Estimation of In Vivo Half-Life From In Vitro Metabolic Clearance, Protein, and Cell Membrane Affinity Assays [0.03%]
基于体外代谢清除率、蛋白结合和细胞膜亲和力测定估算体内半衰期
Carla Pou Miralbell,Sandrine Desrayaud,Berndt Oberhauser et al.
Carla Pou Miralbell et al.
A reliable prediction of the in vivo plasma half-life of drug candidates, from easily accessible in vitro assays, is not yet possible. It is surmised that the existing models, which consider protein binding and metabolic clearance, will be ...
Identification of a New Interesting BAG3 Modulator Able to Disrupt Cancer-Related Pathways [0.03%]
鉴定出一种新的有趣的BAG3调节物能够破坏与癌症相关的途径
Dafne Ruggiero,Eleonora Boccia,Emis Ingenito et al.
Dafne Ruggiero et al.
Continuing our research aimed at discovering new BAG3 modulators as attractive anticancer drug candidates, we performed a screening campaign on an in-house library, including compounds featuring a large variety of scaffolds. The obtained re...
Cyclin-dependent Kinase 11: Cellular Functions and Potential Therapeutic Applications [0.03%]
细胞周期蛋白依赖性激酶11的细胞功能及其潜在治疗应用
Janhabee Shrestha,Jason Blanchard,Solomon Tadesse
Janhabee Shrestha
Cyclin-dependent kinase 11 (CDK11) is a multifunctional serine/threonine protein kinase that plays a pivotal role in transcription and pre-mRNA splicing. It phosphorylates serine 2 of RNA polymerase II C-terminal domain, thereby promoting t...
Adamantane Appended 1,2,3-Triazole Hybrids: Synthesis and α-Glucosidase Inhibition Studies Through Experimental and In Silico Approach [0.03%]
金刚烷偶联三氮唑杂环化合物的合成及通过实验和计算方法研究其α-葡萄糖苷酶抑制活性
Aman Ragshaniya,Subhadip Maity,Lokesh Kumar et al.
Aman Ragshaniya et al.
In search of potent inhibitors of α-glucosidase, we have synthesized amide coupled adamantane derived 1,2,3-triazoles (4a-4f, 6a-6f, and 8a-8f) using Click reaction. After establishing their structure using spectral studies, all the molecu...
Development of Novel Anticancer Pyrazolopyrimidinones Targeting Glioblastoma [0.03%]
新型抗脑肿瘤吡唑并嘧啶酮的研究进展
Kate Byrne,Natalia Bednarz,Ciara McEvoy et al.
Kate Byrne et al.
Glioblastoma (GBM) is the most common and aggressive malignant grade IV brain tumour and is one of the most difficult types of brain cancer to treat with a high incidence of resistance to traditionally used chemotherapeutics. Pyrazolopyrimi...
3'-Dehydroxypurpurogallin-4-Carboxamides as Influenza A Endonuclease Inhibitors: Synthesis, Structure-Activity Relationship Analysis, and Structural Characterization of Protein Complex [0.03%]
3'-脱羟基矢车菊素-4-甲酰胺类化合物作为流感内切酶抑制剂：合成，构效关系分析和蛋白质复合物结构解析
Michal Kráľ,Tomáš Kotačka,Róbert Reiberger et al.
Michal Kráľ et al.
Published Erratum
ChemMedChem. 2025 Jul 3:e2500452. DOI:10.1002/cmdc.202500452 2025
NSAIDS AS MODULATORS OF CATION CHANNELS: FENAMATES REPURPOSING IN CHANNELOPATHIES [0.03%]
非甾体抗炎药作为阳离子通道调节剂：呋喃基苯甲酸盐在通道病中的再利用
Paola Laghetti,Concetta Altamura,Simone Dell&#x;Atti et al.
Paola Laghetti et al.
Cationic ion channels are transmembrane proteins that regulate the flux of cations (potassium, sodium, and calcium) across cell membrane, playing a pivotal role in many cellular functions. Disruptions of their activity can lead to the so-ca...
Recent Progress of Antibacterial Carbon Dots Prepared from Marketed Small Molecule Antibacterial Drugs [0.03%]
基于市售抗菌药物小分子制备的抗菌碳点研究进展
Yuequan Wu,Meng He,Zhi-Hao Li et al.
Yuequan Wu et al.
The massive consumption of antibiotics leads to antibiotic resistance, which is a major concern in the global health crisis. Therefore, the development of non-antibiotic antibacterial drugs occurs simultaneously with the development of anti...
Discovery of a Phenylalanine-derived Natural Compound as a Potential Dual Inhibitor of MDM2 and MDMX [0.03%]
苯丙氨酸衍生物作为MDM2和MDMX双功能抑制剂的发现研究
Ja Young Cho,Sanghwa Park,Taejung Kim et al.
Ja Young Cho et al.
Dual inhibition of the negative p53 regulators MDM2 and MDMX has emerged as an effective strategy in p53-based anticancer therapy. However, dual inhibitors are limited, and many inhibitors exhibit poor pharmacokinetic properties and fast di...
Synthesis and Characterization of Sulfonamide-Imidazole Hybrids with In Vitro Antiproliferative Activity Against Anthracycline-Sensitive and Resistant H69 SCLC Cells [0.03%]
具有抗有氧耐药小细胞肺癌H69细胞活性的磺酰胺-咪唑杂化物的合成与表征
Valdas Vainauskas,Povilas Kavaliauskas,Birutė Grybaitė et al.
Valdas Vainauskas et al.
A series of novel sulfonamide-imidazole hybrid derivatives was synthesized, and their antiproliferative properties were evaluated. The global challenge of cancer, highlighted by rising morbidity and mortality rates, is further intensified b...