Generation of potent and selective kinase inhibitors by combinatorial biosynthesis of glycosylated indolocarbazoles

César Sánchez; Aaroa P Salas; Alfredo F Braña; Martina Palomino; Antonio Pineda-Lucena; Rodrigo J Carbajo; Carmen Méndez; Francisco Moris; José A Salas

doi:10.1039/b905068j

Generation of potent and selective kinase inhibitors by combinatorial biosynthesis of glycosylated indolocarbazoles

Chem Commun (Camb). 2009 Jul 21:(27):4118-20. doi: 10.1039/b905068j. Epub 2009 May 27.

Authors

César Sánchez¹, Aaroa P Salas, Alfredo F Braña, Martina Palomino, Antonio Pineda-Lucena, Rodrigo J Carbajo, Carmen Méndez, Francisco Moris, José A Salas

Affiliation

¹ Department Biología Funcional & Instituto Universitario de Oncología del Principado de Asturias (IUOPA), Universidad de Oviedo, 33006 Oviedo, Spain.

PMID: 19568652
DOI: 10.1039/b905068j

Abstract

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.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Antineoplastic Agents / chemistry*
Antineoplastic Agents / pharmacology
Carbazoles / chemistry*
Carbazoles / pharmacology
Cell Line, Tumor
Cell Proliferation / drug effects
Combinatorial Chemistry Techniques / methods*
Humans
Indole Alkaloids / chemistry*
Indole Alkaloids / pharmacology
Molecular Structure
Multigene Family
Plasmids
Protein Kinase Inhibitors / chemistry*
Protein Kinase Inhibitors / pharmacology
Staurosporine / analogs & derivatives
Staurosporine / biosynthesis
Staurosporine / chemistry
Staurosporine / pharmacology
Streptomyces / enzymology
Streptomyces / genetics*

Substances

Antineoplastic Agents
Carbazoles
Indole Alkaloids
Protein Kinase Inhibitors
arcyriaflavin A
rebeccamycin
Staurosporine