ArticleEuropean journal of medicinal chemistry2026
Developing orally active estrogen receptor degraders by conjugation of boronic tamoxifen and cereblon ligands.
Article in European journal of medicinal chemistry, 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
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.
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.
Who cites it
0 citing papers in PubMed.
No citing paper in PubMed yet.
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
9 authors.
Funding
Abstract
Degradation of estrogen receptor has been clinically proven effective in treating ER+ breast cancer. Proteolysis-Targeting Chimeras (PROTACs) can degrade a target protein by engaging both the target protein and the E3 ligase, bringing them into close physical proximity to effect ubiquitination and proteasomal degradation. We report the design and construction of ER PROTACs that link tamoxifen derivatives to a CRBN E3 ligand to achieve ER protein degradation. The ER degrading efficacy of the synthesized PROTACs was found to depend on the ER binding affinity, the linker structure, and the E3 ligand. Tamoxifen-4-boronic acid conjugated to lenalidomide through a rigid piperidine-methylene-piperazine linker was found to yield degraders that show nanomolar antiestrogenic potency and excellent oral bioavailability. The most active ER degrader with good pharmacokinetic profile, 4r, showed remarkable in vivo efficacy in blocking ER+ (both non-mutant and Y537S mutant) breast tumor growth as a monotherapy or in combination with CDK4/6 inhibitors.
Indexed as
Identifiers
What OpenQuestion holds
Registered trials
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.