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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 DOI: 10.21127/yaoyimr20200023
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.
Recent Advances on Interaction Targets for Anticancer Activity of Caffeine
Titi Liu, Chengting Zi, Xuanjun Wang, Jun Sheng, and Huanhuan Xu
Medicine Research DOI: 10.21127/yaoyimr20200020
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.
Recent Advances on Molecular Modeling Studies of Transient Receptor Potential Ankyrin 1
Carita Sallomy, Maija Lahtela-Kakkonen, and Juri M. Timonen
Medicine Research DOI: 10.21127/yaoyigc20200021
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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