The chemical properties of alicyclic heterocycles are similar to those of the corresponding chain compounds. Compound: 1-Boc-4-(Aminomethyl)piperidine, is researched, Molecular C11H22N2O2, CAS is 144222-22-0, about Discovery, Structure-Activity Relationship, and Biological Activity of Histone-Competitive Inhibitors of Histone Acetyltransferases P300/CBP, the main research direction is histone competitive inhibitor histone acetyltransferase discovery SAR anticancer.Quality Control of 1-Boc-4-(Aminomethyl)piperidine.
Histone acetyltransferase (HAT) p300 and its paralog CBP acetylate histone lysine side chains and play critical roles in regulating gene transcription. The HAT domain of p300/CBP is a potential drug target for cancer. Through compound screening and medicinal chem., novel inhibitors of p300/CBP HAT with their IC50 values as low as 620 nM were discovered. The most potent inhibitor is competitive against histone substrates and exhibits a high selectivity for p300/CBP. It inhibited cellular acetylation and had strong activity with EC50 of 1-3μM against proliferation of several tumor cell lines. Gene expression profiling in estrogen receptor (ER)-pos. breast cancer MCF-7 cells showed that inhibitor treatment recapitulated siRNA-mediated p300 knockdown, inhibited ER-mediated gene transcription, and suppressed expression of numerous cancer-related gene signatures. These results demonstrate that the inhibitor is not only a useful probe for biol. studies of p300/CBP HAT but also a pharmacol. lead for further drug development targeting cancer.
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Reference:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem