Ritonavir does not inhibit calpain in vitro

Dominic Cuerrier; Zilin Nie; Andrew D. Badley; Peter L. Davies

doi:10.1016/j.bbrc.2004.11.161

Ritonavir does not inhibit calpain in vitro

Dominic Cuerrier, Zilin Nie, Andrew D. Badley, Peter L. Davies

Infectious Diseases

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

9 Scopus citations

Abstract

Ritonavir, an inhibitor of HIV-1 protease, has been reported to also inhibit the Ca ²⁺-dependent cysteine protease, calpain. We have investigated these claims with an in vitro study of the effect of ritonavir on the m-calpain and μ-calpain isoforms. Ritonavir failed to block either autolytic or hydrolytic calpain activity, but remained fully capable of inhibiting the HIV-1 protease. Any calpain-related effects of ritonavir in cells must, therefore, arise by a mechanism other than direct inhibition of calpains.

Original language	English (US)
Pages (from-to)	208-211
Number of pages	4
Journal	Biochemical and Biophysical Research Communications
Volume	327
Issue number	1
DOIs	https://doi.org/10.1016/j.bbrc.2004.11.161
State	Published - Feb 4 2005

Keywords

Autolysis
Calpain
Inhibitor
Protease
Ritonavir

ASJC Scopus subject areas

Biophysics
Biochemistry
Molecular Biology
Cell Biology

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10.1016/j.bbrc.2004.11.161

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title = "Ritonavir does not inhibit calpain in vitro",

abstract = "Ritonavir, an inhibitor of HIV-1 protease, has been reported to also inhibit the Ca 2+-dependent cysteine protease, calpain. We have investigated these claims with an in vitro study of the effect of ritonavir on the m-calpain and μ-calpain isoforms. Ritonavir failed to block either autolytic or hydrolytic calpain activity, but remained fully capable of inhibiting the HIV-1 protease. Any calpain-related effects of ritonavir in cells must, therefore, arise by a mechanism other than direct inhibition of calpains.",

keywords = "Autolysis, Calpain, Inhibitor, Protease, Ritonavir",

author = "Dominic Cuerrier and Zilin Nie and Badley, {Andrew D.} and Davies, {Peter L.}",

note = "Funding Information: We thank Dr. David A. Potter for one of the two ritonavir samples used in this work, and Dr. Bernd Keller for mass spectrometry analysis. This work was supported by the Heart and Stroke Foundation of Canada. D. Cuerrier holds an NSERC studentship and P. Davies holds a Canada Research Chair in Protein Engineering.",

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doi = "10.1016/j.bbrc.2004.11.161",

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T1 - Ritonavir does not inhibit calpain in vitro

AU - Cuerrier, Dominic

AU - Nie, Zilin

AU - Badley, Andrew D.

AU - Davies, Peter L.

N1 - Funding Information: We thank Dr. David A. Potter for one of the two ritonavir samples used in this work, and Dr. Bernd Keller for mass spectrometry analysis. This work was supported by the Heart and Stroke Foundation of Canada. D. Cuerrier holds an NSERC studentship and P. Davies holds a Canada Research Chair in Protein Engineering.

PY - 2005/2/4

Y1 - 2005/2/4

N2 - Ritonavir, an inhibitor of HIV-1 protease, has been reported to also inhibit the Ca 2+-dependent cysteine protease, calpain. We have investigated these claims with an in vitro study of the effect of ritonavir on the m-calpain and μ-calpain isoforms. Ritonavir failed to block either autolytic or hydrolytic calpain activity, but remained fully capable of inhibiting the HIV-1 protease. Any calpain-related effects of ritonavir in cells must, therefore, arise by a mechanism other than direct inhibition of calpains.

AB - Ritonavir, an inhibitor of HIV-1 protease, has been reported to also inhibit the Ca 2+-dependent cysteine protease, calpain. We have investigated these claims with an in vitro study of the effect of ritonavir on the m-calpain and μ-calpain isoforms. Ritonavir failed to block either autolytic or hydrolytic calpain activity, but remained fully capable of inhibiting the HIV-1 protease. Any calpain-related effects of ritonavir in cells must, therefore, arise by a mechanism other than direct inhibition of calpains.

KW - Autolysis

KW - Calpain

KW - Inhibitor

KW - Protease

KW - Ritonavir

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JO - Biochemical and Biophysical Research Communications

JF - Biochemical and Biophysical Research Communications

IS - 1

ER -

Ritonavir does not inhibit calpain in vitro

Abstract

Keywords

ASJC Scopus subject areas

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