Structure-Activity Relationships of Highly Potent and Selective A2B Adenosine Receptor Agonists [0.03%]
高效选择性A2B腺苷受体激动剂的构效关系研究
Christopher J Smedley,Jon Kyle Awalt,Anh T N Nguyen et al.
Christopher J Smedley et al.
A series comprised of N6-substituted adenosines designed from the A2B adenosine agonist 4 were synthesized and their A2BR potency was assessed in a cAMP accumulation assay using FlpINCHO cells stably expressing the human A2BR. This study id...
Correction to "Exploring the HIV-1 Reverse Transcriptase p51/p66 Interface: Structure-Based Design and Optimization of Novel 2,4,6-Trisubstituted Pyrimidines as Potent NNRTIs with Improved Resistance Profiles" [0.03%]
“探索HIV-1逆转录酶p51/p66界面：基于结构的设计和优化新型2,4,6-三取代的嘧啶为高效的非核苷类逆转录酶抑制剂并改善耐药性”的纠正通知
Xiangkai Ji,Xiangyi Jiang,Zhen Gao et al.
Xiangkai Ji et al.
Published Erratum
Journal of medicinal chemistry. 2025 Oct 23. DOI:10.1021/acs.jmedchem.5c02923 2025
Scaffold Fusion and SAR Transfer with a Chemical Language Model Generates Novel Liver X Receptor Modulators [0.03%]
基于化学语言模型的支架融合及构效关系跃迁生成新颖的肝脏X受体调节剂
Nils Christiaan Bandomir,Tim Hörmann,Annette Kärcher et al.
Nils Christiaan Bandomir et al.
Liver X receptors (LXRs) are promising targets for metabolic disorders including atherosclerosis and metabolic dysfunction-associated steatotic liver disease (MASLD). In this study, we employed a chemical language model (CLM) for LXR modula...
Precision Chemoradiotherapy via EGFR Targeting with Radiotherapy-Activated Drug Conjugates [0.03%]
用于EGFR靶向的放射激活型药物偶联物的精准化学放疗
Shanmeng Lin,Jinyan Luo,Jinying Yang et al.
Shanmeng Lin et al.
The strategy of concurrent chemoradiotherapy (CCRT) has been developed, aiming to leverage the benefits of chemotherapy and radiotherapy while mitigating their respective limitations. In this study, we innovatively employed an azobenzene st...
Design and Implementation of a High-Throughput Experimentation Platform to Accelerate Drug Discovery [0.03%]
一种用于加速药物发现的高通量实验平台的设计与实现
Amanda W Dombrowski,Ana L Aguirre,Ying Wang
Amanda W Dombrowski
Herein, we describe the development of the high-throughput experimentation platform and function in AbbVie's Discovery Chemistry organization. The strategy and approach tailored specifically to medicinal chemistry needs are discussed. Addit...
Dexamethasone-Appended Activatable Prodrug Overcoming Multidrug Resistance [0.03%]
具有地塞米松的可激活前药克服多药耐药性
Jungryun Kim,Chong Hu,Paramesh Jangili et al.
Jungryun Kim et al.
Residual tumor cells that persist after chemotherapy, even in minimal quantities, often exhibit drug resistance and increased invasiveness, potentially leading to tumor metastasis and recurrence. This study introduces a novel reactive oxyge...
Exploring Chemically Modified Short Activating RNAs to Increase Stability against Nucleases and Enhance Gene Activation [0.03%]
探索化学修饰的短激活RNA以增加稳定性和增强基因激活性能
Jean-Paul Desaulniers,Matthew L Hammill,Ifrodet Giorgees et al.
Jean-Paul Desaulniers et al.
Short activating RNAs (saRNAs) are short duplex RNAs that activate genes in the nucleus of the cell. This induces gene activation, or RNA activation (RNAa), which upregulates gene expression. This activation is in direct contrast to short i...
Water-Soluble NIR-II Photothermal Agent for Sprayable Skin Cancer Therapy [0.03%]
一种用于喷洒式皮肤癌治疗的近红外二区光热疗法水溶性制剂
Liang Zhao,Han Zhu,Qing-Qing Ye et al.
Liang Zhao et al.
Skin cancer therapy demands noninvasive approaches to overcome current treatments' limitations, and second near-infrared window (NIR-II) photothermal agents offer potential solutions with deep tissue penetration and high efficiency. However...
Apoptosis, Oxidative Stress, and Cell Cycle Disruption: Antitumor Effects of a Novel Palladium(II) Complexes [0.03%]
凋亡、氧化应激及细胞周期紊乱：一个新的钯(II)复合物的抗肿瘤效应
Olga Klaudia Szewczyk,Piotr Roszczenko,Nurbey Gulia et al.
Olga Klaudia Szewczyk et al.
The development of novel metal-based anticancer agents with higher selectivity and lower toxicity is a major goal in oncology. In this study, four newly synthesized palladium(II) complexes (1a, 1b, 1c, 2a) were tested for cytotoxicity again...
RTx-303, an Orally Bioavailable Polθ Polymerase Inhibitor That Potentiates PARP Inhibitors in BRCA Mutant Tumors [0.03%]
RTx-303：一种可口服的Polθ聚合酶抑制剂，可通过增强BRCA突变肿瘤的PARP抑制作用来发挥疗效
Gurushankar Chandramouly,William Fried,John Gordon et al.
Gurushankar Chandramouly et al.
DNA polymerase θ (Polθ) is a polymerase-helicase fusion protein that is synthetically lethal with homologous recombination (HR) factors, such as BRCA1/2, and confers resistance to PARP inhibitors (PARPi) and other genotoxic cancer therapi...