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	Kinase Fusion Gene Summary
	Kinase Fusion Gene Sample Information
	Kinase Fusion ORF Analysis
	Kinase Fusion Amino Acid Sequences
	Multiple Sequence Alignment of All Fusion Protein Isoforms
	Kinase Fusion Protein Functional Features
	Kinase Fusion Protein Structures
	Comparison of Fusion Protein Isoforms
	Comparison of Fusion Protein Sequences/Structures with Known Sequences/Structures from PDB
	pLDDT Scores and Difference Analysis of pLDDT Scores Between the Active Sites (Best) and Non-Active Sites.
	Ramachandran Plot of Kinase Fusion Protein Structure
	Potential Active Site Information
	Virtual Screening Results
	Kinase-Substrate Information
	Related Drugs with This Kinase Fusion Protein
	Related Disease with This Kinase Fusion Protein
	Clinical Trials of the Found Drugs/Small Molecules

Kinase Fusion Gene:HIPK2_GRM8

Kinase Fusion Protein Summary

Kinase Fusion gene summary

Kinase Fusion partner gene information	Kinase Fusion gene name: HIPK2_GRM8
	KinaseFusionDB ID: KFG2691
	FusionGDB2.0 ID: KFG2691
		Hgene	Tgene
	Gene symbol	HIPK2	GRM8
	Gene ID	28996	2918
	Gene name	homeodomain interacting protein kinase 2	glutamate metabotropic receptor 8
	Synonyms	PRO0593	GLUR8\|GPRC1H\|MGLUR8\|mGlu8
	Cytomap	7q34	7q31.33
	Type of gene	protein-coding	protein-coding
	Description	homeodomain-interacting protein kinase 2hHIPk2	metabotropic glutamate receptor 8glutamate receptor, metabotropic 8
	Modification date	20240317	20240411
	UniProtAcc	Q9H2X6	O00222
Ensembl transtripts involved in fusion gene	ENST ids	ENST00000342645, ENST00000406875, ENST00000428878,	ENST00000480995, ENST00000339582, ENST00000358373, ENST00000405249, ENST00000444921,
Context (manual curation of fusion genes in KinaseFusionDB)	PubMed: HIPK2 [Title/Abstract] AND GRM8 [Title/Abstract] AND fusion [Title/Abstract]
Most frequent breakpoint (based on all fusion genes of FusionGDB 2.0)	HIPK2(139285163)-GRM8(126249552), # samples:3

Gene ontology of each fusion partner gene with evidence of Inferred from Direct Assay (IDA) from Entrez

Partner	Gene	GO ID	GO term	PubMed ID
Hgene	HIPK2	GO:0006468	protein phosphorylation	19448668
Hgene	HIPK2	GO:0018105	peptidyl-serine phosphorylation	33591310
Hgene	HIPK2	GO:0030330	DNA damage response, signal transduction by p53 class mediator	14647468
Hgene	HIPK2	GO:0045766	positive regulation of angiogenesis	19046997
Hgene	HIPK2	GO:0060395	SMAD protein signal transduction	12874272
Tgene	GRM8	GO:0007193	adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway	11166323

Kinase Fusion gene breakpoints across HIPK2 (5'-gene)
* Click on the image to open the UCSC genome browser with custom track showing this image in a new window.

Kinase Fusion gene breakpoints across GRM8 (3'-gene)
* Click on the image to open the UCSC genome browser with custom track showing this image in a new window.

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Kinase Fusion Gene Sample Information

Kinase Fusion gene information.

Kinase Fusion gene information from four resources (ChiTars 5.0, ChimerDB 4.0, COSMIC, and CCLE)
* All genome coordinats were lifted-over on hg19.
* Click on the break point to see the gene structure around the break point region using the UCSC Genome Browser.

Source	Sample	Hgene	Hchr	Hbp	Tgene	Tchr	Tbp
ChimerDB4	TCGA-39-5011-01A	HIPK2	chr7	139285163	GRM8	chr7	126249552
ChimerDB4	TCGA-39-5011	HIPK2	chr7	139285162	GRM8	chr7	126249552

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Kinase Fusion ORF Analysis

Kinase Fusion information from ORFfinder translation from full-length transcript sequence from KinaseFusionDB.

Henst	Tenst	Hgene	Hchr	Hbp	Tgene	Tchr	Tbp	Seq length (transcript)	Seq length (amino acids)
ENST00000406875	ENST00000405249	HIPK2	chr7	139285163	GRM8	chr7	126249552	2608	820
ENST00000406875	ENST00000405249	HIPK2	chr7	139285162	GRM8	chr7	126249552	2608	820

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Kinase Fusion Amino Acid Sequences

For individual full-length fusion transcript sequence from KinaseFusionDB, we ran ORFfinder and chose the longest ORF among the all predicted ones.

