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...
Design, synthesis, and biological activity evaluation of Pyrimido[4,5-b]pyridine-based derivatives as SOS1 inhibitors [0.03%]
基于嘧啶并吡啶衍生物作为SOS1抑制剂的设计、合成及生物活性研究
Gangsheng Chen,Qin Ban,Zhengyang Wang et al.
Gangsheng Chen et al.
SOS1 represents a promising therapeutic target for pan-RAS inhibition. In this study, we designed and synthesized a series of pyrimido[4,5-b]pyridine derivatives using commercially available (R)-1-phenylethan-1-amine and pyrido[2,3-d]pyrimi...
Identification of non-hydroxamate histone deacetylase 8 inhibitors using deep learning-based screening of two-dimensional molecular images [0.03%]
基于深度学习的二维分子图像筛选非羟胺类组蛋白去乙酰酶8抑制剂识别方法
Yasunobu Yamashita,Juhyun Yun,Ayumu Asai et al.
Yasunobu Yamashita et al.
Histone deacetylase 8 (HDAC8) is a zinc-dependent enzyme that deacetylates proteins and is involved in cancer development, making its inhibition a potential anticancer strategy. Most reported HDAC8 inhibitors contain a hydroxamate zinc-bind...
Recent advances in dual-function fluorescent ligands targeting mitochondrial DNA G-Quadruplexes for Cancer Theranostics [0.03%]
靶向线粒体DNA G-四链体的双功能荧光配体在肿瘤诊疗中的最新进展
Ming-Hao Hu
Ming-Hao Hu
The identification of G-quadruplex (G4) structures in mitochondrial DNA (mtDNA) offers a promising avenue for targeted cancer therapy. Unlike nuclear DNA, mtDNA lacks histone protection and comprehensive repair mechanisms, making mitochondr...
Development of tacrine-based multitarget-directed ligands as dual AChE/EGFR inhibitors with neuroprotective activity [0.03%]
基于Tacrine的多靶点导向配体作为乙酰胆碱酯酶/表皮生长因子受体双重抑制剂的开发及其神经保护作用研究
Yuqing Wei,Ao Zhang,Weimin Qiu et al.
Yuqing Wei et al.
Alzheimer's disease (AD) is a multifaceted neurodegenerative disease for which current therapies primarily rely on cholinesterase inhibitors (ChEIs). Tacrine was the first and potent ChEI, which was soon withdrawn due to hepatic side effect...
Artificial intelligence-driven drug discovery: a new era in therapeutic innovation [0.03%]
人工智能驱动的药物发现：治疗创新的新时代
Qian Ya Swee,Shi Hui Law,Huang-Ju Tu et al.
Qian Ya Swee et al.
Artificial intelligence (AI) is a computer system that performs tasks that require learning, problem-solving and decision-making skills. It mimics humans' cognitive functions, which include pattern recognition. Vast amounts of data serve as...
New potential HIV-1 inhibitors, analogues to efavirenz, containing the isatin core [0.03%]
一类新的HIV-1抑制剂，含异丁酸内核的埃夫拉昔恩类似物
Gustavo P Machado,Pedro A G Costa,Debora I Leite et al.
Gustavo P Machado et al.
HIV/AIDS remains a major global health challenge, with millions of new infections reported annually. Among the available antiretroviral therapies, non-nucleoside reverse transcriptase inhibitors (NNRTIs) play a crucial role by targeting vir...