scholarly journals Structure-Based Design, Synthesis, Evaluation, and Crystallographic Studies of Conformationally Constrained Smac Mimetics as Inhibitors of the X-linked Inhibitor of Apoptosis Protein (XIAP)†

2008 ◽  
Vol 51 (22) ◽  
pp. 7169-7180 ◽  
Author(s):  
Haiying Sun ◽  
Jeanne A. Stuckey ◽  
Zaneta Nikolovska-Coleska ◽  
Dongguang Qin ◽  
Jennifer L. Meagher ◽  
...  
Keyword(s):  
Inhibitor Of Apoptosis ◽  
Design Synthesis ◽  
Conformationally Constrained ◽  
Inhibitor Of Apoptosis Protein ◽  
Apoptosis Protein ◽  
Smac Mimetics

scholarly journals Design, synthesis and evaluation of inhibitor of apoptosis protein (IAP) antagonists that are highly selective for the BIR2 domain of XIAP

2013 ◽  
Vol 23 (14) ◽  
pp. 4253-4257 ◽  
Author(s):  
Robert J. Ardecky ◽  
Kate Welsh ◽  
Darren Finlay ◽  
Pooi San Lee ◽  
Marcos González-López ◽  
...  
Keyword(s):  
Inhibitor Of Apoptosis ◽  
Design Synthesis ◽  
Inhibitor Of Apoptosis Protein ◽  
Apoptosis Protein

scholarly journals Structure-based design, synthesis, and evaluation of the biological activity of novel phosphoroorganic small molecule IAP antagonists

2020 ◽  
Vol 38 (5) ◽  
pp. 1350-1364 ◽  
Author(s):  
Agnieszka Łupicka-Słowik ◽  
Mateusz Psurski ◽  
Renata Grzywa ◽  
Monika Cuprych ◽  
Jarosław Ciekot ◽  
...  
Keyword(s):  
Cancer Cell Line ◽  
Biochemical Properties ◽  
Inhibitor Of Apoptosis ◽  
Binding Motif ◽  
Inhibitory Influence ◽  
Design Synthesis ◽  
Inhibitor Of Apoptosis Protein ◽  
Design And Synthesis ◽  
Apoptosis Protein ◽  
Fluorescence Polarization Assay

Summary One of the strategies employed by novel anticancer therapies is to put the process of apoptosis back on track by blocking the interaction between inhibitor of apoptosis proteins (IAPs) and caspases. The activity of caspases is modulated by the caspases themselves in a caspase/procaspase proteolytic cascade and by their interaction with IAPs. Caspases can be released from the inhibitory influence of IAPs by proapoptotic proteins such as secondary mitochondrial activator of caspases (Smac) that share an IAP binding motif (IBM). The main purpose of the present study was the design and synthesis of phosphorus-based peptidyl antagonists of IAPs that mimic the endogenous Smac protein, which blocks the interaction between IAPs and caspases. Based on the structure of the IAP antagonist and recently reported thiadiazole derivatives, we designed and evaluated the biochemical properties of a series of phosphonic peptides bearing the N-Me-Ala-Val/Chg-Pro-OH motif (Chg: cyclohexylglycine). The ability of the obtained compounds to interact with the binding groove of the X-linked inhibitor of apoptosis protein baculovirus inhibitor of apoptosis protein repeat (XIAP BIR3) domain was examined by a fluorescence polarization assay, while their potential to induce autoubiquitination followed by proteasomal degradation of cellular IAP1 was examined using the MDA-MB-231 breast cancer cell line. The highest potency against BIR3 was observed among peptides containing C-terminal phosphonic phenylalanine analogs, which displayed nanomolar Ki values. Their antiproliferative potential as well as their proapoptotic action, manifested by an increase in caspase-3 activity, was examined using various cell lines.

Design, Synthesis and Characterization of New Embelin Derivatives as Potent Inhibitors of X-Linked Inhibitor of Apoptosis Protein.

