inhibitor

[Dr ehab]

# SP600125, an anthrapyrazolone inhibitor of Jun N-terminal kinase.
Proc Natl Acad Sci U S A Nov 21, 2001
... is a reversible ATP-competitive inhibitor with >20-fold
selectivity vs. a range of kinases and enzymes tested. In cells,
SP600125 dose ... . Our study supports targeting JNK as an important
strategy in inflammatory disease, apoptotic cell death, and cancer.

# Endonuclease G is an apoptotic DNase when released from
mitochondria.
Nature Jul 13, 2001
... (DFF, a caspase-activated deoxyribonuclease (CAD) and its
inhibitor (ICAD)), is capable of inducing DNA fragmentation and ...
specifically activated by apoptotic stimuli and is able to induce
nucleosomal fragmentation of DNA in fibroblast cells from
embryonic ...

# A caspase-activated DNase that degrades DNA during apoptosis, and
its inhibitor ICAD.
Nature Jan 15, 1998
... -activated deoxyribonuclease (CAD) and its inhibitor (ICAD) have
now been identified in the cytoplasmic fraction of mouse lymphoma
cells. CAD is a ... CAD to inhibit its DNase activity; caspases
activated by apoptotic stimuli then cleave ICAD, allowing CAD to ...

# Mediation of poly(ADP-ribose) polymerase-1-dependent cell death by
apoptosis-inducing fact
Science Jul 12, 2002
... DNA damage surveillance network. PARP-1 is also a mediator of cell
death after ischemia-reperfusion injury, glutamate excitotoxicity, ...
d-aspartate induce AIF translocation and cell death, which is
prevented by PARP inhibitors or genetic knockout of PARP-1, ...

# X-linked IAP is a direct inhibitor of cell-death proteases.
Nature Aug 07, 1997
The inhibitor-of-apoptosis (IAP) family of genes has an evolutionarily
conserved role in regulating programmed cell death ... principal
effectors of apoptosis, our findings suggest how IAPs might inhibit
cell death, providing evidence for a mechanism of action ...

# Caspase-independent cell death?
Oncogene Apr 12, 2004
... a lysosomal system. Prior to total collapse and necrosis, cells
that are in trouble can activate numerous physiological pathways ...
manipulation, inhibitor, or the biology of the cell, other routes may
be followed, leading to variant forms of cell death that ...

# IAP proteins: blocking the road to death's door.
Nat Rev Mol Cell Biol Jun 03, 2002
... inhibitor of apoptosis' (IAP) gene family, which was discovered
less than a decade ago, encodes a group of structurally ... proteins
that, in addition to their ability to suppress apoptotic cell death,
are involved in an increasing number of seemingly unrelated ...

# Coupling endoplasmic reticulum stress to the cell death program. An
Apaf-1-independent int
J Biol Chem Jun 10, 2002
... apoptotic insults that induce the intrinsic apoptotic pathway.
While these cells were resistant to cell death initiated by
proapoptotic stimuli ... caspase-8 inhibitors. Cleavage of caspases
and poly(ADP-ribose) polymerase was observed in cell-free extracts ...

# PI3K targeting by the beta-GBP cytokine negates akt gene expression
and leads aggressive breast cancer cells to apoptotic death.
Breast Cancer Res Jan 09, 2009
... the betaGBP cytokine and loss of akt mRNA results in apoptotic
death. We also report a functional correlation between ERK and ...
discovered physiological inhibitor of PI3K, is a selective and potent
inducer of apoptosis in aggressive breast cancer cells. Due ...

# A selective inhibitor of eIF2alpha dephosphorylation protects cells
from ER stress.
Science Feb 11, 2005
... protect cells from endoplasmic reticulum (ER) stress, we
identified salubrinal, a selective inhibitor of cellular ...
infection. More broadly, salubrinal demonstrates the feasibility of
selective pharmacological targeting of cellular dephosphorylation
events ...

