Table 3.
entry | peptidea | AA’sb | DMPC dissolnc | chol effluxd | mouse antiatheroe |
---|---|---|---|---|---|
1 | DWLKAFYDKVAEKLKEAF-P- DWLKAFYDKVAEKLKEAF (37pA) | 37 | 55%f | 440g; +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 | 3400j; +h | |
9 | DWAKAAYDKAAEKAKEAA -P- DWAKAAYDKAAEKAKEAA (10A) | 37 | 14%f | −h | |
10 | Ac-DWFKAFYDKVAEKFKEAF-P- DWFKAFYDKVAEKFKEAF-NH2k (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-NH2o (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).
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.
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).