Identification of the atypical L-type Ca2+ channel blocker diltiazem and its metabolites as ghrelin receptor agonists [0.03%]
地尔硫卓和其代谢产物被鉴定为生长激素释放肽受体激动剂
Jian-Nong Ma,Hans H Schiffer,Anne E Knapp et al.
Jian-Nong Ma et al.
Using a high-throughput functional screen, the atypical L-type Ca2+ channel blocker diltiazem was discovered to be an agonist at the human ghrelin (GHSR1a) receptor. In cellular proliferation, Ca2+ mobilization, and bioluminescence resonanc...
UR-1505, a new salicylate, blocks T cell activation through nuclear factor of activated T cells [0.03%]
UR-1505，一种新的水杨酸盐通过活化T细胞核因子抑制T细胞活化
Juan Román,Alberto Fernández de Arriba,Sonia Barrón et al.
Juan Román et al.
2-Hydroxy-4(-2,2,3,3,3-pentafluoropropoxy)-benzoic acid (UR-1505), a new molecule chemically related to salicylic acid, has immunomodulator properties and is currently under clinical development for treatment of atopic dermatitis. The prese...
Molecular approximations between residues 21 and 23 of secretin and its receptor: development of a model for peptide docking with the amino terminus of the secretin receptor [0.03%]
分泌素及其受体的第21至23位残基间的分子结构近似：分泌素与受体氨基端肽结合模型的发展研究
Maoqing Dong,Polo C-H Lam,Fan Gao et al.
Maoqing Dong et al.
The structurally unique amino-terminal domain of class II G protein-coupled receptors is critically important for ligand binding and receptor activation. Understanding the precise role it plays requires detailed insights into the molecular ...
5-Androstenediol promotes survival of gamma-irradiated human hematopoietic progenitors through induction of nuclear factor-kappaB activation and granulocyte colony-stimulating factor expression [0.03%]
雄甾烯二醇通过诱导核因子κB活化及粒细胞集落刺激因子表达促进γ射线照射的人造血祖细胞的存活
Mang Xiao,Cynthia E Inal,Vaishali I Parekh et al.
Mang Xiao et al.
5-Androstenediol (5-AED) stimulates hematopoiesis and enhances survival in animals exposed to ionizing radiation (IR), suggesting that this steroid may act on hematopoietic progenitor cells. We used gamma-irradiated primary human CD34(+) he...
APETx1 from sea anemone Anthopleura elegantissima is a gating modifier peptide toxin of the human ether-a-go-go- related potassium channel [0.03%]
来自Urticina elegans的APETx1是一种人类 Ether-à-go-go 相关钾通道的门控调节肽毒素
M Zhang,X-S Liu,S Diochot et al.
M Zhang et al.
We studied the mechanism of action and the binding site of APETx1, a peptide toxin purified from sea anemone, on the human ether-a-go-go-related gene (hERG) channel. Similar to the effects of gating modifier toxins (hanatoxin and SGTx) on t...
Beta1 (KCNMB1) subunits mediate lithocholate activation of large-conductance Ca2+-activated K+ channels and dilation in small, resistance-size arteries [0.03%]
胆石酸通过β1亚单位活化大电导钙激活钾通道并导致小阻力血管舒张
Anna N Bukiya,Jianxi Liu,Ligia Toro et al.
Anna N Bukiya et al.
Among the nongenomic effects of steroids, control of vasomotion has received increasing attention. Lithocholate (LC) and other physiologically relevant cholane-derived steroids cause vasodilation, yet the molecular targets and mechanisms un...
Erlotinib, an effective epidermal growth factor receptor tyrosine kinase inhibitor, induces p27KIP1 up-regulation and nuclear translocation in association with cell growth inhibition and G1/S phase arrest in human non-small-cell lung cancer cell lines [0.03%]
厄洛替尼，一种有效的表皮生长因子受体酪氨酸激酶抑制剂，通过上调和促进p27KIP1核转位与G1/S期阻滞相关的细胞增殖抑制来诱导人非小细胞肺癌细胞系中的生长抑制
Yi-He Ling,Tianhong Li,Ziqiang Yuan et al.
Yi-He Ling et al.
Erlotinib, a small-molecule epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor, has been shown to have potent antitumor effects against human non-small-cell lung cancer (NSCLC) cell growth; however, the mechanism of such an e...
Identification and characterization of a new tubulin-binding tetrasubstituted brominated pyrrole [0.03%]
新的结合微管蛋白的四取代溴代吡咯的鉴定与表征
Susan L Mooberry,Kimberly N Weiderhold,Sivanesan Dakshanamurthy et al.
Susan L Mooberry et al.
We studied the mechanism of action of 3,5-dibromo-4-(3,4-dimethoxyphenyl)-1H-pyrrole-2-carboxylic acid ethyl ester (JG-03-14) and found that it is a potent microtubule depolymerizer. JG-03-14 caused a dose-dependent loss of cellular microtu...
Transcriptional regulation of brain-derived neurotrophic factor in the amygdala during consolidation of fear memory [0.03%]
下丘脑内 consolidation 恐惧记忆期间脑源性神经营养因子的转录调控
Li-Chin Ou,Po-Wu Gean
Li-Chin Ou
We have demonstrated previously that brain-derived neurotrophic factor (BDNF) signaling in the amygdala is required for the consolidation of fear memory. This study is designed to characterize the signal cascades by which fear conditioning ...
Site-specific inhibition of glomerulonephritis progression by targeted delivery of dexamethasone to glomerular endothelium [0.03%]
糖皮质激素定点递送抑制系膜增生性肾炎进展
Sigridur A Asgeirsdóttir,Jan A A M Kamps,Hester I Bakker et al.
Sigridur A Asgeirsdóttir et al.
Glomerulonephritis represents a group of renal diseases with glomerular inflammation as a common pathologic finding. Because of the underlying immunologic character of these disorders, they are frequently treated with glucocorticoids and cy...