying Jiang et al.
Superficial tumours can be effectively treated with photodynamic therapy (PDT), which is characterised by its targeted approach and enhanced safety profile. 5-aminolevulinic acid (ALA), a precursor to the endogenous photosensitiser PpIX, ha...
Structure-guided discovery and evaluation of an EGFR L858R-targeting peptide with antiproliferative activity against ovarian cancer cells [0.03%]
基于结构的发现和评估针对卵巢癌细胞增殖抑制作用的EGFR L858R靶向肽
Yinxing Zhu,Hanying Wu,Xiaohao Liu et al.
Yinxing Zhu et al.
EGFR L858R is an activating mutation associated with aberrant EGFR signalling, and molecules capable of recognising this mutant remain of research interest. In this study, a virtual peptide library containing 59 319 heptapeptides was screen...
Selective targeting phosphodiesterase-5 (PDE5): clinical progress, design strategies, and emerging prospects [0.03%]
选择性靶向磷酸二酯酶5(PDE5)的药物：临床进展、设计策略及前景展望
Yanhong Li,Yufeng Ma,Jingkao Chen et al.
Yanhong Li et al.
PDE5 is a subfamily member of the phosphodiesterase (PDE) superfamily. It is encoded by a single PDE5A gene, and its primary function is to specifically hydrolyse cyclic guanosine monophosphate. To date, a few inhibitors targeting PDE5, exe...
Panpan Zheng,Jingyi Dai,Xiao Zheng et al.
Panpan Zheng et al.
The tumour necrosis factor receptor superfamily (TNFRSF) represents a pivotal signalling network that orchestrates immune homeostasis and regulates cell fate decisions. Lymphotoxin β receptor (LTβR, TNFRSF3), a key TNFRSF member, is predo...
Inflammation and carcinogenesis: molecular targets and small-molecule intervention strategies [0.03%]
炎症与肿瘤发生：分子靶标和小分子干预策略
Wan-Jung Lu,Ritu Ojha,Mandeep Rana et al.
Wan-Jung Lu et al.
Inflammation is a finely tuned host defense mechanism whose perpetual activation is a driver, promoter, and supporter of carcinogenesis. Key mediators of chronic inflammatory processes, viz. NF-kB, JAK-STAT, inflammasomes, reactive oxygen s...
New insights into the ACLY-mediated metabolic and epigenetic interplay in macrophages [0.03%]
探讨巨噬细胞中ACLY介导的代谢与表观遗传相互作用的新见解
Leyi Yuan,Tong Wang,Yajuan Song et al.
Leyi Yuan et al.
Macrophages are plastic innate immune cells that polarize into pro-inflammatory M1 or anti-inflammatory M2 phenotypes in response to microenvironmental signals, with their dynamic balance governing inflammation resolution and tissue homeost...
Design, synthesis, and antibacterial activity study of pyrroloquinazoline diamine derivatives [0.03%]
含二胺基吡咯并[2,3-d]嘧啶类衍生物的设计合成及抗菌活性研究
Muchun Cheng,YaJing Tian,JieYa Shang et al.
Muchun Cheng et al.
To combat antimicrobial resistance (AMR), a novel series of pyrrolo[3,2-f]quinazoline-diamine (PQD) derivatives (5a-5z) featuring a flexible benzyl-oxo-benzyl side chain were designed and synthesised via structural optimisation of lead comp...
Nanozymes: bridging nanoscale characteristics and catalytic mechanisms for advanced biomedical applications [0.03%]
纳米酶：用于先进生物医学应用的纳米特性和催化机制之间的桥梁
Yunqin Sun,Yunchang Yang,Xinyao Kang et al.
Yunqin Sun et al.
Nanozymes-nanomaterials with intrinsic enzyme-like activity-have emerged as a transformative paradigm in biomedicine. Their catalytic proficiency is fundamentally dictated by unique nanoscale characteristics, particularly tuneable surface d...
Design, synthesis, and biological evaluation of 6-aryl-3-(3,4,5-trimethoxyphenyl)imidazo[1,2-a]pyridine derivatives as novel tubulin inhibitors with potent anticancer efficacy [0.03%]
设计、合成及生物活性评价新的微管蛋白抑制剂6-芳基-3-(3,4,5-三甲氧基苯基)咪唑并[1,2-a]吡啶衍生物用于抗肿瘤作用研究
Wen Xu,Yujing Zhang,Qianqian Xu et al.
Wen Xu et al.
Tubulin, the fundamental component of microtubules, remains a critical target in anticancer therapy. The development of small-molecule tubulin polymerization inhibitors continues to drive the discovery of novel chemotherapeutic agents. Thro...