Thymol carbamates bearing cyclic amines as potent and selective BuChE inhibitors alleviate memory impairments for Alzheimer's disease therapy [0.03%]
用于缓解阿尔茨海默病记忆障碍的苯甲醛甲胩类化合物可有效选择性地抑制乙酰胆碱酯酶
Chengyao Wu,Yulu Ding,Xiaodan Liu et al.
Chengyao Wu et al.
Thymol, an isomer of carvacrol, exhibits anti-Aβ activity. Thymol carbamates were designed, and their inhibition on cholinesterase (ChE) activity was assessed and analysed, among them, TC-4, TC-6, H4 and H5 bearing cyclic amines exhibited ...
Design and optimisation of meta-substituted bis(arylsulfonamido)benzene inhibitors through a molecular hybridisation strategy targeting the Keap1-Nrf2 protein-protein interaction [0.03%]
基于分子杂交策略通过优化设计靶向Keap1-Nrf2相互作用的meta-取代双芳基磺酰胺类化合物抑制剂的研究
Sumi Lee,Ahmed R Ali,Dhulfiqar Ali Abed et al.
Sumi Lee et al.
Nrf2 is recognised as an attractive therapeutic target for oxidative stress-related disorders through its regulation of antioxidant gene transcription. Direct inhibition of Keap1-Nrf2 protein-protein interaction represents a promising strat...
Synthetic strategies and therapeutic insights into FDA-approved indole-containing drugs [0.03%]
美国FDA批准的吲哚类药物的合成策略和治疗启示
Tengjiao Yang,Yanfeng Zhang,Peng Liu et al.
Tengjiao Yang et al.
Indole is a privileged heteroaromatic scaffold in medicinal chemistry, characterised by its unique physicochemical properties, hydrogen-bonding potential, and bioisosteric versatility. Over the past decades, numerous indole-containing drugs...
Identification of a peptide inhibitor disrupting the PCSK9-LDLR interaction via pharmacophore-based virtual screening, molecular dynamics simulations and in vitro/vivo evaluation [0.03%]
基于药效团的虚拟筛选、分子动力学模拟及体内外评价相结合发现可干扰PCSK9与LDLR相互作用的多肽抑制剂
Wanling Wu,Shudan Yang,Jie Liu et al.
Wanling Wu et al.
The PCSK9-LDLR interaction, driving elevated LDL-C, is a key driver of ASCVD pathogenesis. Identifying peptides disrupting this interaction offers an alternative ASCVD therapy. Herein, via structure-based virtual screening with Pep2-8 as a ...
Cynanchum wilfordii modulates inflammatory responses in LPS-stimulated RAW264.7 cells via the NF-κB and MAPK pathways [0.03%]
Cynanchum wilfordii通过NF-κB和MAPK途径调节LPS刺激的RAW264.7细胞中的炎症反应
Yun-Jeong Ji,Min Hye Kang,Sin Hee Han et al.
Yun-Jeong Ji et al.
Cynanchum wilfordii is a widely used herb in Oriental medicine, known for its wide range of therapeutic applications. The present study was conducted with the aim of evaluating the effects of selected compounds isolated from C. wilfordii, i...
Discovery of novel and highly potent XIAP-targeted peptide inhibitors using virtual screening [0.03%]
基于虚拟筛选的新型高效XIAP靶向肽类抑制剂的发现
Xiaoliang Wang,Mengting Lou,Yuting Wang et al.
Xiaoliang Wang et al.
Lung cancer, a globally prevalent fatal malignancy, remains a major therapeutic challenge. X-linked inhibitor of apoptosis protein (XIAP) is overexpressed in various cancers, driving uncontrolled proliferation, while its specific inhibition...
Identification and biological evaluation of benzimidazole-based compounds as novel TGFβR1 inhibitors [0.03%]
一类新的TGFβR1抑制剂的苯并咪唑类化合物的鉴定及生物活性评估
Hui-Ju Tseng,Yi-Wen Wu,Yan-Ling Chen et al.
Hui-Ju Tseng et al.
TGF-β promotes progression and metastasis in later stages of tumour development, and inhibitors targeting TGF-β or its receptor have faced clinical limitations due to toxicity and poor selectivity. This study aimed to identify novel TGFβ...
Investigation of exercise-mimetic bioactive molecules as modulators of MMP activity and expression in cancer cells [0.03%]
运动模拟生物活性分子调节癌细胞中基质金属蛋白酶活性和表达的机制研究
Ha Vy Thi Vo,Geewoo Nam Patton,Jae Sung Park et al.
Ha Vy Thi Vo et al.
Matrix metalloproteinases (MMPs), particularly MMP-2 and MMP-9, are directly involved in the degradation of the extracellular matrix preceding uncontrolled cancer growth and metastasis. For these reasons, MMPs are considered key therapeutic...
Porcine serum maltase-glucoamylase: structure, kinetics, and inhibition [0.03%]
猪血清麦芽糖葡萄糖淀粉酶：结构、动力学和抑制作用
Ken Watanabe,Takayoshi Tagami,Chihiro Biwa et al.
Ken Watanabe et al.
Maltase-glucoamylase (MGAM) is a small-intestinal enzyme comprising two tandem α-glucosidase units, NtMGAM and CtMGAM, each capable of hydrolysing maltodextrins into glucose. MGAM serves as a therapeutic target for managing postprandial hy...
Mitogen-activated protein kinase kinase 4 (MKK4) as a promising therapeutic target in liver diseases: a review [0.03%]
丝裂原活化蛋白激酶激酶4（MKK4）作为治疗肝病的潜在靶点：综述
Pan Liu,Yangyang Liu,Li Cheng et al.
Pan Liu et al.
The liver is essential for metabolism and detoxification and can regenerate effectively. However, severe injuries or major surgeries can hinder this ability, leading to liver insufficiency or failure. Recent research has identified mitogen-...