Synthesis and testing of peptides for anti-prion activity

Shane Sellarajah; Cyrille Boussard; Tarnuna Lekishvili; David R. Brown; Ian H. Gilbert

doi:10.1016/j.ejmech.2008.01.041

Synthesis and testing of peptides for anti-prion activity

Shane Sellarajah, Cyrille Boussard, Tarnuna Lekishvili, David R. Brown, Ian H. Gilbert

Research output: Contribution to journal › Article › peer-review

3 Citations (Scopus)

Abstract

Creutzfeldt-Jakob disease (CJD) is one of the fatal transmissible spongiform encephalopathies for which there is no known cure. The disease is associated with an abnormally folded prion protein, PrP-res, which is thought to form due to interaction between normal prion PrPC and PrP-es. Small peptides were designed to prevent this interaction. A structure-activity relationship is described for a series of peptides which were synthesised and tested for their activity against two prion disease model assays, an in vitro cellular assay and an in vitro anti-aggregation polymerisation assay. A number of peptides were found to be active at levels of 100 mu M. New libraries were synthesised in order to concentrate on discovering new, shorter peptides which could be leads for developing peptidomimetics. (C) 2008 Elsevier Masson SAS. All rights reserved.

Original language	English
Pages (from-to)	2418-2427
Number of pages	10
Journal	European Journal of Medicinal Chemistry
Volume	43
Issue number	11
DOIs	https://doi.org/10.1016/j.ejmech.2008.01.041
Publication status	Published - Nov 2008

Keywords

Prion
Transmissible spongiform encephalopathy
Peptide
TRANSMISSIBLE SPONGIFORM ENCEPHALOPATHIES
CONGO RED
HIV PROTEINASE
INHIBITION
DISEASES
THERAPEUTICS
PRP
CONSEQUENCES
HAMSTERS
BINDING

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

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10.1016/j.ejmech.2008.01.041

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title = "Synthesis and testing of peptides for anti-prion activity",

abstract = "Creutzfeldt-Jakob disease (CJD) is one of the fatal transmissible spongiform encephalopathies for which there is no known cure. The disease is associated with an abnormally folded prion protein, PrP-res, which is thought to form due to interaction between normal prion PrPC and PrP-es. Small peptides were designed to prevent this interaction. A structure-activity relationship is described for a series of peptides which were synthesised and tested for their activity against two prion disease model assays, an in vitro cellular assay and an in vitro anti-aggregation polymerisation assay. A number of peptides were found to be active at levels of 100 mu M. New libraries were synthesised in order to concentrate on discovering new, shorter peptides which could be leads for developing peptidomimetics. (C) 2008 Elsevier Masson SAS. All rights reserved.",

keywords = "Prion, Transmissible spongiform encephalopathy, Peptide, TRANSMISSIBLE SPONGIFORM ENCEPHALOPATHIES, CONGO RED, HIV PROTEINASE, INHIBITION, DISEASES, THERAPEUTICS, PRP, CONSEQUENCES, HAMSTERS, BINDING",

author = "Shane Sellarajah and Cyrille Boussard and Tarnuna Lekishvili and Brown, {David R.} and Gilbert, {Ian H.}",

year = "2008",

month = nov,

doi = "10.1016/j.ejmech.2008.01.041",

language = "English",

volume = "43",

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journal = "European Journal of Medicinal Chemistry",

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TY - JOUR

T1 - Synthesis and testing of peptides for anti-prion activity

AU - Sellarajah, Shane

AU - Boussard, Cyrille

AU - Lekishvili, Tarnuna

AU - Brown, David R.

AU - Gilbert, Ian H.

PY - 2008/11

Y1 - 2008/11

N2 - Creutzfeldt-Jakob disease (CJD) is one of the fatal transmissible spongiform encephalopathies for which there is no known cure. The disease is associated with an abnormally folded prion protein, PrP-res, which is thought to form due to interaction between normal prion PrPC and PrP-es. Small peptides were designed to prevent this interaction. A structure-activity relationship is described for a series of peptides which were synthesised and tested for their activity against two prion disease model assays, an in vitro cellular assay and an in vitro anti-aggregation polymerisation assay. A number of peptides were found to be active at levels of 100 mu M. New libraries were synthesised in order to concentrate on discovering new, shorter peptides which could be leads for developing peptidomimetics. (C) 2008 Elsevier Masson SAS. All rights reserved.

AB - Creutzfeldt-Jakob disease (CJD) is one of the fatal transmissible spongiform encephalopathies for which there is no known cure. The disease is associated with an abnormally folded prion protein, PrP-res, which is thought to form due to interaction between normal prion PrPC and PrP-es. Small peptides were designed to prevent this interaction. A structure-activity relationship is described for a series of peptides which were synthesised and tested for their activity against two prion disease model assays, an in vitro cellular assay and an in vitro anti-aggregation polymerisation assay. A number of peptides were found to be active at levels of 100 mu M. New libraries were synthesised in order to concentrate on discovering new, shorter peptides which could be leads for developing peptidomimetics. (C) 2008 Elsevier Masson SAS. All rights reserved.

KW - Prion

KW - Transmissible spongiform encephalopathy

KW - Peptide

KW - TRANSMISSIBLE SPONGIFORM ENCEPHALOPATHIES

KW - CONGO RED

KW - HIV PROTEINASE

KW - INHIBITION

KW - DISEASES

KW - THERAPEUTICS

KW - PRP

KW - CONSEQUENCES

KW - HAMSTERS

KW - BINDING

U2 - 10.1016/j.ejmech.2008.01.041

DO - 10.1016/j.ejmech.2008.01.041

M3 - Article

C2 - 18355947

SN - 0223-5234

VL - 43

SP - 2418

EP - 2427

JO - European Journal of Medicinal Chemistry

JF - European Journal of Medicinal Chemistry

IS - 11

ER -

Synthesis and testing of peptides for anti-prion activity

Abstract

Keywords

UN SDGs

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