Call for Papers: Pharmaceutical Innovation and Global Health: Breakthroughs and Future─Celebrating the 90th Anniversary of China Pharmaceutical University [0.03%]
征文通知:医药创新与全球健康:新突破和未来——中国药科大学90周年校庆特刊
Hai Qian,Hongbin Sun,Can Zhang et al.
Hai Qian et al.
Luiza Cruz,Lori Ferrins,William C K Pomerantz et al.
Luiza Cruz et al.
Call for Papers: Medicinal Chemistry Strategies in Accelerated Drug Discovery-Celebrating Fudan University's 120th Anniversary [0.03%]
征稿通知:加速药物发现的医药化学策略——庆祝复旦大学120周年校庆
Shuai Wang,Fener Chen
Shuai Wang
A Structure-guided Active Site Affinity Ligand Unmasks a Stress-Sensitizing Role for BLVRB in the Endoplasmic Reticulum [0.03%]
基于结构的底物类似物诱导BLVRB失活并将其定位在内质网以缓解细胞压力
Rahul Raghavan Thekke Veedu,Jawaad Sheriff,Natasha M Nesbitt et al.
Rahul Raghavan Thekke Veedu et al.
Biliverdin IXb reductase (BLVRB) is an NAD(P)H-dependent oxidoreductase that regulates hematopoiesis and cellular stress, although measurement and sequelae of cellular active site engagement remain undefined. Here, we report the development...
Identification of a New, Potent, and Stable Tetrahydroquinoline-Based 5-LOX/sEH Dual Inhibitor with Polymodal Anti-Inflammatory Activity in Acute Pancreatitis [0.03%]
一种新的、有效的和稳定的四氢异喹啉类5-LOX/sEH双通道抑制剂用于急性胰腺炎的多模式抗炎活性研究
Danilo DAvino,Tania Ciaglia,Paul M Jordan et al.
Danilo DAvino et al.
Acute pancreatitis (AP) is a common, serious, pancreatic inflammation representing an unmet therapeutical need. Here, we report the design and synthesis of a series of compounds as dual 5-lipoxygenase (LOX)/soluble epoxide hydrolase (sEH) i...
Design, Synthesis, and Evaluation of Novel Phenoselenazine Derivatives as Potent Modulators of Aβ42 Aggregation [0.03%]
设计、合成及评估新型苯硒氮杂衍生物作为 potent Aβ42 纤丝化调节剂的效果
Ahmed A Hefny,Rahul C Karuturi,Chandra Mouli R Madhuranthakam et al.
Ahmed A Hefny et al.
A novel class of fused tricyclic phenoselenazine derivatives possessing a redox-active selenium atom were designed, synthesized, and evaluated as Aβ42 aggregation inhibitors with antioxidant activity. They exhibit remarkable inhibition of ...
Molecular Construction and Anti-Bladder Cancer Study of Novel TOP1/PARP1 Dual-Target Inhibitors [0.03%]
新型TOP1/PARP1双靶向抑制剂的合成及抗膀胱癌研究
Wenchao Wang,Dan Li,Jin Liu et al.
Wenchao Wang et al.
Bladder cancer is a malignant tumor with a high incidence and mortality worldwide. Clinically, DNA-damaging agents such as cisplatin, irinotecan, and gemcitabine are commonly used, but their efficacy is often limited by acquired resistance....
A ROS-Responsive Dual-Functional H2S Donor for Synergistic Cardioprotection [0.03%]
一种ROS响应型供H2S试剂在心血管保护中的应用研究
Rong-Hong Zhang,Jin-Feng Long,Yi-Ying Lian et al.
Rong-Hong Zhang et al.
The therapeutic utility of H2S donors in myocardial ischemia/reperfusion injury (MIRI) is hampered by the lack of spatiotemporally controlled release at the site of injury and the poor molecular economy of donor scaffolds. Herein, we design...
Discovery of 1 H-Indole-3-Propionamide Derivatives as Potent, Selective and Orally Available NaV1.7 Inhibitors for Pain Treatment [0.03%]
发现一系列具有痛觉调控作用的钠离子通道NaV1.7抑制剂INDOLE类化合物
Kai Chen,Xi He,Gaoang Wang et al.
Kai Chen et al.
Dysfunction of the voltage-gated sodium channel NaV1.7 underlies multiple pain-sensitivity disorders, making NaV1.7 inhibition an attractive therapeutic strategy. However, currently available NaV1.7 inhibitors, frequently suffer from limite...