>Henst_Tenst_Hgene_Hchr_Hbp_Tgene_Tchr_Tbp_length(fusion AA)_AAseq

>ENST00000406875_ENST00000405249_HIPK2_chr7_139285163_GRM8_chr7_126249552_length(amino acids)=820
MAPVYEGMASHVQVFSPHTLQSSAFCSVKKLKIEPSSNWDMTGYGSHSKVYSQSKNIPLSQPATTTVSTSLPVPNPSLPYEQTIVFPGST
GHIVVTSASSTSVTGQVLGGPHNLMRRSTVSLLDTYQKCGLKRKSEEIENTSSVQIIEEHPPMIQNNASGATVATATTSTATSKNSGSNS
EGDYQLVQHEVLCSMTNTYEVLEFLGRGTFGQVVKCWKRGTNEIVAIKILKNHPSYARQGQIEVSILARLSTESADDYNFVRAYECFQHK
NHTCLVFEMLEQNLYDFLKQNKFSPLPLKYIRPVLQQVATALMKLKSLGLIHADLKPENIMLVDPSRQPYRVKVIDFGSASHVSKAVCST
YLQSRYYRAPEIILGLPFCEAIDMWSLGCVIAELFLGWPLYPGASEYDQIRYISQTQGLPAEYLLSAGTKTTRFFNRDTDSPYPLWRLKT
PDDHEAETGIKSKEARKYIFNCLDDMAQVNMTTDLEGSDMLVEKADRREFIDLLKKMLTIDADKRITPIETLNHPFVTMTHLLDFPHSTH
VKSCFQNMEICKRRVNMYDTVNQSKTPFITHVAPSTSTNLTMTFNNQLTTVHNQAPSSTSATISLANPEVSILNYPSTLYQPSAASMAAV
AQRSMPLQTGTAQICARPDPFQQALIVCPPGFQGLQASPSKHAGYSVRMENAVPIVTQAPGAQPLQIQPGLLAQQAWPSGTQQILLPPAW
QQLTGVATHTSVQHATVIPETMAGTQQLADWRNTHAHGSHYNPIMQQPALLTGHVTLPAAQPLNVGVAHVMRQQPTSTTSSRKSKQHQSS

--------------------------------------------------------------

>ENST00000406875_ENST00000405249_HIPK2_chr7_139285162_GRM8_chr7_126249552_length(amino acids)=820
MAPVYEGMASHVQVFSPHTLQSSAFCSVKKLKIEPSSNWDMTGYGSHSKVYSQSKNIPLSQPATTTVSTSLPVPNPSLPYEQTIVFPGST
GHIVVTSASSTSVTGQVLGGPHNLMRRSTVSLLDTYQKCGLKRKSEEIENTSSVQIIEEHPPMIQNNASGATVATATTSTATSKNSGSNS
EGDYQLVQHEVLCSMTNTYEVLEFLGRGTFGQVVKCWKRGTNEIVAIKILKNHPSYARQGQIEVSILARLSTESADDYNFVRAYECFQHK
NHTCLVFEMLEQNLYDFLKQNKFSPLPLKYIRPVLQQVATALMKLKSLGLIHADLKPENIMLVDPSRQPYRVKVIDFGSASHVSKAVCST
YLQSRYYRAPEIILGLPFCEAIDMWSLGCVIAELFLGWPLYPGASEYDQIRYISQTQGLPAEYLLSAGTKTTRFFNRDTDSPYPLWRLKT
PDDHEAETGIKSKEARKYIFNCLDDMAQVNMTTDLEGSDMLVEKADRREFIDLLKKMLTIDADKRITPIETLNHPFVTMTHLLDFPHSTH
VKSCFQNMEICKRRVNMYDTVNQSKTPFITHVAPSTSTNLTMTFNNQLTTVHNQAPSSTSATISLANPEVSILNYPSTLYQPSAASMAAV
AQRSMPLQTGTAQICARPDPFQQALIVCPPGFQGLQASPSKHAGYSVRMENAVPIVTQAPGAQPLQIQPGLLAQQAWPSGTQQILLPPAW
QQLTGVATHTSVQHATVIPETMAGTQQLADWRNTHAHGSHYNPIMQQPALLTGHVTLPAAQPLNVGVAHVMRQQPTSTTSSRKSKQHQSS

--------------------------------------------------------------

Multiple Sequence Alignment of All Fusion Protein Isoforms

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Kinase Fusion Protein Functional Features

Four levels of functional features of fusion genes
Go to FGviewer search page for the most frequent breakpoint (https://ccsmweb.uth.edu/FGviewer/chr7:139285163/chr7:126249552)
- FGviewer provides the online visualization of the retention search of the protein functional features across DNA, RNA, protein, and pathological levels.
- How to search
1. Put your fusion gene symbol.
2. Press the tab key until there will be shown the breakpoint information filled.
4. Go down and press 'Search' tab twice.
4. Go down to have the hyperlink of the search result.
5. Click the hyperlink.
6. See the FGviewer result for your fusion gene.

