QD-FRET-based biosensing of small molecule analytes using transcription factor-DNA binding

2019 ◽  
Author(s):  
Thuy Nguyen ◽  
Margaret Chern ◽  
R C. Baer ◽  
Andy Fan ◽  
Chloe Grazon ◽  
...  
Keyword(s):  
Transcription Factor ◽  
Dna Binding ◽  
Small Molecule

Abstract 3088: Transcription factor as target: Novel small molecule inhibits FOXM1 DNA binding and oncogenic gene products

2016 ◽  
Author(s):  
Michael Gormally ◽  
Giovanni Marsico ◽  
Ganesha Rai ◽  
Christopher Lowe ◽  
Craig Thomas ◽  
...  
Keyword(s):  
Transcription Factor ◽  
Dna Binding ◽  
Small Molecule ◽  
Gene Products ◽  
Oncogenic Gene

Integrated discovery of FOXO1–DNA stabilizers from marine natural products to restore chemosensitivity to anti-EGFR-based therapy for metastatic lung cancer

2017 ◽  
Vol 13 (2) ◽  
pp. 330-337 ◽  
Author(s):  
Yingjia Sun ◽  
Xinghao Ai ◽  
Jingwen Hou ◽  
Xiangyun Ye ◽  
Ruijun Liu ◽  
...  
Keyword(s):  
Lung Cancer ◽  
Transcription Factor ◽  
Natural Products ◽  
Dna Binding ◽  
Small Molecule ◽  
Marine Natural Products ◽  
Metastatic Lung Cancer ◽  
Binding Conformation ◽  
Metastatic Lung ◽  
Oncogenic Transcription Factor

Small-molecule marine natural products are identified to selectively recognize and stabilize the DNA-binding conformation of FOXO1, an oncogenic transcription factor.

Inhibition of NGLY1 inactivates the transcription factor Nrf1 and potentiates proteasome inhibitor cytotoxicity

2017 ◽  
Author(s):  
Carolyn Bertozzi ◽  
Fred Tomlin ◽  
Ulla Gerling-Driessen ◽  
Yi-Chang Liu ◽  
Ryan Flynn ◽  
...  
Keyword(s):  
Transcription Factor ◽  
Small Molecule ◽  
Proteasome Inhibitor ◽  
Activation Mechanism ◽  
Cancer Drugs ◽  
Small Molecule Library ◽  
Library Screen ◽  
In Cells

We discovered that the proteostasis modulating transcription factor Nrf1 requires cytosolic de-N-glycosylation by the N-glycanase NGly1 as part of its activation mechanism. Through a covalent small molecule library screen, we discovered an inhibitor of NGly1 that blocks Nrf1 activation in cells and potentiates the activity of proteasome inhibitor cancer drugs. The requirement of NGly1 for Nrf1 activity likely underlies several pathologies associated with a rare hereditary deficiency in NGly1.

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