The three-dimensional configuration of the ester heterocycle is basically the same as that of the carbocycle. Compound: 1-Boc-4-(Aminomethyl)piperidine(SMILESS: NCC1CCN(C(OC(C)(C)C)=O)CC1,cas:144222-22-0) is researched.Application In Synthesis of 2,3-Dibromopropionic acid. The article 《Small-molecule inhibitor of AF9/ENL-DOT1L/AF4/AFF4 interactions suppresses malignant gene expression and tumor growth》 in relation to this compound, is published in Theranostics. Let’s take a look at the latest research on this compound (cas:144222-22-0).
Chromosome translocations involving mixed lineage leukemia (MLL) gene cause acute leukemia with a poor prognosis. MLL is frequently fused with transcription cofactors AF4 (~35%), AF9 (25%) or its paralog ENL (10%). The AHD domain of AF9/ENL binds to AF4, its paralog AFF4, or histone-H3 lysine-79 (H3K79) methyltransferase DOT1L. Formation of AF9/ENL/AF4/AFF4-containing super elongation complexes (SEC) and the catalytic activity of DOT1L are essential for MLL-rearranged leukemia. Protein-protein interactions (PPI) between AF9/ENL and DOT1L/AF4/AFF4 are therefore a potential drug target. Compound I was identified to be a novel small-mol. inhibitor of the AF9/ENL-DOT1L/ AF4/AFF4 interaction with IC50s of 0.9-3.5μM. Pharmacol. inhibition of the PPIs significantly reduced SEC and DOT1L-mediated H3K79 methylation in the leukemia cells. Gene profiling shows compound I significantly suppressed the gene signatures related to onco-MLL, DOT1L, HoxA9 and Myc. It selectively inhibited proliferation of onco-MLL- or Myc-driven cancer cells and induced cell differentiation and apoptosis. Compound I exhibited strong antitumor activity in a mouse model of MLL-rearranged leukemia. The AF9/ENL-DOT1L/AF4/AFF4 interactions are validated to be an anticancer target and compound I is a useful in vivo probe for biol. studies as well as a pharmacol. lead for further drug development.
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Reference:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem