Discovery of Novel Isofunctional SARS-CoV‑2 NSP14 RNA Cap Methyltransferase Inhibitors by Structure-Based Virtual Screening [0.03%]
基于结构的虚拟筛选发现新型异功能SARS-CoV-2 NSP14 RNA帽甲基转移酶抑制剂
Cindy Meyer,Mayako Michino,David J Huggins et al.
Cindy Meyer et al.
In early 2020, SARS-CoV-2 spread into a worldwide pandemic, causing more than 7 million deaths. Direct-acting antivirals (DAAs) complementing vaccines and mitigating severe disease in at-risk populations remain important. Here, we used a st...
A Nucleoside Analogue Featuring a C3'-Stereogenic All-Carbon Quaternary Center as a Bioenergetic Disruptor of KRAS-Mutated Pancreatic Cancer Cells [0.03%]
一种具有C3'-立体生成的全碳季碳中心的核苷类似物作为KRAS突变型胰腺癌细胞生物能量破坏剂
Houda Tantawi,Philippe Mochirian,Mathieu Truong et al.
Houda Tantawi et al.
A novel nucleoside analogue, LCB-2151, has been developed to induce cell death in KRAS-mutated pancreatic human cancer cell lines, which exhibit partial resistance to gemcitabine, a widely used anticancer drug. LCB-2151 disrupts the two pri...
Tricyclic and Novel Chemotypes as Selective WRN Helicase Inhibitors for MSI‑H Cancer Therapy [0.03%]
三环和新型结构的WRN解旋酶选择性抑制剂用于MSI-H阳性肿瘤的治疗
Robert B Kargbo
Robert B Kargbo
Recent advances targeting WRN helicase highlight a promising synthetic lethality approach for treating microsatellite instability-high (MSI-H) cancers. GlaxoSmithKline and Moma Therapeutics independently developed small molecule inhibitors ...
Discovery of Potent and Selective Quinoline-Based Toll-like Receptor 9 Antagonists [0.03%]
一类高效特异的喹啉类 toll 样受体 9 拮抗剂的发现
Xue Song,Chen-Guo Feng,Chen Wang et al.
Xue Song et al.
The Toll-like receptor (TLR) family are critical components of the innate immune system, acting as pattern recognition receptors that detect microbial components and initiate immune responses. In humans, 10 TLRs have been identified, each r...
Ram W Sabnis
Ram W Sabnis
Provided herein are novel compounds as 5-HT2A agonists, pharmaceutical compositions, use of such compounds in treating depression, and processes for preparing such compounds. ...
Radiosynthesis and Biological Evaluation of a Small-Molecule Probe for Thyroid-Stimulating Hormone Receptor [0.03%]
甲状腺刺激激素受体的小分子探针的放射合成和生物评价
Yuanyuan Zhou,Ji Tao,Yuanpeng Jiang et al.
Yuanyuan Zhou et al.
The thyroid-stimulating hormone receptor (TSHR) plays a pivotal role in regulating thyroid growth, function, synthesis, and secretion of thyroid hormones, with its overexpression linked to various diseases, especially in tumors. A novel TSH...
Chelator Optimization and Therapeutic Potential of 188Re-FAPI for FAP-Targeted Radionuclide Therapy [0.03%]
优化配体以用于放射性核素治疗中的188Re-FAPI及其治疗潜力
Steven H Liang
Steven H Liang
Fibroblast activation protein (FAP) has emerged as a highly promising molecular target for cancer theranostics, with current research prioritizing the optimization of FAP-targeted radiopharmaceutical pharmacokinetics. The development of div...
Radiosynthesis and Preclinical Evaluation of a Carbon-11 Labeled Phosphodiesterase 7 Inhibitor for PET Neuroimaging [0.03%]
一种用于PET神经影像的放射合成及药理评价磷二酯酶7抑制剂同位素标记碳-11化合物的研究
Zhiwei Xiao,Jiyun Sun,Masayuki Fujinaga et al.
Zhiwei Xiao et al.
Dysfunction of cyclic nucleotide phosphodiesterase 7 (PDE7) has been associated with excess intracellular cAMP concentrations, fueling pathogenic processes that are implicated in neurodegenerative disorders. This study aimed to develop a su...
Ram W Sabnis
Ram W Sabnis
Provided herein are novel tricyclic compounds as ERK5 inhibitors, pharmaceutical compositions, use of such compounds in treating cancer, and processes for preparing such compounds. ...
Novel Fused Heterocycles as 5‑HT2A Receptor Agonists for Treating Neurological Diseases, Namely, Depression, Anxiety, Substance Abuse, and Headaches [0.03%]
新型杂环化合物作为五羟色胺2A受体激动剂用于治疗神经系统疾病(如抑郁、焦虑、药物滥用和头痛)
Ram W Sabnis
Ram W Sabnis
Provided herein are novel fused heterocycles as 5-HT2A receptor agonists, pharmaceutical compositions, use of such compounds in treating neurological diseases, namely depression, anxiety, substance abuse and headaches, and processes for pre...