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Front Cover: Structure‐Activity‐Relationship‐Aided Design and Synthesis of xCT Antiporter Inhibitors (ChemMedChem 17/2021)
Author(s) -
Cirillo Davide,
Sarowar Shahin,
Øyvind Enger Per,
Bjørsvik HansRené
Publication year - 2021
Publication title -
chemmedchem
Language(s) - English
Resource type - Reports
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.202100563
Subject(s) - front cover , chemistry , intracellular , molecule , glutathione , combinatorial chemistry , oxidative stress , biophysics , stereochemistry , biochemistry , cover (algebra) , enzyme , organic chemistry , biology , mechanical engineering , engineering
The Front Cover shows some of the xCT inhibitor molecule candidates that were synthesised through a structure–activity relationship study, in which each candidate molecule was evaluated for its capability to inhibit the xCT antiporter (the blue‐coloured gate) that leads into the orange‐coloured cell. A successful xCT inhibitor candidate operates as a gatekeeper that does not allow cystine molecules arriving from the right‐hand side to enter the cell through the blue gate. The intracellular biosynthesis of glutathione is then hampered, making the cell unable to handle free radicals caused by oxidative stress. The effect from the xCT inhibitor can be used as radiosensitiser for clinical use in combination with radiotherapy. Cover design by Ms. Beatrice Karen Bjørsvik. More information can be found in the Full Paper by Hans‐René Bjørsvik et al.