title: Targeting the transcription factor Myb by small-molecule inhibitors.
abstract: The transcription factor Myb is a key regulator of hematopoietic cell proliferation, differentiation, and survival and has been implicated in the development of leukemia and several other human cancers. Pharmacological inhibition of Myb is therefore emerging as a potential therapeutic strategy. Recently, the first low-molecular-weight compounds that show Myb inhibitory activity have been identified. Characterization of these compounds suggests disruption of the protein-protein-interaction of Myb and the coactivator p300 as a suitable strategy to inhibit Myb.
authors.affiliation: Institute of Oncology Research, Bellinzona, Switzerland.
authors.forename: Sagar
authors.initials: S
authors.lastname: Uttarkar
authors.affiliation: Institute of Cancer and Genomic Sciences, College of Medical and Dental Sciences, University of Birmingham, Edgbaston, Birmingham, United Kingdom.
authors.forename: Jon
authors.initials: J
authors.lastname: Frampton
authors.affiliation: Institute for Biochemistry, Westfälische-Wilhelms-Universität, Münster, Germany. Electronic address: klempna@uni-muenster.de.
authors.forename: Karl-Heinz
authors.initials: KH
authors.lastname: Klempnauer
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D015973:Gene Expression Regulation, Leukemic / Q000187:drug effects; D006801:Humans; D007938:Leukemia / Q000188:drug therapy / Q000209:etiology / Q000378:metabolism; D058990:Molecular Targeted Therapy; D011485:Protein Binding; D020598:Proto-Oncogene Proteins c-myb / Q000037:antagonists & inhibitors* / Q000737:chemistry / Q000235:genetics / Q000378:metabolism; D015398:Signal Transduction / Q000187:drug effects; D014157:Transcription Factors / Q000037:antagonists & inhibitors* / Q000737:chemistry / Q000235:genetics / Q000378:metabolism; D015533:Transcriptional Activation
chemical_list: D000970:Antineoplastic Agents; D020598:Proto-Oncogene Proteins c-myb; D014157:Transcription Factors