Drug intelligence / Profile preview

2'-deoxy-2'-amino-guanosine

Development stage
Discontinued
Lead developer
National Cancer Institute
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, DNA Intercalators/Alkylators → Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
Intravenous
01

Overview

2'-Deoxy-2'-amino-guanosine is a synthetic nucleoside analog characterized by the substitution of the 2'-hydroxyl group of guanosine with an amino group. This modification alters the chemical properties of the ribose sugar and confers resistance to certain nucleases. Historically investigated as an antimetabolite, it functions as a potent inhibitor of DNA synthesis. Its mechanism of action involves intracellular phosphorylation to the active triphosphate form, which subsequently inhibits enzymes such as ribonucleoside-diphosphate reductase and DNA-directed DNA polymerases. Preclinical studies conducted by the National Cancer Institute and academic researchers have demonstrated its potential as an antiviral agent against herpes simplex virus and influenza, as well as an antineoplastic agent against various tumor cell lines. Despite its significant biological activity in research models, it has primarily remained a specialized tool in molecular biology and a building block for modified oligonucleotides and aptamers rather than progressing to clinical approval.

Other names
2'-amino-2'-deoxyguanosine2'-amino-dG2'-AdG2'-amino-2'-deoxy-D-guanosine
02

Targets

RNR (Ribonucleotide reductase)

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