Main function of each fusion partner protein. (from UniProt)

Hgene	Tgene
HIPK2 Q9H2X6	GRM8 O00222
FUNCTION: Serine/threonine-protein kinase involved in transcription regulation, p53/TP53-mediated cellular apoptosis and regulation of the cell cycle. Acts as a corepressor of several transcription factors, including SMAD1 and POU4F1/Brn3a and probably NK homeodomain transcription factors. Phosphorylates PDX1, ATF1, PML, p53/TP53, CREB1, CTBP1, CBX4, RUNX1, EP300, CTNNB1, HMGA1, ZBTB4 and DAZAP2. Inhibits cell growth and promotes apoptosis through the activation of p53/TP53 both at the transcription level and at the protein level (by phosphorylation and indirect acetylation). The phosphorylation of p53/TP53 may be mediated by a p53/TP53-HIPK2-AXIN1 complex. Involved in the response to hypoxia by acting as a transcriptional co-suppressor of HIF1A. Mediates transcriptional activation of TP73. In response to TGFB, cooperates with DAXX to activate JNK. Negative regulator through phosphorylation and subsequent proteasomal degradation of CTNNB1 and the antiapoptotic factor CTBP1. In the Wnt/beta-catenin signaling pathway acts as an intermediate kinase between MAP3K7/TAK1 and NLK to promote the proteasomal degradation of MYB. Phosphorylates CBX4 upon DNA damage and promotes its E3 SUMO-protein ligase activity. Activates CREB1 and ATF1 transcription factors by phosphorylation in response to genotoxic stress. In response to DNA damage, stabilizes PML by phosphorylation. PML, HIPK2 and FBXO3 may act synergically to activate p53/TP53-dependent transactivation. Promotes angiogenesis, and is involved in erythroid differentiation, especially during fetal liver erythropoiesis. Phosphorylation of RUNX1 and EP300 stimulates EP300 transcription regulation activity. Triggers ZBTB4 protein degradation in response to DNA damage. In response to DNA damage, phosphorylates DAZAP2 which localizes DAZAP2 to the nucleus, reduces interaction of DAZAP2 with HIPK2 and prevents DAZAP2-dependent ubiquitination of HIPK2 by E3 ubiquitin-protein ligase SIAH1 and subsequent proteasomal degradation (PubMed:33591310). Modulates HMGA1 DNA-binding affinity. In response to high glucose, triggers phosphorylation-mediated subnuclear localization shifting of PDX1. Involved in the regulation of eye size, lens formation and retinal lamination during late embryogenesis. {ECO:0000269\|PubMed:11740489, ECO:0000269\|PubMed:11925430, ECO:0000269\|PubMed:12851404, ECO:0000269\|PubMed:12874272, ECO:0000269\|PubMed:14678985, ECO:0000269\|PubMed:17018294, ECO:0000269\|PubMed:17960875, ECO:0000269\|PubMed:18695000, ECO:0000269\|PubMed:18809579, ECO:0000269\|PubMed:19015637, ECO:0000269\|PubMed:19046997, ECO:0000269\|PubMed:19448668, ECO:0000269\|PubMed:20307497, ECO:0000269\|PubMed:20573984, ECO:0000269\|PubMed:20637728, ECO:0000269\|PubMed:20980392, ECO:0000269\|PubMed:21192925, ECO:0000269\|PubMed:22825850, ECO:0000269\|PubMed:33591310}.	FUNCTION: G-protein coupled receptor for glutamate. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Signaling inhibits adenylate cyclase activity. {ECO:0000269\|PubMed:9473604}.

Retention analysis result of each fusion partner protein across 39 protein features of UniProt such as six molecule processing features, 13 region features, four site features, six amino acid modification features, two natural variation features, five experimental info features, and 3 secondary structure features. Here, because of limited space for viewing, we only show the protein feature retention information belong to the 13 regional features. All retention annotation result can be downloaded at
download page
* Minus value of BPloci means that the break pointn is located before the CDS.

- Retained domain in the 5'-partner of fusion protein (protein functional feature from UniProt).

784811784811

Partner

Hgeneene

Hbp

Tgeneene

Tbp

ENST

BPexon

TotalExon

Protein feature loci

BPloci

TotalLen

Feature

Note

Hgene

HIPK2

139285162

GRM8

126249552

ENST00000406875

199_527

1172

Domain

Note=Protein kinase;Ontology_term=ECO:0000255;evidence=ECO:0000255|PROSITE-ProRule:PRU00159

Hgene

HIPK2

139285162

GRM8

126249552

ENST00000406875

199_527

1199

Domain

Note=Protein kinase;Ontology_term=ECO:0000255;evidence=ECO:0000255|PROSITE-ProRule:PRU00159

Hgene

HIPK2

139285163

GRM8

126249552

ENST00000406875

199_527

1172

Domain

Note=Protein kinase;Ontology_term=ECO:0000255;evidence=ECO:0000255|PROSITE-ProRule:PRU00159

Hgene

HIPK2

139285163

GRM8

126249552

ENST00000406875

199_527

1199

Domain

Note=Protein kinase;Ontology_term=ECO:0000255;evidence=ECO:0000255|PROSITE-ProRule:PRU00159

- Retained domain in the 3'-partner of fusion protein (protein functional feature from UniProt).

