title: A template-based approach to inhibitors of calpain 2, 20S proteasome, and HIV-1 protease.
abstract: Specificity counts: A template-based approach to protease inhibitors is presented using a core macrocycle that presents a generic β-strand template for binding to protease active sites. This is then specifically functionalized at P2 , and the C and N termini to give inhibitors of calpain 2, 20S proteasome, and HIV-1 protease.
authors.affiliation: School Chemistry and Physics, The University of Adelaide, Adelaide, SA 5005 (Australia).
authors.forename: Seth A
authors.initials: SA
authors.lastname: Jones
authors.forename: Paul M
authors.initials: PM
authors.lastname: Neilsen
authors.forename: Limei
authors.initials: L
authors.lastname: Siew
authors.forename: David F
authors.initials: DF
authors.lastname: Callen
authors.forename: Nathan E
authors.initials: NE
authors.lastname: Goldfarb
authors.forename: Ben M
authors.initials: BM
authors.lastname: Dunn
authors.forename: Andrew D
authors.initials: AD
authors.lastname: Abell
mesh_terms: D002154:Calpain / Q000037:antagonists & inhibitors* / Q000378:metabolism; D020134:Catalytic Domain; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D045325:HCT116 Cells; D016333:HIV Protease / Q000737:chemistry* / Q000378:metabolism; D006801:Humans; D047028:Macrocyclic Compounds / Q000737:chemistry* / Q000378:metabolism / Q000633:toxicity; D057786:Peptidomimetics; D011480:Protease Inhibitors / Q000737:chemistry* / Q000378:metabolism / Q000633:toxicity; D046988:Proteasome Endopeptidase Complex / Q000737:chemistry* / Q000378:metabolism; D011485:Protein Binding; D017433:Protein Structure, Secondary
chemical_list: D047028:Macrocyclic Compounds; D057786:Peptidomimetics; D011480:Protease Inhibitors; D002154:Calpain; D016333:HIV Protease; C514803:p16 protease, Human immunodeficiency virus 1; D046988:Proteasome Endopeptidase Complex
keywords: inhibitors; peptidomimetics; proteases; templates; β-strands