Tchem EPHB2 Ephrin type-B receptor 2

Protein Classes

DTO Classes

Protein / Kinase / Protein Kinase / Tk Group / Eph Family / Ephrin Type-b Receptor 2

Protein Summary

Description

Receptor tyrosine kinase which binds promiscuously transmembrane ephrin-B family ligands residing on adjacent cells, leading to contact-dependent bidirectional signaling into neighboring cells. The signaling pathway downstream of the receptor is referred to as forward signaling while the signaling pathway downstream of the ephrin ligand is referred to as reverse signaling. Functions in axon guidance during development. Involved in the guidance of commissural axons, that form a major interhemispheric connection between the 2 temporal lobes of the cerebral cortex. Also involved in guidance of contralateral inner ear efferent growth cones at the midline and of retinal ganglion cell axons to the optic disk. In addition to axon guidance, also regulates dendritic spines development and maturation and stimulates the formation of excitatory synapses. Upon activation by EFNB1, abolishes the ARHGEF15-mediated negative regulation on excitatory synapse formation. Controls other aspects of development including angiogenesis, palate development and in inner ear development through regulation of endolymph production. Forward and reverse signaling through the EFNB2/EPHB2 complex regulate movement and adhesion of cells that tubularize the urethra and septate the cloaca. May function as a tumor suppressor. This gene encodes a member of the Eph receptor family of receptor tyrosine kinase transmembrane glycoproteins. These receptors are composed of an N-terminal glycosylated ligand-binding domain, a transmembrane region and an intracellular kinase domain. They bind ligands called ephrins and are involved in diverse cellular processes including motility, division, and differentiation. A distinguishing characteristic of Eph-ephrin signaling is that both receptors and ligands are competent to transduce a signaling cascade, resulting in bidirectional signaling. This protein belongs to a subgroup of the Eph receptors called EphB. Proteins of this subgroup are distinguished from other members of the family by sequence homology and preferential binding affinity for membrane-bound ephrin-B ligands. Allelic variants are associated with prostate and brain cancer susceptibility. Alternative splicing results in multiple transcript variants. [provided by RefSeq, May 2015]

Uniprot Accession IDs

• P29323
• O43477
• Q5T0U6
• Q5T0U7
• Q5T0U8

Gene Name

• EPHB2

Ensembl ID

• ENST00000374630
• ENSP00000363761
• ENSG00000133216
• ENST00000374632
• ENSP00000363763
• ENST00000400191
• ENSP00000383053

Symbol

• DRT
• EPHT3
• EPTH3
• ERK
• HEK5
• TYRO5
• DRT
• EK5
• ERK
• CAPB
• Hek5
• PCBC
• EPHT3
• Tyro5

Knowledge Table

Most Knowledge About	Knowledge Value (0 to 1 scale)
co-expressed gene	1
protein domain	1
molecular function	0.99
transcription factor perturbation	0.88
biological process	0.86

IDG Development Level Summary

Tdark

These are targets about which virtually nothing is known. They do not have known drug or small molecule activities
- AND - satisfy two or more of the following criteria:

Pubmed score: 536.81   (req: < 5)

Gene RIFs: 74   (req: <= 3)

Antibodies: 611   (req: <= 50)

Tbio

These targets do not have known drug or small molecule activities
- AND - satisfy two or more of the following criteria:

Pubmed score: 536.81   (req: >= 5)

Gene RIFs: 74   (req: > 3)

Antibodies: 611   (req: > 50)

- OR - satisfy the following criterion:

Gene Ontology Terms: 52

Tchem

Target has at least one ChEMBL compound with an activity cutoff of < 30 nM - AND - satisfies the preceding conditions

Active Ligands: 8

Tclin

Target has at least one approved drug - AND - satisfies the preceding conditions

Active Drugs: 3

Approved Drugs (3)

Explore Approved Drugs

1 – 3 of 3

dasatinib

EPHB2Tchem Kinase

Kd: 9.41

bosutinib

EPHB2Tchem Kinase

Kd: 8.08

tivozanib

EPHB2Tchem Kinase

IC50: 7.76

Active Ligands (8)

Explore Active Ligands

1 – 8 of 8

CHEMBL1230609

EPHB2Tchem Kinase

Kd: 8.41

CHEMBL386051

EPHB2Tchem Kinase

Kd: 7.72

CHEMBL566515

EPHB2Tchem Kinase

IC50: 8.92000008

CHEMBL249097

EPHB2Tchem Kinase

Kd: 8.15

DDR1/2 inhibitor 5n

EPHB2Tchem Kinase

Kd: 6.59000015

compound 20 [PMID: 23489211]

EPHB2Tchem Kinase

IC50: 5.42000008

CHEMBL3426225

EPHB2Tchem Kinase

IC50: 7.58

CHEMBL3426917

EPHB2Tchem Kinase

IC50: 7.57

Protein Data Bank (4)