Partner

Hgeneene

Hbp

Tgeneene

Tbp

ENST

BPexon

TotalExon

Protein feature loci

BPloci

TotalLen

Feature

Note

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Kinase Fusion Protein Structures

CIF files of the predicted kinase fusion proteins
* Here we show the 3D structure of the fusion proteins using Mol*. AlphaFold produces a per-residue confidence score (pLDDT) between 0 and 100. Model confidence is shown from the pLDDT values per residue. pLDDT corresponds to the model’s prediction of its score on the local Distance Difference Test. It is a measure of local accuracy (from AlphfaFold website). To color code individual residues, we transformed individual PDB files into CIF format.

Kinase Fusion protein CIF link (fusion AA seq ID in KinaseFusionDB)	Henst	Tenst	Hgene	Hchr	Hbp	Tgene	Tchr	Tbp	AA seq	Len(AA seq)
PDB file >>>133_HIPK2_GRM8	ENST00000406875	ENST00000405249	HIPK2	chr7	139285162	GRM8	chr7	126249552	MAPVYEGMASHVQVFSPHTLQSSAFCSVKKLKIEPSSNWDMTGYGSHSKVYSQSKNIPLSQPATTTVSTSLPVPNPSLPYEQTIVFPGST GHIVVTSASSTSVTGQVLGGPHNLMRRSTVSLLDTYQKCGLKRKSEEIENTSSVQIIEEHPPMIQNNASGATVATATTSTATSKNSGSNS EGDYQLVQHEVLCSMTNTYEVLEFLGRGTFGQVVKCWKRGTNEIVAIKILKNHPSYARQGQIEVSILARLSTESADDYNFVRAYECFQHK NHTCLVFEMLEQNLYDFLKQNKFSPLPLKYIRPVLQQVATALMKLKSLGLIHADLKPENIMLVDPSRQPYRVKVIDFGSASHVSKAVCST YLQSRYYRAPEIILGLPFCEAIDMWSLGCVIAELFLGWPLYPGASEYDQIRYISQTQGLPAEYLLSAGTKTTRFFNRDTDSPYPLWRLKT PDDHEAETGIKSKEARKYIFNCLDDMAQVNMTTDLEGSDMLVEKADRREFIDLLKKMLTIDADKRITPIETLNHPFVTMTHLLDFPHSTH VKSCFQNMEICKRRVNMYDTVNQSKTPFITHVAPSTSTNLTMTFNNQLTTVHNQAPSSTSATISLANPEVSILNYPSTLYQPSAASMAAV AQRSMPLQTGTAQICARPDPFQQALIVCPPGFQGLQASPSKHAGYSVRMENAVPIVTQAPGAQPLQIQPGLLAQQAWPSGTQQILLPPAW QQLTGVATHTSVQHATVIPETMAGTQQLADWRNTHAHGSHYNPIMQQPALLTGHVTLPAAQPLNVGVAHVMRQQPTSTTSSRKSKQHQSS	820
3D view using mol* of 133_HIPK2_GRM8

