scholarly journals Structure–activity relationships of a small-molecule inhibitor of the PDZ domain of PICK1

2010 ◽  
Vol 8 (19) ◽  
pp. 4281 ◽  
Author(s):  
Anders Bach ◽  
Nicolai Stuhr-Hansen ◽  
Thor S. Thorsen ◽  
Nicolai Bork ◽  
Irina S. Moreira ◽  
...  
Keyword(s):  
Small Molecule ◽  
Pdz Domain ◽  
Small Molecule Inhibitor ◽  
Structure Activity Relationships ◽  
Structure Activity ◽  
Molecule Inhibitor

scholarly journals Identification of a small-molecule inhibitor of the PICK1 PDZ domain that inhibits hippocampal LTP and LTD

2009 ◽  
Vol 107 (1) ◽  
pp. 413-418 ◽  
Author(s):  
T. S. Thorsen ◽  
K. L. Madsen ◽  
N. Rebola ◽  
M. Rathje ◽  
V. Anggono ◽  
...  
Keyword(s):  
Small Molecule ◽  
Pdz Domain ◽  
Small Molecule Inhibitor ◽  
Molecule Inhibitor

Necrosulfonamide inhibits necroptosis by selectively targeting the mixed lineage kinase domain-like protein

MedChemComm ◽  
2014 ◽  
Vol 5 (3) ◽  
pp. 333-337 ◽  
Author(s):  
Daohong Liao ◽  
Liming Sun ◽  
Weilong Liu ◽  
Sudan He ◽  
Xiaodong Wang ◽  
...  
Keyword(s):  
Small Molecule ◽  
High Throughput ◽  
High Throughput Screening ◽  
Kinase Domain ◽  
Small Molecule Inhibitor ◽  
Mixed Lineage Kinase ◽  
Sar Studies ◽  
Structure Activity ◽  
Molecule Inhibitor ◽  
Smac Mimetic

Through high-throughput screening of 200 000 compounds and subsequent structure–activity relationship (SAR) studies we identified necrosulfonamide (NSA) as a potent small molecule inhibitor for necroptosis, induced by a combination of TNF-a, Smac mimetic, and z-VAD-fmk (T/S/Z).

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