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AI-10-49
AI-10-49 is a small molecule inhibitor of leukemic oncoprotein CBFβ-SMHHC developed by the laboratory of John Bushweller (University of Virginia) with efficacy demonstrated by the laboratories of Lucio H. Castilla (University of Massachusetts Medical School) and Monica Guzman (Cornell University).〔Science. 2015 Feb 13;347(6223):779-84〕〔Science. 2015 Feb 13;347(6223):713-4〕〔Nat Chem Biol. 2015 Mar 18;11(4):241〕〔http://www.bloodjournal.org/content/124/21/390?sso-checked=true〕 AI-10-49 allosterically binds to CBFβ-SMMHC and disrupts protein-protein interaction between CBFβ-SMMHC and tumor suppressor RUNX1. This inhibitor is under development as an anti-leukemic drug.
== Core binding factors ==
Core-binding factor (CBF) is a heterodimeric transcription factor composed by the CBFβ and RUNX subunits (the latter is encoded by RUNX1, RUNX2, or RUNX3 genes). CBF plays critical roles in most hematopoietic lineages, regulating gene expression of a variety of genes associated with cell cycle, differentiation, signaling and adhesion.〔Nat Rev Cancer. 2005 May;5(5):376-87〕 In hematopoiesis, CBF regulates progenitor cell fate decisions and differentiation at multiple levels. The function of CBF is essential for the emergence of embryonic hematopoietic stem cells (HSCs) and establishment of definitive hematopoiesis at midgestation.〔Cell. 1996 Jan 26;84(2):321-30.〕〔Proc Natl Acad Sci U S A. 1996 Apr 16;93(8):3444-9.〕〔Cell. 1996 Nov 15;87(4):697-708〕〔EMBO J. 2000 Jun 1;19(11):2465-74.〕〔Nature. 2009 Feb 12;457(7231):887-91〕 Similarly, in adult hematopoiesis, CBF regulates the frequency and differentiation of HSCs, lymphoid and myeloid progenitors,〔Nat Med. 2004 Mar;10(3):299-304〕〔Blood. 2005 Jul 15;106(2):494-504〕 establishing CBF as an master regulator of hematopoietic homeostasis.
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