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Pyrrolo[1,2‐ a ]quinoxalines: Insulin Mimetics that Exhibit Potent and Selective Inhibition against Protein Tyrosine Phosphatase 1B
Author(s) -
GarcíaMarín Javier,
Griera Mercedes,
SánchezAlonso Patricia,
Di Geronimo Bruno,
Mendicuti Francisco,
RodríguezPuyol Manuel,
Alajarín Ramón,
PascualTeresa Beatriz,
Vaquero Juan J.,
RodríguezPuyol Diego
Publication year - 2020
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.202000710
Subject(s) - glucose transporter , biochemistry , protein tyrosine phosphatase , insulin receptor , insulin , chemistry , phosphatase , small molecule , receptor tyrosine kinase , tyrosine , microbiology and biotechnology , biology , receptor , enzyme , endocrinology , insulin resistance
The Front Cover shows a C2C12 cell with the inhibitor 4‐benzylpyrrolo[ 1,2‐a ]quinoxaline targeting the α3/α6/α7 tunnel in the Protein Tyrosine Phosphatase 1B (PTP1B) represented as a ribbon diagram. The insulin receptor (clear green) and the glucose transporter (clear yellow) shown at the cell membrane are involved in the glucose uptake by the cell. The inhibition of PTP1B by this molecule and their analogues produces an insulin mimetic effect. This is indicated by red arrows for the glucose molecules (in sticks) crossing the cell membrane to the cytosol. Cover design by Javier García‐Marín. More information can be found in the Full Paper by Manuel Rodríguez‐Puyol, Ramón Alajarín, Juan J. Vaquero, Diego Rodríguez‐Puyol et al.