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.

Full text not available from this repository.

Abstract

© 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

Actions (login required)

View Item

Downloads

Publication Metrics