Drug intelligence / Profile preview

9-deazaguanine

Development stage
Preclinical
Modality
Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules
01

Overview

9-Deazaguanine is a synthetic analog of guanine and a small molecule inhibitor of purine nucleoside phosphorylase (PNP), with a dissociation constant (Kd) of approximately 160 nM. As an experimental compound, it has been primarily used in research settings to study nucleic acid structure and function, as well as to develop potential antiviral, antineoplastic, and immunosuppressive agents. Inhibitors of PNP like 9-deazaguanine are known to suppress T cell proliferation and have been investigated for their potential use in treating T cell cancers, autoimmune diseases, transplant rejection, psoriasis, and gout. The mechanism involves competitive inhibition at the PNP enzyme active site; this disrupts purine metabolism critical for lymphocyte proliferation. While its exact mechanism is still under investigation, it may also interfere with guanine binding in nucleic acids or proteins and impede DNA/RNA replication[5][7][9].

Other names
9-deazaguanine
02

Targets

PNP (Purine nucleoside phosphorylase)

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