e-ISSN: 3107-6203

Authors: Sanjai Saxena 1, 2

1 Department of Biotechnology, Thapar Institute of Engineering and Technology, Patiala, Punjab 147004. 

2 Founder, Agpharm Bioinnovations LLP, STEP - Thapar Institute of Engineering and Technology, Patiala, Punjab 147004

*Corresponding author: Sanjai Saxena; Email: ssaxena@thapar.edu; sanjaibiotech@yahoo.com

Abstract

Fungi are prolific producers of structurally diverse secondary metabolites, many of which serve as potent enzyme inhibitors with therapeutic potential. Targeting important enzymes linked to cancer, diabetes, neurodegenerative, infectious, and metabolic diseases, this review examines fungal-derived enzyme inhibitors discovered between 2015 and 2025 based on research published in Google Scholar, ScienceDirect, Web of Knowledge, and Scopus. The study highlights fungal metabolites that inhibit proteasomes, tyrosine phosphatases (PTP1B), α-glucosidase, cholinesterase, BACE1, GSK-3, viral neuraminidase, histone acetyltransferases, and isocitrate dehydrogenases, among others. These bioactive compounds, sourced from fungi inhabiting diverse ecological niches—marine, endophytic, soil, and symbiotic—demonstrate unique chemotypes and novel mechanisms of enzyme inhibition. Their broad-spectrum activity and structural novelty present promising scaffolds for drug development. Fungi’s amenability to fermentation, coupled with advances in genomics, synthetic biology, and computational tools, has enabled accelerated discovery and optimization of enzyme inhibitors. However, challenges such as suboptimal pharmacokinetics and potential toxicity necessitate rigorous in silico and experimental screening. The review underscores fungi as an underexploited reservoir for enzyme-targeted therapeutics and advocates continued bioprospecting and molecular characterization to unlock their full pharmaceutical potential. Integrating fungal chemical diversity with modern drug discovery platforms could significantly advance the development of next-generation therapeutics.

Keywords: Bioresource, Drug Discovery, Enzyme Kinetics, Fungi, Inhibitors, Therapeutics.

Document Type: Review Article

Citation: Saxena S. (2026). Fungi as a source of enzyme inhibitors: bioprospecting for new drugs. Mycological Spectrum 2(1),18-49.

Handling Editor: Dr. S.K. Deshmukh | Reviewers: Prof. Abhijeet Kate and Prof. Nihar Ranjan