Table 1. Apolipoprotein A-I mimetic peptides.

Peptide	In vitro effects		Peptide-lipoprotein association and vascular effects	Effect on atherosclerosisa	Study
	Cellular cholesterol efflux	Monocyte chemotactic assay
Monomeric apoA-I class A mimetic peptides
2F Ac18ANH2	No effect	b Weak	Associates with plasma HDL and free protein	No effect	Navab et al. [8]
					Mendez et al. [35]
					Garber et al. [36]
3F-2	N/A	b	Associates with HDL > VLDL > IDL/LDL; binds oxPL at higher affinity than apoA-I	↓ AR lesion in 10-wk apoE-/- mice treated for 6 wk with peptide	Navab et al. [8]
					Handattu et al. [37]
					Van Lenten et al. [22]
3F14	N/A	No effect	Associates with VLDL/IDL/LDL > HDL; binds oxPL with similar affinity as apoA-I	No effect, AR lesion in 10-wkold apoE-/- mice treated for 6 wk with peptide	Navab et al. [8]
					Handattu et al. [37]
					Van Lenten et al.[23••]
4F	b Similar to level of effect of L2F, D2F, or 37pA	b ↓ LOOH in lipoproteins, but ↑ in pre-β HDL	No effect on plasma lipids levels	↓ AR lesion in apoE-/- and LDLR-/- mice	Navab et al. [10]
			↓ Plasma TC 40% by oral D4F but not IP D4F	No effect AR lesion in 20-wk apoE-/- mice fed Western diet (oral or IP D4F)	Li et al. [14]
			↓ Proinflammatory HDL (apoA-I dependent)	N/A	Ou et al. [12]
			↓ apoA-I-associated MPO
			↑ Vasodilatation in LDLR-/- mice on HFD		Ou et al. [30]
		↓ LDL oxidation	Associates with late HDL and late LDL	N/A	Wool et al. [13]
		D and L 4F bind oxPL with much higher affinity than apoA-I	↓ SAA levels (subcutaneous D4F/L4F)	↓ en face aortic lesion in cholesterol-fed NZW rabbits	Van Lenten et al. [11]
			↑ Plasma TG 4–8×, ↓ plasma TC 25%
			N/A	↓ AR apoE-/- mice (oral L4F with niclosamide and pravastatin for 26 wk)	Navab et al. [16••]
			N/A	Dose-dependent ↓ AR in apoE-/- mice (oral D4F)	Navab et al. [15]
			↑ In vivo RCT in apoE-/- mice	N/A	Navab et al. [24]
5F	N/A	b	Associates with plasma HDL and VLDL ↓ HDL 26%	↓ AR lesion 56% in C57BL/6 on cholate diet treated with peptide for 16 wk IP	Navab et al. [8]
					Garber et al. [22]
Tandem apoA-I mimetic peptides
37pA	b	N/A	Associates with plasma HDL and free protein	N/A	Mendez et al. [35]
					Garber et al. [36]
4F-IHS-4F	b	N/A	N/A	N/A	Wool et al. [31•]
4F-Ala-4F	b	N/A	Increases LDL oxidation	N/A	Wool et al. [31•]
4F-Pro-4F	b	N/A	Binds HDL specifically, as compared to L4F	N/A	Wool et al. [31•]

^aAnalyzed in female mice unless noted

^bPromotes cholesterol efflux or is anti-inflammatory in the monocyte chemotaxis assay

ApoA-I apolipoprotein A-I, AR aortic root, HDL high-density lipoprotein, HFD high-fat diet, IDL intermediate-density lipoprotein, IP intraperitoneal, LDL low-density lipoprotein, LDLR-/- low-density lipoprotein receptor deficient, LOOH lipid hydroperoxide, MPO myeloperoxidase, N/A not available, NZW New Zealand white, oxPL oxidized phospholipid, RCT reverse cholesterol transport, SAA serum amyloid A, TC total cholesterol, TG triglyceride, VLDL very low-density lipoprotein