Small-molecule pan-IAP antagonists: a patent review
JA Flygare, WJ Fairbrother - Expert opinion on therapeutic patents, 2010 - Taylor & Francis
Importance of the field: The inhibitor of apoptosis (IAP) proteins are critical regulators of
cancer cell survival that have become important targets for therapeutic intervention in human …
cancer cell survival that have become important targets for therapeutic intervention in human …
Design of small-molecule Smac mimetics as IAP antagonists
S Wang - Small-Molecule Inhibitors of Protein-Protein …, 2010 - Springer
Smac/DIABLO, discovered in 2000 as a protein released from mitochondria into the cytosol
in response to apoptotic stimuli, functions as an endogenous antagonist of X-linked inhibitor …
in response to apoptotic stimuli, functions as an endogenous antagonist of X-linked inhibitor …
Antagonists of inhibitor of apoptosis proteins based on thiazole amide isosteres
F Cohen, MFT Koehler, P Bergeron, LO Elliott… - Bioorganic & medicinal …, 2010 - Elsevier
A series of IAP antagonists based on thiazole or benzothiazole amide isosteres was
designed and synthesized. These compounds were tested for binding to the XIAP-BIR3 and …
designed and synthesized. These compounds were tested for binding to the XIAP-BIR3 and …
Tumor suppressor XIAP‐Associated factor 1 (XAF1) cooperates with tumor necrosis factor‐related apoptosis‐inducing ligand to suppress colon cancer growth and …
SP Tu, YW Sun, JT Cui, B Zou, MCM Lin… - … Journal of the …, 2010 - Wiley Online Library
Abstract BACKGROUND: XIAP‐associated factor 1 (XAF1) antagonizes the anticaspase
activity of XIAP (X‐linked inhibitor of apoptosis) and functions as a tumor suppressor in colon …
activity of XIAP (X‐linked inhibitor of apoptosis) and functions as a tumor suppressor in colon …
BIR domain binding compounds
S Jarvis, A Boudreault, P Bureau, J Jaquith… - US Patent …, 2010 - Google Patents
The present invention is directed towards an isomer, an enan tiomer, a diastereoisomer, or a
tautomer of a pyrrolidine com pound represented by Formula I: in which the substituents R' …
tautomer of a pyrrolidine com pound represented by Formula I: in which the substituents R' …
IAP BIR domain binding compounds
A Boudreault, JB Jaquith, P Bureau, JW Gillard… - US Patent …, 2010 - Google Patents
3.5 A1 S. or a salt thereof, in which R', R, R, R, R, R, A, A, JP 4208.299 7, 1992 BG, Q and
Q'are substituents described herein. Also dis WO WOO2, 30959 4/2002 closed is the use of …
Q'are substituents described herein. Also dis WO WOO2, 30959 4/2002 closed is the use of …
Study on the interactions of SMAC mimetics with XIAP-BIR3 domain by docking and molecular dynamics simulations
Upon receiving an apoptotic stimulus, the mature mitochondrial protein second mitochondria-
derived activator of caspases (Smac)/direct IAP-binding protein with low PI (DIABLO), which …
derived activator of caspases (Smac)/direct IAP-binding protein with low PI (DIABLO), which …
Theoretical studies on the interactions of XIAP-BIR3 domain with bicyclic and tricyclic core monovalent Smac mimetics
B Ling, L Dong, R Zhang, Z Wang, Y Liu… - Journal of Molecular …, 2010 - Elsevier
X-linked IAP can bind caspase-9 and inhibit its activity. Mitochondrial protein Smac/DIABLO
can also interact with XIAP and relieve the inhibition on caspase-9 to induce apoptosis. A …
can also interact with XIAP and relieve the inhibition on caspase-9 to induce apoptosis. A …