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Cover Picture: Identification and Optimization of the First Highly Selective GLUT1 Inhibitor BAY‐876 (ChemMedChem 20/2016)
Author(s) -
Siebeneicher Holger,
Cleve Arwed,
Rehwinkel Hartmut,
Neuhaus Roland,
Heisler Iring,
Müller Thomas,
Bauser Marcus,
Buchmann Bernd
Publication year - 2016
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.201600503
Subject(s) - glut1 , front cover , transporter , glut2 , chemistry , glucose transporter , in vivo , in vitro , cover (algebra) , biochemistry , medicine , biology , engineering , gene , mechanical engineering , gene expression , microbiology and biotechnology , insulin
The front cover picture shows a railway track symbolizing the transport of glucose as energy supply into a tumor cell by the GLUT1‐transporter. This import through the GLUT1‐transporter is blocked by a quinolinedicarboxamide, a compound series inhibiting the glucose transport in a competitive, reversible, and very selective manner against GLUT2, 3, and 4. The structure–activity relationship (SAR) and in vitro pharmacokinetics (PK) of the quinolinedicarboxamides presented in this work ended in the shown lead compound BAY‐876, a chemical probe with an appropriate in vivo PK profile for efficacy studies. More information can be found in the Full Paper by Bernd Buchmann et al. on page 2261 in Issue 20, 2016 (DOI: 10.1002/cmdc.201600276).