Drug intelligence / Profile preview

ATIC-IN-1

Development stage
Preclinical
Lead developer
University of Southampton
Modality
Small Molecules
01

Overview

ATIC-IN-1 is a small molecule inhibitor that functions by preventing the homodimerization of Aminoimidazole carboxamide ribonucleotide transformylase/inosine monophosphate cyclohydrolase (ATIC). ATIC is a bifunctional homodimeric enzyme crucial for the last two steps of de novo purine biosynthesis. Its homodimerization is essential for its AICAR transformylase activity. By inhibiting ATIC homodimerization, ATIC-IN-1 blocks this enzymatic activity, leading to an increase in intracellular levels of 5-aminoimidazole-4-carboxamide ribonucleotide (AICAR or ZMP). This accumulation of ZMP subsequently activates AMP-activated protein kinase (AMPK). The compound has demonstrated anti-tumor activity by reducing cell proliferation and cell division rates in breast cancer cell lines and has been investigated for its potential in cancer therapy and metabolic disorders. Initial research and development of this small molecule inhibitor were conducted by the University of Southampton.

Other names
ATIC homodimerization inhibitorATIC Dimerization InhibitorAICAR Tfase InhibitorAICAR Transformylase InhibitorAICAR Tranformylase/Inosine Monophosphate Cyclohydrolase Dimerization Inhibitor
02

Targets

AMPK (Adenosine monophosphate–activated protein kinase)ATIC (Aminoimidazole carboxamide ribonucleotide transformylase)

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