Evaluation of phenylcyclopropylamine compounds by enzymatic assay of lysine-specific demethylase 2 in the presence of NPAC peptide

Bioorganic & Medicinal Chemistry Letters
Taeko KakizawaTakayoshi Suzuki

Abstract

Lysine-specific demethylase 2 (LSD2) demethylates mono- and dimethylated Lys-4 of histone H3 (H3K4me1 and H3K4me2). NPAC protein is known to interact with LSD2 and promote its H3K4 demethylase activity. In this study, we established a demethylation assay system that utilizes recombinant LSD2 in the presence of a synthetic NPAC peptide. Several phenylcyclopropylamine (PCPA)-based inhibitors were examined for their LSD2 inhibitory activity in the LSD2 enzymatic assay with the NPAC peptide. The assay results showed that the PCPA derivatives, including NCD41, selectively inhibited LSD1 in preference to LSD2.

References

Mar 1, 1990·International Journal of Peptide and Protein Research·G B Fields, R L Noble
Dec 3, 2009·Journal of the American Chemical Society·Rie UedaNaoki Miyata
Jan 14, 2011·Bioorganic & Medicinal Chemistry·Daisuke OgasawaraNaoki Miyata
Oct 1, 2011·Journal of Medicinal Chemistry·Takayoshi Suzuki, Naoki Miyata
Jul 5, 2013·Angewandte Chemie·Daisuke OgasawaraTakayoshi Suzuki
Nov 16, 2013·Nature Reviews. Drug Discovery·Jonas W HøjfeldtKristian Helin
Apr 24, 2014·Computational and Structural Biotechnology Journal·Yukihiro ItohTakayoshi Suzuki
Jul 19, 2014·Bioscience, Biotechnology, and Biochemistry·Koshiki MinoTamio Mizukami

❮ Previous
Next ❯

Citations

Jul 11, 2019·Scientific Reports·Eishin MitsuiTamio Mizukami
Mar 10, 2017·Epigenetics : Official Journal of the DNA Methylation Society·Hideaki Niwa, Takashi Umehara
Sep 17, 2016·The Journal of Biological Chemistry·Emily L RicqStephen J Haggarty
Apr 26, 2017·Clinical Epigenetics·Sheraz Gul
Dec 5, 2017·Bioorganic & Medicinal Chemistry Letters·Taeko KakizawaTakayoshi Suzuki

❮ Previous
Next ❯

Related Concepts

Trending Feeds

COVID-19

Coronaviruses encompass a large family of viruses that cause the common cold as well as more serious diseases, such as the ongoing outbreak of coronavirus disease 2019 (COVID-19; formally known as 2019-nCoV). Coronaviruses can spread from animals to humans; symptoms include fever, cough, shortness of breath, and breathing difficulties; in more severe cases, infection can lead to death. This feed covers recent research on COVID-19.

Blastomycosis

Blastomycosis fungal infections spread through inhaling Blastomyces dermatitidis spores. Discover the latest research on blastomycosis fungal infections here.

Nuclear Pore Complex in ALS/FTD

Alterations in nucleocytoplasmic transport, controlled by the nuclear pore complex, may be involved in the pathomechanism underlying multiple neurodegenerative diseases including Amyotrophic Lateral Sclerosis and Frontotemporal Dementia. Here is the latest research on the nuclear pore complex in ALS and FTD.

Applications of Molecular Barcoding

The concept of molecular barcoding is that each original DNA or RNA molecule is attached to a unique sequence barcode. Sequence reads having different barcodes represent different original molecules, while sequence reads having the same barcode are results of PCR duplication from one original molecule. Discover the latest research on molecular barcoding here.

Chronic Fatigue Syndrome

Chronic fatigue syndrome is a disease characterized by unexplained disabling fatigue; the pathology of which is incompletely understood. Discover the latest research on chronic fatigue syndrome here.

Evolution of Pluripotency

Pluripotency refers to the ability of a cell to develop into three primary germ cell layers of the embryo. This feed focuses on the mechanisms that underlie the evolution of pluripotency. Here is the latest research.

Position Effect Variegation

Position Effect Variagation occurs when a gene is inactivated due to its positioning near heterochromatic regions within a chromosome. Discover the latest research on Position Effect Variagation here.

STING Receptor Agonists

Stimulator of IFN genes (STING) are a group of transmembrane proteins that are involved in the induction of type I interferon that is important in the innate immune response. The stimulation of STING has been an active area of research in the treatment of cancer and infectious diseases. Here is the latest research on STING receptor agonists.

Microbicide

Microbicides are products that can be applied to vaginal or rectal mucosal surfaces with the goal of preventing, or at least significantly reducing, the transmission of sexually transmitted infections. Here is the latest research on microbicides.