Evidence map›Paper›PMID 39022350›Full record

ArticleACS pharmacology & translational science2024

Structure-Activity Relationship Study of Tris-Benzamides as Estrogen Receptor Coregulator Binding Modulators.

Tae-Kyung Lee, Kara Kassees, Chia-Yuan Chen, Suryavathi Viswanadhapalli, Karla Parra, Ratna K Vadlamudi, Jung-Mo Ahn

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in ACS pharmacology & translational science, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 1 paper.

0numbers the graph read from it
0cells of the map it votes in
1citing papers in PubMed
–field-weighted citation impact
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

1 citing paper in PubMed.

  1. Article
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

7 authors.

Tae-Kyung LeeDepartment of Chemistry and Biochemistry, University of Texas at Dallas, Richardson, Texas 75080, United States.
Kara KasseesDepartment of Chemistry and Biochemistry, University of Texas at Dallas, Richardson, Texas 75080, United States.
Chia-Yuan ChenDepartment of Chemistry and Biochemistry, University of Texas at Dallas, Richardson, Texas 75080, United States.
Suryavathi ViswanadhapalliDepartment of Obstetrics and Gynecology, University of Texas Health, San Antonio, Texas 78229, United States.
Karla ParraDepartments of Urology and Pharmacology, University of Texas Southwestern Medical Center, Dallas, Texas 75390, United States.
Ratna K VadlamudiDepartment of Obstetrics and Gynecology, University of Texas Health, San Antonio, Texas 78229, United States.
Jung-Mo AhnDepartment of Chemistry and Biochemistry, University of Texas at Dallas, Richardson, Texas 75080, United States.ORCID https://orcid.org/0000-0002-9104-525X

Funding

Therapeutic agents targeting nuclear receptor signaling in distinct molecular subtypes of breast cancerR01CA223828 · NCI · UNIVERSITY OF TEXAS HLTH SCIENCE CENTER · PI RAJ, GANESH V, VADLAMUDI, RATNA K · 2018 to 2022
$3.0M
Enhancing endoplasmic reticulum stress in ovarian cancerR01CA262757 · NCI · UNIVERSITY OF TEXAS HLTH SCIENCE CENTER · PI JUNG-MO AHN, Ratna K Vadlamudi · 2022 to 2026
$2.6M
NCI NIH HHS R01 CA223828NCI NIH HHS R01 CA262757
6 · The paper itself

Abstract

Estrogen receptor coregulator binding modulators (ERXs) are a novel class of molecules targeting the interaction between estrogen receptor α (ERα) and its coregulator proteins, which has proven to be an attractive strategy for overcoming endocrine resistance in breast cancer. We previously reported ERX-11, an orally bioavailable tris-benzamide, that demonstrated promising antitumor activity against ERα-positive breast cancer cells. To comprehend the significance of the substituents in ERX-11, we carried out structure-activity relationship studies. In addition, we introduced additional alkyl substituents at either the N- or C-terminus to improve binding affinity and biological activity. Further optimization guided by conformational restriction led to the identification of a

Identifiers

PMID39022350
PMCPMC11249634

What OpenQuestion holds

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Registered trials

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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.