ArticleMedChemComm2013
The structure-activity relationships of L3MBTL3 inhibitors: flexibility of the dimer interface.
Article in MedChemComm, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers.
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
9 citing papers in PubMed.
- A First-in-Class High-Throughput Screen to Discover Modulators of the Alternative Lengthening of Telomeres (ALT) Pathway.ACS pharmacology & translational science · 2024Article
- Targeting protein methylation: from chemical tools to precision medicines.Cellular and molecular life sciences : CMLS · 2019Review
- Chemical modulators for epigenome reader domains as emerging epigenetic therapies for cancer and inflammation.Current opinion in chemical biology · 2017Review
- The EED protein-protein interaction inhibitor A-395 inactivates the PRC2 complex.Nature chemical biology · 2017Article
- A fast, open source implementation of adaptive biasing potentials uncovers a ligand design strategy for the chromatin regulator BRD4.The Journal of chemical physics · 2016Article
- Chemical probes for methyl lysine reader domains.Current opinion in chemical biology · 2016Review
- The L3MBTL3 Methyl-Lysine Reader Domain Functions As a Dimer.ACS chemical biology · 2016Article
- Selective Inhibition of CBX6: A Methyllysine Reader Protein in the Polycomb Family.ACS medicinal chemistry letters · 2016Article
- Discovery and development of potent and selective inhibitors of histone methyltransferase g9a.ACS medicinal chemistry letters · 2014Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
11 authors.
Funding
Abstract
We recently reported the discovery of UNC1215, a potent and selective chemical probe for the L3MBTL3 methyllysine reader domain. In this article, we describe the development of structure-activity relationships (SAR) of a second series of potent L3MBTL3 antagonists which evolved from the structure of the chemical probe UNC1215. These compounds are selective for L3MBTL3 against a panel of methyllysine reader proteins, particularly the related MBT family proteins, L3MBTL1 and MBTD1. A co-crystal structure of L3MBTL3 and one of the most potent compounds suggests that the L3MBTL3 dimer rotates about the dimer interface to accommodate ligand binding.
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.