ArticleJournal of medicinal chemistry2026
Utilizing the HiBiT System to Identify CARM1 Degraders for Targeted Cancer Therapy.
Article in 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
15 authors.
Funding
Abstract
Preclinical studies validated coactivator-associated arginine methyltransferase 1 (CARM1) as a targetable therapeutic vulnerability, leading to the development of Proteolysis-Targeting Chimeras that specifically degrade CARM1. These compounds face significant translational challenges, including poor oral bioavailability and limited metabolic stability, which require extensive optimization. To identify more drug-like CARM1 degraders, we developed a high-throughput screening platform. We enabled antibody-free monitoring of CARM1 levels by fusing a HiBiT tag to CARM1 in MCF7 breast cancer cells. Complementation with LgBiT produces luciferase activity. Using this platform, we screened 1408 plant-derived natural product fractions to identify compounds that reduce CARM1 protein levels. This screen revealed two promising natural compounds, kusunokinin and exostemin, that specifically target CARM1 for degradation with selectivity over other protein arginine methyltransferases. Both compounds demonstrated functional anticancer activity, significantly inhibiting breast cancer cell colony formation and migration. Kusunokinin and exostemin represent lead compounds for developing next-generation CARM1-targeted therapeutics with enhanced translational potential.
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.