Article
Pharmacology & Pharmacy
Yangming Ding, Haiting Liu, Furun Wang, Lei Fu, Hui Zhu, Shuang Fu, Ning Wang, Xiaomei Zhuang, Yu Lu
Summary: The combination of BDQ and TBI-166 significantly reduces exposure to toxic metabolite M2 by inhibiting the activity of the CYP3A4 pathway.
FRONTIERS IN PHARMACOLOGY
(2023)
Article
Medical Laboratory Technology
Pasindu Wickramarachchi, Jessica M. Boyd, Dennis J. Orton
Summary: The study defined the biological variability of clozapine metabolism and found a significant relationship between kidney function and levels of CLO and NCLO.
CLINICA CHIMICA ACTA
(2022)
Article
Engineering, Biomedical
Yao Lu, Li Lin, Jian Ye
Summary: Metabolites are significant biomarkers that provide direct information about cellular activities and physical conditions. Surface-enhanced Raman spectroscopy (SERS) is a novel and powerful tool for metabolite detection, offering rapid, accurate, and non-destructive detection of metabolites.
MATERIALS TODAY BIO
(2022)
Article
Biotechnology & Applied Microbiology
Jiaye Liu, Junyi Shen, Chunyang Mu, Yang Liu, Dongsheng He, Han Luo, Wenshuang Wu, Xun Zheng, Yi Liu, Sunrui Chen, Qiuwei Pan, Yiguo Hu, Yinyun Ni, Yang Wang, Yong Liu, Zhihui Li
Summary: The study demonstrates a new method involving the one-step self-assembly of calcitriol and amphiphilic cholesterol-based conjugates to form a stable minimalist micellar nanosystem for anticancer treatment, which shows promising efficacy and biocompatibility.
BIOENGINEERING & TRANSLATIONAL MEDICINE
(2022)
Article
Biochemistry & Molecular Biology
Laura E. J. Peeters, Leonardien K. Tjong, Wim J. R. Rietdijk, Teun van Gelder, Birgit C. P. Koch, Jorie Versmissen
Summary: This study aimed to investigate sex differences in blood concentrations of spironolactone and the active metabolite canrenone in resistant hypertension patients, as well as adherence to spironolactone and other antihypertensive drugs (AHDs) between sexes. The findings showed no significant sex differences in spironolactone and canrenone concentrations after adjusting for dose and time. Non-adherence to spironolactone was not significantly different between males and females, but it was associated with non-adherence to other AHDs. Although not statistically significant, females were more likely to be non-adherent to spironolactone compared to males, and thus more likely to be non-adherent to other AHDs.
Review
Plant Sciences
Jhon Venegas-Molina, Francisco J. Molina-Hidalgo, Elke Clicque, Alain Goossens
Summary: The interaction between metabolites and proteins plays a crucial role in cellular regulatory processes within and between organisms. Recent studies have shown that plant metabolites have diverse biological activities beyond their traditional roles, and technologies to study metabolite-protein interactions are being reviewed. This discussion provides insights from both plant and human perspectives, contributing to a better understanding of plant metabolic networks and facilitating agrochemical and drug discoveries.
TRENDS IN PLANT SCIENCE
(2021)
Article
Biochemistry & Molecular Biology
Jun Wang, Xiao Cui, Chen Cheng, Yi Wang, Wei Sun, Cheng-Ke Huang, Rui-Jie Chen, Zhe Wang
Summary: The study found that ketoconazole and voriconazole significantly increased the exposure of sunitinib, decreased the exposure of N-desethyl sunitinib, and inhibited the metabolism of sunitinib in rats. However, itraconazole showed only a weak effect on pharmacokinetics and metabolism. Coadministration of sunitinib with ketoconazole and voriconazole should be avoided or closely monitored.
CHEMICO-BIOLOGICAL INTERACTIONS
(2021)
Article
Biology
Xiuhong Li, Hao Yuan, Xiaoliang Wu, Chengyi Wang, Hongbo Shi, Yingli Lv
Summary: Metabolic processes in the human body are crucial for maintaining normal life activities, and abnormal concentrations of metabolites are closely linked to disease occurrence and development. Drug usage has a significant impact on metabolism, as drug metabolites can influence efficacy, toxicity, and interactions. However, our understanding of metabolite-drug associations remains incomplete, and individual data sources are often incomplete and noisy. Thus, there is an urgent need to integrate various data sources to infer reliable metabolite-drug associations.
COMPUTERS IN BIOLOGY AND MEDICINE
(2023)
Article
Biochemistry & Molecular Biology
Johanna Weiss, Gzona Bajraktari-Sylejmani, Walter Emil Haefeli
Summary: The study found that camostat mesylate and its metabolite GBPA do not significantly inhibit important transporters except for OATP2B1, warranting further investigation. Induction experiments showed no induction of relevant genes by camostat mesylate and GBPA, suggesting a low potential for pharmacokinetic drug-drug interactions. The summary of product characteristics also indicates minimal inhibition of key enzymes in vitro.
CHEMICO-BIOLOGICAL INTERACTIONS
(2021)
Review
Pharmacology & Pharmacy
Amelia Palermo
Summary: Metabolomics enables the analysis of metabolites and lipids in biological systems, and can guide the discovery of lead compounds from natural sources. In combination with other omics, metabolomics can elucidate compound toxicity and mode of action. This article discusses the workflows, limitations, and future opportunities of metabolomics and big data in streamlining pharmaceutical discovery and development.
