Investigation of the combinatorial anticancer effects of imidazolium-based ionic liquids and lysosomotropic detergents with cisplatin and doxorubicin [0.03%]
基于咪唑
Anastasiia Gryniukova,Sergiy Rogalsky,Petro Borysko et al.
Anastasiia Gryniukova et al.
In the context of rapidly developing resistance caused by mutations in genes that control oncogenic pathways and cancer cell survival, as well as to known and widely accessible antitumor drugs, combined strategies are critical as a modern a...
Synthesis of dehydroabietic acid derivatives as mast cell stabilizers [0.03%]
茋类化合物茋醌和茋醇的分离鉴定及茋茋的新合成方法学研究
Tao Zeng,Wenchao Yu,Chenming Gu et al.
Tao Zeng et al.
Mast cell degranulation plays a central role in IgE-driven allergic diseases, yet the therapeutic options for stabilizers remain limited. Rosinane diterpenoids, a class of natural polyphenols known for their anti-inflammatory properties, re...
Synthesis of novel 6-azacytidine prodrugs as potent influenza A inhibitors [0.03%]
新型的6-氮杂胞苷前药作为有效的A型流感抑制剂的研究与合成
Omar Moukha-Chafiq,Larry D Bratton,Shuklendu D Karyakarte et al.
Omar Moukha-Chafiq et al.
We report the synthesis and evaluation of novel prodrugs of 6-azacytidine (6-AzaCyd) to identify potent and bioavailable inhibitors of influenza A viruses. Prodrug N4-2-propylpentanamide 6-AzaCyd 6a was identified, through a nucleoside prod...
Precision engineering of adalimumab fab variants enhances TNF-α neutralization and structural stability [0.03%]
精确工程学制备的阿达利姆单抗Fab片段变异体提高了TNF-α中和作用及结构稳定性
Abida Khan,Abdullah R Alzahrani,Zia Ur Rehman et al.
Abida Khan et al.
The pro-inflammatory cytokine tumour necrosis factor-alpha (TNF-α) plays a substantial role in the advancement of various autoimmune diseases and is mostly suppressed by the monoclonal antibody adalimumab (Humira). This study utilized a ra...
Structure-based discovery of sulfamoyl-ethyl-4-oxo-3,4-dihydro-7H-pyrrolo[2,3-d]pyrimidine amides and sulfonamides as potent B-Cell Lymphoma 6 (BCL6)-BTB inhibitors [0.03%]
基于结构的硫胺基乙基-4-氧代-3,4-二氢-7H-吡咯并[2,3-d]嘧啶酰胺和磺酰胺类化合物作为B细胞淋巴瘤6（BCL6）-BTB抑制剂的研究
Ahmed Mamai,Mohammed M Morshed,Michael Prakesch et al.
Ahmed Mamai et al.
Diffuse Large B-Cell Lymphoma (DLBCL) is one of the most aggressive forms of lymphoid malignancies. About 40 % of patients eventually relapse and succumb to the disease within 5 years after diagnosis, underscoring the need for new treatment...
Worm-like gold nanocrystals fabricated using a self-assembling peptide and inducing cell death upon exposure to near infrared light [0.03%]
近红外光照射下能诱导细胞凋亡的棒状金纳米晶的制备及性质研究
Soo-Ang Ahn,Kazutoshi Ishida,Ryuki Watanabe et al.
Soo-Ang Ahn et al.
Gold nanorods (GNRs) can perform photothermal energy conversion by absorbing near-infrared (NIR) light and converting it to heat, and are therefore promising for applications in photothermal cancer therapy. However, to synthesize these nano...
Identification of a novel small-molecule inhibitor of heterochromatin protein 1 [0.03%]
异染色质蛋白1的一种新型小分子抑制剂的鉴定
Akari Tokuyama,Yasunobu Yamashita,Ryo Maeda et al.
Akari Tokuyama et al.
Heterochromatin protein 1 (HP1), one of the epigenetic "reader" proteins, recognizes trimethylated lysine 9 of histone H3 (H3K9me3) to repressively regulate gene transcription by promoting chromatin aggregation. Overexpression of HP1 plays ...
Evaluation of the antibacterial activity of diverse coumarin [3,4]-fused Tetrahydroheterocycles [0.03%]
评估[3,4]并四氢杂环的多种香豆素类化合物的抗菌活性
Xiyan Tang,Jie Pang,Yanmin Huang et al.
Xiyan Tang et al.
This study systematically evaluated the antibacterial activity of three classes of coumarin-fused [3,4]-tetrahydroheterocycles against two animal-derived pathogenic bacteria-Staphylococcus aureus and Escherichia coli-as well as three plant ...
Lysine-reactive tag system for cell-surface protein labeling via N-acyl-N-alkyl sulfonamide chemistry [0.03%]
基于N-酰基-N-烷基磺胺化学的亮氨酸反应性标记系统在细胞表面蛋白质标签中的应用
Vikram Thimaradka,Tomonori Tamura,Itaru Hamachi
Vikram Thimaradka
Target-selective and site-specific incorporation of a desired functionality into a membrane protein endogenously expressed in cells is a great challenge in chemical biology. Here, we describe a versatile strategy for covalent chemical modif...
Targeting telomerase for lung cancer: design and synthesis of acridine hybrids with in vitro and in vivo evaluation [0.03%]
靶向端粒酶的肺癌治疗：设计、合成与体内体外评估的吖啶杂合物
Keerti Vishwakarma,Rajdeep Dey,Hardik Bhatt
Keerti Vishwakarma
Lung cancer remains the leading cause of cancer-related deaths worldwide, emphasizing the need for effective targeted therapeutics. Telomerase, which is aberrantly activated in most lung tumors, is an attractive molecular target; however, t...