PDB file >>>HKFP_194_HIPK2_GRM8	ENST00000406875	ENST00000405249	HIPK2	chr7	139285163	GRM8	chr7	126249552	MAPVYEGMASHVQVFSPHTLQSSAFCSVKKLKIEPSSNWDMTGYGSHSKVYSQSKNIPLSQPATTTVSTSLPVPNPSLPYEQTIVFPGST GHIVVTSASSTSVTGQVLGGPHNLMRRSTVSLLDTYQKCGLKRKSEEIENTSSVQIIEEHPPMIQNNASGATVATATTSTATSKNSGSNS EGDYQLVQHEVLCSMTNTYEVLEFLGRGTFGQVVKCWKRGTNEIVAIKILKNHPSYARQGQIEVSILARLSTESADDYNFVRAYECFQHK NHTCLVFEMLEQNLYDFLKQNKFSPLPLKYIRPVLQQVATALMKLKSLGLIHADLKPENIMLVDPSRQPYRVKVIDFGSASHVSKAVCST YLQSRYYRAPEIILGLPFCEAIDMWSLGCVIAELFLGWPLYPGASEYDQIRYISQTQGLPAEYLLSAGTKTTRFFNRDTDSPYPLWRLKT PDDHEAETGIKSKEARKYIFNCLDDMAQVNMTTDLEGSDMLVEKADRREFIDLLKKMLTIDADKRITPIETLNHPFVTMTHLLDFPHSTH VKSCFQNMEICKRRVNMYDTVNQSKTPFITHVAPSTSTNLTMTFNNQLTTVHNQAPSSTSATISLANPEVSILNYPSTLYQPSAASMAAV AQRSMPLQTGTAQICARPDPFQQALIVCPPGFQGLQASPSKHAGYSVRMENAVPIVTQAPGAQPLQIQPGLLAQQAWPSGTQQILLPPAW QQLTGVATHTSVQHATVIPETMAGTQQLADWRNTHAHGSHYNPIMQQPALLTGHVTLPAAQPLNVGVAHVMRQQPTSTTSSRKSKQHQSS	820_HIPK2_GRM8
PDB file >>>HKFP_195_HIPK2_GRM8	ENST00000406875	ENST00000405249	HIPK2	chr7	139285162	GRM8	chr7	126249552	MAPVYEGMASHVQVFSPHTLQSSAFCSVKKLKIEPSSNWDMTGYGSHSKVYSQSKNIPLSQPATTTVSTSLPVPNPSLPYEQTIVFPGST GHIVVTSASSTSVTGQVLGGPHNLMRRSTVSLLDTYQKCGLKRKSEEIENTSSVQIIEEHPPMIQNNASGATVATATTSTATSKNSGSNS EGDYQLVQHEVLCSMTNTYEVLEFLGRGTFGQVVKCWKRGTNEIVAIKILKNHPSYARQGQIEVSILARLSTESADDYNFVRAYECFQHK NHTCLVFEMLEQNLYDFLKQNKFSPLPLKYIRPVLQQVATALMKLKSLGLIHADLKPENIMLVDPSRQPYRVKVIDFGSASHVSKAVCST YLQSRYYRAPEIILGLPFCEAIDMWSLGCVIAELFLGWPLYPGASEYDQIRYISQTQGLPAEYLLSAGTKTTRFFNRDTDSPYPLWRLKT PDDHEAETGIKSKEARKYIFNCLDDMAQVNMTTDLEGSDMLVEKADRREFIDLLKKMLTIDADKRITPIETLNHPFVTMTHLLDFPHSTH VKSCFQNMEICKRRVNMYDTVNQSKTPFITHVAPSTSTNLTMTFNNQLTTVHNQAPSSTSATISLANPEVSILNYPSTLYQPSAASMAAV AQRSMPLQTGTAQICARPDPFQQALIVCPPGFQGLQASPSKHAGYSVRMENAVPIVTQAPGAQPLQIQPGLLAQQAWPSGTQQILLPPAW QQLTGVATHTSVQHATVIPETMAGTQQLADWRNTHAHGSHYNPIMQQPALLTGHVTLPAAQPLNVGVAHVMRQQPTSTTSSRKSKQHQSS	820_HIPK2_GRM8

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Comparison of Fusion Protein Isoforms

Superimpose the 3D Structures Among All Fusion Protein Isoforms
* Download the pdb file and open it from the molstar online viewer.

Comparison of the Secondary Structures of Fusion Protein Isoforms

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Comparison of Fusion Protein Sequences/Structures with Known Sequences/Structures from PDB

HIPK2_GRM8 does not have any known PDB structures.

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pLDDT score distribution

pLDDT score distribution of the predicted fusion protein structures from AlphaFold2
* AlphaFold produces a per-residue confidence score (pLDDT) between 0 and 100.
* The blue color at the bottom marks the best active site residues.

133_HIPK2_GRM8.png

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Potential Active Site Information

The potential binding sites of these fusion proteins were identified using SiteMap, a module of the Schrodinger suite.

Kinase Fusion AA seq ID in KinaseFusionDB

Site score

Size

Dscore

Volume

Exposure

Enclosure

Contact

Phobic

Philic

Balance

Don/Acc

Residues

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Ramachandran Plot of Kinase Fusion Protein Structure

Ramachandran plot of the torsional angles - phi (φ)and psi (ψ) - of the residues (amino acids) contained in this fusion protein peptide.

133_HIPK2_GRM8_ramachandran.png

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Virtual Screening Results

Distribution of the average docking score across all approved kinase inhibitors.
Distribution of the number of occurrence across all approved kinase inhibitors.

5'-kinase fusion protein case

3'-kinase fusion protein case

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Drug information from DrugBank of the top 20 interacting small molecules.
* The detailed information of individual kinase inhibitors are available in the download page.

