Topics

Selective Inhibitors of AlkB Family of Nucleic Acid Demethylases.

08:00 EDT 11th October 2019 | BioPortfolio

Summary of "Selective Inhibitors of AlkB Family of Nucleic Acid Demethylases."

The α-ketoglutarate-dependent (AlkB) superfamily of FeII/2-oxoglutarate (2-OG) -dependent dioxygenases consists of a unique class of nucleic acid repair enzymes which reversibly remove alkyl substituents from nucleobases through oxidative dealkylation. Recent studies have verified the involvement of AlkB dioxygenases in a variety of human diseases. However, the development of small organic molecules that can function as enzyme inhibitors to block the action of oxidative dealkylation is still in its infancy. These purposeful chemical motifs, if capable of influencing the dealkylation activity, would have a potential clinical value by controlling genetic information expression. In this Perspective, we will summarize some of the most updated inhibitors of AlkB family demethylases, and hope to provide a thought for the follow-up screening optimization.

Affiliation

Journal Details

This article was published in the following journal.

Name: Biochemistry
ISSN: 1520-4995
Pages:

Links

DeepDyve research library

PubMed Articles [17451 Associated PubMed Articles listed on BioPortfolio]

Understanding the variability of the S1' pocket to improve matrix metalloproteinase inhibitor selectivity profiles.

Matrix metalloproteinases (MMPs) are a family of proteins involved in a range of pathologies. Given that MMP broad-spectrum inhibition is associated with severe adverse effects, selectivity has become...

High selective spectroelectrochemical biosensor for HCV-RNA detection based on a specific peptide nucleic acid.

Hepatitis C virus (HCV) is a blood-borne virus that causes infectious chronic hepatitis. Egypt has the largest epidemic of HCV in the world, with about 14.7% of the Egyptian population. Thus, HCV, whi...

Development of substituted pyrido3,2-dpyrimidines as potent and selective dihydrofolate reductase inhibitors for pneumocystis pneumonia infection.

Pneumocystis pneumonia (PCP) caused by Pneumocystis jirovecii (pj) can lead to serious health consequences in patients with an immunocompromised system. Trimethoprim (TMP), used as first-line therapy ...

Targeting dynamic ATP-binding site features allows discrimination between highly homologous protein kinases.

ATP-competitive inhibitors that demonstrate exquisite selectivity for specific members of the human kinome have been developed. Despite this success, the identification of highly selective inhibitors ...

Rationally Designed Small Nucleic Acid-Based Inhibitors of CRISPR-Cas9.

Clustered regularly interspaced short palindromic repeat (CRISPR) RNAs and their associated effector (Cas) enzymes are being developed into promising therapeutics to treat disease. However, CRISPR-Cas...

Clinical Trials [7216 Associated Clinical Trials listed on BioPortfolio]

TBTC NAA Study: Pilot Study of Surrogate Markers for Outcome of TB Treatment

This is a pilot study to evaluate the performance of several nucleic acid amplification methodologies in the diagnosis and management of active tuberculosis

Validation of a Simple and Cost-Effective Nucleic Acid Test for HIV Detection

Validate a simple and cost-effective Nucleic Acid Test for HIV Detection in order to develop a rapid, highly sensitive and specific, one-stage test for the diagnosis of HIV infection. Bloo...

Study In Patients With Depression Not Responding to Selective Serotonin Re-uptake Inhibitors

This study is designed to evaluate the efficacy and safety in depressive patients who did not respond sufficiently to selective serotonin re-uptake inhibitors (SSRI).

Evaluation of the Alere i Influenza A&B Nucleic Acid Amplification Versus Xpert Flu/RSV

The rapid and accurate detection of influenza virus in respiratory specimens is required for optimal management of patients with acute respiratory infections. Because of the variability of...

Performance of Nucleic Acid Amplification Tests for the Detection of NG and CT

The purpose of this study is to provide data and analyses to support 510(k) applications to the FDA for multiple nucleic acid amplification tests (NAATs) diagnostic platforms.

Medical and Biotech [MESH] Definitions

A family of alpha- KETOGLUTARIC ACID and Fe(II)-dependent dioxygenases that are homologous to AlkB, an enzyme that repairs alkylated nucleic acids in E. coli. The mammalian homologs have diverse substrate specificities and functions that include DNA REPAIR, generating unique wobble modifications in URIDINE tRNA, demethylation of nucleotides in DNA and RNA, and demethylation of LYSINE residues on certain proteins, including ACTIN and histones (HISTONE CODE).

Techniques for measuring specific nucleic acid interaction with another nucleic acid or with a protein by digestion of the non-interacting nucleic acid by various nucleases. After all non-interacting regions are eliminated by nuclease digestion, the protected nucleic acid that remains is analyzed. DNA FOOTPRINTING utilizes this technique to analyze the DNA contact sites of DNA-BINDING PROTEINS.

Double-stranded nucleic acid molecules (DNA-DNA or DNA-RNA) which contain regions of nucleotide mismatches (non-complementary). In vivo, these heteroduplexes can result from mutation or genetic recombination; in vitro, they are formed by nucleic acid hybridization. Electron microscopic analysis of the resulting heteroduplexes facilitates the mapping of regions of base sequence homology of nucleic acids.

Compounds that inhibit cell production of DNA or RNA.

A family of histone demethylases that share a conserved Jumonji C domain. The enzymes function via an iron-dependent dioxygenase mechanism that couples the conversion of 2-oxoglutarate to succinate to the hydroxylation of N-methyl groups.

Quick Search


DeepDyve research library

Relevant Topic

Enzymes
Enzymes are proteins that catalyze (i.e., increase the rates of) chemical reactions. In enzymatic reactions, the molecules at the beginning of the process, called substrates, are converted into different molecules, called products. Almost all chemical re...


Searches Linking to this Article