Relevance of Reactive Metabolites and Covalent Binding to Drug Candidate Selection [0.03%]
反应性代谢物与共价结合在候选药物选择中的作用
Jack Uetrecht
Jack Uetrecht
Idiosyncratic drug reactions (IDRs)represent a major risk for drug development. Current methods do not reliably predict IDR risk. There is strong evidence that most IDRs are immune-mediated. An adaptive immune response requires 2 signals: s...
Rasha A Guneidy
Rasha A Guneidy
Chemoresistance remains a major barrier in cancer therapy, frequently resulting in treatment failure and reduced patient survival. This multifaceted phenomenon arises from the interplay of well-established mechanisms such as genetic mutatio...
Pregnane X Receptor (PXR/NR1I2): Linking Drug Metabolism, Bile Acid Detoxification, and Cholesterol Homeostasis [0.03%]
孕烷X受体(PXR/NR1I2)与药物代谢、胆汁酸解毒和胆固醇稳态之间的联系
Nila Ganamurali,Sarvesh Sabarathinam
Nila Ganamurali
Pregnane X receptor (PXR; NR1I2) is a promiscuous ligand-activated nuclear receptor traditionally recognized as a master regulator of xenobiotic detoxification. Beyond xenobiotic detoxification, emerging evidence implicates PXR as a pivotal...
CYP24A1: The Pivotal Regulator of Vitamin D Homeostasis, Pathophysiology in Metabolic and Genetic Disease, and Emerging Target for Precision Medicine [0.03%]
CYP24A1维生素D稳态的关键调节因子及其在代谢和遗传性疾病中的病理生理作用和作为精准医学新兴靶点的作用
NavodiSandamini Jayathilaka,Weththasinghe A V,Wijekoon D M K J et al.
NavodiSandamini Jayathilaka et al.
CYP24A1 (25-hydroxyvitamin D3 24-hydroxylase) functions as the essential catabolic "off-switch" of the vitamin D endocrine axis. As a mitochondrial cytochrome P450 enzyme, it tightly regulates calcitriol (1,25(OH)2D3) levels through a remar...
Role of Herbal Extracts in Modulating Drug Metabolism: Implications for Pharmacokinetics, Enzyme Regulation, and Therapeutic Outcome [0.03%]
herbal extracts在调节药物代谢中的作用：对药代动力学、酶调控和治疗效果的影响
Alina Khan,Gadah Abdulaziz Al-Hamoud,Musarat Amina et al.
Alina Khan et al.
Herbal medicines are widely used worldwide, often alongside prescription drugs, creating the potential for clinically significant herb-drug interactions. These interactions are frequently mediated by effects on drug-metabolizing enzymes, pa...
Pharmacokinetic considerations and strategies for antibody-based therapeutics [0.03%]
抗体药物的药代动力学考虑和策略
Juanhong Zhang,Rong Chang,Anpeng Zhao et al.
Juanhong Zhang et al.
Antibody-based therapeutics are specifically designed to bind to antigens, thereby facilitating the treatment of various diseases, including tumors and autoimmune disorders, resulting in significant therapeutic effects. Notably, the therape...
Phase II Metabolism in Xenobiotic Biotransformation: General Mechanisms and the Underestimated Role of Microbial Systems [0.03%]
外来化合物生物转化中的二期代谢：一般机制及其微生物系统的 underestimated 作用
Aleksandra Pietrzak,Barbara Dąbrówka,Justyna Popiół et al.
Aleksandra Pietrzak et al.
Microbial phase II biotransformation, involving conjugation reactions such as glycosylation, sulfation, and glucuronidation, is increasingly recognized as a valuable in vitro model for mammalian xenobiotic metabolism, particularly drug meta...
Cunzhen Zhang,Yan Fang,Lin Jia et al.
Cunzhen Zhang et al.
Cytochrome P450 (CYP450) enzymes play a crucial role in drug metabolism, and their content and activity are important parameters in pharmacokinetic studies. However, due to variations in sample size, background information, and detection me...
Multimolecular interactions from Chinese medicines activate nuclear receptor conformational changes: a potential strategy for anti-inflammatory therapy [0.03%]
中药多分子间相互作用可激活核受体构象改变：抗炎治疗的新策略
Xuechun Yu,Ying Zhang,Bingxin Wu et al.
Xuechun Yu et al.
Nuclear receptors (NRs) are among the most common transcriptional regulators in the human body. Currently, liver X receptor (LXR), pregnane X receptor (PXR), farnesoid X receptor (FXR), and peroxisome proliferator-activated receptor (PPAR) ...
Analytical Techniques for Methyldopa and Metabolites: A Comprehensive Review [0.03%]
甲基多巴及其代谢产物的分析技术：综述
Hemn A H Barzani,Seerwan Hamadameen Sulaiman,Rebaz Anwar Omer et al.
Hemn A H Barzani et al.
Methyldopa, a centrally acting α2-adrenergic agonist, remains a key antihypertensive drug, particularly prescribed for pregnant and renal-impaired patients. Its clinical significance has led to extensive research aimed at developing reliab...