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  8. Activin receptor type-1B

Tchem Activin receptor type-1B

Transmembrane serine/threonine kinase activin type-1 receptor forming an activin receptor complex with activin receptor type-2 (ACVR2A or ACVR2B). Transduces the activin signal from the cell surface to the cytoplasm and is thus regulating a many physiological and pathological processes including neuronal differentiation and neuronal survival, hair follicle development and cycling, FSH production by the pituitary gland, wound healing, extracellular matrix production, immunosuppression and carcinogenesis. Activin is also thought to have a paracrine or autocrine role in follicular development in the ovary. Within the receptor complex, type-2 receptors (ACVR2A and/or ACVR2B) act as a primary activin receptors whereas the type-1 receptors like ACVR1B act as downstream transducers of activin signals. Activin binds to type-2 receptor at the plasma membrane and activates its serine-threonine kinase. The activated receptor type-2 then phosphorylates and activates the type-1 receptor such as ACVR1B. Once activated, the type-1 receptor binds and phosphorylates the SMAD proteins SMAD2 and SMAD3, on serine residues of the C-terminal tail. Soon after their association with the activin receptor and subsequent phosphorylation, SMAD2 and SMAD3 are released into the cytoplasm where they interact with the common partner SMAD4. This SMAD complex translocates into the nucleus where it mediates activin-induced transcription. Inhibitory SMAD7, which is recruited to ACVR1B through FKBP1A, can prevent the association of SMAD2 and SMAD3 with the activin receptor complex, thereby blocking the activin signal. Activin signal transduction is also antagonized by the binding to the receptor of inhibin-B via the IGSF1 inhibin coreceptor. ACVR1B also phosphorylates TDP2.

This gene encodes an activin A type IB receptor. Activins are dimeric growth and differentiation factors which belong to the transforming growth factor-beta (TGF-beta) superfamily of structurally related signaling proteins. Activins signal through a heteromeric complex of receptor serine kinases which include at least two type I and two type II receptors. This protein is a type I receptor which is essential for signaling. Mutations in this gene are associated with pituitary tumors. Alternate splicing results in multiple transcript variants.[provided by RefSeq, Jun 2010]

 Comments

Property Summary

Ligand Count 7
NCBI Gene PubMed Count 64
PubMed Score 91.16
PubTator Score 61.62

Knowledge Summary

Patent (13,317)

TINX Plot

  Disease (4)

Disease Target Count Z-score Confidence
Carcinoma 11493 0.0 1.2
Kidney cancer 2613 0.0 0.8
Disease Target Count Z-score Confidence
Cancer 2499 3.047 1.5
Disease Target Count
Carcinoma of pancreas 5

Expression

  Differential Expression (10)

Disease log2 FC p
adult high grade glioma -1.100 2.6e-03
astrocytic glioma -1.100 3.5e-03
atypical teratoid / rhabdoid tumor -1.200 2.6e-05
glioblastoma -1.100 6.8e-04
interstitial cystitis -1.200 3.9e-04
malignant mesothelioma -1.200 1.1e-05
osteosarcoma 1.382 1.7e-06
ovarian cancer 1.300 5.9e-04
psoriasis -1.200 2.4e-02
ulcerative colitis -1.300 1.6e-05

Synonym

Accession P36896 B7Z5L8 B7Z5W5 Q15479 Q15480 Q15481 Q15482
Symbols ALK4
SKR2
ACTRIB
ACVRLK4

Gene

ACVR1B

PANTHER Protein Class (4)

  Ortholog (10)

Species Source Disease
OMA EggNOG
Inparanoid OMA EggNOG
Inparanoid OMA EggNOG
Inparanoid OMA EggNOG
Inparanoid OMA EggNOG
Inparanoid OMA EggNOG
Inparanoid OMA EggNOG
Inparanoid OMA EggNOG
Inparanoid OMA
Inparanoid OMA

 UniProt Keyword (21)

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 GO Function (10)

 GO Component (7)

 GO Process (21)

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 Compartment GO Term (41)

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 IMPC Phenotype (12)

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 OMIM Phenotype (1)

 MGI Phenotype (13)

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 GWAS Trait (10)

 HCA RNA Cell Line (56)

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Pathway (17)

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Ligand (7)

Structure of CHEMBL492634

CHEMBL492634
pIC50 7.64

Structure of CHEMBL3260567

CHEMBL3260567
pIC50 7.89

Structure of CHEMBL1908395

CHEMBL1908395
pKd 8.00

Structure of compound 13d [PMID: 23639540]

compound 13d [PMID: 23639540]
pIC50 6.49

Structure of compound 13r [PMID: 23639540]

compound 13r [PMID: 23639540]
pIC50 6.74

Structure of galunisertib

galunisertib
pIC50 7.11

Structure of vactosertib

vactosertib
pIC50 7.89

Gene RIF (29)

AA Sequence 

MAESAGASSFFPLVVLLLAGSGGSGPRGVQALLCACTSCLQANYTCETDGACMVSIFNLDGMEHHVRTCI      1 - 70
PKVELVPAGKPFYCLSSEDLRNTHCCYTDYCNRIDLRVPSGHLKEPEHPSMWGPVELVGIIAGPVFLLFL     71 - 140
IIIIVFLVINYHQRVYHNRQRLDMEDPSCEMCLSKDKTLQDLVYDLSTSGSGSGLPLFVQRTVARTIVLQ    141 - 210
EIIGKGRFGEVWRGRWRGGDVAVKIFSSREERSWFREAEIYQTVMLRHENILGFIAADNKDNGTWTQLWL    211 - 280
VSDYHEHGSLFDYLNRYTVTIEGMIKLALSAASGLAHLHMEIVGTQGKPGIAHRDLKSKNILVKKNGMCA    281 - 350
IADLGLAVRHDAVTDTIDIAPNQRVGTKRYMAPEVLDETINMKHFDSFKCADIYALGLVYWEIARRCNSG    351 - 420
GVHEEYQLPYYDLVPSDPSIEEMRKVVCDQKLRPNIPNWWQSYEALRVMGKMMRECWYANGAARLTALRI    421 - 490
KKTLSQLSVQEDVKI                                                           491 - 505
//

Text Mined References (68)

PMID Year Title