A preliminary study of phosphodiesterases and adenylyl cyclase ...
2023年9月15日 · RBC deformability is a key factor in the pathogenesis of SCD, and is affected by various factors. In this study, we investigated the effects of adenylyl cyclase (AC) signaling pathway modulation and different phosphodiesterase (PDE) modulatory molecules on the deformability and mechanical stress responses of RBC from SCD patients (HbSS genotype ...
Role of phosphodiesterase type 3A and 3B in regulating ... - PubMed
Phosphodiesterase type 3 (PDE3) is an important regulator of cAMP-mediated responses within the cardiovascular system. PDE3 exists as two subtypes: PDE3A and PDE3B, with distinct cellular and subcellular locations. Due to the lack of subtype-specific pharmacological tools, the definitive role of eac …
Therapeutic targeting of 3′,5′-cyclic nucleotide ... - Nature
2019年8月6日 · Phosphodiesterases (PDEs), enzymes that degrade 3′,5′-cyclic nucleotides, are being pursued as therapeutic targets for several diseases, including those affecting the...
Reduced deformability contributes to impaired deoxygenation …
The findings from Study 2 suggest that this may be the case given that treatment with cilostazol to target PDE3, which is multiple steps downstream of the initial haemoglobin deoxygenation stimulus in the proposed RBC signalling cascade for deoxygenation-induced ATP release (Ellsworth & Sprague, 2012), had no effect on impaired ATP release from ...
Human Erythrocyte Acetylcholinesterase in Health and Disease
The biochemical properties of erythrocyte or human red blood cell (RBC) membrane acetylcholinesterase (AChE) and its applications on laboratory class and on research are reviewed. Evidence of the biochemical and the pathophysiological properties ...
Structure of PDE3A–SLFN12 complex and structure-based design …
2021年10月27日 · In this work, we report the high-resolution cryo-electron microscopy structure of PDE3A-SLFN12 complexes isolated from cultured HeLa cells pre-treated with either anagrelide, or nauclefine, or...
磷酸二酯酶(PDE)及其抑制剂概述.ppt 30页 - 原创力文档
2017年3月4日 · PDE3被抑制时，细胞内cAMP的分解代谢受阻，cAMP可激活多种蛋白激酶，肌浆网上大量Ca2+大量释放，进而使心肌收缩增强和周围血管扩张。 氨力农 作用机制 抑制细胞因子的产生 抑制NO的过度产生 对神经激素的影响 药理作用研究 可改善血管疾病患者的微循环 有较强的抗血栓形成作用 通过改善血流动力学，增加呼吸肌收缩力，改善肺顺应性 对冠状动脉血流动力学有改善作用 增加出血性休克的生存率 米力农 氨力农长期治疗的效果不佳，口服反而使心力衰 …
磷酸二酯酶(PDEs) - 知乎 - 知乎专栏
pde3：分布于心脏、血管平滑肌、血小板、肾、肝、免疫细胞等;其作用包括:调节心肌收缩力、血小板聚集、血管平滑肌收缩、肾素释放及胰岛素信号转导等；
【文献分享】PDE3A-SLFN12复合物的结构以及基于该复合物的药 …
该文章利用冷冻电镜解析了三种结构不同的小分子化合物 (anagrelide, nauclefine, DNMDP) 处理条件下的PDE3A-SLFN12复合物结构，通过对复合物结构的分析，获得小分子与蛋白复合物相互作用的关键结构信息。 基于所获得的PDE3A-SLFN12复合物结构模型与结合模式，作者选用了临床上药代动力学、药效学和安全性都较好的anagrelide作为目标分子进行计算机模拟和进一步优化改造。 结果表明，改造后的anagrelide类似物诱导细胞发生凋亡的活性更高，且在小鼠成瘤模型实 …
用于治疗呼吸系统疾病的双靶点PDE3/4抑制剂研究进展
2021年1月8日 · 慢性阻塞性肺病和哮喘是以气道阻塞为主要表现的复杂炎症性疾病, 已成为严重影响人类健康的呼吸道常见疾病。与临床单独使用pde3或pde4抑制剂相比, 双靶点pde3/4抑制剂具有协同的抗炎和支气管扩张作用, 近年来引起广泛关注。本文综述目前处于临床前和临床 ...