# HtrA2 promotes cell death through its serine protease activity and
its ability to antagoni
J Biol Chem Jan 04, 2002
Inhibitor of apoptosis (IAP) proteins inhibit caspases, a function
counteracted by IAP antagonists, insect Grim, HID, ... catalytic
serine residue reduces the ability of HtrA2 to promote cell death,
whereas a complete loss in proapoptotic activity is observed ...

# The E3 Ubiquitin Ligase Itch Couples JNK Activation to TNFalpha-
induced Cell Death by Indu
Cell Feb 10, 2006
... tumor necrosis factor (TNF) alpha signals both cell survival and
death. The biological outcome of TNFalpha treatment is determined ...
degradation. JNK1 or Itch deficiency or treatment with a JNK inhibitor
renders mice resistant in three distinct models of ...

# Lipopolysaccharides-activated human astroglioma cells induce
apoptotic death of T-lymphocy
Neurosci Res Mar 13, 2006
... ) and consequently abrogated in the presence of the specific JNK
inhibitor SP600125. The up-regulation of TRAIL expression was well co-
related with AP- ... . Activated human astroglioma cells markedly
induced the apoptotic death of T-lymphocytes. Pre-treatment ...

# The c-IAP-1 and c-IAP-2 proteins are direct inhibitors of specific
caspases.
EMBO J Jan 29, 1998
... inhibitor of apoptosis (IAP) family of proteins are highly
conserved through evolution. However, the mechanisms by which these
proteins interfere ... XIAP, can bind to and potently inhibit specific
cell death proteases (caspases) that function in the distal ...

# Glycogen synthase kinase-3 inhibitors augment TRAIL-induced
apoptotic death in human hepatoma cells.
Biochem Pharmacol Oct 21, 2008
... downstream recruitment of the mitochondrial machinery. GSK-3
inhibitors also stabilized p53 and the down-regulation of p53 by RNA
interference ... TRAIL apoptotic signaling in hepatoma cells, which
can be greatly alleviated by GSK-3 inhibitors. Therefore, GSK- ...

# Allosteric Akt (PKB) inhibitors: discovery and SAR of isozyme
selective inhibitors.
Bioorg Med Chem Lett Jan 24, 2005
... describes the development of two series of potent and selective
allosteric Akt kinase inhibitors that display an unprecedented level
of ... approach quickly provided a highly selective Akt1/Akt2
inhibitor that induces apoptosis in tumor cells and inhibits Akt ...

# HIV type 1-infected dendritic cells induce apoptotic death in
infected and uninfected prim
AIDS Res Hum Retroviruses Mar 15, 2004
... + T cell lines. This apoptosis was inhibited by a mixture of FasL,
TRAIL, TNF-alpha, and TWEAK inhibitors. Indeed, ... early stages of
infection. It may also contribute to elimination of infected cells in
vivo, thereby enhancing cross-presentation of HIV by ...

# Identification of Omi/HtrA2 as a mitochondrial apoptotic serine
protease that disrupts inh
J Biol Chem Jan 04, 2002
... the Smac and caspase-9 binding pocket on the baculoviral inhibitor
of apoptosis protein (IAP) repeat 3 (BIR3) domain ... involvement of a
mitochondrial serine protease in the apoptotic pathway, emphasizing
the critical role of the mitochondria in cell death.

# FOWLPOX VIRUS ENCODES A BCL-2 HOMOLOGUE THAT PROTECTS CELLS FROM
APOPTOTIC DEATH THROUGH I
J Virol Aug 09, 2007
... a recombinant vaccinia virus lacking F1L, the endogenous apoptotic
inhibitor in vaccinia virus, and expressing FPV039. In ... , FPV039
prevented the activation of Bak and protected infected cells from
apoptosis induced by staurosporine and virus infection. ...

# In vivo antitumor activity of NVP-AEW541-A novel, potent, and
selective inhibitor of the I
Cancer Cell Mar 30, 2004
... related InsR (IC50 = 2.3 microM) in cells. As expected for a
specific IGF-IR kinase inhibitor, NVP-AEW541 abrogates IGF-I-mediated
survival ... -AEW541 represents a class of selective, small molecule
IGF-IR kinase inhibitors with proven in vivo antitumor ...

[Dr ehab]

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