KAT6A–inhibitor co-crystal structures: tackling a challenging crystallization target via two alternative approaches

Puetter, V.; Bouché, L.; Nowak-Reppel, K.; Ferrara, S.J.; Gradl, S.N.; Korr, D.; Strathdee, C.A.; ter Laak, A.; Hillig, R.C.

doi:10.1107/S2059798326008545

Figure 1
Selected examples of KAT6A/B inhibitors discussed in this study. IC₅₀ values listed here are for inhibition of KAT6A, but due to the high similarity within the inhibitor-binding site, all of these inhibitors also inhibit KAT6B. IC₅₀ values for WM-8014 are from Baell et al. (2018

), that for the 1,2,4-thiadiazine Example 41 is from Morrow et al. (2018

) (this compound is also called compound 27n in Suwandi et al., 2026

), the K_i value for PF-07248144/Prifetrastat is from Bozikis et al. (2019

), the IC₅₀ value for BAY-184 is from ter Laak et al. (2024

) and those for compound 1 and compound 2 are from this study.

STRUCTURAL
BIOLOGY

ISSN: 2059-7983

Volume 82| Part 9| September 2026| Pages 1111-1124

https://doi.org/10.1107/S2059798326008545

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