Abstract
This review summarises the current knowledge of Gomesin (Gm), an 18-residue long, cationic anti-microbial peptide originally isolated from the haemocytes of the Brazilian tarantula Acanthoscurria gomesiana. The peptide shows potent cytotoxic activity against clinically relevant microbes including Gram-positive and Gram-negative bacteria, fungi, and parasites. In addition, Gm shows in-vitro and in-vivo anti-cancer activities against several human and murine cancers. The peptide exerts its cytotoxic activity by permeabilising cell membranes, but the underlying molecular mechanism of action is still unclear. Due to its potential as a therapeutic agent, the structure and membrane-binding properties, as well as the leakage and cytotoxic activities of Gm have been studied using a range of techniques. This review provides a summary of these studies, with a particular focus on biophysical characterisation studies of peptide variants that have attempted to establish a structure-activity relationship. Future studies are still needed to rationalise the binding affinity and cell-type-specific selectivity of Gm and its variants, while more pre-clinical studies are required to develop Gm into a therapeutically useful peptide.
Highlights
Gomesin (Gm) is a cationic anti-microbial peptide (AMP) that was originally isolated from the haemocytes of the unchallenged Brazilian tarantula Acanthoscurria gomesiana [1]
Since its original discovery and isolation, a number of studies have confirmed the cytotoxic activity of Gm against a range of clinically-relevant microbes as well as cancer cells
The biophysical characterisation of Gm and Gm variants has shown that the β-sheet structure is required for its anti-microbial and anti-cancer activity, as well as its serum stability
Summary
Gomesin (Gm) is a cationic anti-microbial peptide (AMP) that was originally isolated from the haemocytes of the unchallenged Brazilian tarantula Acanthoscurria gomesiana [1]. A number of studies have successfully used different types of chemical modifications, such as cyclisation and/or amino acid substitution, to increase the anti-microbial or anti-cancer properties of Gm [3,8,9,18]. This wide range of cytotoxic activity, combined with its high serum stability [3,6,8,9] and moderate levels of haemolysis [1,6,7,8,9], make Gm of interest for the development of therapeutics to treat microbial infections and cancer
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