DRUG DISCOVERY TODAY
(2023)
Article
Chemistry, Analytical
Natarajan Karikalan, Periyasamy Sundaresan, Jun-Hee Na, Tae Yoon Lee
Summary: The rapid advancement of the modern healthcare system calls for cutting-edge technologies in therapeutic drug monitoring. This study introduces a new method for the extraction and determination of drugs from human samples. Through the use of HSA/FeM/rGO system, the drugs can be detected directly without the need for additional sample cleanup.
SENSORS AND ACTUATORS B-CHEMICAL
(2022)
Review
Biochemistry & Molecular Biology
Yali Wu, Lulu Pan, Zhendong Chen, Yuandong Zheng, Xingxing Diao, Dafang Zhong
Summary: Identification of metabolites plays a crucial role in drug development by influencing drug behavior and safety assessment, requiring appropriate methods and strategies for comprehensive identification.
CURRENT DRUG METABOLISM
(2021)
Article
Biochemical Research Methods
Ryo Matsuyama, Yuki Okada, Shuichi Shimma
Summary: The study on APAP-induced liver injury has shown the localization of NAPQI metabolites and changes in endogenous substances in the injured liver, providing insights into the mechanism underlying APAP-ILI. The findings suggest that analyzing tissue damage regions with MALDI-MSI could aid in identifying novel biomarkers for drug-induced liver injury.
ANALYTICAL AND BIOANALYTICAL CHEMISTRY
(2022)
Article
Pharmacology & Pharmacy
Johanna Weiss, Kathrin Isabelle Foerster, Maria Weber, Jurgen Burhenne, Gerd Mikus, Thorsten Lehr, Walter Emil Haefeli
Summary: The metabolite of ketoconazole, N-deacetyl ketoconazole (DAK), is found to inhibit several enzymes and drug transporters in humans, which might affect the efficacy of ketoconazole.
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
(2022)
Article
Environmental Sciences
D. Cerveny, J. Fick, J. Klaminder, E. S. McCallum, M. G. Bertram, N. A. Castillo, T. Brodin
Summary: This study investigated the effects of temperature on the bioconcentration, biotransformation, and accumulation of anxiolytic drugs in aquatic organisms. The results showed that temperature significantly influenced the bioconcentration of temazepam in perch, as well as its biotransformation and accumulation of its metabolite oxazepam. In contrast, dragonfly larvae showed no temperature dependency for temazepam bioconcentration and no detectable biotransformation leading to oxazepam accumulation.
ENVIRONMENT INTERNATIONAL
(2021)
Article
Chemistry, Medicinal
Shibin Zhao, Julian Maceren, Mia Chung, Samantha Stone, Raphael Geiben, Melissa L. Boby, Bradley S. Sherborne, Derek S. Tan
Summary: Antibiotic resistance is a major threat to public health, with Gram-negative bacteria presenting unique challenges due to their low permeability and efflux pumps. Limited understanding of the chemical rules for overcoming these barriers hinders antibacterial drug discovery. Efforts to address this issue, such as screening compound libraries and using cheminformatic analysis, have led to the design of sulfamidoadenosines with diverse substituents, showing potential utility in accumulation in Escherichia coli.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Jichun Li, Qing Li, Shuai Xia, Jiahuang Tu, Longbo Zheng, Qian Wang, Shibo Jiang, Chao Wang
Summary: This study successfully developed a short peptide mimetic as a MERS-CoV fusion inhibitor by reproducing the key recognition features of the HR2 helix. The resulting 23-mer lipopeptide showed comparable inhibitory effect to the 36-mer HR2 peptide HR2P-M2. This has important implications for developing short peptide-based antiviral agents to treat MERS-CoV infection.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Krista Jaunsleine, Linda Supe, Jana Spura, Sten van Beek, Anna Sandstrom, Jessica Olsen, Carina Halleskog, Tore Bengtsson, Ilga Mutule, Benjamin Pelcman
Summary: Beta(2)-adrenergic receptor agonists can stimulate glucose uptake by skeletal muscle cells and are therefore potential treatments for type 2 diabetes. The chirality of compounds has a significant impact on the activity of these agonists. This study found that certain synthesized compounds showed higher glucose uptake activity. These findings provide important information for the design of novel beta(2)AR agonists for T2D treatment.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Xin Xu, Jia Chen, Guan Wang, Xiaojuan Zhang, Qiang Li, Xiaobo Zhou, Fengying Guo, Min Li
Summary: The study focuses on EZH2, a promising therapeutic target for various types of cancers. Researchers designed and synthesized a series of novel derivatives aiming to enhance the EZH2 inhibition activity. Among them, compound 28 displayed potent EZH2 inhibition activity and showed high anti-proliferative effects in lymphoma cell lines and xenograft mouse models. The study suggests that compound 28 has potential as a therapeutic candidate for EZH2-associated cancers.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Wei Zhang, Wei Liu, Ya-Dong Zhao, Li-Zi Xing, Ji Xu, Rui-Jun Li, Yun-Xiao Zhang
Summary: This study developed a series of aromatic amide derivatives based on Rhein and investigated their inhibitory activity against alpha-Syn aggregation. Two of these compounds showed promising potential in treating Parkinson's disease by stabilizing alpha-Syn's conformation and disassembling alpha-Syn oligomers and fibrils.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Mani Sharma, S. S. S. S. Sudha Ambadipudi, Neeraj Kumar Chouhan, V. Lakshma Nayak, Srihari Pabbaraja, Sai Balaji Andugulapati, Ramakrishna Sistla
Summary: Therapeutically active lipids in drug delivery systems can enhance the safety and efficacy of treatment. The liposome formulation created using synthesized biologically active lipids showed additive anti-cancer effects and reduced tumorigenic potential.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)