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Article Dans Une Revue Current Topics in Medicinal Chemistry Année : 2010

Proteasome inhibitors: recent advances and new perspectives in medicinal chemistry

Résumé

The search for proteasome inhibitors began fifteen years ago. These inhibitors proved to be powerful tools for investigating many important cellular processes regulated by the ubiquitinproteasome pathway. Targeting the proteasome pathway can also lead to new treatments for disorders like cancer, muscular dystrophies, inflammation and immune diseases. This is already true for cancer; the FDA approved bortezomib, a potent proteasome inhibitor, for treating multiple myeloma in 2003, and mantle cell lymphoma in 2006. The chemical structures identified in some of the early proteasome inhibitors have led to the development of new anti-cancer drugs (CEP-18770, Carfilzomib, NPI-0052). All these molecules are covalent bonding inhibitors that react with the catalytic Thr1-O of the three types of active site. This review covers recent developments in medicinal chemistry of natural and synthetic proteasome inhibitors. Advances in non-covalent inhibitors that have no reactive group will be highlighted as they should minimize side-effects. New structures and new modes of action have been recently identified that open the door to new drug candidates for treating a range of diseases.

Domaines

Chimie organique
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Dates et versions

hal-00807658 , version 1 (04-04-2013)

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Emilie Génin, Michèle Reboud-Ravaux, Joëlle Vidal. Proteasome inhibitors: recent advances and new perspectives in medicinal chemistry. Current Topics in Medicinal Chemistry, 2010, 10 (3), pp.232-256. ⟨10.2174/156802610790725515⟩. ⟨hal-00807658⟩
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