title: Macrocyclic proteasome inhibitors.
abstract: Proteasome inhibitors have proven to be effective anticancer agents. Despite the success of the first on the market proteasome inhibitor bortezomib in chemotherapy, alternative clinically useful proteasome inhibitors are still urgently needed as bortezomib therapy causes severe side effects and is limited by arising drug resistance. Experience from previous proteasome inhibitor studies has thereby demonstrated that the identification of proteasome inhibitor structures with suitable pharmacological properties is a key factor for a successful development of clinically useful proteasome inhibitors. Macrocycles often show distinct and in comparison to linear small molecules superior pharmacological properties. Consequently, macrocyclic proteasome inhibitors might represent promising small molecules for drug development. Here, we want to highlight the current state of the art of macrocyclic proteasome inhibitor research. To this end, we give an overview and critically discuss currently known classes of macrocyclic proteasome inhibitors.
authors: Zentrum für Medizinische Biotechnologie, Fakultät Biologie, Universität Duisburg-Essen, Universitätsstr. 2, 45117 Essen, Germany.
authors: D
authors: D
authors: Krahn
authors: C
authors: C
authors: Ottmann
authors: M
authors: M
authors: Kaiser
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry* / Q000627:therapeutic use; D001897:Boronic Acids / Q000737:chemistry / Q000627:therapeutic use; D000069286:Bortezomib; D015195:Drug Design; D006801:Humans; D047028:Macrocyclic Compounds / Q000737:chemistry* / Q000627:therapeutic use; D009369:Neoplasms / Q000188:drug therapy; D011480:Protease Inhibitors / Q000737:chemistry* / Q000627:therapeutic use; D046988:Proteasome Endopeptidase Complex / Q000378:metabolism; D061988:Proteasome Inhibitors; D011719:Pyrazines / Q000737:chemistry / Q000627:therapeutic use
chemical_list: D000970:Antineoplastic Agents; D001897:Boronic Acids; D047028:Macrocyclic Compounds; D011480:Protease Inhibitors; D061988:Proteasome Inhibitors; D011719:Pyrazines; D000069286:Bortezomib; D046988:Proteasome Endopeptidase Complex