New TRPM8 Amino Acid-Based Antagonists Induce Antiproliferative Effect on 2D and 3D Melanoma and Prostate Cancer Models [0.03%]
新型TRPM8氨基酸拮抗剂对二维和三维黑色素瘤及前列腺癌模型的抗增殖作用
Tania Ciaglia,Marzia Di Donato,Veronica Di Sarno et al.
Tania Ciaglia et al.
The pharmacological potential of TRPM8 modulators ranges from neuropathic pain to tumor treatment, as this channel is involved in intracellular calcium homeostasis. We acquired considerable expertise in developing TRPM8 antagonists, which w...
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 D&#x;Avino,Tania Ciaglia,Paul M Jordan et al.
Danilo D&#x;Avino 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...