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Functional Complementation Analysis FCA: A Laboratory Exercise Designed and Implemented to Supplement the Teaching of Biochemical Pathways

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Exploring Aspartate Transcarbamoylase: A Promising Broad-Spectrum Target for Drug Development.

Siyao Chen¹, Queenie Mondile², XiaoChen Du¹

¹Department of Chemical and Pharmaceutical Biology, University of Groningen, Antonius Deusinglaan 1, 9731AV, Groningen, The Netherlands.

Chembiochem : a European Journal of Chemical Biology

|February 12, 2025

Summary

Allosteric inhibitors targeting aspartate transcarbamoylase (ATCase) show promise for treating diseases like malaria, tuberculosis, and cancer. This research explores their potential against neglected diseases and as herbicides.

Keywords:

Allosteric Inhibition Aspartate Transcarbamoylase Broad spectrum drug discover Infectious diseases de novo Pyrimidine Biosynthesis

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Preparation and In Vivo Use of an Activity-based Probe for N-acylethanolamine Acid Amidase

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Published on: November 23, 2016

Area of Science:

Biochemistry
Medicinal Chemistry
Drug Discovery

Background:

Pyrimidine nucleotides are vital for cellular processes, synthesized via salvage or de novo pathways.
De novo pyrimidine biosynthesis is crucial for rapidly proliferating cells, including cancer and pathogens.
Aspartate transcarbamoylase (ATCase) is the rate-limiting enzyme in de novo pyrimidine synthesis, making it a key therapeutic target.

Purpose of the Study:

To review the development of allosteric ATCase inhibitors.
To explore their therapeutic potential in malaria, tuberculosis, cancer, neglected tropical diseases, and antimicrobial resistance.
To investigate their application as herbicides and analyze the conserved allosteric pocket.

Main Methods:

Structure and sequence-based analysis of the ATCase allosteric pocket.
Review of existing allosteric ATCase inhibitor development.
Comparative analysis across different organisms and applications.

Main Results:

Allosteric ATCase inhibitors show potential across a range of diseases and agricultural applications.
Identification of a conserved allosteric pocket across various ATCase targets.
Structure-activity relationship insights for inhibitor design.

Conclusions:

Allosteric ATCase inhibitors represent a versatile therapeutic and agricultural development platform.
Continued research is warranted due to the broad applicability in human health and agriculture.
Targeting ATCase offers a strategy for combating infectious diseases, cancer, and enhancing crop protection.