PH-002

An inhibitor of ApoE4 domain interactions

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Background

PH-002 is an inhibitor of the interaction between the amino- and carboxy-terminal domains of apolipoprotein E4 (ApoE4; IC₅₀ = 116 nM in a FRET reporter assay for domain interaction).^1,2 It restores intracellular trafficking of ApoE4 to the endoplasmic reticulum and Golgi apparatus in Neuro-2a cells expressing EGFP-ApoE4 or EGFP-ApoE4-R61T, a mutation that impairs ApoE4 domain interactions, when used at a concentration of 100 nM. PH-002 also prevents impairments in neurite outgrowth and dendritic spine development induced by expression of ApoE4 in Neuro-2a cells. It restores levels of mitochondrial complex IV subunit 1 in Neuro-2a cells expressing ApoE4 (EC₅₀ = 39 nM) and increases mitochondrial motility in PC12 cells expressing ApoE4 (EC₅₀ = <1 nM).¹

1.Chen, H.-K., Liu, Z., Meyer-Franke, A., et al.Small molecule structure correctors abolish detrimental effects of apolipoprotein E4 in cultured neuronsJ. Biol. Chem.287(8)5253-5266(2012) 2.Brodbeck, J., McGuire, J., Liu, Z., et al.Structure-dependent impairment of intracellular apolipoprotein E4 trafficking and its detrimental effects are rescued by small-molecule structure correctorsJ. Biol. Chem.286(19)17217-17226(2011)

Protocol

Cell experiment:

Neuro-2a cells stably expressing apoE3 or apoE4 are seeded at 7500-8000 cells/well on PLlysine-coated 24-well plates containing Opti-MEM with either 0.03% DMSO (control) or DMSO plus compound PH-002 (100 nM)[1].

参考文献:

[1]. Brodbeck J, et al. Structure-dependent impairment of intracellular apolipoprotein E4 trafficking and its detrimental effects are rescued by small-molecule structure correctors. J Biol Chem. 2011 May 13;286(19):17217-26.
[2]. Chen HK, et al. Small molecule structure correctors abolish detrimental effects of apolipoprotein E4 in cultured neurons. J Biol Chem. 2012 Feb 17;287(8):5253-66.