Evidence map›Paper›PMID 39585895›Full record

ArticleJournal of medicinal chemistry2024

Discovery of ERD-12310A as an Exceptionally Potent and Orally Efficacious PROTAC Degrader of Estrogen Receptor α (ERα).

Rohan Kalyan Rej, Biao Hu, Zhixiang Chen, Ranjan Kumar Acharyya, Dimin Wu, Hoda Metwally, Donna McEachern, Yu Wang, Wei Jiang, Longchuan Bai and 14 more

Abstract read
In one paragraph

Article in Journal of medicinal chemistry, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.

0numbers the graph read from it
0cells of the map it votes in
10citing 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

10 citing papers in PubMed.

  1. Evolving CRBN ligands enhance the drug-like properties of protein degraders.Journal of enzyme inhibition and medicinal chemistry · 2026
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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

24 authors.

Rohan Kalyan RejDepartment of Internal Medicine, Division of Hematology/Oncology, University of Michigan, Ann Arbor 48109, United States.ORCID 0000-0003-0904-9137
Biao HuDepartment of Internal Medicine, Division of Hematology/Oncology, University of Michigan, Ann Arbor 48109, United States.ORCID 0000-0002-4691-6490
Zhixiang ChenDepartment of Internal Medicine, Division of Hematology/Oncology, University of Michigan, Ann Arbor 48109, United States.ORCID 0009-0007-4526-1588
Ranjan Kumar AcharyyaDepartment of Internal Medicine, Division of Hematology/Oncology, University of Michigan, Ann Arbor 48109, United States.ORCID 0000-0002-1562-0216
Dimin WuDepartment of Internal Medicine, Division of Hematology/Oncology, University of Michigan, Ann Arbor 48109, United States.
Hoda MetwallyDepartment of Internal Medicine, Division of Hematology/Oncology, University of Michigan, Ann Arbor 48109, United States.
Donna McEachernDepartment of Internal Medicine, Division of Hematology/Oncology, University of Michigan, Ann Arbor 48109, United States.
Yu WangDepartment of Internal Medicine, Division of Hematology/Oncology, University of Michigan, Ann Arbor 48109, United States.
Wei JiangDepartment of Internal Medicine, Division of Hematology/Oncology, University of Michigan, Ann Arbor 48109, United States.
Longchuan BaiDepartment of Internal Medicine, Division of Hematology/Oncology, University of Michigan, Ann Arbor 48109, United States.
Leticia S NishimuraDepartment of Internal Medicine, Division of Hematology/Oncology, University of Michigan, Ann Arbor 48109, United States.
Christina L GerschDepartment of Internal Medicine, Division of Hematology/Oncology, University of Michigan, Ann Arbor 48109, United States.
Meilin WangDepartment of Pharmaceutical Sciences, College of Pharmacy, University of Michigan, Ann Arbor 48109, United States.
Bo WenDepartment of Pharmaceutical Sciences, College of Pharmacy, University of Michigan, Ann Arbor 48109, United States.
Duxin SunDepartment of Pharmaceutical Sciences, College of Pharmacy, University of Michigan, Ann Arbor 48109, United States.ORCID 0000-0002-6406-2126
Kathryn CarlsonDepartment of Chemistry, University of Illinois, 600 South Mathews Avenue, Urbana 61801, United States.
John A KatzenellenbogenDepartment of Chemistry, University of Illinois, 600 South Mathews Avenue, Urbana 61801, United States.ORCID 0000-0003-0914-0010
Guozhang XuSK Life Science Laboratories, 2500 Renaissance Boulevard, King of Prussia 09406, United States.
Weihong ZhangSK Life Science Laboratories, 2500 Renaissance Boulevard, King of Prussia 09406, United States.
Wenxue WuSK Life Science Laboratories, 2500 Renaissance Boulevard, King of Prussia 09406, United States.ORCID 0000-0002-5979-9350
E Scott PriestleySK Life Science Laboratories, 2500 Renaissance Boulevard, King of Prussia 09406, United States.ORCID 0000-0001-8390-1143
Zhihua SuiSK Life Science Laboratories, 2500 Renaissance Boulevard, King of Prussia 09406, United States.
James M RaeDepartment of Internal Medicine, Division of Hematology/Oncology, University of Michigan, Ann Arbor 48109, United States.
Shaomeng WangDepartment of Internal Medicine, Division of Hematology/Oncology, University of Michigan, Ann Arbor 48109, United States.ORCID 0000-0002-8782-6950

Funding

XenograftP30CA046592 · NCI · UNIVERSITY OF MICHIGAN AT ANN ARBOR · PI THEODORE S LAWRENCE · 1988 to 2026
$178.2M
NCI NIH HHS P30 CA046592
6 · The paper itself

Abstract

Inhibition of estrogen receptor alpha (ERα) signaling is an established therapeutic approach for the treatment of ER-positive (ER+) breast cancers, but new therapeutic strategies are urgently needed to overcome clinical resistance. In the present study, we describe the discovery and extensive evaluation of ERD-12310A as an exceptionally potent and orally efficacious PROTAC degrader of ERα. ERD-12310A achieved a DC

Indexed as

Breast NeoplasmsEstrogen Receptor alphaAdministration, OralAnimalsAntineoplastic AgentsCell ProliferationDrug DiscoveryFemaleHumansMCF-7 CellsMiceMice, NudeRatsRats, Sprague-DawleyStructure-Activity RelationshipXenograft Model Antitumor AssaysAntineoplastic AgentsESR1 protein, humanEstrogen Receptor alpha

Identifiers

PMID39585895
PMCPMC12981312

What OpenQuestion holds

Textmetadata
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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.