Abstract 2976: Confirmation of in-cell target engagement using the proteolysis targeting chimeras (PROTACs) against pirin

2018 ◽  
Author(s):  
Swee Y. Sharp ◽  
Nicola E. Chessum ◽  
John J. Caldwell ◽  
Marissa V. Powers ◽  
A Elisa Pasqua ◽  
...  
Keyword(s):  
Target Engagement ◽  
Cell Target

scholarly journals Structure-Guided Design and In-Cell Target Profiling of a Cell-Active Target Engagement Probe for PARP Inhibitors

2020 ◽  
Vol 15 (2) ◽  
pp. 325-333 ◽  
Author(s):  
Ryan T. Howard ◽  
Paul Hemsley ◽  
Philip Petteruti ◽  
Charlie N. Saunders ◽  
Javier A. Molina Bermejo ◽  
...  
Keyword(s):  
Parp Inhibitors ◽  
Target Engagement ◽  
Active Target ◽  
Cell Target ◽  
A Cell

scholarly journals Design of a GAK/EGFR inhibitor set to interrogate the relationship of EGFR and GAK in chordoma

2018 ◽  
Author(s):  
Christopher R. M. Asquith ◽  
Kaleb M. Naegeli ◽  
Michael P. East ◽  
Tuomo Laitinen ◽  
Tammy M. Havener ◽  
...  
Keyword(s):  
Epidermal Growth Factor Receptor ◽  
Growth Factor Receptor ◽  
Egfr Inhibitor ◽  
Target Engagement ◽  
Cell Target ◽  
Epidermal Growth ◽  
Cyclin G ◽  
Relationship Of ◽  
The Relationship

ABSTRACTWe describe the design of a set of inhibitors to investigate the relationship between cyclin G associated kinase (GAK) and epidermal growth factor receptor (EGFR) in chordoma bone cancers. These compounds were characterized both in vitro and using in cell target engagement assays. The most potent chordoma inhibitors were further characterized in a kinome-wide screen demonstrating narrow spectrum profiles.

Whole Cell Target Engagement Identifies Novel Inhibitors ofMycobacterium tuberculosisDecaprenylphosphoryl-β-d-ribose Oxidase

2015 ◽  
Vol 1 (12) ◽  
pp. 615-626 ◽  
Author(s):  
Sarah M. Batt ◽  
Monica Cacho Izquierdo ◽  
Julia Castro Pichel ◽  
Christopher J. Stubbs ◽  
Laura Vela-Glez Del Peral ◽  
...  
Keyword(s):  
Target Engagement ◽  
Whole Cell ◽  
Cell Target

scholarly journals Demonstrating In-Cell Target Engagement Using a Pirin Protein Degradation Probe (CCT367766)

2018 ◽  
Vol 61 (3) ◽  
pp. 918-933 ◽  
Author(s):  
Nicola E. A. Chessum ◽  
Swee Y. Sharp ◽  
John J. Caldwell ◽  
A. Elisa Pasqua ◽  
Birgit Wilding ◽  
...  
Keyword(s):  
Protein Degradation ◽  
Target Engagement ◽  
Cell Target

P2-027: TARGET ENGAGEMENT IN A PHASE II CLINICAL TRIAL OF AAV2-NGF GENE THERAPY FOR ALZHEIMER'S DISEASE

2006 ◽  
Vol 14 (7S_Part_12) ◽  
pp. P677-P677
Author(s):  
Michael J. Castle ◽  
Fernando Calvo Baltanas ◽  
Imre Kovacs ◽  
Alan H. Nagahara ◽  
Krystof S. Bankiewicz ◽  
...  
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Clinical Trial ◽  
Gene Therapy ◽  
Phase Ii ◽  
Phase Ii Clinical Trial ◽  
Target Engagement ◽  
Ngf Gene
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