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. 2021 Oct 27;11:21179. doi: 10.1038/s41598-021-00654-3

Table 2.

Summary of potency profiles of all PYY analogues lipidated from the N-terminal to position 32. In all analogues the fatty diacid (FA) moiety C18 diacid-γGlu-2xAdo was attached to the side chain of a lysine residue (analogues 2-30 and 52) or to the N-terminus (peptide 1). pEC50 is calculated as the mean of at least three independent experiments, and the 95% confidence interval (CI) is given as [lower; upper]. The mean EC50 in nM is calculated from the mean pEC50. For analogue 9 and 20 (data marked with *) two independent experiments were recorded.

No FA Y2 receptor Y1 receptor Y4 receptor
Position EC50 (nM) pEC50 [95% CI] EC50 (nM) pEC50 [95% CI] EC50 (nM) pEC50 [95% CI]
PYY3-36 none 0.60 9.2 [9.2:9.1] 7.9 8.1 [8.2:7.9] 320 6.5 [6.7;6.4]
1 10 8.0 [8.3;7.8] 25 7.6 [7.9;7.3] 250 6.6 [6.6;6.5]
2 4 25 7.6 [8.1;7.6] 200 6.7 [7.0;6.7] 630 6.2 [6.5;6.4]
3 5 25 7.6 [7.8;7.4] 100 7.0 [7.3;6.7] 400 6.4 [6.5;6.2]
4 6 7.9 8.1 [8.3;7.9] 50 7.3 [7.5;7.1] 320 6.5 [6.7;6.3]
5 7 2.0 8.7 [9.0;8.3] 63 7.2 [7.2;7.1] 250 6.6 [7.3;5.9]
6 8 40 7.4 [7.6;7.2] 250 6.6 [7.0;6.3] 790 6.1 [6.2;5.9]
7 9 13 7.9 [8.2;7.6] 200 6.7 [6.9;6.5] 630 6.2 [6.4;6.1]
8 10 1.3 8.9 [9.3;8.6] 50 7.3 [7.6;7.0] 500 6.3 [6.6;6.0]
9 11 5.0 8.3 [8.6;8.1] 50* 7.3*[-.-;-.-*] > 1000 <6.0
10 12 16 7.8 [7.8;7.7] 200 6.7 [6.8;6.5] 500 6.3 [6.4;6.1]
11 13 32 7.5 [7.8;7.2] 320 6.5 [6.7;6.4] 500 6.3 [6.5;6.0]
12 14 4.0 8.4 [8.8;9.9] 63 7.2 [7.5;6.8] 1000 6.0 [6.2;5.9]
13 15 10 8.0 [8.3;7.8] 63 7.2 [7.3;7.1] 1000 6.0 [6.1;6.0]
14 16 20 7.7 [8.2;7.3] 160 6.8 [7.3;6.2] > 1000 6.0
15 17 5.0 8.3 [8.9;7.6] 100 7.0 [7.5;6.5] 500 6.3 [7.1;5.5]
16 18 7.9 8.1 [8.3;7.9] 63 7.2 [7.5;7.0] 400 6.4 [6.6;6.1]
17 19 4.0 8.4 [8.8;8.0] 63 7.2 [7.4;7.0] 500 6.3 [7.1;5.6]
18 20 20 7.7 [8.0;7.4] 790 6.1 [6.2;6.0] > 1000 <6.0
19 21 4.0 8.4 [8.7;8.0] 130 6.9 [7.2;6.7] > 1000 <6.0
20 22 2.0* 8,7*[-.-;-.-*] 40 7.4 [7.4;7,3] 500* 6.3*[−.−; −.−*]
21 23 13 7.9 [8.4;7.5] 63 7.2 [7.4;7.0] 400 6.4 [6.5;6.3]
22 24 50 7.3 [7.6;7.0] 400 6.4 [6.6;6.3] 790 6.1 [6.4;5.8]
23 25 79 7.1 [8.0;6.1] 500 6.3 [6.9;5.7] 630 6.2 [6.6;5.7]
24 26 40 7.4 [7.5;7.3] 320 6.5 [6.5;6.4] 500 6.3 [6.6;6.0]
25 27 32 7.5 [8.0;6.9] 320 6.5 [6.8;6.2] 400 6.4 [6.6;6.3]
26 28 32 7.5 [7.7;7.3] 1000 6.0 [6.2;5.9] >1000 <6.0
27 29 500 6.3 [6.8;5.8] 500 6.3 [7.0;5.6] 790 6.1 [6.5;5.8]
28 30 5.0 8.3 [8.5;8.2] 630 6.2 [6.4;5.9] 79 7.1 [7.3;6.9]
29 31 79 7.1 [7.2;7.1] 320 6.5 [6.6;6.4] 630 6.2 [6.4;6.1]
30 32 50 7.3 [7.4;7.2] >1000 <6.0 >1000 <6.0
52 30 4.0 8.4 [8.6;8.3] 500 6.3 [6.5;6.0] 40 7.4 [7.4;7.3]