Abstract 3491: Enhancing nab-paclitaxel antitumor activity through addition of BMS-754807, a small-molecule inhibitor of IGF-1R/IR, in experimental pancreatic cancer

2015 ◽  
Author(s):  
Niranjan Awasthi ◽  
Margaret A. Schwarz ◽  
Roderich E. Schwarz
Keyword(s):  
Pancreatic Cancer ◽  
Antitumor Activity ◽  
Small Molecule ◽  
Small Molecule Inhibitor ◽  
Molecule Inhibitor ◽  
Experimental Pancreatic Cancer

scholarly journals A Novel Small-Molecule Inhibitor of Protein Kinase D Blocks Pancreatic Cancer Growth In vitro and In vivo

2010 ◽  
Vol 9 (5) ◽  
pp. 1136-1146 ◽  
Author(s):  
Kuzhuvelil B. Harikumar ◽  
Ajaikumar B. Kunnumakkara ◽  
Nobuo Ochi ◽  
Zhimin Tong ◽  
Amit Deorukhkar ◽  
...  
Keyword(s):  
Pancreatic Cancer ◽  
Protein Kinase ◽  
Small Molecule ◽  
Small Molecule Inhibitor ◽  
Cancer Growth ◽  
Protein Kinase D ◽  
Molecule Inhibitor

scholarly journals A Novel Chemical Attack on Notch-mediated transcription by targeting the NACK ATPase

2021 ◽  
Author(s):  
G. Diluvio ◽  
T. T. Kelley ◽  
M. Lahiry ◽  
A. Alvarez Trotta ◽  
E. M. Kolb ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Mouse Models ◽  
Small Molecule ◽  
Ternary Complex ◽  
Small Molecule Inhibitor ◽  
Chemical Attack ◽  
Dependent Function ◽  
Molecule Inhibitor ◽  
Efficacious Treatment ◽  
Notch Activation

Abstract Notch Activation Complex Kinase, NACK, is a component of the Notch transcriptional machinery critical to Notch-mediated tumorigenesis. However, the mechanism by which NACK regulates the Notch-mediated transcription is not well understood. Here we demonstrate that NACK binds and hydrolyses ATP and that only ATP-bound NACK is able to bind to the Notch Ternary Complex (NTC). Considering this we sought to identify inhibitors of this ATP-Dependent function and, using computational pipelines, discovered the first small molecule inhibitor of NACK, Z271-0326, that directly blocks the activity of Notch-mediated transcription and shows potent antitumor activity in PDX mouse models. In conclusion, we have discovered the first inhibitor that holds promise for efficacious treatment of Notch-driven cancers by blocking the Notch downstream NTC activity.

scholarly journals A covalent small molecule inhibitor of glutamate-oxaloacetate transaminase 1 impairs pancreatic cancer growth

2020 ◽  
Vol 522 (3) ◽  
pp. 633-638 ◽  
Author(s):  
Tomohiro Yoshida ◽  
Shingo Yamasaki ◽  
Osamu Kaneko ◽  
Naofumi Taoka ◽  
Yusuke Tomimoto ◽  
...  
Keyword(s):  
Pancreatic Cancer ◽  
Small Molecule ◽  
Small Molecule Inhibitor ◽  
Cancer Growth ◽  
Glutamate Oxaloacetate Transaminase ◽  
Molecule Inhibitor

TW-37, A NONPEPTIDIC SMALL-MOLECULE INHIBITOR OF BCL-2, INHIBITS INVASION AND ANGIOGENESIS IN PANCREATIC CANCER

Pancreas ◽  
2007 ◽  
Vol 35 (4) ◽  
pp. 434-435
Author(s):  
Z. Wang ◽  
W. Song ◽  
A. Aboukameel ◽  
G. Wang ◽  
S. Wang ◽  
...  
Keyword(s):  
Pancreatic Cancer ◽  
Small Molecule ◽  
Small Molecule Inhibitor ◽  
Molecule Inhibitor
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