Evidence map›Paper›PMID 37808197›Full record

ReviewFrontiers in pharmacology2023

Optimization of small molecule degraders and antagonists for targeting estrogen receptor based on breast cancer: current status and future.

Jiaqi Yao, Yiran Tao, Zelin Hu, Junjie Li, Ziyi Xue, Ya Zhang, Yi Lei

Open access · goldAbstract readReview
In one paragraph

Review in Frontiers in pharmacology, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 5 papers.

0numbers the graph read from it
0cells of the map it votes in
5citing papers in PubMed
2.8field-weighted citation impact, top 9% 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

5 citing papers in PubMed, 9 citations in OpenAlex.

  1. Review
  2. Article
  3. Article
  4. Article
  5. Review
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 at 3 institutions in 2 countries.

Jiaqi Yao *General Practice Ward/International Medical Center, General Practice Medical Center, West China Hospital, Sichuan University, Chengdu, Sichuan, China.
Yiran Tao *West China-California Research Center for Predictive Intervention Medicine, West China Hospital, Sichuan University, Chengdu, Sichuan, China.
Zelin Hu *General Practice Ward/International Medical Center, General Practice Medical Center, West China Hospital, Sichuan University, Chengdu, Sichuan, China.
Junjie LiPrecision Medicine Key Laboratory of Sichuan Province and Precision Medicine Research Center, West China Hospital, Sichuan University, Chengdu, Sichuan, China.
Ziyi XueDepartment of Statistics, College of Liberal Arts and Sciences, University of Illinois Urbana-Champaign, Champaign, IL, United States.
Ya ZhangWest China-California Research Center for Predictive Intervention Medicine, West China Hospital, Sichuan University, Chengdu, Sichuan, China.
Yi LeiGeneral Practice Ward/International Medical Center, General Practice Medical Center, West China Hospital, Sichuan University, Chengdu, Sichuan, China.
Sichuan University · CNUniversity of Illinois Urbana-Champaign · USWest China Medical Center of Sichuan University · CN

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

The estrogen receptor (ER) is a classical receptor protein that plays a crucial role in mediating multiple signaling pathways in various target organs. It has been shown that ER-targeting therapies inhibit breast cancer cell proliferation, enhance neuronal protection, and promote osteoclast formation. Several drugs have been designed to specifically target ER in ER-positive (ER+) breast cancer, including selective estrogen receptor modulators (SERM) such as Tamoxifen. However, the emergence of drug resistance in ER+ breast cancer and the potential side effects on the endometrium which has high ER expression has posed significant challenges in clinical practice. Recently, novel ER-targeted drugs, namely, selective estrogen receptor degrader (SERD) and selective estrogen receptor covalent antagonist (SERCA) have shown promise in addressing these concerns. This paper provides a comprehensive review of the structural functions of ER and highlights recent advancements in SERD and SERCA-related small molecule drugs, especially focusing on their structural optimization strategies and future optimization directions. Additionally, the therapeutic potential and challenges of novel SERDs and SERCAs in breast cancer and other ER-related diseases have been discussed.

Indexed as

estrogen receptorselective estrogen receptor covalent antagonistselective estrogen receptor degradersmall molecule drugsstructural optimization

Identifiers

PMID37808197
PMCPMC10551544
OpenAlexW4386964049

What OpenQuestion holds

Textmetadata
LicenceCC BY
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.