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Leupeptazin, a highly modified tripeptide isolated from cultures of a Streptomyces sp. inhibits cathepsin K.
Kruglyak, Natasha; Williams, David E; Chen, Henry; Law, Simon; Kaleta, Jadwiga; Villanueva, Ivan; Davies, Julian E; Andersen, Raymond J; Brömme, Dieter.
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  • Kruglyak N; Department of Biochemistry and Molecular Biology, University of British Columbia, 2350 Health Sciences Mall, Vancouver, British Columbia V6T 1Z3, Canada; Present address: Department of Biochemistry, University of Toronto, 101 College St, TMDT 5-401, Toronto, Ontario M5G 1L7, Canada. Electronic addre
  • Williams DE; Departments of Chemistry and Earth, Ocean & Atmospheric Sciences, University of British Columbia, 2207 Main Mall, Vancouver, British Columbia V6T 1Z4, Canada.
  • Chen H; Department of Biochemistry and Molecular Biology, University of British Columbia, 2350 Health Sciences Mall, Vancouver, British Columbia V6T 1Z3, Canada.
  • Law S; Department of Biochemistry and Molecular Biology, University of British Columbia, 2350 Health Sciences Mall, Vancouver, British Columbia V6T 1Z3, Canada.
  • Kaleta J; Department of Oral, Biological and Medical Sciences, University of British Columbia, 2151 Westbrook Mall, Vancouver, British Columbia V6T 1Z3, Canada.
  • Villanueva I; Department of Microbiology and Immunology, University of British Columbia, 2350 Health Sciences Mall, Vancouver, British Columbia V6T 1Z3, Canada.
  • Davies JE; Department of Microbiology and Immunology, University of British Columbia, 2350 Health Sciences Mall, Vancouver, British Columbia V6T 1Z3, Canada.
  • Andersen RJ; Departments of Chemistry and Earth, Ocean & Atmospheric Sciences, University of British Columbia, 2207 Main Mall, Vancouver, British Columbia V6T 1Z4, Canada.
  • Brömme D; Department of Biochemistry and Molecular Biology, University of British Columbia, 2350 Health Sciences Mall, Vancouver, British Columbia V6T 1Z3, Canada; Department of Oral, Biological and Medical Sciences, University of British Columbia, 2151 Westbrook Mall, Vancouver, British Columbia V6T 1Z3, Can
Bioorg Med Chem Lett ; 27(6): 1397-1400, 2017 03 15.
Article en En | MEDLINE | ID: mdl-28228366
Using a human cathepsin K-targeting inhibitor screen, a new leupeptin analogue, leupeptazin (1), containing an unprecedented piperidinotriazine moiety, was isolated from a liquid culture of soil Streptomyces sp. IS2-4 collected in northern Italy. The structure of leupeptazin was established using HRESIMS as well as 1D and 2D NMR data. The inhibitory activity of the compound towards the collagenase cathepsin K was tested in vitro to reveal moderate activity with an inhibition constant, Ki, of 44µM.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Oligopéptidos / Streptomyces / Catepsina K Límite: Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2017 Tipo del documento: Article Pais de publicación: Reino Unido
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Oligopéptidos / Streptomyces / Catepsina K Límite: Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2017 Tipo del documento: Article Pais de publicación: Reino Unido