TY  - JOUR
AU  - Mori, Mattia
AU  - Vignaroli, Giulia
AU  - Cau, Ylenia
AU  - Dinić, Jelena
AU  - Hill, Richard
AU  - Rossi, Matteo
AU  - Colecchia, David
AU  - Pešić, Milica
AU  - Link, Wolfgang
AU  - Chiariello, Mario
AU  - Ottmann, Christian
AU  - Botta, Maurizio
PY  - 2014
UR  - https://chemistry-europe.onlinelibrary.wiley.com/doi/full/10.1002/cmdc.201400044
UR  - https://radar.ibiss.bg.ac.rs/123456789/3886
AB  - 14-3-3 is a family of highly conserved adapter proteins that is attracting much interest among medicinal chemists. Small-molecule inhibitors of 14-3-3 protein-protein interactions (PPIs) are in high demand, both as tools to increase our understanding of 14-3-3 actions in human diseases and as leads to develop innovative therapeutic agents. Herein we present the discovery of novel 14-3-3 PPI inhibitors through a multidisciplinary strategy combining molecular modeling, organic synthesis, image-based high-content analysis of reporter cells, and in vitro assays using cancer cells. Notably, the two most active compounds promoted the translocation of c-Abl and FOXO pro-apoptotic factors into the nucleus and sensitized multidrug-resistant cancer cells to apoptotic inducers such as doxorubicin and the pan-Akt inhibitor GSK690693, thus becoming valuable lead candidates for further optimization. Our results emphasize the possible role of 14-3-3 PPI inhibitors in anticancer combination therapies.
PB  - Weinheim : Wiley-VCH
T2  - ChemMedChem
T1  - Discovery of 14‐3‐3 Protein–Protein Interaction Inhibitors that Sensitize Multidrug‐Resistant Cancer Cells to Doxorubicin and the Akt Inhibitor GSK690693
IS  - 5
VL  - 9
DO  - 10.1002/cmdc.201400044
SP  - 973
EP  - 983
ER  - 

@article{
author = "Mori, Mattia and Vignaroli, Giulia and Cau, Ylenia and Dinić, Jelena and Hill, Richard and Rossi, Matteo and Colecchia, David and Pešić, Milica and Link, Wolfgang and Chiariello, Mario and Ottmann, Christian and Botta, Maurizio",
year = "2014",
abstract = "14-3-3 is a family of highly conserved adapter proteins that is attracting much interest among medicinal chemists. Small-molecule inhibitors of 14-3-3 protein-protein interactions (PPIs) are in high demand, both as tools to increase our understanding of 14-3-3 actions in human diseases and as leads to develop innovative therapeutic agents. Herein we present the discovery of novel 14-3-3 PPI inhibitors through a multidisciplinary strategy combining molecular modeling, organic synthesis, image-based high-content analysis of reporter cells, and in vitro assays using cancer cells. Notably, the two most active compounds promoted the translocation of c-Abl and FOXO pro-apoptotic factors into the nucleus and sensitized multidrug-resistant cancer cells to apoptotic inducers such as doxorubicin and the pan-Akt inhibitor GSK690693, thus becoming valuable lead candidates for further optimization. Our results emphasize the possible role of 14-3-3 PPI inhibitors in anticancer combination therapies.",
publisher = "Weinheim : Wiley-VCH",
journal = "ChemMedChem",
title = "Discovery of 14‐3‐3 Protein–Protein Interaction Inhibitors that Sensitize Multidrug‐Resistant Cancer Cells to Doxorubicin and the Akt Inhibitor GSK690693",
number = "5",
volume = "9",
doi = "10.1002/cmdc.201400044",
pages = "973-983"
}

Mori, M., Vignaroli, G., Cau, Y., Dinić, J., Hill, R., Rossi, M., Colecchia, D., Pešić, M., Link, W., Chiariello, M., Ottmann, C.,& Botta, M.. (2014). Discovery of 14‐3‐3 Protein–Protein Interaction Inhibitors that Sensitize Multidrug‐Resistant Cancer Cells to Doxorubicin and the Akt Inhibitor GSK690693. in ChemMedChem
Weinheim : Wiley-VCH., 9(5), 973-983.
https://doi.org/10.1002/cmdc.201400044

Mori M, Vignaroli G, Cau Y, Dinić J, Hill R, Rossi M, Colecchia D, Pešić M, Link W, Chiariello M, Ottmann C, Botta M. Discovery of 14‐3‐3 Protein–Protein Interaction Inhibitors that Sensitize Multidrug‐Resistant Cancer Cells to Doxorubicin and the Akt Inhibitor GSK690693. in ChemMedChem. 2014;9(5):973-983.
doi:10.1002/cmdc.201400044 .

Mori, Mattia, Vignaroli, Giulia, Cau, Ylenia, Dinić, Jelena, Hill, Richard, Rossi, Matteo, Colecchia, David, Pešić, Milica, Link, Wolfgang, Chiariello, Mario, Ottmann, Christian, Botta, Maurizio, "Discovery of 14‐3‐3 Protein–Protein Interaction Inhibitors that Sensitize Multidrug‐Resistant Cancer Cells to Doxorubicin and the Akt Inhibitor GSK690693" in ChemMedChem, 9, no. 5 (2014):973-983,
https://doi.org/10.1002/cmdc.201400044 . .

