Evidence map›Paper›PMID 35792153›Full record

ArticleSteroids2022

Computational approaches to identify a novel binding site of BHPI on estrogen receptor alpha.

Monica L Bean, Reham A Alkohaif, Ahed Anbari, Caela P Fedraw, Vishnu Ghantasala, Florina Gojcaj, Philopateer Hanein, Myles R Harris, Dennis Kim, Destiny L D Proffett and 5 more

Open access · greenAbstract read
In one paragraph

Article in Steroids, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.

0numbers the graph read from it
0cells of the map it votes in
0citing papers in PubMed
–field-weighted citation impact, top 90% 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

0 citing papers in PubMed, 0 citations in OpenAlex.

No citing paper in PubMed yet.

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

15 authors at 2 institutions in 1 country.

Monica L BeanUniversity of Detroit Mercy. 4001 W. McNichols Rd, Detroit, MI 48221, US; Meharry Medical College. 1005 Dr DB Todd Jr Blvd, Nashville, TN 37208, US.
Reham A AlkohaifUniversity of Detroit Mercy. 4001 W. McNichols Rd, Detroit, MI 48221, US.
Ahed AnbariUniversity of Detroit Mercy. 4001 W. McNichols Rd, Detroit, MI 48221, US.
Caela P FedrawUniversity of Detroit Mercy. 4001 W. McNichols Rd, Detroit, MI 48221, US.
Vishnu GhantasalaUniversity of Detroit Mercy. 4001 W. McNichols Rd, Detroit, MI 48221, US.
Florina GojcajUniversity of Detroit Mercy. 4001 W. McNichols Rd, Detroit, MI 48221, US.
Philopateer HaneinUniversity of Detroit Mercy. 4001 W. McNichols Rd, Detroit, MI 48221, US.
Myles R HarrisUniversity of Detroit Mercy. 4001 W. McNichols Rd, Detroit, MI 48221, US.
Dennis KimUniversity of Detroit Mercy. 4001 W. McNichols Rd, Detroit, MI 48221, US.
Destiny L D ProffettUniversity of Detroit Mercy. 4001 W. McNichols Rd, Detroit, MI 48221, US.
Mahdi H HusseiniUniversity of Detroit Mercy. 4001 W. McNichols Rd, Detroit, MI 48221, US.
Elizabeth A JamesUniversity of Detroit Mercy. 4001 W. McNichols Rd, Detroit, MI 48221, US; Xavier University of Louisiana. 1 Drexel Dr, New Orleans, LA 70125, US.
Brendan M O'RourkeUniversity of Detroit Mercy. 4001 W. McNichols Rd, Detroit, MI 48221, US.
Laila H SareiniUniversity of Detroit Mercy. 4001 W. McNichols Rd, Detroit, MI 48221, US.
Mara R LivezeyUniversity of Detroit Mercy. 4001 W. McNichols Rd, Detroit, MI 48221, US. Electronic address: livezemr@udmercy.edu.
University of Detroit Mercy · USMeharry Medical College · US

Funding

Research Enhancement for BUILDing Detroit (ReBUILDetroit)TL4GM118983 · NIGMS · UNIVERSITY OF DETROIT MERCY · PI BRYANT-FRIEDRICH, AMANDA C, SNYDER, KATHERINE E · 2015 to 2023
$17.0M
Research Enhancement for BUILDing Detroit (ReBUILDetroit)UL1GM118982 · NIGMS · UNIVERSITY OF DETROIT MERCY · PI SNYDER, KATHERINE E · 2015 to 2023
$10.8M
Research Enhancement for BUILDing Detroit (ReBUILDetroit)RL5GM118981 · NIGMS · UNIVERSITY OF DETROIT MERCY · PI BRYANT-FRIEDRICH, AMANDA C, SNYDER, KATHERINE E · 2015 to 2023
$4.8M
NIGMS NIH HHS RL5 GM118981NIGMS NIH HHS TL4 GM118983NIGMS NIH HHS UL1 GM118982
6 · The paper itself

Abstract

3,3-bis(4-hydroxyphenyl)-7-methyl-1,3,dihydro-2H-indol-2-one (BHPI) is a biomodulator of Estrogen Receptor alpha (ERα) that targets ERα positive cancer cells by activating the unfolded protein response (UPR). BHPI induces strong and sustained activation of this pathway, eventually resulting in necrotic cell death. While much is known about how BHPI triggers the UPR leading to necrotic cell death, it is not known how BHPI binds to its putative molecular target, ERα. In an effort to identify the binding site of BHPI on ERα, molecular docking studies in AutoDock Vina were utilized. Unexpectedly, BHPI was found to dock more frequently and with significantly better binding affinity to a newly described surface pocket on the ERα ligand-binding domain, compared to the ligand-binding pocket. This work uncovers a novel binding site for small molecules on ERα that is not targeted by classical ligands, such as estrogen and tamoxifen, and may allow for the design of additional anti-cancer drugs that work in distinct ways.

Indexed as

Estrogen Receptor alphaTamoxifenBinding SitesLigandsMolecular Docking SimulationProtein BindingEstrogen Receptor alphaLigandsTamoxifenAnti-cancer drugsEstrogen receptor positive cancerMolecular dockingUnfolded protein response

Identifiers

PMID35792153
PMCPMC11733981
OpenAlexW4283770765

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.