Discovery of potential covalent TYK2 inhibitors targeting Cys736 for the treatment of psoriasis [0.03%]
用于治疗银屑病的靶向半胱天冬酶736的潜在共价TYK2抑制剂的发现
Han Wang,Chang Liu,Tong Liu et al.
Han Wang et al.
TYK2 regulates the signaling of pro-inflammatory cytokines such as IL-12, IL-23, and type I interferons, which directly modulates immune cell activation and inflammatory responses, thereby has emerged as a promising therapeutic target for p...
Design and evaluation of the bactericidal activity of new hydroxamic acid and hydrazide derivatives against mature S. aureus biofilms [0.03%]
新型羟胺酸和肼衍生物的杀菌活性的设计、评价及其对成熟金黄色葡萄球菌生物被膜的作用
Maëva Corneiller,Allison Faure,Rémy Tisserand et al.
Maëva Corneiller et al.
Bacterial biofilms represent a major clinical challenge due to their high tolerance to conventional antibiotics and their implication in persistent infections. Staphylococcus aureus is particularly known for its ability to form biofilms tha...
Borneol-loaded liposomes modified with 5-hydroxy-1H-pyrazole-3-carboxylic acid enhance neuroprotection and brain specific for ischemic stroke therapy [0.03%]
负载薄荷脑的5-羟基-1H-吡唑-3-羧酸修饰脂质体增强神经保护作用并具有脑靶向性以治疗缺血性中风
Yulu Wu,Siyi Li,Ru Xiao et al.
Yulu Wu et al.
Ischemic stroke is a cardiovascular and cerebrovascular disease with high mortality and disability rates, characterized by complex pathophysiological mechanisms. In this study, 5-hydroxy-1H-pyrazole-3-carboxylic acid compound (3g) was ident...
PROTACs for central nervous system disorders: challenges and opportunities [0.03%]
蛋白降解嵌合体用于中枢神经系统疾病：挑战与机遇
Na Zheng,Jikuan Shao,Baichen Xiong et al.
Na Zheng et al.
Central nervous system (CNS) disorders, particularly neurodegenerative diseases and brain tumors, pose substantial and long-standing challenges to the global public health system. Current therapeutic approaches for CNS disorders are primari...
Efficient gram-scale synthesis and preclinical evaluation of an escin-derived therapeutic for ovarian cancer [0.03%]
高效克级合成和卵巢癌治疗的Escin衍生物药物的临床前评估
Chin Leong Wong,Tiffany Yuen Kwan Au,Chi-Shing Chan
Chin Leong Wong
Ovarian cancer is the most lethal gynecologic malignancy, characterized by a poor five-year survival rate for patients with advanced-stage disease. EV-S008, an escin derivative, exhibits potent anti-ovarian cancer activity; however, its pre...
Novel 1H-imidazo[4,5-c]quinoline derivatives as TLR-7 modulators with pro-apoptotic properties in breast cancer cell line [0.03%]
新型1h-咪唑并[4,5-c]喹啉衍生物作为tlr-7调节剂在乳腺癌细胞系中具有促凋亡特性
Katarzyna Grychowska,Olga Szewczyk-Roszczenko,Piotr Roszczenko et al.
Katarzyna Grychowska et al.
A new class of 4-chloro-substituted 1H-imidazo[4,5-c]quinoline derivatives was identified as functional TLR7 agonists. Molecular modeling suggests that, in selected cases, replacing the C4 amino group with chlorine does not abolish receptor...
Molecular functions and applications of peptide agonists acting on mouse neuromedin U receptor 1 [0.03%]
神经调节蛋白U受体1的肽类激动剂的作用及应用
Kentaro Takayama,Kenji Mori,Erina Nomura et al.
Kentaro Takayama et al.
Neuromedin U (NMU), a neuropeptide, activates two types of NMU receptors (NMUR1 and NMUR2). The anti-obesity drug development focused on appetite suppression among physiological actions of NMU have been attempted worldwide; however, several...
Synthesis and mechanistic insights of carbazole-based inhibitors targeting FTO by spectroscopic characterization and molecular simulation [0.03%]
基于卡唑的FTO抑制剂的合成及其作用机制的光谱表征和分子模拟研究
Miao Zhang,Leyao Chen,Xiaoyu Chang et al.
Miao Zhang et al.
FTO (Fat mass and obesity-associated protein) is an RNA demethylase crucial for epitranscriptomic regulation, catalyzing the removal of N6-methyladenosine (m6A) modifications. We designed a series of carbazole derivatives and identified com...
Recent progress in small-molecule targeted therapies for melanoma treatment [0.03%]
小分子靶向疗法在黑色素瘤治疗中的新进展
Xinrui Yuan,Hongyan Xu,Yifeng Pei et al.
Xinrui Yuan et al.
Melanoma is an aggressive form of skin cancer that originates from melanocytes and has a high risk of metastasis to distant organs. The identification of specific mutations and the subsequent development of targeted therapies have revolutio...
Oleic acid modification enables lysosomal escape of phthalocyanine photosensitizer for effective bladder cancer treatment [0.03%]
油酸修饰使酞菁光敏剂实现溶酶体逃逸有效治疗膀胱癌
Aoyun Cui,Haowen Liu,Ke Wang et al.
Aoyun Cui et al.
Lysosomal sequestration, driven by acidic hydrolases, degrades and inactivates therapeutics, severely compromising their efficacy. While unsaturated fatty acid (UFA) modifications confer robust lysosomal escape capabilities to nanomedicines...