IAP-targeted therapies for cancer

EC LaCasse, DJ Mahoney, HH Cheung, S Plenchette… - Oncogene, 2008 - nature.com
DNA damage, chromosomal abnormalities, oncogene activation, viral infection, substrate
detachment and hypoxia can all trigger apoptosis in normal cells. However, cancer cells …

Design of small-molecule peptidic and nonpeptidic Smac mimetics

H Sun, Z Nikolovska-Coleska, CY Yang… - Accounts of chemical …, 2008 - ACS Publications
Smac/DIABLO is a protein released from mitochondria into the cytosol in response to
apoptotic stimuli. Smac promotes apoptosis at least in part through antagonizing inhibitor of …

Drug-like inhibitors of protein-protein interactions: a structural examination of effective protein mimicry

DC Fry - Current Protein and Peptide Science, 2008 - ingentaconnect.com
Protein-protein interactions represent targets for drug discovery that are highly relevant in a
biological sense, but have proven difficult in a practical sense. Nevertheless, there have …

[HTML][HTML] The mechanism of peptide-binding specificity of IAP BIR domains

BP Eckelman, M Drag, SJ Snipas… - Cell Death & …, 2008 - nature.com
We describe the peptide-binding specificity of the baculoviral IAP repeat (BIR) domains of
the human inhibitor of apoptosis (IAP) proteins, X-linked IAP, cellular IAP1 and neuronal …

Interaction of a cyclic, bivalent Smac mimetic with the X-linked inhibitor of apoptosis protein

Z Nikolovska-Coleska, JL Meagher, S Jiang… - Biochemistry, 2008 - ACS Publications
We have designed and synthesized a cyclic, bivalent Smac mimetic (compound 3) and
characterized its interaction with the X-linked inhibitor of apoptosis protein (XIAP) …

Design and characterization of bivalent Smac-based peptides as antagonists of XIAP and development and validation of a fluorescence polarization assay for XIAP …

Z Nikolovska-Coleska, JL Meagher, S Jiang… - Analytical …, 2008 - Elsevier
XIAP (X-chromosome-linked inhibitor of apoptosis protein) is an inhibitor of apoptosis by
binding to and inhibition of caspase-3 and caspase-7 through its BIR2 domain and caspase …

Targeting the X-linked inhibitor of apoptosis protein through 4-substituted azabicyclo [5.3. 0] alkane smac mimetics. Structure, activity, and recognition principles

E Mastrangelo, F Cossu, M Milani, G Sorrentino… - Journal of molecular …, 2008 - Elsevier
The X-linked inhibitor of apoptosis protein (XIAP) is overexpressed in several malignant
cells where it prevents apoptosis by binding to, and blocking, the activation of caspase-3,-7 …

Protein–protein recognition as a first step towards the inhibition of XIAP and Survivin anti‐apoptotic proteins

C Obiol‐Pardo, JM Granadino‐Roldán… - Journal of Molecular …, 2008 - Wiley Online Library
Apoptosis, also called programmed cell death, is a conserved mechanism inherent to all
cells that sentences them to death when they receive the appropriate external stimuli …

[图书][B] Disrupting the protein-protein recognition in cancer pathways by molecular modeling.

C Obiol Pardo - 2008 - diposit.ub.edu
[eng] Cancer is the second disease leading cause of death in industrialized countries.
Although early detection and more efficient drugs are responsible of the reduction of …

Structural studies of proteins in apoptosis and lipid signaling

MD Herman Moreno - 2008 - diva-portal.org
Signaling pathways control the fate of the cell. For example, they promote cell survival or
commit the cell to death (apoptosis) in response to cell injury or developmental stimuli …