Inhibition of Growth Factor Signaling by Small-Molecule Inhibitors of ErbB, Raf, and MEK

2006 ◽  
pp. 83-132
Author(s):  
Eli M. Wallace ◽  
Tammie C. Yeh ◽  
Ellen R. Laird ◽  
James F. Blake ◽  
Joseph Lyssikatos
Keyword(s):  
Growth Factor ◽  
Small Molecule ◽  
Small Molecule Inhibitors ◽  
Growth Factor Signaling ◽  
Inhibition Of Growth

The exosomal compartment protects epidermal growth factor receptor from small molecule inhibitors

2019 ◽  
Vol 510 (1) ◽  
pp. 42-47
Author(s):  
Yu Hung ◽  
Yuan-Liang Wang ◽  
You-Zhe Lin ◽  
Shu-Fen Chiang ◽  
Wan-Rong Wu ◽  
...  
Keyword(s):  
Epidermal Growth Factor Receptor ◽  
Growth Factor ◽  
Epidermal Growth Factor ◽  
Small Molecule ◽  
Small Molecule Inhibitors ◽  
Growth Factor Receptor ◽  
Epidermal Growth

scholarly journals The same site on the integrase-binding domain of lens epithelium–derived growth factor is a therapeutic target for MLL leukemia and HIV

Blood ◽  
2014 ◽  
Vol 124 (25) ◽  
pp. 3730-3737 ◽  
Author(s):  
Marcelo J. Murai ◽  
Jonathan Pollock ◽  
Shihan He ◽  
Hongzhi Miao ◽  
Trupta Purohit ◽  
...  
Keyword(s):  
Growth Factor ◽  
Small Molecule ◽  
Therapeutic Target ◽  
Small Molecule Inhibitors ◽  
Binding Domain ◽  
Lens Epithelium ◽  
New Drugs ◽  
Structural Studies ◽  
Key Points

Key Points Inhibiting LEDGF interaction with a novel fragment of MLL represents an attractive approach to develop new drugs for MLL leukemias. Structural studies reveal a new pocket on the LEDGF IBD suitable for targeting by small-molecule inhibitors.

Structure-based discovery of novel small molecule inhibitors of platelet-derived growth factor-B

2020 ◽  
Vol 94 ◽  
pp. 103374 ◽  
Author(s):  
Omid Zarei ◽  
Niki Sarri ◽  
Siavoush Dastmalchi ◽  
Fateme Zokai ◽  
Natalia Papadopoulos ◽  
...  
Keyword(s):  
Growth Factor ◽  
Small Molecule ◽  
Small Molecule Inhibitors ◽  
Platelet Derived Growth Factor ◽  
Factor B

scholarly journals Small Molecule Inhibitors of the Neuropilin-1 Vascular Endothelial Growth Factor A (VEGF-A) Interaction

2010 ◽  
Vol 53 (5) ◽  
pp. 2215-2226 ◽  
Author(s):  
Ashley Jarvis ◽  
Charles K. Allerston ◽  
Haiyan Jia ◽  
Birger Herzog ◽  
Acely Garza-Garcia ◽  
...  
Keyword(s):  
Vascular Endothelial Growth Factor ◽  
Growth Factor ◽  
Small Molecule ◽  
Small Molecule Inhibitors ◽  
Vascular Endothelial ◽  
Neuropilin 1 ◽  
Endothelial Growth Factor

scholarly journals The mTOR-Regulated Phosphoproteome Reveals a Mechanism of mTORC1-Mediated Inhibition of Growth Factor Signaling

Science ◽  
2011 ◽  
Vol 332 (6035) ◽  
pp. 1317-1322 ◽  
Author(s):  
P. P. Hsu ◽  
S. A. Kang ◽  
J. Rameseder ◽  
Y. Zhang ◽  
K. A. Ottina ◽  
...  
Keyword(s):  
Growth Factor ◽  
Growth Factor Signaling ◽  
Inhibition Of Growth

scholarly journals A Surface Plasmon Resonance Spectroscopy Method for Characterizing Small-Molecule Binding to Nerve Growth Factor

2015 ◽  
Vol 21 (1) ◽  
pp. 96-100 ◽  
Author(s):  
Allison E. Kennedy ◽  
Kristen S. Sheffield ◽  
Joseph K. Eibl ◽  
Michael B. Murphy ◽  
Rahul Vohra ◽  
...  
Keyword(s):  
Surface Plasmon Resonance ◽  
Nerve Growth Factor ◽  
Growth Factor ◽  
Surface Plasmon ◽  
Small Molecule ◽  
Plasmon Resonance ◽  
Small Molecule Inhibitors ◽  
Resonance Spectroscopy ◽  
Nerve Growth ◽  
Binding Event

Small-molecule inhibitors have been previously investigated to identify possible therapeutics for the treatment of chronic pain. In the present study, known nerve growth factor (NGF) inhibitors identified by 125I-NGF binding were characterized using affinity and binding evaluations by surface plasmon resonance (SPR) spectroscopy. A novel strategy for characterizing NGF inhibitors was used to determine the binding affinity (KD) and saturation ability of each compound with immobilized NGF. Seventy-four percent of compounds screened demonstrated a positive binding event to NGF. A KD less than 10 μM and a percent saturation greater than 50% were used as thresholds to identify inhibitors that would warrant further investigation. This study details for the first time a methodology that can be used to directly characterize the binding event between small-molecule inhibitors and NGF.

Sign in / Sign up

Export Citation Format

Share Document