Fusion gene name info	Drug	Docking score	Glide g score	Glide energy
133_HIPK2_GRM8-DOCK_HTVS_1-001	Midostaurin	-10.2695	-10.2695	-49.0431
133_HIPK2_GRM8-DOCK_HTVS_1-001	Midostaurin	-8.74986	-8.74986	-51.9222
133_HIPK2_GRM8-DOCK_HTVS_1-001	Tepotinib	-8.69132	-8.69242	-55.5966
133_HIPK2_GRM8-DOCK_HTVS_1-001	Capmatinib	-8.40714	-8.41274	-47.5464
133_HIPK2_GRM8-DOCK_HTVS_1-001	Midostaurin	-8.15264	-8.15264	-44.901
133_HIPK2_GRM8-DOCK_HTVS_1-001	Lapatinib	-8.11317	-8.20197	-63.131
133_HIPK2_GRM8-DOCK_HTVS_1-001	Lapatinib	-8.01677	-8.10557	-65.2636
133_HIPK2_GRM8-DOCK_HTVS_1-001	Palbociclib	-7.86424	-8.271139999999999	-49.1336
133_HIPK2_GRM8-DOCK_HTVS_1-001	Palbociclib	-7.86424	-8.271139999999999	-49.1336
133_HIPK2_GRM8-DOCK_HTVS_1-001	Larotrectinib	-7.772589999999999	-7.772589999999999	-42.5986
133_HIPK2_GRM8-DOCK_HTVS_1-001	Midostaurin	-7.7645	-7.7645	-53.1042
133_HIPK2_GRM8-DOCK_HTVS_1-001	Palbociclib	-7.619219999999999	-8.08872	-47.8685
133_HIPK2_GRM8-DOCK_HTVS_1-001	Palbociclib	-7.619219999999999	-8.08872	-47.8685
133_HIPK2_GRM8-DOCK_HTVS_1-001	Palbociclib	-7.619219999999999	-8.08872	-47.8685
133_HIPK2_GRM8-DOCK_HTVS_1-001	Belumosudil	-7.53728	-7.544980000000001	-50.6016
133_HIPK2_GRM8-DOCK_HTVS_1-001	Belumosudil	-7.5126	-7.5203	-50.4026
133_HIPK2_GRM8-DOCK_HTVS_1-001	Gefitinib	-7.50413	-7.91913	-52.9329
133_HIPK2_GRM8-DOCK_HTVS_1-001	Gefitinib	-7.50413	-7.91913	-52.9329
133_HIPK2_GRM8-DOCK_HTVS_1-001	Palbociclib	-7.4569	-7.8638	-49.5897
133_HIPK2_GRM8-DOCK_HTVS_1-001	Nilotinib	-7.35438	-7.4939800000000005	-59.5306

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Kinase-Substrate Information of HIPK2_GRM8

Phosphorylation target of the kinase
(phosphosite, 03-17-2024)

