Pharmacological advances in Candida auris: emerging antifungal mechanisms and next-generation therapeutic strategies [0.03%]
药理学在耳念珠菌研究中的进展：新型抗真菌机制和下一代治疗策略
Shuaibu Abdullahi Hudu,Najlaa Saadi,Emad A Morad et al.
Shuaibu Abdullahi Hudu et al.
Candida auris is a major public health concern worldwide due to its efficient transmission, environmental persistence, and broad resistance to approved antifungal classes. This review consolidates recent pharmacological developments in this...
A multipurpose probe for identification and mechanistic analysis of prenylation inhibitors [0.03%]
一种用于异戊二烯基化抑制剂鉴定和机理分析的多功能探针
Ruba Yehia,Moshe Giladi,Yoni Haitin
Ruba Yehia
Protein prenylation is a critical post-translational modification that controls many cancer-related signalling pathways and represents an important therapeutic target currently lacking effective pharmacological agents. Here, we establish th...
Discovery of a novel STING-binding peptide associated with reduced cGAMP-induced inflammatory gene expression [0.03%]
一种新型的STING结合肽与降低cGAMP诱导的炎性基因表达有关的发现
Junling Lu,Rui Dong,Shudan Yang et al.
Junling Lu et al.
cGAMP-induced STING activation contributes to inflammatory and interferon-related signalling, making STING a relevant target for inhibitor development. In this study, a 59,319-sequence peptide library was screened against STING by molecular...
Influence of adrenomedullin on the enzymatic activity of dipeptidyl peptidase 3 in vitro [0.03%]
肾上腺髓质素对自由基引发的DNA损伤和体外二肽基肽酶3酶活性的影响
Ruqayyah Nissen,Amin Yourdkhani,Marie-Louise Hollerbach et al.
Ruqayyah Nissen et al.
Circulating Dipeptidyl Peptidase 3 (DPP3) hydrolyses dipeptides from the amino terminus of its substrates and excess levels represent a target for the treatment of cardiogenic shock. Known substrates include Angiotensin II (Ang II), but the...
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...