ChemInform ◽  
2007 ◽  
Vol 38 (13) ◽  
Author(s):  
Jianyong Chen ◽  
Zaneta Nikolovska-Coleska ◽  
Guoping Wang ◽  
Su Qiu ◽  
Shaomeng Wang
Keyword(s):  
Synthesis And Characterization ◽  
Inhibitor Of Apoptosis ◽  
Design Synthesis ◽  
Inhibitor Of Apoptosis Protein ◽  
Apoptosis Protein

163 POSTER Characterization of novel Smac mimetics as highly potent and effective antagonists of X-linked inhibitor of apoptosis protein

2006 ◽  
Vol 4 (12) ◽  
pp. 52
Author(s):  
Z. Nikolovska-Coleska ◽  
H. Sun ◽  
J. Lu ◽  
S. Qiu ◽  
J. Meagher ◽  
...  
Keyword(s):  
Inhibitor Of Apoptosis ◽  
Inhibitor Of Apoptosis Protein ◽  
Apoptosis Protein ◽  
Smac Mimetics

Targeting the X-Linked Inhibitor of Apoptosis Protein through 4-Substituted Azabicyclo[5.3.0]alkane Smac Mimetics. Structure, Activity, and Recognition Principles

2008 ◽  
Vol 384 (3) ◽  
pp. 673-689 ◽  
Author(s):  
Eloise Mastrangelo ◽  
Federica Cossu ◽  
Mario Milani ◽  
Graziella Sorrentino ◽  
Daniele Lecis ◽  
...  
Keyword(s):  
Inhibitor Of Apoptosis ◽  
Inhibitor Of Apoptosis Protein ◽  
Structure Activity ◽  
Apoptosis Protein ◽  
Smac Mimetics

Design, synthesis, and characterization of new embelin derivatives as potent inhibitors of X-linked inhibitor of apoptosis protein

2006 ◽  
Vol 16 (22) ◽  
pp. 5805-5808 ◽  
Author(s):  
Jianyong Chen ◽  
Zaneta Nikolovska-Coleska ◽  
Guoping Wang ◽  
Su Qiu ◽  
Shaomeng Wang
Keyword(s):  
Synthesis And Characterization ◽  
Inhibitor Of Apoptosis ◽  
Design Synthesis ◽  
Inhibitor Of Apoptosis Protein ◽  
Apoptosis Protein

Prognostic significance of X‐linked inhibitor of apoptosis protein in solid tumors: A systematic review and meta‐analysis

2019 ◽  
Vol 234 (10) ◽  
pp. 18111-18122 ◽  
Author(s):  
Shimeng Li ◽  
Baoxiang Pan ◽  
Lihong Li ◽  
Bo Shi ◽  
Feng Xie ◽  
...  
Keyword(s):  
Systematic Review ◽  
Solid Tumors ◽  
Meta Analysis ◽  
Prognostic Significance ◽  
Inhibitor Of Apoptosis ◽  
Inhibitor Of Apoptosis Protein ◽  
Apoptosis Protein

scholarly journals Targeting X-Linked Inhibitor of Apoptosis Protein to Increase the Efficacy of Endoplasmic Reticulum Stress-Induced Apoptosis for Melanoma Therapy

2010 ◽  
Vol 130 (9) ◽  
pp. 2250-2258 ◽  
Author(s):  
Emma L. Hiscutt ◽  
David S. Hill ◽  
Shaun Martin ◽  
Ryan Kerr ◽  
Andrew Harbottle ◽  
...  
Keyword(s):  
Endoplasmic Reticulum ◽  
Endoplasmic Reticulum Stress ◽  
Inhibitor Of Apoptosis ◽  
Inhibitor Of Apoptosis Protein ◽  
Apoptosis Protein ◽  
Induced Apoptosis ◽  
Melanoma Therapy

scholarly journals X-Linked Inhibitor of Apoptosis Protein Expression and the Regulation of Apoptosis During Human Placental Development1

2001 ◽  
Vol 64 (4) ◽  
pp. 1264-1272 ◽  
Author(s):  
Andrée Gruslin ◽  
Qing Qiu ◽  
Benjamin K. Tsang
Keyword(s):  
Protein Expression ◽  
Inhibitor Of Apoptosis ◽  
Inhibitor Of Apoptosis Protein ◽  
Apoptosis Protein
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