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Back Cover: Selective Inhibitors of Glutathione Transferase P1 with Trioxane Structure as Anticancer Agents (ChemMedChem 4/2015)
Author(s) -
Bräutigam Maria,
Teusch Nicole,
Schenk Tobias,
Sheikh Miriam,
Aricioglu Rocky Z.,
Borowski Swantje H.,
Neudörfl JörgMartin,
Baumann Ulrich,
Griesbeck Axel G.,
Pietsch Markus
Publication year - 2015
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.201590010
Subject(s) - chemistry , trioxane , glutathione , stereochemistry , transferase , small molecule , molecule , enzyme , substrate (aquarium) , combinatorial chemistry , biochemistry , organic chemistry , biology , ecology , copolymer , polymer
The back cover picture shows a 3D model of the tumor‐relevant, homodimeric form of human glutathione transferase P1 (GSTP1, PDB: 5GSS) and inhibition of its enzymatic activity by a synthetic 1,2,4‐trioxane. This compound and analogous derivatives are able to interact with the glutathione binding site of each GSTP1 monomer and often exhibit a parabolic competitive mode of inhibition where two molecules of inhibitor compete with one substrate molecule for binding. For further details, see the Full Paper by Markus Pietsch et al. on p. 629 ff.