Table 1 Sequences of peptides synthesised after the first selection, and the rationally designed PADI4_3_H4(2)

From: Discovering covalent cyclic peptide inhibitors of peptidyl arginine deiminase 4 (PADI4) using mRNA-display with a genetically encoded electrophilic warhead

Peptide Name

Sequence

IC50 Values (µΜ)

  

0 h preincubation

1 h preincubation

cP4_2

yIWGL(2)D(2)SCG

>50

0.87 ± 0.06

cP4_4

ySKYD(2)RSPRDCG

4.4 ± 0.07

0.070 ± 0.004

cP4_7

yVYS(2)KEWKYCG

8.0 ± 1.2

0.16 ± 0.02

cP4_10

yWY(2)NWDFNKRCG

3.1 ± 0.01

0.093 ± 0.002

cP4_15

yLD(2)HYSSKLYCG

1.6 ± 0.03

0.052 ± 0.002

cP4_165

yVY(2)DCEWINRAG

11.8 ± 4.9

0.17 ± 0.01

PADI4_3_H4(2)

yRD(2)HYRHPKYCG

2.0 ± 0.01

0.065 ± 0.007

  1. Where (2) is the FAO warhead and y is chloroacetyl-D-tyrosine which is cyclised with the cysteine residue in each peptide. Their corresponding IC50 values from COLDER assay with or without 1 h preincubation of peptide and PADI4 are also shown. Data shows mean ± SEM of two independent replicates.
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