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Cover Illustration
2021, Vol.5  No.1
The cover picture shows computational drug design methods that have been applied for examining transient receptor potential ankyrin 1 (TRPA1) and its ligands. Three binding sites of ligands have been proposed for TRPA1 so far. The binding of various ligands into TRPA1 has been explored with molecular docking and molecular dynamics.More details are discussed in the article by Timonen et al. on page 200021.

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  • Table of Content
      20 January 2021, Volume 5 Issue 1 Previous Issue    Next Issue
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    Prodrug Systems (II): A Perspective of Polymer-Based Doxorubicin Prodrug Systems towards Chemotherapy
    Zhao Wang, Filipe Olim, Jingjing Sun, Ana Rute Neves, Fátima Mendes, Helena Tomás, and Ruilong Sheng
    Medicine Research. 2021, 5 (1): 200023.   DOI: 10.21127/yaoyimr20200023
    Abstract   PDF (669KB) ( )
    Utilizing biocompatible polymers as platforms to covalently conjugate with chemotherapeutics to construct polymer-based prodrugs and their nano drug delivery systems has attracted great attention in recent years. This perspective reviewed state-of-the-arts for polymer-based doxorubicin prodrugs and the related nanodelivery systems, including: (1) pH-responsive polymer-doxorubicin prodrugs/conjugates; (2) pH/redox- dual responsive prodrugs/conjugates; (3) reactive oxygen species/hypoxia-responsive polymer-doxorubicin prodrugs; (4) tumor receptor targeting polymer prodrugs; (5) enzyme-responsive polymer-doxorubicin prodrugs. Finally, possible future perspectives were also stated and discussed.
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    Recent Advances on Interaction Targets for Anticancer Activity of Caffeine
    Titi Liu, Chengting Zi, Xuanjun Wang, Jun Sheng, and Huanhuan Xu
    Medicine Research. 2021, 5 (1): 200020.   DOI: 10.21127/yaoyimr20200020
    Abstract   PDF (416KB) ( )
    Caffeine (1,3,7-trimethylxanthine) is the most frequently ingested neuroactive drug in the world and has enigmatic effects on tumor cells. Convincing evidence from in vitro, animal and human studies suggests that caffeine can inhibit cancer development and progression. Caffeine can easily pass through biological mem-branes and cross the blood-brain barrier, and it is thereby possible to bind to extracellular or intracellular molecules to exert its functions. This review mainly focuses on recent advances in the direct interaction targets of caffeine in the inhibition of malignancies and will hopefully provide valuable insights into the clinical application of caffeine to the treatment of cancers.
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    Recent Advances on Molecular Modeling Studies of Transient Receptor Potential Ankyrin 1
    Carita Sallomy, Maija Lahtela-Kakkonen, and Juri M. Timonen
    Medicine Research. 2021, 5 (1): 200021.   DOI: 10.21127/yaoyigc20200021
    Abstract   PDF (753KB) ( )
    Transient receptor potential ankyrin 1 (TRPA1) is an ion channel involved in nociception. In addition, TRPA1 activation triggers an inflammatory response, which intensifies the sensation of pain. The role of TRPA1 in pain makes it an attractive target for painkiller drug design. The research on TRPA1 antagonists and agonists has increased in recent years with the focus on discovering novel and effective TRPA1 antagonists. This minireview describes some computational drug design methods that have been applied for examining TRPA1 and its ligands. So far, three ligand binding sites have been proposed for TRPA1. The binding of various ligands into TRPA1 has been explored with molecular docking and molecular dynamics. This is the first review that con-centrates on TRPA1 computational studies.
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    Recent Advances on Small-Molecule Tubulin Inhibitors
    Xiu-Li Sun, Yin-Rong Xie, Ning Zhang, Cheng-Ting Zi, Xuan-Jun Wang, and Jun Sheng
    Medicine Research. 2021, 5 (1): 200024.   DOI: 10.21127/yaoyimr20200024
    Abstract   PDF (778KB) ( )
    Microtubules are heterodimers composed of α/β tubulin and make up the cytoskeleton. It plays an important role in maintaining cellular morphology, cell division, signal transduction and other processes. At present, six tubulin inhibitor binding sites have been identified. The inhibitors can be divided into two categories: a type of microtubule polymerization agent includes colchicine site, vinblastine site, maytansine site and prionetin site inhibitors; another category is paclitaxel and laulimalide/peloruside binding site inhibitors are called microtubule depolymerization. Herein, we summarize relevant inhibitors acting on these 6 sites and their research status. With extensive research on tubulin binding sites and inhibitors, anti-tumor tubulin inhibitors will possess very broad clinical prospects.
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    Adverse Reactions and Resistance of Anticancer Drug Cisplatin
    Zhonglie Yang, Li Lin, Xiaoyan Peng, Xinyi Yu, Xiaobin Zhang, Hezhong Jiang, and Jiahong Li
    Medicine Research. 2021, 5 (1): 200022.   DOI: 10.21127/yaoyimr20200022
    Abstract   PDF (546KB) ( )
    Since 1978, cisplatin has become a leading anticancer drug for its high efficacy and unique mechanism of action. As a representative of platinum anticancer drugs, cisplatin has an excellent curative effect and broad application range of cancer. However, its application is limited by high toxicity and drug resistance. This review mainly focuses on adverse reactions and drug resistance of cisplatin.
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