Direct and selective small-molecule activation of proapoptotic BAX (Q36741892)

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:22634637%20AND%20SRC:MED&resulttype=core&format=json

2 February 2020

title

Direct and selective small-molecule activation of proapoptotic BAX (English)

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2 February 2020

author

Evripidis Gavathiotis

1

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2 February 2020

5

Loren D Walensky

1 reference

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2 February 2020

author name string

Denis E Reyna

2

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2 February 2020

Joseph A Bellairs

3

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2 February 2020

Elizaveta S Leshchiner

4

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2 February 2020

publication date

27 May 2012

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2 February 2020

published in

Nature Chemical Biology

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2 February 2020

volume

8

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2 February 2020

issue

7

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2 February 2020

page(s)

639-645

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Substantial susceptibility of chronic lymphocytic leukemia to BCL2 inhibition: results of a phase I study of navitoclax in patients with relapsed or refractory disease

2 February 2020

cites work

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BAX unleashed: the biochemical transformation of an inactive cytosolic monomer into a toxic mitochondrial pore

29 September 2017

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Phase I study of Navitoclax (ABT-263), a novel Bcl-2 family inhibitor, in patients with small-cell lung cancer and other solid tumors

29 September 2017

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BID, BIM, and PUMA are essential for activation of the BAX- and BAK-dependent cell death program

29 September 2017

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Navitoclax, a targeted high-affinity inhibitor of BCL-2, in lymphoid malignancies: a phase 1 dose-escalation study of safety, pharmacokinetics, pharmacodynamics, and antitumour activity

29 September 2017

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29 September 2017

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The MCL-1 BH3 helix is an exclusive MCL-1 inhibitor and apoptosis sensitizer

29 September 2017

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Stepwise activation of BAX and BAK by tBID, BIM, and PUMA initiates mitochondrial apoptosis.

29 September 2017

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Membrane binding by tBid initiates an ordered series of events culminating in membrane permeabilization by Bax

29 September 2017

1 reference

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BAX activation is initiated at a novel interaction site

29 September 2017

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Phase I study of obatoclax mesylate (GX15-070), a small molecule pan-Bcl-2 family antagonist, in patients with advanced chronic lymphocytic leukemia

29 September 2017

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ABT-263: a potent and orally bioavailable Bcl-2 family inhibitor

29 September 2017

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The BCL-2 protein family: opposing activities that mediate cell death

29 September 2017

1 reference

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Small molecule obatoclax (GX15-070) antagonizes MCL-1 and overcomes MCL-1-mediated resistance to apoptosis

29 September 2017

1 reference

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A stapled BID BH3 helix directly binds and activates BAX

29 September 2017

1 reference

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Extra precision glide: docking and scoring incorporating a model of hydrophobic enclosure for protein-ligand complexes

29 September 2017

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Structure-based design of potent small-molecule inhibitors of anti-apoptotic Bcl-2 proteins

29 September 2017

1 reference

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Mitochondria primed by death signals determine cellular addiction to antiapoptotic BCL-2 family members

29 September 2017

1 reference

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Essential role of BAX,BAK in B cell homeostasis and prevention of autoimmune disease

29 September 2017

1 reference

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An inhibitor of Bcl-2 family proteins induces regression of solid tumours

29 September 2017

1 reference

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BH3 domains of BH3-only proteins differentially regulate Bax-mediated mitochondrial membrane permeabilization both directly and indirectly

29 September 2017

1 reference

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29 September 2017

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The first alpha helix of Bax plays a necessary role in its ligand-induced activation by the BH3-only proteins Bid and PUMA.

29 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3617124

Activation of apoptosis in vivo by a hydrocarbon-stapled BH3 helix

29 September 2017

1 reference

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Glide: a new approach for rapid, accurate docking and scoring. 1. Method and assessment of docking accuracy

29 September 2017

1 reference

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Cell death: critical control points

29 September 2017

1 reference

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Interaction with a membrane surface triggers a reversible conformational change in Bax normally associated with induction of apoptosis

29 September 2017

1 reference

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Bid, Bax, and lipids cooperate to form supramolecular openings in the outer mitochondrial membrane

29 September 2017

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Distinct BH3 domains either sensitize or activate mitochondrial apoptosis, serving as prototype cancer therapeutics

29 September 2017

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Proapoptotic BAX and BAK: a requisite gateway to mitochondrial dysfunction and death

29 September 2017

1 reference

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Structure of Bax: coregulation of dimer formation and intracellular localization

29 September 2017

1 reference

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tBID, a membrane-targeted death ligand, oligomerizes BAK to release cytochrome c

29 September 2017

1 reference

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29 September 2017

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Cytochrome c and dATP-dependent formation of Apaf-1/caspase-9 complex initiates an apoptotic protease cascade

29 September 2017

1 reference

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Structure of Bcl-xL-Bak peptide complex: recognition between regulators of apoptosis

29 September 2017

1 reference

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BID: a novel BH3 domain-only death agonist

29 September 2017

1 reference

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X-ray and NMR structure of human Bcl-xL, an inhibitor of programmed cell death

29 September 2017

1 reference

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Induction of apoptotic program in cell-free extracts: requirement for dATP and cytochrome c

29 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3617124

From mitochondrial biology to magic bullet: navitoclax disarms BCL-2 in chronic lymphocytic leukemia

29 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3617124

BH3-triggered structural reorganization drives the activation of proapoptotic BAX.

28 June 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3617124

Dissection of the BCL-2 family signaling network with stabilized alpha-helices of BCL-2 domains

5 September 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3617124

Nonionic detergents induce dimerization among members of the Bcl-2 family

5 September 2018

1 reference

PubMed

https://pubmed.ncbi.nlm.nih.gov/22634637

inferred from PubMed ID database lookup

12 December 2020

based on heuristic

Hierarchical regulation of mitochondrion-dependent apoptosis by BCL-2 subfamilies

1 reference

PubMed

https://pubmed.ncbi.nlm.nih.gov/22634637

inferred from PubMed ID database lookup

12 December 2020

based on heuristic

Membrane-insertion fragments of Bcl-xL, Bax, and Bid

1 reference

PubMed

https://pubmed.ncbi.nlm.nih.gov/22634637

inferred from PubMed ID database lookup

12 December 2020

based on heuristic

Identifiers

DOI

10.1038/NCHEMBIO.995

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:22634637%20AND%20SRC:MED&resulttype=core&format=json

2 February 2020

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:22634637%20AND%20SRC:MED&resulttype=core&format=json

2 February 2020

PubMed publication ID

22634637

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:22634637%20AND%20SRC:MED&resulttype=core&format=json