20S proteasome inhibition: Designing noncovalent linear peptide mimics of the natural product TMC-95A

Michael Groll; Nerea Gallastegui; Xavier Maréchal; Virginie Le Ravalec; Nicolas Basse; Nicolas Richy; Emilie Genin; Robert Huber; Luis Moroder; Jölle Vidal; Michèle Reboud-Ravaux

doi:10.1002/cmdc.201000293

20S proteasome inhibition: Designing noncovalent linear peptide mimics of the natural product TMC-95A

Michael Groll, Nerea Gallastegui, Xavier Maréchal, Virginie Le Ravalec, Nicolas Basse, Nicolas Richy, Emilie Genin, Robert Huber, Luis Moroder, Jölle Vidal, Michèle Reboud-Ravaux

Chair of Biochemistry

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

47 Scopus citations

Abstract

Stop the shredder: The 20S proteasome maintains homeostasis and regulates important intracellular processes by subjecting most intracellular proteins to endoproteolytic cleavage. This complex hydrolysis machinery has received considerable attention for the treatment of many diseases, including cancer. We report a new set of noncovalent peptide mimics based on TMC-95A and our rational approach to inhibitor optimization using both crystallographic and kinetic studies. (Chemical Presented).

Original language	English
Pages (from-to)	1701-1705
Number of pages	5
Journal	ChemMedChem
Volume	5
Issue number	10
DOIs	https://doi.org/10.1002/cmdc.201000293
State	Published - 4 Oct 2010

Keywords

Crystallographic analysis
Enzymes
Inhibitors
Natural products
Proteasomes

UN SDGs

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

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10.1002/cmdc.201000293

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abstract = "Stop the shredder: The 20S proteasome maintains homeostasis and regulates important intracellular processes by subjecting most intracellular proteins to endoproteolytic cleavage. This complex hydrolysis machinery has received considerable attention for the treatment of many diseases, including cancer. We report a new set of noncovalent peptide mimics based on TMC-95A and our rational approach to inhibitor optimization using both crystallographic and kinetic studies. (Chemical Presented).",

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AU - Groll, Michael

AU - Gallastegui, Nerea

AU - Maréchal, Xavier

AU - Le Ravalec, Virginie

AU - Basse, Nicolas

AU - Richy, Nicolas

AU - Genin, Emilie

AU - Huber, Robert

AU - Moroder, Luis

AU - Vidal, Jölle

AU - Reboud-Ravaux, Michèle

PY - 2010/10/4

Y1 - 2010/10/4

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KW - Crystallographic analysis

KW - Enzymes

KW - Inhibitors

KW - Natural products

KW - Proteasomes

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JO - ChemMedChem

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ER -

20S proteasome inhibition: Designing noncovalent linear peptide mimics of the natural product TMC-95A

Abstract

Keywords

UN SDGs

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