Table 1 Summary of published pseudokinase crystal structures

Abbreviations: P-PCP, β,γ-methyleneadenosine 5′-triphosphate; AMP-PN, AMP phosphoramidate. *Crystallized with surface mutations (W659A, W777A, F794H). †Inferred from biochemical data or close homology to published structures showing the nt-binding mode. ‡Can be made cation-dependent with four point mutations [83]. §Mutated as explained in [77]. Not identical with ROP2 sequence in 2W1Z.

Crystal structures
ProteinPDB IDSpeciesLigandComplexKd for ATPBinding modeOther
KSR22Y4IHomo sapiensATP + MgMEK1Unknown1 cationActive, phosphorylates MEK1 [4]
HER34OTWH. sapiensBosutinib10−6 M [5]1 cationActive, autophosphorylates its own intracellular region, when immobilized on vesicles [5]
4RIWH. sapiensAMP-PNP + MgEGFR KD (V624R, F973A, L977A)
4RIX (Q709R)H. sapiensAMP-PNP + MgEGFR KD (V624R, F973A, L977A)
4RIY (E909G)H. sapiensAMP-PNP + MgEGFR KD (V624R, F973A, L977A)
3KEXH. sapiensAMP-PNP + Mg
3LMGH. sapiensAMP-PNP + Mg
TYK2 JH23ZONH. sapiensIKK110−5 M [37]1 cationInactive [37]
4WOVH. sapiensBMS-066
4OLIH. sapiensInhibitor 7012JH2-JH1 (D1023N)
5C03H. sapiensATPγS + Mg
5C01H. sapiensPyrazine inhibitor
JAK2 JH24FVP*H. sapiens10−6 M [6,45]1 cationActive, autophosphorylates on S523 and Y570 [6]
4FVQ*H. sapiensATP + Mg
4FVR (V617F)*H. sapiensATP + Mg
JAK1 JH24L00H. sapiens10−6 M [45]1 cationInactive [65]
4L01 (V658F)H. sapiens
MLKL4BTFMus musculus10−5 M (TSA) [26]No cation [9,25,26]Inactive [25]
4MWIH. sapiens
4M67H. sapiens
4M68M. musculus
4M69M. musculusRIP3 KD
STRADα3GNIH. sapiensATPMO2510−4–10−6 M [39,82]No cation [9]Inactive [140]
2WTKH. sapiensAMP-PNPMO25 + LKB1
VRK32JIIH. sapiensNoneN/AInactive
ILK3KMWH. sapiensATP + Mgα-Parvin10−6 M [34]1 cationInactive [34,40]
3KMUH. sapiensα-Parvin
3REPH. sapiensATP + Mnα-Parvin
CASK3C0GH. sapiens3′-AMP10−3 M [7,9]No cationActive, cations inhibit binding and activity. [7,24,83]
3C0IH. sapiens3′-AMP
3C0HH. sapiensAMP-PNP (only AMP visible)
3TACH. sapiensLiprin-α2
3MFS (4M)H. sapiensAMP-PNP
3MFU (4M)H. sapiensAMP-PNP + Mn
3MFT (4M)H. sapiens
3MFR (4M)H. sapiens
ROR23ZZWH. sapiensNone [55]N/AInactive [55,102]
4GT4H. sapiens
BIR24L68Arabidopsis thalianaNone [94]N/AInactive [94]
BSK84I92A. thalianaUnknown1 cationInactive [76]
4I93A. thaliana
4I94A. thalianaAMP-PNP
Titin4JNWH. sapiens10−4 M [113]UnknownDisputed [112114]
1TKIH. sapiens
PAN34CYIChaetomium thermophilumATP + MgUnknown, but probably rather high affinity [78]1 cationUnknown, physiological role of PKD is to shuttle polyribonucleotides to PAN2 [81]
4CYJC. thermophilumATP + MgPAN2
4CZYNeurospora crassaAMP-PNP + MgPAN2
4BWKN. crassaATPγS
4BWX§N. crassaATPγS + Mg
4BWPDrosophila melanogasterAMP-PN
4XR7Saccharomyces cerevisiaePAN2
ROP22W1ZT. gondiiNone [43]N/AInactive [43]
3DZOT. gondiiMg
ROP5B3Q5ZT. gondiiUnknown2 cationsInactive [110]
3Q60T. gondiiATP + Mg
4LV5T. gondiiADPIRGa6 (M. musculus)
ROP5C4LV8T. gondiiADP + MgIRGa6 (M. musculus)Unknown1 cationUnknown
ROP83BYVT. gondiiMgUnknownUnknownUnknown
RNase L4O1OSus scrofa2-5A10−3 M [53]2 cationsInactive [5254]
4O1PS. scrofaAMP-PNP + Mg2-5A
4OAUH. sapiensADP + Mg2-5A
4OAVH. sapiensAMP-PCP + MgRNA + pUp
WNK14Q2ARattus norvegicusBrUnknownUnknownActive [124]
3FPQR. norvegicus
4PWNH. sapiens
MviN3OTVMycobacterium tuberculosisNone [47]UnknownInactive [47]
3OUKM. tuberculosis
3OUNM. tuberculosisFhaA
3UQCM. tuberculosis
ADCK34PEDH. sapiensBinds preferentially ADP [108]UnknownInactive, can be activated with a single Gly-rich loop mutation [108]