1 – 4 of 4

PDB Structure Id	Ligand	Method	Resolution (Å)	M.W. (kDa)	Pub Year	Title

PDB Structure Id	M.W.	Resolution	Pub Year

Pathways (208)

Reactome (6)

KEGG (1)

PathwayCommons (7)

WikiPathways (194)

Axon guidance (R-HSA-422475)

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Items per page:

5

1 – 5 of 6

Data Source	Name	Explore in Pharos	Explore in Source
Reactome	Axon guidance	533 targets	R-HSA-422475
Reactome	Developmental Biology	1055 targets	R-HSA-1266738
Reactome	EPH-Ephrin signaling	92 targets	R-HSA-2682334
Reactome	EPH-ephrin mediated repulsion of cells	49 targets	R-HSA-3928665
Reactome	Ephrin signaling	19 targets	R-HSA-3928664

Name	Explore in Pharos	Explore in Source
Axon guidance	533 targets	R-HSA-422475
Developmental Biology	1055 targets	R-HSA-1266738
EPH-Ephrin signaling	92 targets	R-HSA-2682334
EPH-ephrin mediated repulsion of cells	49 targets	R-HSA-3928665
Ephrin signaling	19 targets	R-HSA-3928664

Gene Ontology Terms (67)

Functions (10)

Components (15)

Processes (42)

Items per page:

10

1 – 10 of 10

GO Term	Evidence	Assigned by
protein tyrosine kinase activity	Inferred from Experiment (EXP)	Reactome
transmembrane receptor protein tyrosine kinase activity	Inferred from Biological aspect of Ancestor (IBA)	GO_Central
transmembrane signaling receptor activity	Inferred from Biological aspect of Ancestor (IBA)	GO_Central
amyloid-beta binding	Inferred from Sequence or structural Similarity (ISS)	ARUK-UCL
protein-containing complex binding	Inferred from Sequence or structural Similarity (ISS)	ARUK-UCL
transmembrane-ephrin receptor activity	Inferred from Sequence or structural Similarity (ISS)	UniProtKB
ATP binding	Inferred from Electronic Annotation (IEA)	UniProtKB-KW
axon guidance receptor activity	Inferred from Electronic Annotation (IEA)	Ensembl
identical protein binding	Inferred from Electronic Annotation (IEA)	Ensembl
signaling receptor binding	Inferred from Electronic Annotation (IEA)	Ensembl

Protein-Protein Interactions (245)

