Generation of potent and selective kinase inhibitors by combinatorial biosynthesis of glycosylated indolocarbazoles.
We report the generation of novel glycosylated indolocarbazoles by combinatorial biosynthesis, and the identification of two novel potent and selective compounds inhibitors of JAK2 and Ikkb kinases.
Sánchez
César
C
Department Biología Funcional & Instituto Universitario de Oncología del Principado de Asturias (IUOPA), Universidad de Oviedo, 33006 Oviedo, Spain.
Salas
Aaroa P
AP
Braña
Alfredo F
AF
Palomino
Martina
M
Pineda-Lucena
Antonio
A
Carbajo
Rodrigo J
RJ
Méndez
Carmen
C
Moris
Francisco
F
Salas
José A
JA
D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology; D002227:Carbazoles / Q000737:chemistry* / Q000494:pharmacology; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D020650:Combinatorial Chemistry Techniques / Q000379:methods*; D006801:Humans; D026121:Indole Alkaloids / Q000737:chemistry* / Q000494:pharmacology; D015394:Molecular Structure; D005810:Multigene Family; D010957:Plasmids; D047428:Protein Kinase Inhibitors / Q000737:chemistry* / Q000494:pharmacology; D019311:Staurosporine / Q000031:analogs & derivatives / Q000096:biosynthesis / Q000737:chemistry / Q000494:pharmacology; D013302:Streptomyces / Q000201:enzymology / Q000235:genetics*
D000970:Antineoplastic Agents; D002227:Carbazoles; D026121:Indole Alkaloids; D047428:Protein Kinase Inhibitors; C089657:arcyriaflavin A; C053339:rebeccamycin; D019311:Staurosporine