Kinase	Kinase UniProt Acc	Kinase species	Substrate	Substrate UniProt Acc	Substrate phosphorylated residues	Substrate phosphorylated sites (+/-7AA)	Domain
HIPK2	Q9H2X6	human	HIPK2	Q9H2X6	T838	SKRVKENtPPRCAMV
HIPK2	Q9H2X6	human	ZBTB4	Q9P1Z0	T797	ERPGGtPtPVIAYsK
HIPK2	Q9H2X6	human	KLF3	P57682	S78	sPPsAGNsPSSLKFP
HIPK2	Q9H2X6	human	SIAH2	O43255	S68	GGGAGPVsPQHHELT
HIPK2	Q9H2X6	human	HMGA1	P17096	T78	ktrkttttPGrkPrG
HIPK2	Q9H2X6	human	HIPK2	Q9H2X6	S827	SSSQAIssPQRSKRV
HIPK2	Q9H2X6	human	CTBP1	Q13363	S422	AHPPHAPsPGQTVkP
HIPK2	Q9H2X6	human	PML	P29590	S36	PSEGRQPsPsPsPtE
HIPK2	Q9H2X6	human	TLE1	Q04724	S289	DAsssPAstAsSASS
HIPK2	Q9H2X6	human	SIAH2	O43255	T119	PTCRGALtPSIRNLA
HIPK2	Q9H2X6	human	MECP2	P51608	S216	VkRVLEKsPGkLLVk
HIPK2	Q9H2X6	human	MECP2	P51608	S80	AVPEAsAsPKQRRsI
HIPK2	Q9H2X6	human	TP53	P04637	S46	AMDDLMLsPDDIEQW	TAD2
HIPK2	Q9H2X6	human	SIRT1	Q96EB6	S682	SDSGTCQsPSLEEPM
HIPK2	Q9H2X6	human	RUNX1	Q01196	S276	VHPAtPIsPGRASGM
HIPK2	Q9H2X6	human	PML	P29590	S8	MEPAPARsPRPQQDP
HIPK2	Q9H2X6	human	EP300	Q09472	S2279	PVQPNPMsPQQHMLP
HIPK2	Q9H2X6	human	HIPK2	Q9H2X6	T880	QTIVIPDtPsPTVSV
HIPK2	Q9H2X6	human	CBX4	O00257	T497	SLQVkPEtPASAAVA
HIPK2	Q9H2X6	human	HIPK2	Q9H2X6	Y361	SkAVCstyLQsRYyR	Pkinase
HIPK2	Q9H2X6	human	KLF3	P57682	S108	sPPIKKysPPsPGVQ
HIPK2	Q9H2X6	human	KLF3	P57682	S101	GLsMPsssPPIKKys
HIPK2	Q9H2X6	human	TLE1	Q04724	S286	LKkDAsssPAstAsS
HIPK2	Q9H2X6	human	CEBPB	P17676	S76	HERAIDFsPyLEPLG
HIPK2	Q9H2X6	human	ZBTB4	Q9P1Z0	T983	AAPPAPPtPPPPTLP
HIPK2	Q9H2X6	human	HMGA1	P17096	S36	PRkQPPVsPGtALVG
HIPK2	Q9H2X6	human	SIRT1	Q96EB6	S27	ADREAAssPAGEPLR
HIPK2	Q9H2X6	human	HIPK2	Q9H2X6	S364	VCstyLQsRYyRAPE	Pkinase
HIPK2	Q9H2X6	human	HDAC3	O15379	S374	KMLNHAPsVQIHDVP
HIPK2	Q9H2X6	human	TP63	Q9H3D4	T491	PQQRNALtPTTIPDG
HIPK2	Q9H2X6	human	HIPK2	Q9H2X6	S924	SCVTVHDsPYSDSSS
HIPK2	Q9H2X6	human	RUNX1	Q01196	S249	DTRQIQPsPPWsyDQ
HIPK2	Q9H2X6	human	TLE1	Q04724	S239	KDSsHYDsDGDKsDD
HIPK2	Q9H2X6	human	KLF3	P57682	S250	KRPLPVEsPDtQRKR
HIPK2	Q9H2X6	human	NOTCH1	P46531	T2511	VPEHPFLtPsPEsPD
HIPK2	Q9H2X6	human	SIAH2	O43255	T26	PPPQPQHtPsPAAPP
HIPK2	Q9H2X6	human	CTBP2	P56545	S428	AHPSQAPsPNQPTKH
HIPK2	Q9H2X6	human	HMGA1	P17096-2	T67	kTRkTTTtPGRkPrG
HIPK2	Q9H2X6	human	HIPK2	Q9H2X6	S848	RCAMVHSsPACSTSV
HIPK2	Q9H2X6	human	PPM1D	O15297	S85	PLPDAGAsPAPsRCC	PP2C
HIPK2	Q9H2X6	human	RUNX1	Q01196	T273	sPsVHPAtPIsPGRA
HIPK2	Q9H2X6	human	HIPK2	Q9H2X6	S934	SDSSSNTsPYSVQQR
HIPK2	Q9H2X6	human	KLF3	P57682	S224	PPLMNsVsPPQALLQ
HIPK2	Q9H2X6	human	KLF3	P57682	S111	IKKysPPsPGVQPFG
HIPK2	Q9H2X6	human	HMGA1	P17096	T53	kEPsEVPtPkRPrGr
HIPK2	Q9H2X6	human	KLF3	P57682	S71	LTVNKRSsPPsAGNs
HIPK2	Q9H2X6	human	PPM1D	O15297	S54	QPLPPRPsPAALPGG
HIPK2	Q9H2X6	human	HIPK2	Q9H2X6	S668	GFQGLQAsPSkHAGY
HIPK2	Q9H2X6	human	CDKN1B	P46527	S10	NVRVSNGsPsLErMD
HIPK2	Q9H2X6	human	HIPK2	Q9H2X6	S882	IVIPDtPsPTVSVIT
HIPK2	Q9H2X6	human	ZBTB4	Q9P1Z0	T795	AAERPGGtPtPVIAY
HIPK2	Q9H2X6	human	ELF4	Q99607	S369	ASLELGPsLDEEIPT
HIPK2	Q9H2X6	human	CREB1	P16220	S257	PGVVMAssPALPTQP
HIPK2	Q9H2X6	human	KLF3	P57682	S92	PSSHRRAsPGLsMPs
HIPK2	Q9H2X6	human	PML	P29590	S38	EGRQPsPsPsPtERA
HIPK2	Q9H2X6	human	HMGA1	P17096-2	T42	kEPsEVPtPkrPrGr
HIPK2	Q9H2X6	human	SIAH2	O43255	S28	PQPQHtPsPAAPPAA
HIPK2	Q9H2X6	human	CEBPB	P17676	T235	SsssPPGtPSPADAK
HIPK2	Q9H2X6	human	KLF3	P57682	S216	DYYPEEMsPPLMNsV
HIPK2	Q9H2X6	human	SPAST	Q9UBP0	S268	sGHHRAPsySGLSMV

Biological Network Integration of This Kinase and Substrates
(GeneMANIA website)

Enriched GO biological processes of the phosphorylation target genes of the kinase