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1 – 10 of 245

• See Interactions on String-DB

SPSB2

Tbio

Novelty: 0.07794377

p_int: 0.999999981

p_ni: 1.7e-8

p_wrong: 2e-9

Score: 0.557

Data Source: BioPlex,STRINGDB

EFNB2

Tbio

Novelty: 0.00309066

p_int: 0.999999861

p_ni: 5.9e-8

p_wrong: 8e-8

Score: 0.999

Data Source: BioPlex,STRINGDB

MYCBP2

Tbio

Family: Enzyme

Novelty: 0.00336142

p_int: 0.999796533

p_ni: 0.000203468

Data Source: BioPlex

FBXO45

Tbio

Novelty: 0.08978487

p_int: 0.999685567

p_ni: 0.000305167

p_wrong: 0.000009266

Data Source: BioPlex

HSPA5

Tchem

Novelty: 0.00051387

p_int: 0.90002893

p_ni: 0.09997107

Score: 0.157

Data Source: BioPlex,STRINGDB

EFNA5

Tbio

Novelty: 0.00173565

Score: 0.999

Data Source: STRINGDB

EFNB1

Tbio

Novelty: 0.00491089

Score: 0.997

Data Source: STRINGDB

EFNA1

Tbio

Family: Kinase

Novelty: 0.00738582

Score: 0.993

Data Source: STRINGDB

EFNA3

Tbio

Novelty: 0.01717372

Score: 0.993

Data Source: STRINGDB

EFNA2

Tbio

Novelty: 0.0109729

Score: 0.993

Data Source: STRINGDB

Publication Statistics

PubMed Score  536.81

PubMed score by year

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PubTator Score  379.27

PubTator score by year

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Patents

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Amino Acid Sequence

Residue Counts

Sequence

MALRRLGAALLLLPLLAAVEETLMDSTTATAELGWMVHPPSGWEEVSGYDENMNTIRTYQVCNVFESSQN

1-70

NWLRTKFIRRRGAHRIHVEMKFSVRDCSSIPSVPGSCKETFNLYYYEADFDSATKTFPNWMENPWVKVDT

70-140

IAADESFSQVDLGGRVMKINTEVRSFGPVSRSGFYLAFQDYGGCMSLIAVRVFYRKCPRIIQNGAIFQET

140-210

LSGAESTSLVAARGSCIANAEEVDVPIKLYCNGDGEWLVPIGRCMCKAGFEAVENGTVCRGCPSGTFKAN

210-280

QGDEACTHCPINSRTTSEGATNCVCRNGYYRADLDPLDMPCTTIPSAPQAVISSVNETSLMLEWTPPRDS

280-350

GGREDLVYNIICKSCGSGRGACTRCGDNVQYAPRQLGLTEPRIYISDLLAHTQYTFEIQAVNGVTDQSPF

350-420

SPQFASVNITTNQAAPSAVSIMHQVSRTVDSITLSWSQPDQPNGVILDYELQYYEKELSEYNATAIKSPT

420-490

NTVTVQGLKAGAIYVFQVRARTVAGYGRYSGKMYFQTMTEAEYQTSIQEKLPLIIGSSAAGLVFLIAVVV

490-560

IAIVCNRRGFERADSEYTDKLQHYTSGHMTPGMKIYIDPFTYEDPNEAVREFAKEIDISCVKIEQVIGAG

560-630

EFGEVCSGHLKLPGKREIFVAIKTLKSGYTEKQRRDFLSEASIMGQFDHPNVIHLEGVVTKSTPVMIITE

630-700

FMENGSLDSFLRQNDGQFTVIQLVGMLRGIAAGMKYLADMNYVHRDLAARNILVNSNLVCKVSDFGLSRF

700-770

LEDDTSDPTYTSALGGKIPIRWTAPEAIQYRKFTSASDVWSYGIVMWEVMSYGERPYWDMTNQDVINAIE

770-840

QDYRLPPPMDCPSALHQLMLDCWQKDRNHRPKFGQIVNTLDKMIRNPNSLKAMAPLSSGINLPLLDRTIP

840-910

DYTSFNTVDEWLEAIKMGQYKESFANAGFTSFDVVSQMMMEDILRVGVTLAGHQKKILNSIQVMRAQMNQ

910-980

IQSVEGQPLARRPRATGRTKRCQPRDVTKKTCNSNDGKKKGMGKKKTDPGRGREIQGIFFKEDSHKESND

980-1050

CSCGG

1050-1055

MALRRLGAALLLLPLLAAVEETLMDSTTATAELGWMVHPPSGWEEVSGYDENMNTIRTYQVCNVFESSQNNWLRTKFIRRRGAHRIHVEMKFSVRDCSSIPSVPGSCKETFNLYYYEADFDSATKTFPNWMENPWVKVDTIAADESFSQVDLGGRVMKINTEVRSFGPVSRSGFYLAFQDYGGCMSLIAVRVFYRKCPRIIQNGAIFQETLSGAESTSLVAARGSCIANAEEVDVPIKLYCNGDGEWLVPIGRCMCKAGFEAVENGTVCRGCPSGTFKANQGDEACTHCPINSRTTSEGATNCVCRNGYYRADLDPLDMPCTTIPSAPQAVISSVNETSLMLEWTPPRDSGGREDLVYNIICKSCGSGRGACTRCGDNVQYAPRQLGLTEPRIYISDLLAHTQYTFEIQAVNGVTDQSPFSPQFASVNITTNQAAPSAVSIMHQVSRTVDSITLSWSQPDQPNGVILDYELQYYEKELSEYNATAIKSPTNTVTVQGLKAGAIYVFQVRARTVAGYGRYSGKMYFQTMTEAEYQTSIQEKLPLIIGSSAAGLVFLIAVVVIAIVCNRRGFERADSEYTDKLQHYTSGHMTPGMKIYIDPFTYEDPNEAVREFAKEIDISCVKIEQVIGAGEFGEVCSGHLKLPGKREIFVAIKTLKSGYTEKQRRDFLSEASIMGQFDHPNVIHLEGVVTKSTPVMIITEFMENGSLDSFLRQNDGQFTVIQLVGMLRGIAAGMKYLADMNYVHRDLAARNILVNSNLVCKVSDFGLSRFLEDDTSDPTYTSALGGKIPIRWTAPEAIQYRKFTSASDVWSYGIVMWEVMSYGERPYWDMTNQDVINAIEQDYRLPPPMDCPSALHQLMLDCWQKDRNHRPKFGQIVNTLDKMIRNPNSLKAMAPLSSGINLPLLDRTIPDYTSFNTVDEWLEAIKMGQYKESFANAGFTSFDVVSQMMMEDILRVGVTLAGHQKKILNSIQVMRAQMNQIQSVEGQPLARRPRATGRTKRCQPRDVTKKTCNSNDGKKKGMGKKKTDPGRGREIQGIFFKEDSHKESNDCSCGG

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Uniprot Keyword

3D-structure
Alternative splicing
ATP-binding
Cell membrane
Cell projection
Complete proteome
Developmental protein
Disease mutation
Disulfide bond
Glycoprotein