. Author manuscript; available in PMC: 2015 Mar 27.

Published in final edited form as: J Med Chem. 2013 Oct 29;57(6):2169–2196. doi: 10.1021/jm4005847

Table 3.

ApoA-I Mimetic Peptides: Multiple Helices

entry	peptide^a	AA’s^b	DMPC dissoln^c	chol efflux^d	mouse antiathero^e
1	DWLKAFYDKVAEKLKEAF-P- DWLKAFYDKVAEKLKEAF (37pA)	37	55%^f	440^g; +^h,ⁱ
2	DWLKAFYDKVAEKLKEAF-A- DWLKAFYDKVAEKLKEAF (37aA)	37	+ⁱ
3	DWLKAFYDKVAEKLKEAF- DWLKAFYDKVAEKLKEAF (36A)	36
4	DWLKAFYDKVAEKLKEAF-P- DWLKAFYDKVAEKAKEAF (1A)	37	75%^f	+^h
5	DWLKAFYDKVAEKLKEAF-P- DWLKAFYDKVAEKAKEAA (2A)	37	65%^f	+^h
6	DWLKAFYDKVAEKLKEAF-P- DWFKAFYDKAAEKAKEAA (3A)	37	70%^f	+^h
7	DWLKAFYDKVAEKLKEAF-P- DWFKAAYDKAAEKAKEAA (4A)	37	70%^f	+^h
8	DWLKAFYDKVAEKLKEAF-P- DWAKAAYDKAAEKAKEAA (5A)	37	80%^f	3400^j; +^h
9	DWAKAAYDKAAEKAKEAA -P- DWAKAAYDKAAEKAKEAA (10A)	37	14%^f	−^h
10	Ac-DWFKAFYDKVAEKFKEAF-P- DWFKAFYDKVAEKFKEAF-NH₂^k (4F-P-4F)	37	60%^l	+^l	0%^m
11	Ac-DWFKAFYDKVAEKFKEAF-A- DWFKAFYDKVAEKFKEAF-NH₂ⁿ (4F-A-4F)	37	0%^l
12	Ac-DWFKAFYDKVAEKFKEAF-KVEPLRA- DWFKAFYDKVAEKFKEAF-NH₂^o (4F-IHS-4F)	43	66%^l	+^l

Interhelix linkers: -P-, -A-, -KVEPLRA-. For entries 4–9, italicized A’s are for clarity in comparison.

Number of amino acids.

Dissolution of DMPC; reported as percent decrease in turbidity, from relative absorbance or optical density, at 30 min (0% at t = 0), unless otherwise noted.

Efflux of cholesterol from cholesterol-laden mouse macrophages (EC₅₀ values in nM units; apoA-I = 53 nM in ref 88; 100 nM in ref 98), unless otherwise noted. A plus sign (+) signifies activity, but without quantification (ref 101, ²²⁹).

Inhibition of atherosclerotic lesion formation in mice fed a high-fat diet, reported as percent reduction of mean aortic lesion area relative to vehicle baseline, unless otherwise noted.

Ref 102.

Ref 88.

Efflux of cholesterol from ABCA1-transfected HeLa cells. A positive sign (+) signifies activity, but without quantification; a negative sign (−) signifies inactivity (ref 102).

ⁱ

Ref ²²⁹.

Ref 98.

Tandem dimer of 4F linked by Pro (ref 101).

Ref 101. Clarification of turbidity of a DMPC suspension as measured by light scattering (value for 4F in this work was 90%).

Ref ²³⁰. Inhibition of arterial atherosclerotic lesion size in chow-fed, 20-week-old, apoE-null mice after 8 weeks of i.p. administration (100 μg) every other day.

ⁿ

Tandem dimer of 4F linked by Ala (ref 101).

Tandem dimer of 4F linked by KVEPLRA, the 7-amino acid, interhelical segment between helices 4 and 5 of human apoA-I (“HIS”) (ref 101).