Synthesis of a fluorescent probe for the selective detection of cysteine and its application in cell imaging [0.03%]
用于选择性检测半胱氨酸的荧光探针的合成及其细胞成像应用研究
Mengzhou Wang,Guangzhou Lin,Zuheng Shan et al.
Mengzhou Wang et al.
Cysteine plays a significant role in biological systems, and changes in its content are closely correlated with many human diseases. The specific identification and detection of cysteine concentrations remains a research focus. In this stud...
Development of palladium-based multivalent lectin-directed artificial metalloenzymes [0.03%]
基于钯的人工金属酶的发展用于多价 lectin定向作用
Jing Huang,Yufei Li,Pik Kwan Lo et al.
Jing Huang et al.
By instilling artificial metalloenzymes (ArMs) with cancer targeting properties, these biocatalysts can be used in prodrug therapies to chemoselectively activate prodrugs within the local tumor environment. In this study, another example of...
Discovery of a potent thienodiazepine derivative as a novel BRD4 degrader [0.03%]
发现一种具有潜力的噻唑并二氮杂卓衍生物作为新型BRD4降解剂
Mayu Shigekuni,Yasuki Niwa,Kiyomi Ohba et al.
Mayu Shigekuni et al.
We discovered bromodomain-containing protein 4 (BRD4) degraders as novel antitumor therapeutics leveraging our internal knowledge on Y-803 (birabresib, OTX015/MK-8628), which was discovered by our company as the first-in-class BRD4 inhibito...
Inhibition of amyloid formation of keratin-derived peptide by rosmarinic acid [0.03%]
鼠李糖酸抑制角蛋白衍生肽淀粉样纤维形成
Haruka Hirao,Takahiro Watanabe,Tamotsu Zako
Haruka Hirao
Primary localized cutaneous amyloidosis (PLCA) is caused by the deposition of keratin amyloids in the skin and leads to severe symptoms. It is difficult to cure PLCA completely; therefore, prevention is essential. In this study, amyloid for...
Design, synthesis and characterization of a novel GCP derivative as a potential 14-3-3 sigma homodimer stabilizer [0.03%]
设计、合成及表征一种新型GCP衍生物作为潜在的14-3-3σ同二聚体稳定剂
Edward Kong Weng Tan,Aik-Hong Teh,Beow Keat Yap
Edward Kong Weng Tan
This study reports the design and characterization of a novel dimer stabilizer targeting the 14-3-3σ protein, a signaling protein with purported tumor-suppressive roles. Using an in silico design strategy based on the derivatization of GCP...
Design, synthesis, and activity evaluation of novel potential PPARα agonists [0.03%]
新型PPARα激动剂的设计、合成及活性评价
Xiaoqian Wang,Weinan Wang,Jixuan Guo et al.
Xiaoqian Wang et al.
Peroxisome proliferator-activated receptor α (PPARα), an important member of the nuclear receptor superfamily, plays a crucial role in regulating lipid metabolism, glucose homeostasis, and inflammation. Its dysfunction is associated with ...
Branislav Pavilek,Dana Hajduová,Dušan Bortňák et al.
Branislav Pavilek et al.
This review provides a comprehensive overview of kynurenic acid (KYNA) derivatives with specific focus on KYNA amides as an emerging class of multi-target directing drugs (MTDDs) for the treatment of Alzheimer's disease (AD). It highlights ...
Synthesis and bioactive study of tricyclic cyclopentaimidazopyridin-6-carboxylates grafting benzylpiperazyl groups as cytoprotectant agents [0.03%]
苯基哌嗪并环状化合物的合成及细胞保护活性研究
Wei-Zheng Zeng,Shi-Chi Wang,Chun-Han Cha et al.
Wei-Zheng Zeng et al.
A series of modified Genipin derivatives 6a-d and 7-10, grafted with benzylpiperazyl groups, were synthesized from the tricyclic cyclopentaimidazopyridin-6-carboxylates 3a-d to evaluate their anti-inflammatory and neuroprotective activities...
From pain relief to proliferation arrest: Synthesis and biological evaluation of novel diclofenac-tethered Schiff bases as VEGFR-2 inhibitors and apoptosis inducers, guided by in silico molecular docking and ADME profiling [0.03%]
从止痛到增殖阻滞：基于分子对接和ADME特征的体内外实验相结合设计新型舒林酸 Schiff 碱类化合物作为血管内皮生长因子受体-2 抑制剂及凋亡诱导剂
Nadia A Khalil,Peter A Halim,Alaa Magdy et al.
Nadia A Khalil et al.
This research is principally focused on designing and developing new diclofenac-tethered Schiff base derivatives with anticipated anticancer potentials. The structures of the synthesized compounds were examined by applying diverse spectrosc...
Machine learning-driven computational drug repurposing to identify new tubulin inhibitors against cancer [0.03%]
基于机器学习的计算药物再定位研究以发现新的抗肿瘤微管抑制剂
Neelima Neelima,Hussein Elrewey,Sneha Smarakan et al.
Neelima Neelima et al.
Tubulin is a validated anticancer target, yet the clinical translation of colchicine-binding site inhibitors remains limited by toxicity and resistance. To accelerate the discovery of safer tubulin-targeting agents, we employed a machine le...