Peptide substrates recognisable by a botulinum toxin A, BoNT/A and the use thereof

A technology for botulinum toxin and peptide substrates, which is applied in the fields of peptides, desipeptides, fluorescence/phosphorescence, etc., which can solve the problems of time-consuming and expensive and not evaluating the biological activity of therapeutic toxin preparations

Inactive Publication Date: 2007-05-23
PHARMALEADS SA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although very sensitive in that it can detect 5 to 10 pg of BoNT / A, the method has many drawbacks: the response time is several days and does not appear to be the most accurate method for assessing the biological activity of therapeutic toxin preparations (Pearce et al. (1994) Tox. Applied Pharmacol., 128, 69-77)
However, the method is time consuming and expensive

Method used

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  • Peptide substrates recognisable by a botulinum toxin A, BoNT/A and the use thereof
  • Peptide substrates recognisable by a botulinum toxin A, BoNT/A and the use thereof
  • Peptide substrates recognisable by a botulinum toxin A, BoNT/A and the use thereof

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Experimental program
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Embodiment Construction

[0159] 1) Synthesis of peptides

[0160]The desired compound can be obtained by the usual solid-phase synthesis method on an automated synthesizer such as Applied Biosystem's Apparatus 431A according to the method of Merrifield. The chemistry used corresponds to the Fmoc technique. Side chain deprotection and cleavage of peptidyl resins by trichloroacetic acid, as described by E. Atherton and R.C. Sheppard (1989) in "Solid phase peptides synthesis: a practical approach", IRL Press , Oxford). The coupling is carried out according to conventional techniques, using coupling agents such as HATU, Bop, PyBrop, and preferably dicyclohexylcarbodiimide in the presence of hydroxybenzotriazole (HOBT) ( DCC). The details of the technology used can be found in the publications reporting the synthesis of very large peptides carried out by the inventors (Cornille F. et al., J.Pept.Res., 1999, 54, 427-435; Cornille F. et al. , Nucleic Ac.Res., 1998, 26, 2143-2149; Cornille F. et al., Int.J....

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Abstract

The invention relates to a peptide substrate selectively recognisable by a botulinum toxin A, BoNT / A comprising a Nop-(Z)-Pya fragment in the peptide structure thereof, wherein Z is an aminoacid chain, preferably RA and said fragment is cleaved by the toxin. Said invention also relates to the substrate use, in particular for carrying out methods for detecting, identifying and / or dosing the botulinum toxin A at very low concentrations (of order of 20 pg) or the inhibitors and / or activators of the toxin metallopeptidase activity, thereby making it possible to quantify the power thereof.

Description

technical field [0001] The present invention relates to peptide substrates selectively recognized by botulinum toxin type A BoNT / A and uses thereof, more particularly for the detection, identification and / or quantification of botulinum toxin type A or metals of said toxin Methods of Inhibitors and / or Activators of Peptidase Activity. Background technique [0002] Neurotoxin type A (BoNT / A) forms part of a family of seven related proteins (botulinum toxins A to G) produced by different strains of the anaerobic bacterium "Clostridium botulinum". The two most commonly encountered and most dangerous forms are type A and B toxins. The LD50 lethal dose in mice by the intraperitoneal route is 2 pg of type A toxin and about 50 to 100 pg of type B toxin. They act in humans and various animal species at the level of the peripheral nervous system by inducing "botulism" characterized by flaccid paralysis of skeletal muscles that can lead to death. [0003] The main form of intoxicati...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C12Q1/37G01N21/64C07K7/08C07K14/00C07K2/00C07K5/107C07K14/33
CPCC07K5/1016C12Q1/37
Inventor M－C·富尼耶－扎卢斯基B·P·罗克
Owner PHARMALEADS SA
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