Skip to main content
. 2016 Jan 15;36(1):e00282. doi: 10.1042/BSR20150226

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
Protein PDB ID Species Ligand Complex Kd for ATP Binding mode Other
KSR2 2Y4I Homo sapiens ATP + Mg MEK1 Unknown 1 cation Active, phosphorylates MEK1 [4]
HER3 4OTW H. sapiens Bosutinib 10−6 M [5] 1 cation Active, autophosphorylates its own intracellular region, when immobilized on vesicles [5]
4RIW H. sapiens AMP-PNP + Mg EGFR KD (V624R, F973A, L977A)
4RIX (Q709R) H. sapiens AMP-PNP + Mg EGFR KD (V624R, F973A, L977A)
4RIY (E909G) H. sapiens AMP-PNP + Mg EGFR KD (V624R, F973A, L977A)
3KEX H. sapiens AMP-PNP + Mg
3LMG H. sapiens AMP-PNP + Mg
TYK2 JH2 3ZON H. sapiens IKK1 10−5 M [37] 1 cation Inactive [37]
4WOV H. sapiens BMS-066
4OLI H. sapiens Inhibitor 7012 JH2-JH1 (D1023N)
5C03 H. sapiens ATPγS + Mg
5C01 H. sapiens Pyrazine inhibitor
JAK2 JH2 4FVP* H. sapiens 10−6 M [6,45] 1 cation Active, autophosphorylates on S523 and Y570 [6]
4FVQ* H. sapiens ATP + Mg
4FVR (V617F)* H. sapiens ATP + Mg
JAK1 JH2 4L00 H. sapiens 10−6 M [45] 1 cation Inactive [65]
4L01 (V658F) H. sapiens
MLKL 4BTF Mus musculus 10−5 M (TSA) [26] No cation [9,25,26] Inactive [25]
4MWI H. sapiens
4M67 H. sapiens
4M68 M. musculus
4M69 M. musculus RIP3 KD
STRADα 3GNI H. sapiens ATP MO25 10−4–10−6 M [39,82] No cation [9] Inactive [140]
2WTK H. sapiens AMP-PNP MO25 + LKB1
VRK3 2JII H. sapiens None N/A Inactive
ILK 3KMW H. sapiens ATP + Mg α-Parvin 10−6 M [34] 1 cation Inactive [34,40]
3KMU H. sapiens α-Parvin
3REP H. sapiens ATP + Mn α-Parvin
CASK 3C0G H. sapiens 3′-AMP 10−3 M [7,9] No cation Active, cations inhibit binding and activity. [7,24,83]
3C0I H. sapiens 3′-AMP
3C0H H. sapiens AMP-PNP (only AMP visible)
3TAC H. sapiens Liprin-α2
3MFS (4M) H. sapiens AMP-PNP
3MFU (4M) H. sapiens AMP-PNP + Mn
3MFT (4M) H. sapiens
3MFR (4M) H. sapiens
ROR2 3ZZW H. sapiens None [55] N/A Inactive [55,102]
4GT4 H. sapiens
BIR2 4L68 Arabidopsis thaliana None [94] N/A Inactive [94]
BSK8 4I92 A. thaliana Unknown 1 cation Inactive [76]
4I93 A. thaliana
4I94 A. thaliana AMP-PNP
Titin 4JNW H. sapiens 10−4 M [113] Unknown Disputed [112114]
1TKI H. sapiens
PAN3 4CYI Chaetomium thermophilum ATP + Mg Unknown, but probably rather high affinity [78] 1 cation Unknown, physiological role of PKD is to shuttle polyribonucleotides to PAN2 [81]
4CYJ C. thermophilum ATP + Mg PAN2
4CZY Neurospora crassa AMP-PNP + Mg PAN2
4BWK N. crassa ATPγS
4BWX§ N. crassa ATPγS + Mg
4BWP Drosophila melanogaster AMP-PN
4XR7 Saccharomyces cerevisiae PAN2
ROP2 2W1Z T. gondii None [43] N/A Inactive [43]
3DZO T. gondii Mg
ROP5B 3Q5Z T. gondii Unknown 2 cations Inactive [110]
3Q60 T. gondii ATP + Mg
4LV5 T. gondii ADP IRGa6 (M. musculus)
ROP5C 4LV8 T. gondii ADP + Mg IRGa6 (M. musculus) Unknown 1 cation Unknown
ROP8 3BYV T. gondii Mg Unknown Unknown Unknown
RNase L 4O1O Sus scrofa 2-5A 10−3 M [53] 2 cations Inactive [5254]
4O1P S. scrofa AMP-PNP + Mg 2-5A
4OAU H. sapiens ADP + Mg 2-5A
4OAV H. sapiens AMP-PCP + Mg RNA + pUp
WNK1 4Q2A Rattus norvegicus Br Unknown Unknown Active [124]
3FPQ R. norvegicus
4PWN H. sapiens
MviN 3OTV Mycobacterium tuberculosis None [47] Unknown Inactive [47]
3OUK M. tuberculosis
3OUN M. tuberculosis FhaA
3UQC M. tuberculosis
ADCK3 4PED H. sapiens Binds preferentially ADP [108] Unknown Inactive, can be activated with a single Gly-rich loop mutation [108]