Evidence map›Paper›PMID 20121050›Full record

ArticleBiochemistry2010

Novel small molecules relieve prothymosin alpha-mediated inhibition of apoptosome formation by blocking its interaction with Apaf-1.

Xin Qi, Lai Wang, Fenghe Du

Open access · greenAbstract read
In one paragraph

Article in Biochemistry, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.

0numbers the graph read from it
0cells of the map it votes in
11citing papers in PubMed
1.2field-weighted citation impact, top 22% of its field
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

11 citing papers in PubMed, 28 citations in OpenAlex.

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4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

3 authors at 2 institutions in 1 country.

Xin QiHoward Hughes Medical Institute and Department of Biochemistry, University of Texas Southwestern Medical Center, Dallas, Texas 75390, USA. xqi@scripps.edu
Lai Wang
Fenghe Du
The University of Texas Southwestern Medical Center · USSouthwestern Medical Center · US

Funding

Structure guided discovery of small molecule antagonists of Smac (DIABLO)/XIPAP01CA095471 · NCI · UT SOUTHWESTERN MEDICAL CENTER · PI MCKNIGHT, STEVEN L · 2002 to 2011
$34.1M
Howard Hughes Medical InstituteNCI NIH HHS P01 CA095471NCI NIH HHS P01 CA95471-01
6 · The paper itself

Abstract

Structurally diverse small molecules, including 5-(2-benzofuryl)-4-phenyl-1,2,4-triazole-3-thiol (BETT), have been identified via high-throughput screening as activators of caspase-3 in HeLa cell extracts. However, little is known about their mechanism of action. In this study, we investigate how BETT regulates prothymosin alpha (ProT), a nuclear protein previously shown to play essential roles in apoptosis. We first showed that Apaf-1 is the direct target protein of BETT. We further demonstrated that BETT relieved ProT-mediated inhibition of apoptosome formation by blocking the interaction between Apaf-1 and ProT. Using two-dimensional (1)H-(15)N heteronuclear single-quantum correlation (HSQC) experiments, we were also able to examine the interaction between Apaf-1 and (15)N-labeled ProT alpha. Furthermore, we were able to reconstitute the entire caspase-3 activation pathway using purified ProT, Apaf-1, procaspase-9, procaspase-3, Hsp70, cytochrome c, PHAPI, CAS, and regulatory compounds to mimic stress-induced apoptosis in vitro. Together, these studies would lead to novel and specific methods for the prevention, diagnosis, and treatment of human cancer.

Indexed as

AnimalsApoptosisApoptosomesApoptotic Protease-Activating Factor 1Caspase 3Caspase InhibitorsCell Line, TumorDrug Delivery SystemsHeLa CellsHumansMitochondriaProtein BindingProtein PrecursorsRecombinant ProteinsSpodopteraThymosin5-(2-benzofuryl)-4-phenyl-1,2,4-triazole-3-thiolAPAF1 protein, humanApoptosomesApoptotic Protease-Activating Factor 1Caspase 3Caspase InhibitorsProtein Precursorsprothymosin alphaRecombinant ProteinsThymosinTriazoles

Identifiers

PMID20121050
PMCPMC2852139
OpenAlexW2036648967

What OpenQuestion holds

Textmetadata
LicenceTDM
Read underepoch 390

Registered trials

None linked

Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.