Hydrocarbon stapling strategy and antitumor activity of antimicrobial peptide Lasioglossum III [0.03%]
取链细菌素Lasioglossum III的烃基连接策略及抗肿瘤活性研究
Jinqiu Li,Jiayi Zhu,Xinhao Wei et al.
Jinqiu Li et al.
The identification of novel candidate molecules with breakthrough potential is critical for advancing breast cancer therapy. Lasioglossum-III (LL-III), a linear peptide isolated from wild bee venom, has emerged as a promising lead compound ...
Exploring the potential of heterocyclic-containing tail approach in the development of novel covalent inhibitors dual-targeting EGFR and HER-2: design, synthesis and biological evaluation [0.03%]
含杂环尾部结构的共价抑制剂双靶向EGFR和HER-2的研究：设计、合成及生物活性评价
Shuang Hao,Jing-Han Yan,Rui Wang et al.
Shuang Hao et al.
Based on the structure of the existing drug afatinib, this study employed the heterocyclic-containing tail modification strategy to design and synthesize a series of novel pyrimidine derivatives, aiming to develop highly selective and low-t...
Intracellular oxygen monitoring and oxygen demand assessment using Ir(ppy)3-encapsulated polymeric micelles [0.03%]
利用封装Ir(ppy)3的高分子聚合物胶束进行细胞内氧监测及耗氧量评估研究
Narufumi Kitamura,Keiji Kajiwara,Shoichi Yamamoto et al.
Narufumi Kitamura et al.
Intracellular oxygen concentration is a pivotal indicator of cellular metabolic and functional states that may be influenced by pathologic conditions, including hypoxia in solid tumors and hyperglycemia. Currently, methods for quantifying c...
Incorporation of an alpha-hydroxy substituent modulates activity of triazole bisphosphonate-based geranylgeranyl diphosphate synthase inhibitors [0.03%]
α-羟基取代基的引入可调节三唑双膦酸类牻牛儿牻牛儿基焦磷酸合酶抑制剂的作用机制
Md Ayub Ali,Dan Feng,Staci L Haney et al.
Md Ayub Ali et al.
Geranylgeranyl diphosphate synthase (GGDPS), the enzyme responsible for producing the isoprenoid substrate used in protein geranylgeranylation reactions, represents a novel therapeutic target in cancer, including malignancies such as multip...
MN42-81: A novel PD-L1-targeted immunomodulatory cisplatin prodrug for highly efficient synergistic chemo-immunotherapy of cancer [0.03%]
一种新型PD-L1靶向免疫调控顺铂前药用于高效协同癌症化疗免疫治疗
Mengyao Peng,Mengni He,Jie Wang et al.
Mengyao Peng et al.
Cisplatin is a widely used chemotherapeutic agent, but its clinical application is limited by toxic side effects and an "immunological paradox": while chemotherapy kills tumor cells, it also induces upregulation of PD-L1, leading to immune ...
Design, synthesis and evaluation of trofinetide prodrug based on diketopiperazine strategy [0.03%]
基于二酮哌嗪策略的trofinetide前药的设计、合成及评价
Xue Feng,Yuanzhen Dong,Chen Guo et al.
Xue Feng et al.
Trofinetide is the only drug approved worldwide for the treatment of Rett syndrome, a rare pediatric disease. However, its extremely short half-life, large oral dose, high incidence of gastrointestinal adverse reactions, and consequently hi...
Optimization of CaMKII inhibitory peptide with N-terminal fatty acid chain modification and its study on anti-kidney fibrosis [0.03%]
含脂肪链修饰的肌球蛋白轻链激酶抑制肽的优化及其抗肾纤维化研究
Hong Lei,Xiaocui Feng,Runling Yang et al.
Hong Lei et al.
Renal fibrosis, as the ultimate common pathway for the development of various kidney diseases, is characterized by abnormal accumulation of extracellular matrix (ECM) and destruction of renal structure, resulting in progressive, irreversibl...
Employing an integrated computational simulation strategy to identify high-affinity ligands for TDP-43 amyloid proteins [0.03%]
运用集成计算模拟策略识别TDP-43淀粉样蛋白的高亲和力配体
Yunqing Gao,Zhenghao Sun,Qiumei Wei et al.
Yunqing Gao et al.
Developing high-affinity ligands targeting TDP-43 amyloid species is a potential therapeutic approach for amyotrophic lateral sclerosis (ALS). Here, we propose an integrated computational simulation strategy, which integrates multiple virtu...
Design, synthesis, and biological evaluation of small-molecule HMGB1 inhibitors for the alleviation of radiation-induced skin injury [0.03%]
设计、合成和生物活性评价小分子HMGB1抑制剂以缓解放射性皮肤损伤
Yilong Zhuang,Yaowen Cui,Tingting Chen et al.
Yilong Zhuang et al.
Radiation-induced skin injury (RSI) is a common and debilitating complication of radiotherapy, significantly impairing patients' quality of life. High-Mobility Group Box 1 (HMGB1), a key damage-associated molecular pattern (DAMP) protein, p...
Discovery and characterization of steroid derivatives as hCES2A inhibitors [0.03%]
新型甾体衍生物HCES2A抑制剂的发现及活性评价研究
Yueyang Cao,Jiayi Luo,Yong Yang et al.
Yueyang Cao et al.
Human carboxylesterase 2A (hCES2A) is a key mediator of drug metabolism and chemotherapeutic side effects, necessitating potent and selective inhibitors. Herein, 42 novel steroid derivatives were rationally designed via hCES2A homology mode...