Abstract B242: Antitumor activity of SEL120: An orally available small-molecule inhibitor of Haspin kinase for standalone and combination therapy with AuroraB inhibitors in colorectal cancer.

2011 ◽  
Author(s):  
Tomasz Rzymski ◽  
Adrian Zarebski ◽  
Renata Windak ◽  
Zaneta Sibinska ◽  
Karolina Krawczynska ◽  
...  
Keyword(s):  
Colorectal Cancer ◽  
Antitumor Activity ◽  
Combination Therapy ◽  
Small Molecule ◽  
Small Molecule Inhibitor ◽  
Molecule Inhibitor

Small-molecule inhibitor PD-1/PD-L1 interaction for colorectal cancer treatment

2021 ◽  
Vol 10 (6) ◽  
pp. 245-250
Author(s):  
Maricruz Anaya-Ruiz ◽  
Martin Perez-Santos
Keyword(s):  
Colorectal Cancer ◽  
Clinical Trials ◽  
Antitumor Activity ◽  
Cancer Treatment ◽  
Small Molecule ◽  
Small Molecule Inhibitor ◽  
Biological Assays ◽  
New Therapies ◽  
Molecule Inhibitor ◽  
Colorectal Cancer Treatment

Inhibition of the PD-1/PD-L1 pathway is a target for the development of new therapies. US10710986 patent describes a small molecule that targets PDL-1/PD-1 interactions and triggers antitumor activity against colorectal cancer. However, it does not describe biological assays that allow us to suppose that this small molecule may be active in other types of cancer. So far, there are no reports of clinical trials to evaluate the safety, toxicity and efficacy, but it will be of great interest to analyze in the future if this compound surpasses the action of therapy in cancer.

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 Small Molecule Inhibitor of the β-Catenin-TCF4 Interaction Suppresses Colorectal Cancer Growth In Vitro and In Vivo

EBioMedicine ◽  
2017 ◽  
Vol 25 ◽  
pp. 22-31 ◽  
Author(s):  
Seung Ho Shin ◽  
Do Young Lim ◽  
Kanamata Reddy ◽  
Margarita Malakhova ◽  
Fangfang Liu ◽  
...  
Keyword(s):  
Colorectal Cancer ◽  
Small Molecule ◽  
Small Molecule Inhibitor ◽  
Cancer Growth ◽  
Molecule Inhibitor
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