Small-molecule pan-IAP antagonists: a patent review (Q37680967)

21 August 2017

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title

Small-molecule pan-IAP antagonists: a patent review (English)

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21 August 2017

John A Flygare

1

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21 August 2017

Wayne J Fairbrother

series ordinal

2

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21 August 2017

language of work or name

English

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publication date

1 February 2010

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Expert Opinion on Therapeutic Patents

21 August 2017

published in

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21 August 2017

volume

20

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21 August 2017

issue

2

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21 August 2017

page(s)

251-267

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Apoptosis control by death and decoy receptors

21 August 2017

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21 January 2018

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21 January 2018

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21 January 2018

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21 January 2018

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21 January 2018

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Inhibitor of apoptosis proteins: translating basic knowledge into clinical practice

21 January 2018

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Reawakening the cellular death program in neoplasia through the therapeutic blockade of IAP function

21 January 2018

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The inhibitor of apoptosis proteins as therapeutic targets in cancer

21 January 2018

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Livin, a novel inhibitor of apoptosis protein family member

21 January 2018

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Inhibitor of apoptosis protein-1 promotes tumor cell survival in mesothelioma

21 January 2018

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Role of XIAP in the malignant phenotype of transitional cell cancer (TCC) and therapeutic activity of XIAP antisense oligonucleotides against multidrug-resistant TCC in vitro.

21 January 2018

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Induction of apoptosis in tumor cells by siRNA-mediated silencing of the livin/ML-IAP/KIAP gene

21 January 2018

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X-linked inhibitor of apoptosis protein (XIAP) is a nonredundant modulator of tumor necrosis factor-related apoptosis-inducing ligand (TRAIL)-mediated apoptosis in human cancer cells

21 January 2018

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An antisense oligonucleotide to cIAP-1 sensitizes prostate cancer cells to fas and TNFalpha mediated apoptosis

21 January 2018

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Loss of XIAP protein expression by RNAi and antisense approaches sensitizes cancer cells to functionally diverse chemotherapeutics

21 January 2018

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Isoform-specific silencing of the Livin gene by RNA interference defines Livin beta as key mediator of apoptosis inhibition in HeLa cells

21 January 2018

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Targeted inhibition of Livin resensitizes renal cancer cells towards apoptosis

21 January 2018

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Suppression of tumor necrosis factor-induced cell death by inhibitor of apoptosis c-IAP2 is under NF-kappaB control

21 January 2018

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X-linked inhibitor of apoptosis protein functions as a cofactor in transforming growth factor-beta signaling

21 January 2018

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IAP suppression of apoptosis involves distinct mechanisms: the TAK1/JNK1 signaling cascade and caspase inhibition

21 January 2018

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Tumor necrosis factor receptor 2 signaling induces selective c-IAP1-dependent ASK1 ubiquitination and terminates mitogen-activated protein kinase signaling

21 January 2018

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c-IAP1 cooperates with Myc by acting as a ubiquitin ligase for Mad1.

21 January 2018

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IAP antagonists induce autoubiquitination of c-IAPs, NF-kappaB activation, and TNFalpha-dependent apoptosis

21 January 2018

1 reference

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X-linked and cellular IAPs modulate the stability of C-RAF kinase and cell motility

21 January 2018

1 reference

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cIAP1 and cIAP2 facilitate cancer cell survival by functioning as E3 ligases that promote RIP1 ubiquitination

21 January 2018

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https://api.crossref.org/works/10.1517%2F13543770903567077

Both cIAP1 and cIAP2 regulate TNFalpha-mediated NF-kappaB activation

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543770903567077

c-IAP1 and c-IAP2 are critical mediators of tumor necrosis factor alpha (TNFalpha)-induced NF-kappaB activation

21 January 2018

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https://api.crossref.org/works/10.1517%2F13543770903567077

(Un)expected roles of c-IAPs in apoptotic and NFkappaB signaling pathways

21 January 2018

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IAPs, RINGs and ubiquitylation

21 January 2018

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IAPs contain an evolutionarily conserved ubiquitin-binding domain that regulates NF-kappaB as well as cell survival and oncogenesis

21 January 2018

1 reference

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Ubiquitin binding modulates IAP antagonist-stimulated proteasomal degradation of c-IAP1 and c-IAP2(1)

21 January 2018

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A single BIR domain of XIAP sufficient for inhibiting caspases

21 January 2018

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NMR structure and mutagenesis of the inhibitor-of-apoptosis protein XIAP

21 January 2018

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Structural basis of caspase-7 inhibition by XIAP

21 January 2018

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Structural basis for the inhibition of caspase-3 by XIAP

