protein kinase D2 | Protein kinase D (PKD) family | IUPHAR/BPS Guide to PHARMACOLOGY

protein kinase D2

Target id: 2173

Nomenclature: protein kinase D2

Abbreviated Name: PKD2

Family: Protein kinase D (PKD) family

Annotation status:  image of an orange circle Annotated and awaiting review. Please contact us if you can help with reviewing.  » Email us

   GtoImmuPdb view: OFF :     Currently no data for protein kinase D2 in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 878 19q13.2 PRKD2 protein kinase D2
Mouse - 875 7 A2 Prkd2 protein kinase D2
Rat - 875 1 q21 Prkd2 protein kinase D2
Database Links
BRENDA
CATH/Gene3D
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Solution structure of the PH domain of protein kinase C, D2 type from human
PDB Id:  2COA
Resolution:  0.0Å
Species:  Human
References: 
Image of receptor 3D structure from RCSB PDB
Description:  Crystal Structure of PKD2 Phosphopeptide Bound to Human Class I MHC HLA-A2
PDB Id:  3BGM
Resolution:  1.6Å
Species:  Human
References:  5
Enzyme Reaction
EC Number: 2.7.11.13

Download all structure-activity data for this target as a CSV file

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
CRT 0066101 Hs Inhibition 8.6 pIC50 4
pIC50 8.6 (IC50 2.5x10-9 M) [4]
BPKDi Hs Inhibition 8.1 pIC50 6
pIC50 8.1 (IC50 9x10-9 M) [6]
Description: In a biochemical enzyme assay.
DiscoveRx KINOMEscan® screen
A screen of 72 inhibitors against 456 human kinases. Quantitative data were derived using DiscoveRx KINOMEscan® platform.
http://www.discoverx.com/services/drug-discovery-development-services/kinase-profiling/kinomescan
Reference: 2,7

Key to terms and symbols Click column headers to sort
Target used in screen: PRKD2
Ligand Sp. Type Action Affinity Units
lestaurtinib Hs Inhibitor Inhibition 8.1 pKd
staurosporine Hs Inhibitor Inhibition 7.1 pKd
NVP-TAE684 Hs Inhibitor Inhibition 6.8 pKd
JNJ-28312141 Hs Inhibitor Inhibition 6.5 pKd
sunitinib Hs Inhibitor Inhibition 6.4 pKd
BI-2536 Hs Inhibitor Inhibition 6.3 pKd
ruboxistaurin Hs Inhibitor Inhibition 6.1 pKd
AST-487 Hs Inhibitor Inhibition 6.0 pKd
alvocidib Hs Inhibitor Inhibition 6.0 pKd
neratinib Hs Inhibitor Inhibition 6.0 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »
EMD Millipore KinaseProfilerTM screen/Reaction Biology Kinase HotspotSM screen
A screen profiling 158 kinase inhibitors (Calbiochem Protein Kinase Inhibitor Library I and II, catalogue numbers 539744 and 539745) for their inhibitory activity at 1µM and 10µM against 234 human recombinant kinases using the EMD Millipore KinaseProfilerTM service.

A screen profiling the inhibitory activity of 178 commercially available kinase inhibitors at 0.5µM against a panel of 300 recombinant protein kinases using the Reaction Biology Corporation Kinase HotspotSM platform.

http://www.millipore.com/techpublications/tech1/pf3036
http://www.reactionbiology.com/webapps/main/pages/kinase.aspx


Reference: 1,3

Key to terms and symbols Click column headers to sort
Target used in screen: PKD2/PKD2(PRKD2)
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
staurosporine Hs Inhibitor Inhibition 1.0 5.0 0.5
K-252a Hs Inhibitor Inhibition 1.4 2.0 0.0
SB 218078 Hs Inhibitor Inhibition 2.0 92.0 90.0
JAK3 inhibitor VI Hs Inhibitor Inhibition 2.2 25.0 4.0
PKR inhibitor Hs Inhibitor Inhibition 4.2 30.0 3.0
JAK inhibitor I Hs Inhibitor Inhibition 6.1 40.0 22.0
Cdk1/2 inhibitor III Hs Inhibitor Inhibition 9.1 45.0 6.0
SU11652 Hs Inhibitor Inhibition 11.9 73.0 16.0
Gö 6976 Hs Inhibitor Inhibition 18.7 29.0 32.0
sunitinib Hs Inhibitor Inhibition 21.1
Displaying the top 10 most potent ligands  View all ligands in screen »

References

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1. Anastassiadis T, Deacon SW, Devarajan K, Ma H, Peterson JR. (2011) Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity. Nat. Biotechnol., 29 (11): 1039-45. [PMID:22037377]

2. Davis MI, Hunt JP, Herrgard S, Ciceri P, Wodicka LM, Pallares G, Hocker M, Treiber DK, Zarrinkar PP. (2011) Comprehensive analysis of kinase inhibitor selectivity. Nat. Biotechnol., 29 (11): 1046-51. [PMID:22037378]

3. Gao Y, Davies SP, Augustin M, Woodward A, Patel UA, Kovelman R, Harvey KJ. (2013) A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. Biochem. J., 451 (2): 313-28. [PMID:23398362]

4. Harikumar KB, Kunnumakkara AB, Ochi N, Tong Z, Deorukhkar A, Sung B, Kelland L, Jamieson S, Sutherland R, Raynham T et al.. (2010) A novel small-molecule inhibitor of protein kinase D blocks pancreatic cancer growth in vitro and in vivo. Mol. Cancer Ther., 9 (5): 1136-46. [PMID:20442301]

5. Mohammed F, Cobbold M, Zarling AL, Salim M, Barrett-Wilt GA, Shabanowitz J, Hunt DF, Engelhard VH, Willcox BE. (2008) Phosphorylation-dependent interaction between antigenic peptides and MHC class I: a molecular basis for the presentation of transformed self. Nat. Immunol., 9 (11): 1236-43. [PMID:18836451]

6. Monovich L, Vega RB, Meredith E, Miranda K, Rao C, Capparelli M, Lemon DD, Phan D, Koch KA, Chapo JA et al.. (2010) A novel kinase inhibitor establishes a predominant role for protein kinase D as a cardiac class IIa histone deacetylase kinase. FEBS Lett., 584 (3): 631-7. [PMID:20018189]

7. Wodicka LM, Ciceri P, Davis MI, Hunt JP, Floyd M, Salerno S, Hua XH, Ford JM, Armstrong RC, Zarrinkar PP et al.. (2010) Activation state-dependent binding of small molecule kinase inhibitors: structural insights from biochemistry. Chem. Biol., 17 (11): 1241-9. [PMID:21095574]

How to cite this page

Protein kinase D (PKD) family: protein kinase D2. Last modified on 08/11/2016. Accessed on 15/11/2018. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2173.