Homoharringtonine
Protein synthesis inhibitor / A plant alkaloid, originally isolated from the Hainan plum yew, that binds to the large ribosomal subunit A-site, competing with aminoacyl-tRNA amino acid side chains, thereby inhibiting the initial elongation step of protein synthesis.1 It also binds to transcription factors NKRF (NF-κB repressing factor) and SP1, down-regulating the Myc pathway.2,3 Dramatically decreases global DNA 5-hydroxymethylcytosine levels via the SP1/TET1 axis.3 Induces apoptosis in tyrosine kinase inhibitor-resistant NSCLC cells4, and is a clinically useful agent for CML and AML5.
Biochemicals & reagents
26833-87-4
HHT; NSC141633; Omacetaxine mepesuccinate
1 Gürel et al. (2009), U2504 determines the species specificity of the A-site cleft antibiotics: the structures of tiamulin, homoharringtonine, and bruceantin bound to the ribosome; J.Mol.Biol. 389 146 2 Chen (2019), Homoharringtonine deregulates MYC transcriptional expression by directly binding NF-κB repressing factor; Proc. Natl. Acad. Sci. USA. 116 2220 3 Li et al. (2020), Homoharringtonine exhibits potent anti-tumor effect and modulates DNA epigenome in acute myeloid leukemia by targeting SP1/TET1/5hmC; Haematologica 105 148 4 Cao et al. (2015), Homoharringtonine induces apoptosis and inhibits STAT3 via IL-6/JAK1/STAT3 signal pathway in Gefitinib-resistant lung cancer cells; Sci. Rep. 5 8477 5 Lu and Wang (2014), Homoharringtonine and omacetaxine for myeloid hematological malignancies; J. Hematol. Oncol. 7 2
-20°C
TARGET: Ribosome; Antibiotic; DNA -- PATHWAY: NFkappaB; Myc; Cell cycle; Apoptosis inducer; Protein synthesis; Transcription -- RESEARCH AREA: Cell death; Epigenetics -- DISEASE AREA: Infectious disease; Cancer