2020 Vol. 10, No. 3

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Preface for special issue on new analytical techniques and methods in drug metabolism and pharmacokinetics
Guangbo Ge, Mingshe Zhu
2020, 10(3): 前插1-前插2.
Abstract(163) PDF(7)
Abstract:
Analytical technologies and approaches for drug metabolism and pharmacokinetics (DMPK) research in the pharmaceutical industry and academic research institutes have evolved rapidly over the past decade. On one hand. the discovery and development of small molecule drug candidates requires earlier and...
Current status and future directions of high-throughput ADME screening in drug discovery
Wilson Z. Shou
2020, 10(3): 201-208.
Abstract(267) PDF(16) [Cited by] (62)
Abstract:
During the last decade high-throughput in vitro absorption, distribution, metabolism and excretion (HT-ADME) screening has become an essential part of any drug discovery effort of synthetic molecules. The conduct of HT-ADME screening has been"industrialized"due to the extensive development of softwa...
Current LC-MS-based strategies for characterization and quantification of antibody-drug conjugates
Xiaoyu Zhu, Shihan Huo, Chao Xue, Bo An, Jun Qu
2020, 10(3): 209-220.
Abstract(410) PDF(21) [Cited by] (61)
Abstract:
The past few years have witnessed enormous progresses in the development of antibody-drug conju-gates (ADCs). Consequently, comprehensive analysis of ADCs in biological systems is critical in sup-porting discovery, development and evaluation of these agents. Liquid chromatography-mass spectrometry (...
Current status of in vivo bioanalysis of nano drug delivery systems
Tingting Wang, Di Zhang, Dong Sun, Jingkai Gu
2020, 10(3): 221-232.
Abstract(251) PDF(4) [Cited by] (44)
Abstract:
The development of nano drug delivery systems (NDDSs) provides new approaches to fighting against diseases. The NDDSs are specially designed to serve as carriers for the delivery of active pharmaceutical ingredients (APIs) to their target sites, which would certainly extend the benefit of their uniq...
Ultra-sensitive bioanalysis of the therapeutic peptide exenatide for accurate pharmacokinetic analyses at effective plasma concentrations utilizing UPLC-MS/MS
Max Sauter, Philipp Uhl, Jürgen Burhenne, Walter E. Haefeli
2020, 10(3): 233-239.
Abstract(215) PDF(10) [Cited by] (7)
Abstract:
Exenatide is the first approved glucagon-like peptide 1 receptor agonist subcutaneously or intramus-cularly injected for the treatment of type 2 diabetes mellitus. Typical therapeutic plasma concentrations are in the low pg/mL range, therefore requiring ultra-sensitive quantification. To enable the ...
Software-aided detection and structural characterization of cyclic peptide metabolites in biological matrix by high-resolution mass spectrometry
Ming Yao, Tingting Cai, Eva Duchoslav, Li Ma, Xu Guo, Mingshe Zhu
2020, 10(3): 240-246.
Abstract(225) PDF(5) [Cited by] (6)
Abstract:
Compared to their linear counterparts, cyclic peptides show better biological activities, such as anti-bacterial, immunosuppressive, and anti-tumor activities, and pharmaceutical properties due to their conformational rigidity. However, cyclic peptides could form numerous putative metabolites from p...
Quantitation of DNA by nuclease P1 digestion and UPLC-MS/MS to assess binding efficiency of pyrrolobenzodiazepine
Yong Ma, Buyun Chen, Donglu Zhang
2020, 10(3): 247-252.
Abstract(154) PDF(3) [Cited by] (4)
Abstract:
Accurate DNA quantitation is a prerequisite in many biomedical and pharmaceutical studies. Here we established a new DNA quantitation method by nuclease P1 digestion and UPLC-MS/MS analysis. DNA fragments can be efficiently hydrolyzed to single deoxyribonucleotides by nuclease P1 in a short time. Th...
Rapid bioluminescence assay for monitoring rat CES1 activity and its alteration by traditional Chinese medicines
Jun Zhang, Dandan Wang, Liwei Zou, Min Xiao, Yufeng Zhang, Ziwei Li, Ling Yang, Guangbo Ge, Zhong Zuo
2020, 10(3): 253-262.
Abstract(153) PDF(3) [Cited by] (8)
Abstract:
In traditional Chinese medicine herbs (TCM), including Radix Salviae Miltiorrhizae (Danshen), Radix Puerariae Lobatae (Gegen), Radix Angelicae Sinensis (Danggui), and Rhizoma Chuanxiong (Chuanxiong) are widely used for the prevention and treatment of cardiovascular diseases and also often co-adminis...
An ultra-sensitive and easy-to-use assay for sensing human UGT1A1 activities in biological systems
Ya-Di Zhu, Hui-Lin Pang, Qi-Hang Zhou, Zi-Fei Qin, Qiang Jin, Moshe Finel, Yi-Nan Wang, Wei-Wei Qin, Yin Lu, Dan-Dan Wang, Guang-Bo Ge
2020, 10(3): 263-270.
Abstract(133) PDF(4) [Cited by] (12)
Abstract:
The human UDP-glucuronosyltransferase 1A1 (UGT1A1), one of the most essential conjugative enzymes, is responsible for the metabolism and detoxification of bilirubin and other endogenous substances, as well as many different xenobiotic compounds. Deciphering UGT1A1 relevance to human diseases and cha...
Screening of the whole human cytochrome P450 complement (CYPome) with enzyme bag cocktails
Sangeeta Shrestha Sharma, Shishir Sharma, Matthias Bureik
2020, 10(3): 271-276.
Abstract(197) PDF(1) [Cited by] (11)
Abstract:
We have previously introduced the use of permeabilized fission yeast cells (enzyme bags) that recom-binantly express full-length CYPs for drug metabolism studies. Such enzyme bags are cells with pores that function as enzymes in situ. They can easily be prepared without a need for ultracentrifugatio...

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