Targeting Protein Folding: A Novel Approach for the Treatment of Pathogenic Bacteria

Nicolas J Scheuplein, Nicole M Bzdyl, Emily A Kibble, Theresa Lohr, Ulrike Holzgrabe, Mitali Sarkar-Tyson

Research output: Contribution to journalArticlepeer-review

8 Citations (Scopus)


Infectious diseases are a major cause of morbidity and mortality worldwide, exacerbated by increasing antibiotic resistance in many bacterial species. The development of drugs with new modes of action is essential. A leading strategy is antivirulence, with the aim to target bacterial proteins that are important in disease causation and progression but do not affect growth, resulting in reduced selective pressure for resistance. Immunophilins, a superfamily of peptidyl-prolyl cis-trans isomerase (PPIase) enzymes have been shown to be important for virulence in a broad-spectrum of pathogenic bacteria. This Perspective will provide an overview of the recent advances made in understanding the role of each immunophilin family, cyclophilins, FK506 binding proteins (FKBPs), and parvulins in bacteria. Inhibitor design and medicinal chemistry strategies for development of novel drugs against bacterial FKBPs will be discussed. Furthermore, drugs against human cyclophilins and parvulins will be reviewed in their current indication as antiviral and anticancer therapies.

Original languageEnglish
Pages (from-to)13355-13388
Number of pages34
JournalJournal of Medicinal Chemistry
Issue number22
Early online date13 Aug 2020
Publication statusPublished - 25 Nov 2020


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