TY  - JOUR
AU  - Mori, Mattia
AU  - Vignaroli, Giulia
AU  - Cau, Ylenia
AU  - Dinić, Jelena
AU  - Hill, Richard
AU  - Rossi, Matteo
AU  - Colecchia, David
AU  - Pešić, Milica
AU  - Link, Wolfgang
AU  - Chiariello, Mario
AU  - Ottmann, Christian
AU  - Botta, Maurizio
PY  - 2014
UR  - https://radar.ibiss.bg.ac.rs/handle/123456789/2215
AB  - 14-3-3 is a family of highly conserved adapter proteins that is
   attracting much interest among medicinal chemists. Small-molecule
   inhibitors of 14-3-3 protein-protein interactions (PPIs) are in high
   demand, both as tools to increase our understanding of 14-3-3 actions in
   human diseases and as leads to develop innovative therapeutic agents.
   Herein we present the discovery of novel 14-3-3 PPI inhibitors through a
   multidisciplinary strategy combining molecular modeling, organic
   synthesis, image-based high-content analysis of reporter cells, and in
   vitro assays using cancer cells. Notably, the two most active compounds
   promoted the translocation of c-Abl and FOXO pro-apoptotic factors into
   the nucleus and sensitized multidrug-resistant cancer cells to apoptotic
   inducers such as doxorubicin and the pan-Akt inhibitor GSK690693, thus
   becoming valuable lead candidates for further optimization. Our results
   emphasize the possible role of 14-3-3 PPI inhibitors in anticancer
   combination therapies.
T2  - Chemmedchem
T1  - Discovery of 14-3-3 Protein- Protein Interaction Inhibitors that
 Sensitize Multidrug- Resistant Cancer Cells to Doxorubicin and the Akt
 Inhibitor GSK690693
IS  - 5, SI
VL  - 9
DO  - 10.1002/cmdc.201400044
SP  - 973
EP  - 983
ER  - 

@article{
author = "Mori, Mattia and Vignaroli, Giulia and Cau, Ylenia and Dinić, Jelena and Hill, Richard and Rossi, Matteo and Colecchia, David and Pešić, Milica and Link, Wolfgang and Chiariello, Mario and Ottmann, Christian and Botta, Maurizio",
year = "2014",
abstract = "14-3-3 is a family of highly conserved adapter proteins that is
   attracting much interest among medicinal chemists. Small-molecule
   inhibitors of 14-3-3 protein-protein interactions (PPIs) are in high
   demand, both as tools to increase our understanding of 14-3-3 actions in
   human diseases and as leads to develop innovative therapeutic agents.
   Herein we present the discovery of novel 14-3-3 PPI inhibitors through a
   multidisciplinary strategy combining molecular modeling, organic
   synthesis, image-based high-content analysis of reporter cells, and in
   vitro assays using cancer cells. Notably, the two most active compounds
   promoted the translocation of c-Abl and FOXO pro-apoptotic factors into
   the nucleus and sensitized multidrug-resistant cancer cells to apoptotic
   inducers such as doxorubicin and the pan-Akt inhibitor GSK690693, thus
   becoming valuable lead candidates for further optimization. Our results
   emphasize the possible role of 14-3-3 PPI inhibitors in anticancer
   combination therapies.",
journal = "Chemmedchem",
title = "Discovery of 14-3-3 Protein- Protein Interaction Inhibitors that
 Sensitize Multidrug- Resistant Cancer Cells to Doxorubicin and the Akt
 Inhibitor GSK690693",
number = "5, SI",
volume = "9",
doi = "10.1002/cmdc.201400044",
pages = "973-983"
}

Mori, M., Vignaroli, G., Cau, Y., Dinić, J., Hill, R., Rossi, M., Colecchia, D., Pešić, M., Link, W., Chiariello, M., Ottmann, C.,& Botta, M.. (2014). Discovery of 14-3-3 Protein- Protein Interaction Inhibitors that
 Sensitize Multidrug- Resistant Cancer Cells to Doxorubicin and the Akt
 Inhibitor GSK690693. in Chemmedchem, 9(5, SI), 973-983.
https://doi.org/10.1002/cmdc.201400044

Mori M, Vignaroli G, Cau Y, Dinić J, Hill R, Rossi M, Colecchia D, Pešić M, Link W, Chiariello M, Ottmann C, Botta M. Discovery of 14-3-3 Protein- Protein Interaction Inhibitors that
 Sensitize Multidrug- Resistant Cancer Cells to Doxorubicin and the Akt
 Inhibitor GSK690693. in Chemmedchem. 2014;9(5, SI):973-983.
doi:10.1002/cmdc.201400044 .

Mori, Mattia, Vignaroli, Giulia, Cau, Ylenia, Dinić, Jelena, Hill, Richard, Rossi, Matteo, Colecchia, David, Pešić, Milica, Link, Wolfgang, Chiariello, Mario, Ottmann, Christian, Botta, Maurizio, "Discovery of 14-3-3 Protein- Protein Interaction Inhibitors that
 Sensitize Multidrug- Resistant Cancer Cells to Doxorubicin and the Akt
 Inhibitor GSK690693" in Chemmedchem, 9, no. 5, SI (2014):973-983,
https://doi.org/10.1002/cmdc.201400044 . .