Emerging chemical strategies for CD38 inhibition: restoring NAD+ metabolism and disease control [0.03%]
新兴的CD38抑制化学策略:恢复NAD+代谢和疾病控制
Zeyu Zhang,Arshad J Ansari,Ethan R Fayne et al.
Zeyu Zhang et al.
Cluster of differentiation 38 (CD38) is a multifunctional ectoenzyme regulating immune functions, calcium signaling, and nicotinamide adenine dinucleotide (NAD+) metabolism. Through rapid hydrolytic degradation of NAD+, CD38 drives cellular...
Development and preclinical evaluation of [111In]In-DTPA-EphA2-57-1: a single-photon emission computed tomography probe targeting EphA2-expressing tumors [0.03%]
111In标记的DTPA-EphA2-57-1:一种针对表达EphA2肿瘤的单光子发射计算机断层成像技术探针的研究及临床前评估
Minon Sasaki,Hiroyuki Kimura,Takumi Iwasawa et al.
Minon Sasaki et al.
Erythropoietin-producing hepatocellular receptor A2 (EphA2) is overexpressed in various malignant tumors and represents a promising target for cancer-specific imaging and therapy. However, many therapeutics (as well as imaging probes) targe...
Chemoselective and quantitative detection of acrolein based on pyrene excimer fluorescence via cycloaddition reaction of conjugated imine [0.03%]
基于共轭亚胺的环加成反应定量检测丙烯醛的化学选择性检测新方法
Masayuki Takamatsu,Hiroya Tsuchida,Hinako Nabetani et al.
Masayuki Takamatsu et al.
Acrolein is a highly reactive and toxic aldehyde generated in various biological and environmental contexts, including tobacco combustion and cellular oxidative stress. Herein, we present a novel quantitative method for acrolein detection u...
Design, synthesis, and biological evaluation of Chromene-Phenylpiperazine-Chalcone hybrids as multi-target-directed ligands for the treatment of Alzheimer's disease [0.03%]
基于色烯-苯哌嗪-查尔酮杂环衍生物的多靶点配体设计、合成及其对阿尔茨海默病的作用研究
Yuanxiu Liu,Zhenze Jiang,Die Chen et al.
Yuanxiu Liu et al.
A novel series of chromene-phenylpiperazine-chalcone hybrids was rationally designed, synthesized and evaluated as multi-target-directed ligands (MTDLs) for Alzheimer's disease (AD). Among them, compound 9 s exhibited selective equine serum...
Discovery of 1H-pyrazolo[3,4-d]pyrimidin-4-ylamine derivatives as potent PI3Kδ/BTK dual-target inhibitors for the treatment of B-cell lymphoma [0.03%]
作为B细胞淋巴瘤治疗药物的PI3Kδ/BTK双靶点抑制剂1H-吡唑并[3,4-d]嘧啶-4-胺衍生物的研究与发现
Zunyuan Wang,Yingqiao Ye,Youkun Kang et al.
Zunyuan Wang et al.
B-cell lymphoma (BCL) is a hematological system malignant tumor with a relatively high incidence, and PI3Kδ and BTK play an important role in the development of BCL. In the preliminary investigation, we found that when the PI3K inhibitor a...
Identification of daurioxoisoporphine D and moringamine I as blood-brain barrier-permeable natural inhibitors of amyloid-β aggregation and neuronal toxicity [0.03%]
鉴定可穿透血脑屏障的天然抑制淀粉样蛋白聚集和神经毒性的大牻吲哚异卟啉D和幕尼甘胺I
Hayato Yoshikawa,Emi Yoshida,Takahiro Matsumoto et al.
Hayato Yoshikawa et al.
Early Alzheimer's disease (AD) is characterized by extracellular accumulation of amyloid-β (Aβ) peptides and degeneration of basal forebrain cholinergic neurons. Currently, acetylcholinesterase inhibitors and costly anti-Aβ antibodies ar...
Exploration and optimization of indole derivatives as novel anti-HBV agent with potential TLR7-agonistic effect [0.03%]
作为新型抗HBV化合物的吲哚衍生物的探索和优化及其潜在TLR7激动剂效应研究
Lihua Yang,Zibin Qiu,Xincheng Li et al.
Lihua Yang et al.
Hepatitis B virus (HBV) remains a major worldwide health challenge, with disease progression being closely associated with host immune dysregulation, and limited by the resistance of the current anti-HBV drugs. In this study, twenty-six ind...
Discovery of novel 1,2,4-triazoles derivatives acting as NF1 activators against cervical cancer [0.03%]
作为宫颈癌NF1激活剂的新型1,2,4-三唑衍生物的发现
Yao Yin,Zhibing Song,Luqi Wang et al.
Yao Yin et al.
The 1,2,4-triazole scaffold represents a class of bioactive molecules with distinctive physicochemical properties and broad-spectrum biological activities. Previous studies have explored compounds bearing triazole rings for their anti-tumor...
Development of Thieno[2,3-b]pyridin-6(7H)-one derivatives against drug-resistant Mycobacterium tuberculosis [0.03%]
用于抗药性结核分枝杆菌的噻诺并吡啶衍生物的研发
Qin Zha,Zhiyong Liu,Wanwen Li et al.
Qin Zha et al.
In this study, two series of thieno[2,3-b]pyridin-6(7H)-one derivatives were rationally designed via substituent swapping and scaffold flipping strategies. Structure-activity relationship (SAR) analysis identified four compounds exhibiting ...
BNANC clamp PCR for simple and sensitive detection of KRAS and EGFR mutations [0.03%]
适用于KRAS和EGFR突变简单灵敏检测的BNANC clamp PCR方法
Ikuya Ban,Ayako Orita,Haruhisa Yoshikawa et al.
Ikuya Ban et al.
2',4'-BNANC (BNANC)-modified oligonucleotides, which have excellent binding affinity to complementary RNA and DNA strands and high nuclease resistance, were successfully used to develop a new clamp polymerase chain reaction (PCR) method for...