High-Throughput CETSA Identifies Small Molecule Modulators of ILT3 (LILRB4) with Functional Activity in Human iPSC-Derived Microglia for Alzheimer's Disease [0.03%]
高通量CETSA识别出对阿尔茨海默病诱导 pluripotent干细胞来源的小胶质细胞具有功能活性的ILT3（LILRB4）小分子调节剂
Somaya A Abdel-Rahman,Moustafa Gabr
Somaya A Abdel-Rahman
Immune inhibitory signaling in microglia contributes to impaired amyloid-β (Aβ) clearance and neuroinflammation in Alzheimer's disease (AD), yet small molecule modulators targeting these pathways remain largely unexplored. Here, we report...
Novel Substituted Heterocyclic Carboxamindes as α2C-ARs Antagonists [0.03%]
新型杂环羧酸胺类α2C-肾上腺素受体拮抗剂及其制备和应用
Jian Rong,Steven H Liang
Jian Rong
This patent describes heterocyclic carboxamindes as new, highly effective α2C-Adrenergic receptor (α2C-AR) antagonists, suitable for treating α2C-ARs-associated disorders. It offers detailed information on the heterocyclic carboxamindes,...
Correction to "Mechanistic Insights from Differences in the Aggregate Morphologies of Amphotericin B and Its Less Toxic Variant Am-2-19" [0.03%]
关于“两性霉素B及其低毒突变体Am-2-19聚集形态差异的机制见解”的勘误通知
Luke Ting-Williams,Martin Stroet,Evelyne Deplazes
Luke Ting-Williams
[This corrects the article DOI: 10.1021/acsmedchemlett.6c00070.]. © 2026 American Chemical Society.
Published Erratum
ACS medicinal chemistry letters. 2026 Jun 24;17(7):1675. DOI:10.1021/acsmedchemlett.6c00306 2026
Correction to "Novel Small Molecule-Derived, Highly Selective Substrates for Fibroblast Activation Protein (FAP)" [0.03%]
“新型小分子衍生物纤维激活蛋白（FAP）的高度选择性底物”的勘误通知
An De Decker,Gwendolyn Vliegen,Dries Van Rompaey et al.
An De Decker et al.
[This corrects the article DOI: 10.1021/acsmedchemlett.9b00191.]. © 2026 American Chemical Society.
A Dual-Action Gold(I) Prodrug Targeting Redox Homeostasis and Extracellular Matrix Remodeling in Ovarian Cancer [0.03%]
一种靶向氧化还原平衡和细胞外基质重塑的抗卵巢癌金(I)前药Dual-Action Gold(I) Prodrug Targeting Redox Homeostasis and Extracellular Matrix Remodeling in Ovarian Cancer
Riccardo Di Leo,Enrico Crispino,Lorenzo Chiaverini et al.
Riccardo Di Leo et al.
Ovarian cancer is characterized by early metastatic dissemination, frequent relapses, and limited therapeutic options following the onset of platinum resistance. To address these challenges, a dual-action gold-(I) prodrug, RDL-15, was desig...
Xin Zhou,Steven H Liang
Xin Zhou
PARP1 is a key DNA damage response enzyme that supports tumor-cell survival through PARP-mediated DNA repair. Although FDA-approved PARP inhibitors have validated this therapeutic strategy, limited PARP1/PARP2 selectivity may cause adverse ...
Ligand-Engineered Cu(II) Complexes Suppress Stemness and Drug Resistance in Triple-Negative Breast Cancer [0.03%]
配体工程化Cu(II)复合物可抑制三阴性乳腺癌的干细胞特性及耐药性
Vemavarapu Durga Prasad,Suriya Panneerselvam,Jyotirmoy Dutta et al.
Vemavarapu Durga Prasad et al.
Triple-negative breast cancer (TNBC) is an aggressive malignancy characterized by cancer stem cell (CSC) enrichment and multidrug resistance. Here, we report a series of Cu-(II) complexes (Cu1-Cu4) designed to investigate the impact of liga...
Vasicine-Based Synergistic Antifungal Agents against FLC-Resistant Candida albicans Targeting Ras/cAMP/PKA Pathway [0.03%]
一种针对FLC耐药性白念珠菌的雷琐辛为基础的联用抗真菌制剂作用于Ras/cAMP/PKA途径
Di Zhao,Wengang Wang,Zhichang Xu et al.
Di Zhao et al.
A series of novel vasicine-based derivatives were designed and synthesized, and in vitro antifungal activities were evaluated. Most compounds showed synergistic antifungal effects with fluconazole (FLC) against FLC-resistant C. albicans. Co...
Discovery of Biased Dual-Agonists of Glucagon-Like Peptide 1 and Glucagon Receptors through Mutation of a Conserved Aspartate [0.03%]
通过突变保守天冬氨酸发现胰高血糖素样肽1和胰高血糖素受体的偏置双激动剂
Robert E Thompson,Aditya J Desai,Dmitri Pissarnitski et al.
Robert E Thompson et al.
Peptide agonists of the glucagon-like peptide 1 receptor (GLP-1R) have demonstrated clinical efficacy for the management of type 2 diabetes and promote weight loss in addition to glucose-dependent insulin secretion. Monomolecular dual- or t...
Novel Bridged Tricyclic Carbamoylpyridone Compounds as HIV Integrase Inhibitors for Treating HIV Infection [0.03%]
新型桥连三环 carbamoylpyridone 化合物作为 HIV 整合酶抑制剂用于治疗 HIV 感染
Ram W Sabnis
Ram W Sabnis
Provided herein are novel bridged tricyclic carbamoylpyridone compounds as HIV integrase inhibitors, pharmaceutical compositions, use of such compounds in treating HIV infection, and processes for preparing such compounds. ...