Design and synthesis of novel GluN2A NMDAR positive allosteric modulators via scaffold hopping strategy as anti-stroke therapeutic agents [0.03%]
通过支架跳转策略设计和合成新型的GluN2A NMDAR阳性变构调节剂作为抗中风药物
Xin Chen,Hongyu Zhu,Xuequan Liu et al.
Xin Chen et al.
NMDA receptor subunits have differential roles in mediating excitotoxic neuronal death both in vitro and in vivo . Activation of NR2A-containing NMDA receptors promotes neuronal survival and exerts a neuroprotective action, whereas over act...
Development of sulfonium tethered peptides conjugated with HDAC inhibitor to improve selective toxicity for cancer cells [0.03%]
一种新的组蛋白去乙酰化酶抑制剂-肽缀合物用于提高抗癌选择性毒性的研究
Li Du,Chunli Song,Jingjing Du et al.
Li Du et al.
The anti-cancer peptides emerged as new weapons for cancer therapy due to their potent toxicity toward various cancer cells. However, their therapeutic promise is often limited by non-specific toxicity to normal cells. How to improve peptid...
18F-Labeled o‑aminopyridyl alkynyl radioligands targeting colony-stimulating factor 1 receptor for neuroinflammation imaging [0.03%]
18F标记的o-氨基吡啶基丙炔型放射配体结合集落刺激因子1受体用于神经炎症成像
Xiaodan An,Jingqi Wang,Linjiang Tong et al.
Xiaodan An et al.
We report the design, synthesis and evaluation of five o‑aminopyridyl alkynyl derivatives as colony-stimulating factor 1 receptor (CSF-1R) ligands. Compounds 4 and 5 with the fluoroethoxy group at the meta- or para-position of the phenyl r...
Examination of aminophenol-containing compounds designed as antiproliferative agents and potential atypical retinoids [0.03%]
用作抗增殖剂和潜在非典型维甲酸的含氨基酚化合物的研究
Ramesh M Chingle,Masahiko Imai,Sarah Altman et al.
Ramesh M Chingle et al.
Retinoic acid (RA, 1), an oxidized form of vitamin A, binds to retinoic acid receptors (RAR) and retinoid X receptors (RXR) to regulate gene expression and has important functions such as cell proliferation and differentiation. Synthetic li...
Design, synthesis and biological evaluation of the tumor hypoxia-activated PROTACs bearing caged CRBN E3 ligase ligands [0.03%]
基于笼状CRBN E3连接酶配体的肿瘤低氧激活型PROTAC的设计、合成及生物活性评价
Weiyan Cheng,Shasha Li,Siyuan Han et al.
Weiyan Cheng et al.
Tumor hypoxia-activated proteolysis targeting chimeras (ha-PROTACs) 9 and 10 were designed and synthesized by incorporating the hypoxia-activated leaving group (1-methyl-2-nitro-1H-imidazol-5-yl)methyl or 4‑nitrobenzyl into the structure o...
Synthesis, biological activity and mechanism of action of novel allosecurinine derivatives as potential antitumor agents [0.03%]
新型L- allosecurinine衍生物的合成、生物活性及其抗肿瘤作用机制研究
Xin-Liang Xu,Jin-Xia Lan,Hao Huang et al.
Xin-Liang Xu et al.
Cancer with low survival rates is the second main cause of death among all diseases in the world and consequently, effective antineoplastic agents are urgently needed. Allosecurinine is a plant-derived indolicidine securinega alkaloid shown...
A novel selective estrogen receptor degrader induces cell cycle arrest in breast cancer via ERα degradation and the autophagy-lysosome pathway [0.03%]
一种新型选择性雌激素受体降解剂可通过降解ERα和自噬溶酶体途径诱导乳腺癌细胞周期停滞
Jiawei Zhou,Rong Shen,Jing Liu et al.
Jiawei Zhou et al.
Breast cancer (BC), a well-known estrogen-dependent cancer, is the most common cancer among women and the leading cause of cancer deaths. One of the most important therapeutic approaches for BC is endocrine therapy targeting estrogen recept...
Brian P Callahan,Zihan Xu
Brian P Callahan
A native enzyme's usual assurance in recognizing their physiological substrate(s) at the ground state and on going to the transition state can be undermined by interactions with selected small molecule antagonists, leading to the generation...
Simple monocyclic pyrimidine analogs as microtubule targeting agents binding to the colchicine site [0.03%]
简单的单环嘧啶类似物作为微管靶向(colчиcin结合位点)药物
Shruti Choudhary,Krishna Kaku,Andrew J Robles et al.
Shruti Choudhary et al.
Complex natural products that bind to tubulin/microtubules come under the broad category of microtubule binding agents. The design of simplified analogs of previously reported bicyclic, microtubule depolymerizer, pyrrolo[2,3-d]pyrimidine, p...
LC-MS/MS analysis of elastin crosslinker desmosines and microscopic evaluation in clinical samples of patients with hypertrophy of ligamentum flavum [0.03%]
腰椎黄韧带肥厚患者临床样本中弹性蛋白交联物desmosine的LC-MS/MS分析及显微镜下评估
Christian Nanga Chick,Tomoo Inoue,Natsuki Mori et al.
Christian Nanga Chick et al.
Ligamentum flavum (LF) pathologies often lead to severe myelopathy or radiculopathy characterized by reduced elasticity, obvious thickening, or worsened ossification. Elastin endows critical mechanical properties to tissues and organs such ...