Kinase	GOID	GO term	P.adjust
HIPK2	ID	Description	0.00e+00
HIPK2	GO:0042771	intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediator	2.63e-08
HIPK2	GO:0072331	signal transduction by p53 class mediator	2.70e-08
HIPK2	GO:0030330	DNA damage respons	3.46e-10
HIPK2	GO:0048511	rhythmic process	6.19e-07
HIPK2	GO:0001666	response to hypoxia	6.19e-07
HIPK2	GO:0008630	intrinsic apoptotic signaling pathway in response to DNA damage	6.82e-07
HIPK2	GO:0036293	response to decreased oxygen levels	7.18e-07
HIPK2	GO:0090398	cellular senescence	8.24e-07
HIPK2	GO:0007623	circadian rhythm	8.24e-07
HIPK2	GO:0070482	response to oxygen levels	1.02e-06
HIPK2	GO:0097193	intrinsic apoptotic signaling pathway	1.48e-05
HIPK2	GO:0042770	signal transduction in response to DNA damage	1.48e-05
HIPK2	GO:1901796	regulation of signal transduction by p53 class mediator	2.66e-05
HIPK2	GO:0040029	epigenetic regulation of gene expression	3.99e-05
HIPK2	GO:0045444	fat cell differentiation	5.98e-05
HIPK2	GO:0030099	myeloid cell differentiation	7.90e-05
HIPK2	GO:0048732	gland development	9.11e-05
HIPK2	GO:0071456	cellular response to hypoxia	9.32e-05
HIPK2	GO:0051402	neuron apoptotic process	9.32e-05
HIPK2	GO:0050872	white fat cell differentiation	1.03e-04
HIPK2	GO:0070059	intrinsic apoptotic signaling pathway in response to endoplasmic reticulum stress	1.05e-04
HIPK2	GO:0036294	cellular response to decreased oxygen levels	1.08e-04
HIPK2	GO:0006977	DNA damage respons	1.46e-06
HIPK2	GO:0051170	import into nucleus	1.26e-04
HIPK2	GO:0071453	cellular response to oxygen levels	1.54e-04
HIPK2	GO:0048638	regulation of developmental growth	1.68e-04
HIPK2	GO:0006913	nucleocytoplasmic transport	1.68e-04
HIPK2	GO:0051169	nuclear transport	1.68e-04
HIPK2	GO:0030324	lung development	1.95e-04
HIPK2	GO:0030323	respiratory tube development	2.10e-04
HIPK2	GO:0060541	respiratory system development	3.30e-04
HIPK2	GO:0031571	mitotic G1 DNA damage checkpoint signaling	3.30e-04
HIPK2	GO:0044819	mitotic G1/S transition checkpoint signaling	3.30e-04
HIPK2	GO:0018205	peptidyl-lysine modification	3.54e-04
HIPK2	GO:1990830	cellular response to leukemia inhibitory factor	4.10e-04
HIPK2	GO:0007179	transforming growth factor beta receptor signaling pathway	4.17e-04
HIPK2	GO:1990823	response to leukemia inhibitory factor	4.20e-04
HIPK2	GO:0043523	regulation of neuron apoptotic process	4.22e-04
HIPK2	GO:0007178	transmembrane receptor protein serine/threonine kinase signaling pathway	4.27e-04
HIPK2	GO:0042752	regulation of circadian rhythm	5.10e-04
HIPK2	GO:0009314	response to radiation	5.10e-04
HIPK2	GO:0031112	positive regulation of microtubule polymerization or depolymerization	5.10e-04
HIPK2	GO:0016570	histone modification	5.82e-04
HIPK2	GO:0046660	female sex differentiation	5.82e-04
HIPK2	GO:0022612	gland morphogenesis	6.08e-04
HIPK2	GO:0072089	stem cell proliferation	6.55e-04
HIPK2	GO:0060251	regulation of glial cell proliferation	6.80e-04
HIPK2	GO:0044772	mitotic cell cycle phase transition	7.59e-04
HIPK2	GO:0014014	negative regulation of gliogenesis	8.67e-04

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Related Drugs to HIPK2_GRM8

Drugs used for this fusion-positive patient.
(Manual curation of PubMed, 04-30-2022 + MyCancerGenome)

Hgene

Tgene

Drug

Source

PMID

Distribution of the number of studies mentioning HIPK2-GRM8 and kinase inhibitors the PubMed Abstract (04-01-2024)

Fusion gene - drug pair 1

Fusion gene - drug pair 2

PMID

Publication date

DOI

Study title

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Related Diseases to HIPK2_GRM8

Diseases that have this fusion gene.
(Manual curation of PubMed, 04-30-2022 + MyCancerGenome)

Hgene

Tgene

Disease

Source

PMID

Related diseases from the literature mentioned this fusion gene and drug.
(PubMed, 04-01-2024)

MeSH ID

MeSH term

Diseases associated with fusion partners.
(DisGeNet 4.0)

Partner

Gene

Disease ID

Disease name

# pubmeds

Source

Top

Clinical Trials of the Found Drugs/Small Molecules

Statistics of the Clinical Trials of the Found Kinase Inibitors from clinicaltrials.gov (06-17-2024)

Clinical Trials from clinicaltrials.gov (06-17-2024)

Fusion Gene

Kinase Inhibitor

NCT ID

Study Status

Phases

Disease

# Enrolment

Date