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543770903567077

Cleavage of human inhibitor of apoptosis protein XIAP results in fragments with distinct specificities for caspases

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543770903567077

NMR structure and mutagenesis of the third Bir domain of the inhibitor of apoptosis protein XIAP

21 January 2018

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https://api.crossref.org/works/10.1517%2F13543770903567077

A conserved XIAP-interaction motif in caspase-9 and Smac/DIABLO regulates caspase activity and apoptosis

21 January 2018

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https://api.crossref.org/works/10.1517%2F13543770903567077

Mechanism of XIAP-mediated inhibition of caspase-9

21 January 2018

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https://api.crossref.org/works/10.1517%2F13543770903567077

The anti-apoptotic activity of XIAP is retained upon mutation of both the caspase 3- and caspase 9-interacting sites

21 January 2018

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Smac, a mitochondrial protein that promotes cytochrome c-dependent caspase activation by eliminating IAP inhibition

21 January 2018

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Identification of DIABLO, a mammalian protein that promotes apoptosis by binding to and antagonizing IAP proteins

21 January 2018

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Structural and biochemical basis of apoptotic activation by Smac/DIABLO

21 January 2018

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https://api.crossref.org/works/10.1517%2F13543770903567077

Structural basis for binding of Smac/DIABLO to the XIAP BIR3 domain

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543770903567077

Structural basis of IAP recognition by Smac/DIABLO

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543770903567077

sickle, a novel Drosophila death gene in the reaper/hid/grim region, encodes an IAP-inhibitory protein

21 January 2018

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Structure and function analysis of peptide antagonists of melanoma inhibitor of apoptosis (ML-IAP)

21 January 2018

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Structural analysis of a functional DIAP1 fragment bound to grim and hid peptides

21 January 2018

1 reference

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XIAP inhibits caspase-3 and -7 using two binding sites: evolutionarily conserved mechanism of IAPs.

21 January 2018

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Engineering ML-IAP to produce an extraordinarily potent caspase 9 inhibitor: implications for Smac-dependent anti-apoptotic activity of ML-IAP.

21 January 2018

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https://api.crossref.org/works/10.1517%2F13543770903567077

The human anti-apoptotic proteins cIAP1 and cIAP2 bind but do not inhibit caspases

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543770903567077

Human inhibitor of apoptosis proteins: why XIAP is the black sheep of the family

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543770903567077

The BIR domain of IAP-like protein 2 is conformationally unstable: implications for caspase inhibition

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543770903567077

IAP proteins: sticking it to Smac

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543770903567077

SMAC negatively regulates the anti-apoptotic activity of melanoma inhibitor of apoptosis (ML-IAP)

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543770903567077

Ectopic overexpression of second mitochondria-derived activator of caspases (Smac/DIABLO) or cotreatment with N-terminus of Smac/DIABLO peptide potentiates epothilone B derivative-(BMS 247550) and Apo-2L/TRAIL-induced apoptosis

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543770903567077

Synthetic Smac/DIABLO peptides enhance the effects of chemotherapeutic agents by binding XIAP and cIAP1 in situ

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543770903567077

IAP antagonists target cIAP1 to induce TNFalpha-dependent apoptosis

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543770903567077

Autocrine TNFalpha signaling renders human cancer cells susceptible to Smac-mimetic-induced apoptosis

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543770903567077

TNF-alpha induces two distinct caspase-8 activation pathways

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543770903567077

Antagonism of c-IAP and XIAP proteins is required for efficient induction of cell death by small-molecule IAP antagonists

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543770903567077

Molecular targeting of inhibitor of apoptosis proteins based on small molecule mimics of natural binding partners

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543770903567077

Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancer

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543770903567077

Targeting mitochondrial factor Smac/DIABLO as therapy for multiple myeloma (MM)

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543770903567077

Design, synthesis, and biological activity of a potent Smac mimetic that sensitizes cancer cells to apoptosis by antagonizing IAPs

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543770903567077

Orally bioavailable antagonists of inhibitor of apoptosis proteins based on an azabicyclooctane scaffold

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543770903567077

A small molecule Smac mimic potentiates TRAIL- and TNFalpha-mediated cell death

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543770903567077

Structural basis for bivalent Smac-mimetics recognition in the IAP protein family

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543770903567077

Design, synthesis, and characterization of a potent, nonpeptide, cell-permeable, bivalent Smac mimetic that concurrently targets both the BIR2 and BIR3 domains in XIAP

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543770903567077

10.1517/13543770903567077

21 January 2018

Identifiers

DOI

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21 August 2017

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