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Target not currently curated in GtoImmuPdb
Target id: 2192
Nomenclature: receptor interacting serine/threonine kinase 4
Abbreviated Name: ANKRD3
Gene and Protein Information | ||||||
Species | TM | AA | Chromosomal Location | Gene Symbol | Gene Name | Reference |
Human | - | 832 | 21q22.3 | RIPK4 | receptor interacting serine/threonine kinase 4 | |
Mouse | - | 786 | 16 C4 | Ripk4 | receptor-interacting serine-threonine kinase 4 | |
Rat | - | 786 | 11q12 | Ripk4 | receptor-interacting serine-threonine kinase 4 |
Previous and Unofficial Names |
ANKK2 | ankyrin repeat domain 3 | DIK | PKC-delta-interacting protein kinase | PKK | protein kinase C-associated kinase | RIP4 |
Database Links | |
Alphafold | P57078 (Hs), Q9ERK0 (Mm) |
BRENDA | 2.7.11.1 |
CATH/Gene3D | 1.25.40.20 |
ChEMBL Target | CHEMBL6083 (Hs) |
Ensembl Gene | ENSG00000183421 (Hs), ENSMUSG00000005251 (Mm), ENSRNOG00000001618 (Rn) |
Entrez Gene | 54101 (Hs), 72388 (Mm), 304053 (Rn) |
Human Protein Atlas | ENSG00000183421 (Hs) |
KEGG Enzyme | 2.7.11.1 |
KEGG Gene | hsa:54101 (Hs), mmu:72388 (Mm), rno:304053 (Rn) |
OMIM | 605706 (Hs) |
Orphanet | ORPHA291802 (Hs) |
Pharos | P57078 (Hs) |
RefSeq Nucleotide | NM_020639 (Hs), NM_023663 (Mm), NM_001107103 (Rn) |
RefSeq Protein | NP_065690 (Hs), NP_076152 (Mm), NP_001100573 (Rn) |
UniProtKB | P57078 (Hs), Q9ERK0 (Mm) |
Wikipedia | RIPK4 (Hs) |
Selected 3D Structures | |||||||||||||
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Enzyme Reaction | ||||
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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: 2,5 |
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Key to terms and symbols | Click column headers to sort | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Target used in screen: RIPK4 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Displaying the top 10 most potent ligands View all ligands in screen » |
Clinically-Relevant Mutations and Pathophysiology | ||||||||||||||
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General Comments |
In humans RIPK4 acts as a protein kinase C (PKC)-δ-interacting protein kinase that is expressed in the epithelium and most non-nervous tissues. It is required for activation of both the NF-κB and JNK-AP-1 pathways in HEK-293T cells [1], and may play a role in Wnt signalling [4]. Huang et al. (2018) have demonstrated in crystallographic studies that a dimeric structure of mouse Ripk4 is required for catalytic activity [3]. |
1. Chen L, Haider K, Ponda M, Cariappa A, Rowitch D, Pillai S. (2001) Protein kinase C-associated kinase (PKK), a novel membrane-associated, ankyrin repeat-containing protein kinase. J Biol Chem, 276 (24): 21737-44. [PMID:11278382]
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. Huang CS, Oberbeck N, Hsiao YC, Liu P, Johnson AR, Dixit VM, Hymowitz SG. (2018) Crystal Structure of Ripk4 Reveals Dimerization-Dependent Kinase Activity. Structure, 26 (5): 767-777.e5. [PMID:29706531]
4. Huang X, McGann JC, Liu BY, Hannoush RN, Lill JR, Pham V, Newton K, Kakunda M, Liu J, Yu C et al.. (2013) Phosphorylation of Dishevelled by protein kinase RIPK4 regulates Wnt signaling. Science, 339 (6126): 1441-5. [PMID:23371553]
5. 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]
Receptor interacting protein kinase (RIPK) family: receptor interacting serine/threonine kinase 4. Last modified on 26/09/2018. Accessed on 04/10/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2192.