C-Terminal Amidation of Chlorotoxin Does Not Affect Tumour Cell Proliferation and Has No Effect on Toxin Cytotoxicity

AYED, A.S., OMRAN, M.A.A.A., NABIL, Z.I., STRONG, P.N., NEWTON, K.A. and ABDEL-RAHMAN, M.A. (2020). C-Terminal Amidation of Chlorotoxin Does Not Affect Tumour Cell Proliferation and Has No Effect on Toxin Cytotoxicity. International Journal of Peptide Research and Therapeutics.

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Official URL: https://link.springer.com/article/10.1007/s10989-0...
Link to published version:: https://doi.org/10.1007/s10989-020-10117-4


© 2020, Springer Nature B.V. Chlorotoxin (Cltx), a cell-penetrating peptide from the venom of the scorpion Leiurus quinquestriatus has selective activity on a range of neuroectodermal tumours and related cell lines. Although the precise mechanism of Cltx action is not clear, Cltx has been shown to be a useful tumour imaging agent and radiolabelled Cltx has undergone clinical trials for targeted glioma radiotherapy. The native peptide (and synthetic material, TM601) is amidated at its C-terminus (Cltx-CONH2). A recombinant form produced in E. coli is not processed and has a free C-terminal carboxyl group (Cltx-COOH). The amidated form appears to have no effects on proliferation and cytotoxicity, whereas studies on the free carboxyl form are contradictory. Cltx-CONH2 and Cltx-COOH have been used interchangeably over many years and this has resulted in confusion in the literature; the significance of any difference is extremely important one with respect to the use of the toxin in a clinical diagnostic or therapeutic setting. This study was carried out to investigate, in parallel, the effects of Cltx-CONH2 and Cltx-COOH on cell proliferation and cytotoxicity on a variety of representative tumour cell lines (U87MG, MCF-7, PC3 and A549) using cell Titer Glo and cell Tox Green assays, respectively. Neither Cltx-CONH2 nor Cltx-COOH affected cell proliferation or cytotoxicity, indicating that terminal arginine amidation does not play an important role in cytotoxic or cytostatic properties of Cltx.

Item Type: Article
Uncontrolled Keywords: Amidated chlorotoxin; Carboxylated chlorotoxin; C-terminal; Proliferation; Cytotoxicity; Organic Chemistry; 0601 Biochemistry and Cell Biology; 1101 Medical Biochemistry and Metabolomics
Identification Number: https://doi.org/10.1007/s10989-020-10117-4
SWORD Depositor: Symplectic Elements
Depositing User: Symplectic Elements
Date Deposited: 30 Nov 2020 17:26
Last Modified: 17 Mar 2021 19:45
URI: https://shura.shu.ac.uk/id/eprint/27692

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