Physiologically Based Pharmacokinetic Model for Clinical Translation and Prediction of Drug Interaction of the Major Kratom Alkaloid, Mitragynine [0.03%]
基于生理的药代动力学模型在 kratom 主要生物碱美屈矿临床转化和药物相互作用预测中的应用
Yi-Hua Chiang,Siva Rama Raju Kanumuri,Erin C Berthold et al.
Yi-Hua Chiang et al.
The opioid crisis presents a significant public health issue and underscores the urgency of developing effective treatments for opioid use disorder (OUD). Mitragynine (MTG), the major active alkaloid found in kratom (Mitragyna speciosa), pr...
Bioisosteric Replacement of Amides with 1,2,3-Triazoles Improves Dopamine D4 Receptor Ligand Pharmacokinetics [0.03%]
1,2,3-三氮唑等生物电子等排体替换改善多巴胺D4受体配体的药代动力学性质
Mohammad Alkhatib,Franziska M Jakobs,John N Hanson et al.
Mohammad Alkhatib et al.
Dopamine D4 receptor (D4R) signaling affects decision-making, memory formation, cognition, and attention. Previously developed D4R-selective ligands were metabolically unstable in vivo due to amide bond linker hydrolysis. In this study, ana...
Target Class Repurposing Across Membrane Transporter Families Provides Privileged Ligands to Address Specific and Undruggable Pharmacological Targets [0.03%]
跨膜转运蛋白家族的目标类再定位提供了针对特定和难以成药的药理学靶标的特权配体
Muhammad Rafehi,Franziska Tägl,Nike Sophia Arlt et al.
Muhammad Rafehi et al.
Altogether, 60-70% of the ATP-binding cassette (ABC) and solute carrier (SLC) transporters can currently not be targeted by drugs, despite their involvement in human diseases. The design of potential drug candidates relies on hit identifica...
Correction to "Newly Synthesized Indolylacetic Derivatives Reduce Tumor Necrosis Factor-Mediated Neuroinflammation and Prolong Survival in Amyotrophic Lateral Sclerosis Mice" [0.03%]
有关“新合成的吲哚乙酸衍生物可降低肿瘤坏死因子介导的神经炎症并延长渐冻症小鼠生存期”的勘误通知
Angela Corvino,Giuseppe Caliendo,Ferdinando Fiorino et al.
Angela Corvino et al.
[This corrects the article DOI: 10.1021/acsptsci.4c00098.]. © 2026 American Chemical Society.
Published Erratum
ACS pharmacology & translational science. 2026 Feb 2;9(2):461. DOI:10.1021/acsptsci.6c00037 2026
When Neutrophils Go Rogue: Dysregulated Inflammation in Airway Diseases and Implications for Therapy [0.03%]
当中性粒细胞不受控制时：气道疾病中的炎症失调及其对治疗的启示
Yimin Zhu,Sarmi Sardar,Jane E Bourke et al.
Yimin Zhu et al.
Failure to resolve the neutrophilic inflammation during the innate immune response results in neutrophil accumulation in the airways. These cells exhibit prolonged survival, increased necrosis, and impaired phagocytic capacity. Paradoxicall...
Correction to "Comprehensive Characterization of Bruton's Tyrosine Kinase Inhibitor Specificity, Potency, and Biological Effects: Insights into Covalent and Noncovalent Mechanistic Signatures" [0.03%]
“布鲁顿酪氨酸激酶抑制剂的特异性、活性及生物学效应的全面特征分析：共价和非共价作用机制的新见解”的勘误证
Antonia C Darragh,Andrew M Hanna,Justin Lipner et al.
Antonia C Darragh et al.
[This corrects the article DOI: 10.1021/acsptsci.4c00540.]. © 2026 The Authors. Published by American Chemical Society.
Published Erratum
ACS pharmacology & translational science. 2026 Jan 9;9(2):460. DOI:10.1021/acsptsci.5c00551 2026
Adenosine-Specific Transcriptional Programs in Murine Connective Tissue-Type Mast Cells [0.03%]
小鼠连接结缔组织型肥大细胞的特异性转录谱系
Qihua Liang,Volodymyr Tsvilovskyy,Anouar Belkacemi et al.
Qihua Liang et al.
Mast cells are tissue-resident immune cells that are critical for the pathogenesis of allergic and inflammatory disorders. Their physiological functions include host defense against parasites and, more recently, food quality control through...
The Neuroprotective Effects of Agomelatine in a 3‑Nitropropionic Acid-Induced Rat Model of Huntington's Disease via Brain-Derived Neurotrophic Factor (BDNF)/tropomyosin-Related Kinase Receptor Type B (TrKB)/Phosphoinositide 3‑Kinase (PI3K)/Protein Kinase B (AKT) Activation and Rho-Associated Protein Kinase 1 (ROCK1) Pathway Inhibition [0.03%]
阿戈美拉汀通过激活脑源性神经营养因子/原肌球蛋白受体激酶B/磷脂酰肌醇3-激酶/蛋白激酶B信号通路和抑制Rho相关卷曲调节蛋白激酶1信号通路对3-硝基丙酸诱导的亨廷顿舞蹈病大鼠模型发挥神经保护作用
Hossam H Abouzaid,Rabab H Sayed,Walaa Wadie et al.
Hossam H Abouzaid et al.
The accumulation of CAG nucleotide duplicates in the huntingtin (HTT) gene triggers a neurological ailment described as Huntington's disease (HD), which is an irreversible, progressive, and inherited condition and affects both motor and cog...
Navigating the Landscape of Antibiotic Safety: Traditional Approaches and Emerging Strategies to Overcome Host Ribonucleic Acid (RNA) Off-Target Toxicity [0.03%]
抗生素安全性的探索之路：克服宿主核糖核酸(RNA)脱靶毒性的传统方法和新兴策略
Tanya Jamal,Rinni Singh,Mukul Bajpai et al.
Tanya Jamal et al.
Antibiotics inhibit bacterial reproduction by blocking cell wall synthesis, protein synthesis, and nucleic acid synthesis as well as altering the cell membrane. Bacteria live in hosts like normal flora. However, they can become pathogenic d...
Peptide-Functionalized Liposomal Nanocarriers for Targeted Therapy of Liver Fibrosis and Hepatocellular Carcinoma: Design, Mechanisms, and Clinical Prospects [0.03%]
用于肝纤维化和肝细胞癌靶向治疗的肽功能脂质体纳米载体：设计、机制及临床前景
Kashif Maroof,Ronald Fook Seng Lee,Pinar Karacabey et al.
Kashif Maroof et al.
Liver fibrosis and hepatocellular carcinoma (HCC) remain major global health burdens, in part due to limited drug specificity, off-target toxicity, and the complex hepatic microenvironment. Peptide-functionalized liposomal nanocarriers have...