Novel indole-based indoleamine 2,3-dioxygenase-1 (IDO1) inhibitors: design, synthesis, and antidepressant evaluation [0.03%]
新型吲哚胺2,3-双加氧酶1(IDO1)抑制剂的设计、合成及抗抑郁活性评价
Juan Zhang,Wen-Jing Gao,Yu-Xi Zheng et al.
Juan Zhang et al.
Indoleamine 2,3-dioxygenase-1 (IDO1) has emerged as a promising therapeutic target for antidepressant development. The present study performed scaffold hopping-based structural optimization of a known benzimidazole-derived IDO1 inhibitor C-...
Repurposing the USFDA-approved small molecules for their affinity against the colchicine binding site (CBS) in the tubulin: Corroborating the in-silico findings through biological assessment [0.03%]
通过生物评估验证针对与微管蛋白科尔克amicin结合位点(CBS)的亲和力的美国FDA批准的小分子再利用：通过生物评估验证计算机预测结果
Kumar Rohit,Bibekananda Sarkar
Kumar Rohit
The microtubules are known to possess inimitable characteristics termed 'exquisite dynamic behavior,' which allows cells to maintain their shape and assist in cellular division. This exquisite dynamicity is lost in the case of cancer, and c...
Novel benzoxazole-based hybrids as multi-target inhibitors of aromatase, EGFR, and PI3K with potential anti-breast cancer activity [0.03%]
新型苯并恶唑类芳香化酶、EGFR和PI3K多靶标抑制剂及其抗乳腺癌活性研究
Mai S El-Shoukrofy,Mai E Amr,Tarek M Okda et al.
Mai S El-Shoukrofy et al.
Novel anti-breast cancer benzoxazoles were synthesized applying the scaffold hopping and molecular hybridization approaches. MTT assay showed that 6 and 9b were 4.5 and 2 times more potent than doxorubicin against MCF-7 cells, while 9a and ...
Discovery of novel hybrids of coumarin and quinoline as potential anti-Alzheimer's disease agent [0.03%]
一类新型香豆素-喹啉杂环化合物作为治疗阿尔茨海默病的潜在药物研究
Shun Li,Xinrui Li,Shuanglong Li et al.
Shun Li et al.
The multifaceted nature of Alzheimer's disease (AD) spurred growing interest in developing multi-target-directed ligands (MTDLs) for its prevention and treatment. Coumarin and quinoline scaffolds, recognized for their broad spectrum of AD-r...
Phoebe R Rubio,Gavin A Clausen,Zachary D Ruighaver et al.
Phoebe R Rubio et al.
We report the development of a new benzothiazole sulfone (BTS) tool for peptide modification and cleavage. Benzothiazole sulfones are electrophiles that rapidly react with thiols in nucleophilic aromatic substitution (SNAr) reactions. Alkyn...
Maxwell Ampomah-Wireko,Yuequan Wu,Ye Qu et al.
Maxwell Ampomah-Wireko et al.
Drug-resistant bacteria and biofilm-associated infections remain major challenges in anti-infective therapy, contributing to high morbidity and mortality and emphasizing the need to develop novel antimicrobial agents with a low potential to...
Discovery of thiosemicarbazone derivatives as promising SARS-CoV-2 Mpro inhibitors by spectroscopy and microscale thermophoresis [0.03%]
光谱学和微量热泳分析发现有前途的SARS-CoV-2 Mpro抑制剂硫代半卡巴肼衍生物
Xing Xue,Leyao Chen,Miao Zhang et al.
Xing Xue et al.
Since the outbreak of COVID-19, one key strategy has been to screen inhibitors of the SARS-CoV-2 main protease (Mpro). Mpro is critical for viral replication and a key target for therapeutic development. In this work, we report the design a...
In vitro and in vivo activity profiles of broad-spectrum bacterial ATP synthase inhibitors [0.03%]
广谱细菌ATP合成酶抑制剂的体外和体内活性谱型分析
Suzanne Chamberland,Audrey Larose,Guillaume Millette et al.
Suzanne Chamberland et al.
Tomatidine (TO), a natural steroidal alkaloid derived from Solanaceae (e.g., tomato), is recognized for its narrow-spectrum antibiotic activity, particularly against persistent forms of Staphylococcus aureus, such as small-colony variants (...
Versatile fluorescent homobifunctional crosslinkers: expedient synthesis and application to di-affibody constructs for specific HER2+ cancer cell recognition [0.03%]
多功能荧光均二功能交联剂的简便合成及其在双 affibody 构建子对特定 her2 阳性癌细胞识别中的应用
Eric Kaya,Fabienne Fasani,Carlo Pifferi et al.
Eric Kaya et al.
In this contribution we report on the design of new versatile fluorescent linkers (L1-L3, L1N) suitable for the covalent assembly of specific recognition motifs to bind biologically relevant targets such as HER2 receptors. The central fluor...
Screening of one-bead one-compound cyclic peptide libraries using unpurified proteins from the wheat germ cell-free system to identify protein-protein interaction inhibitors [0.03%]
基于小麦胚细胞无细胞蛋白合成体系的蛋白质抑制剂筛选
Miki Hasegawa,Akira Nozawa,Yoshihito Tanaka et al.
Miki Hasegawa et al.
Protein-protein interactions (PPIs) are recognized as both attractive and challenging therapeutic targets. Cyclic peptides are particularly well-suited for PPI inhibition due to their ability to effectively interfere with the extensive surf...