Table 2. Affinities for Interactions between LSD1 and Linear Monosubstituted Analogues of H31-11 (4) Determined by an SPR Biosensor Assay.
N | sequencea | Xb | KD (μM) |
---|---|---|---|
4 | ARTMQ TARKS T-OH | 140 | |
9 | ARTKQ TARKS T-NH2 | >100 | |
11 | PRTMQ TARKS T-NH2 | 10 | |
12 | XRTMQ TARKS T-NH2 | Tle | nic |
13 | AXTMQ TARKS T-NH2 | Cit | ni |
14 | ARTMQ TAXKS T-NH2 | Cit | ni |
15 | ARTXQ TARKS T-NH2 | Nle | >200 |
16 | ARTXQ TARKS T-NH2 | Aoc | >200 |
17 | ARTXQ TARKS T-NH2 | homo-Phe | >200 |
All peptides had a N-terminal amine.
Substitutions at X: Tle: l-tert-leucine, Cit: citrulline, Nle: norleucine, Aoc: 2-S-amino octanoic acid, homo-Phe: l-homophenylalanine.
ni: no interaction observed.