Discovery of R-185 as a Potent and Orally Efficacious GPR52 Agonist with Potential for Treating Schizophrenia and Related Neuropsychiatric Disorders [0.03%]
发现R-185为潜在治疗精神分裂症和相关神经精神疾病的高效口服有效的GPR52激动剂
Haoran Li,Shuli Xia,Pengqi Zhang et al.
Haoran Li et al.
G protein-coupled receptor 52 (GPR52) has been identified as a promising therapeutic target for the treatment of schizophrenia, psychiatric disorders, and other human neurological diseases. A series of novel 2,3-disubstituted pyrazine deriv...
Design and Evaluation of 68Ga-Labeled Peptide-Based PET Probes for Noninvasive Imaging of ROR1 Expression in Tumor Models [0.03%]
用于非侵入性成像肿瘤模型中ROR1表达的基于肽的放射性显影剂68 Ga标记PET探针的设计与评价
Tao Yang,Qi An,Siying Lin et al.
Tao Yang et al.
The receptor tyrosine kinase-like orphan receptor 1 (ROR1) is aberrantly overexpressed in multiple malignancies and has emerged as a clinically relevant biomarker for tumor staging and therapeutic decision-making. Here, we developed a serie...
Pyridoimidazolyl Sulfonamide Compound 2: A Superior Dual-Acting Drug Candidate with Potent URAT1 Inhibition and Anti-Inflammatory Activity for Gout Management [0.03%]
嘧啶并吡咯磺酰胺类化合物2：一种用于治疗痛风的高效URAT1抑制和抗炎活性的双效药物候选物
Xiaoyu Shi,Cheng Shi,Mingyu Yang et al.
Xiaoyu Shi et al.
The management of hyperuricemia and gout remains constrained by the narrow therapeutic index of current drugs. To improve the druggability of our previously identified URAT1 inhibitor T7, we replaced its carboxylic acid with a sulfonamide g...
Discovery of Pyrrolo[1',2':1,6]pyrimido[5,4- c]pyridazin-6(5 H)-one Derivatives as Ectonucleotide Pyrophosphatase/Phosphodiesterase 1 Inhibitors [0.03%]
作为ectonucleotide焦磷酸酶/磷酸二酯酶1抑制剂的嘧啶并[5,4-c]哒嗪-6(5H)-酮衍生物类化合物的研究发现
Cuijie Nong,Mengyuan Zhu,Weilun Zheng et al.
Cuijie Nong et al.
ENPP1 is emerging as a potential target for cancer immunotherapy due to its negatively regulatory effect on the STING pathway via hydrolysis of cGAMP. Herein, we report the identification and optimization of compound A25 starting from hit c...
Development of a Light-Triggered Biotin-Bioorthogonal System for Targeted Anti-Tumor Therapy [0.03%]
一种光控生物素-生物正交系统用于肿瘤靶向治疗的研究与发展
Youlu Pan,Chaonan Tang,Zhiqiang Zeng et al.
Youlu Pan et al.
Recently, bioorthogonal reactions have been widely applied in drug delivery. However, conventional bioorthogonal reactions, such as the uncontrollable coupling between tetrazine (TZ) and trans-cyclooctene (TCO), lack effective control. To a...
Postmodification of Daptomycin at Tryptophan Enables the Discovery of Aryl-Daptomycin Antibiofilm Activity against MRSA [0.03%]
色氨酸后修饰的达托霉素使发现对抗MRSA的抗生物膜活性 Aryl-达托霉素抗菌素活动发现
Tiantian Yan,Jingyue Li,Yiping Li et al.
Tiantian Yan et al.
Biofilm-related infections pose a growing global health threat and demand novel therapeutic agents. Although Daptomycin is effective against Gram-positive bacteria and biofilms, the emergence of resistant strains necessitates next-generatio...
Unique Thiazolidinedione Conjugation of Metronidazole to Largely Enhance the Antibacterial Performance of Natural Berberine against Bacterial Pathogens [0.03%]
一种独特的苯并噻唑衍生物结合甲硝唑使天然小分子 berberine 具有广谱抗菌效果
Yu Zhou,Shi-Yu Huang,Zhen-Zhen Li et al.
Yu Zhou et al.
This work performed a unique conjugation of metronidazole with berberine via thiazolidinedione to afford a novel structural skeleton of metronidazolyl vinylthiazolidionyl tetrahydroberberines (MVTs) with multitargeting antibacterial potenti...
First-in-Class Covalent Inhibitors of PFKFB3: Discovery and Characterization in PDAC Models [0.03%]
新型共价PFKFB3抑制剂的发现及PDAC模型中的作用机制研究
Alessandra Fiore,Antonio Scarano,Giulia Antonini et al.
Alessandra Fiore et al.
Pancreatic ductal adenocarcinoma (PDAC) is an aggressive cancer, driven by metabolic reprogramming. Since direct glycolytic enzyme inhibition is limited by toxicity, indirect glycolysis modulation through inhibition of the kinase activity o...
Identification and Validation of 3-Cyano-Quinoline Ligands Targeting Integrin-Linked Kinase (ILK) [0.03%]
用于靶向整合素连接激酶（ILK）的3-氰基喹啉配体的鉴定与验证
Francesco Aleksy Greco,Kamal Rayees Abdul Azeez,Marko Mitrović et al.
Francesco Aleksy Greco et al.
Integrin-linked kinase (ILK) is a pseudokinase that directly interacts with β-integrins and plays a pivotal role in regulating focal adhesion function. ILK has been implicated in the development of various diseases, particularly cancer. Ho...
Correction to "Discovery of Imidazo[2,1- b][1,3,4]thiadiazole-Based MNK Inhibitors with Anti-inflammatory Efficacy via Dual Suppression of eIF4E Phosphorylation and NF-κB Signaling" [0.03%]
关于“基于咪唑并[2，1- b][1,3,4]噻二唑的MNK抑制剂的发现：此类抑制剂可通过双重抑制eIF4E磷酸化和NF-κB信号传导发挥抗炎作用”一文的更正通知
Hongwei Li,Huiying Zhuang,Dianxi Zhang et al.
Hongwei Li et al.
Published Erratum
Journal of medicinal chemistry. 2026 May 25. DOI:10.1021/acs.jmedchem.6c01548 2026