ArticleJournal of medicinal chemistry2012
Low molecular weight amidoximes that act as potent inhibitors of lysine-specific demethylase 1.
Article in Journal of medicinal chemistry, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.
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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.
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Who cites it
20 citing papers in PubMed.
- Hit-to-lead optimization of heteroaryl amino-carboxamides as LSD1 inhibitors: part II.Journal of computer-aided molecular design · 2026Article
- The Synthesis and Evaluation of Amidoximes as Cytotoxic Agents on Model BacterialMaterials (Basel, Switzerland) · 2021Article
- Epigenetic Reexpression of Hemoglobin F Using Reversible LSD1 Inhibitors: Potential Therapies for Sickle Cell Disease.ACS omega · 2020Article
- Pharmacological Inhibition of LSD1 for Cancer Treatment.Molecules (Basel, Switzerland) · 2018Review
- Inhibitors of Protein Methyltransferases and Demethylases.Chemical reviews · 2018Review
- Computer-Aided Drug Design in Epigenetics.Frontiers in chemistry · 2018Review
- Structural insight into inhibitors of flavin adenine dinucleotide-dependent lysine demethylases.Epigenetics · 2017Review
- Discovery of [1,2,3]Triazolo[4,5-ACS medicinal chemistry letters · 2017Article
- LSD1: biologic roles and therapeutic targeting.Epigenomics · 2016Review
- Review
- Bioactive heterocycles containing endocyclic N-hydroxy groups.European journal of medicinal chemistry · 2015Review
- Structure-activity study for (bis)ureidopropyl- and (bis)thioureidopropyldiamine LSD1 inhibitors with 3-5-3 and 3-6-3 carbon backbone architectures.Bioorganic & medicinal chemistry · 2015Article
- 3,5-Diamino-1,2,4-triazoles as a novel scaffold for potent, reversible LSD1 (KDM1A) inhibitors.MedChemComm · 2014Article
- A selective phenelzine analogue inhibitor of histone demethylase LSD1.ACS chemical biology · 2014Article
- Synthesis and evaluation of novel cyclic Peptide inhibitors of lysine-specific demethylase 1.ACS medicinal chemistry letters · 2014Article
- Design of small molecule epigenetic modulators.Bioorganic & medicinal chemistry letters · 2014Review
- Triazole-dithiocarbamate based selective lysine specific demethylase 1 (LSD1) inactivators inhibit gastric cancer cell growth, invasion, and migration.Journal of medicinal chemistry · 2013Article
- Small molecule epigenetic inhibitors targeted to histone lysine methyltransferases and demethylases.Quarterly reviews of biophysics · 2013Review
- Pre-clinical studies of epigenetic therapies targeting histone modifiers in lung cancer.Frontiers in oncology · 2013Review
- Polyamines and cancer: implications for chemotherapy and chemoprevention.Expert reviews in molecular medicine · 2013Review
Corrections and comments
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Authors and funding
7 authors.
Funding
Abstract
The recently discovered enzyme lysine-specific demethylase 1 (LSD1) plays an important role in the epigenetic control of gene expression, and aberrant gene silencing secondary to LSD1 dysregulation is thought to contribute to the development of cancer. We reported that (bis)guanidines, (bis)biguanides, and their urea- and thiourea isosteres are potent inhibitors of LSD1 and induce the re-expression of aberrantly silenced tumor suppressor genes in tumor cells in vitro. We now report a series of small molecule amidoximes that are moderate inhibitors of recombinant LSD1 but that produce dramatic changes in methylation at the histone 3 lysine 4 (H3K4) chromatin mark, a specific target of LSD1, in Calu-6 lung carcinoma cells. In addition, these analogues increase cellular levels of secreted frizzle-related protein (SFRP) 2, H-cadherin (HCAD), and the transcription factor GATA4. These compounds represent leads for an important new series of drug-like epigenetic modulators with the potential for use as antitumor agents.
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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.