Receptors for ACTIVINS are membrane protein kinases belonging to the family of PROTEIN-SERINE-THREONINE KINASES, thus also named activin receptor-like kinases (ALK's). Activin receptors also bind TRANSFORMING GROWTH FACTOR BETA. As those transmembrane receptors of the TGF-beta superfamily (RECEPTORS, TRANSFORMING GROWTH FACTOR BETA), ALK's consist of two different but related protein kinases, Type I and Type II. Activins initiate cellular signal transduction by first binding to the type II receptors (ACTIVIN RECEPTORS, TYPE II ) which then recruit and phosphorylate the type I receptors (ACTIVIN RECEPTORS, TYPE I ) with subsequent activation of the type I kinase activity.
Activin Receptors, Type II
Activin Receptors, Type I
Glycoproteins that inhibit pituitary FOLLICLE STIMULATING HORMONE secretion. Inhibins are secreted by the Sertoli cells of the testes, the granulosa cells of the ovarian follicles, the placenta, and other tissues. Inhibins and ACTIVINS are modulators of FOLLICLE STIMULATING HORMONE secretions; both groups belong to the TGF-beta superfamily, as the TRANSFORMING GROWTH FACTOR BETA. Inhibins consist of a disulfide-linked heterodimer with a unique alpha linked to either a beta A or a beta B subunit to form inhibin A or inhibin B, respectively
A broadly distributed protein that binds directly to ACTIVINS. It functions as an activin antagonist, inhibits FOLLICLE STIMULATING HORMONE secretion, regulates CELL DIFFERENTIATION, and plays an important role in embryogenesis. Follistatin is a single glycosylated polypeptide chain of approximately 37-kDa and is not a member of the inhibin family (INHIBINS). Follistatin also binds and neutralizes many members of the TRANSFORMING GROWTH FACTOR BETA family.
Receptors, Growth Factor
Receptors, Transforming Growth Factor beta
Cell-surface proteins that bind transforming growth factor beta and trigger changes influencing the behavior of cells. Two types of transforming growth factor receptors have been recognized. They differ in affinity for different members of the transforming growth factor beta family and in cellular mechanisms of action.
The founding member of the nodal signaling ligand family of proteins. Nodal protein was originally discovered in the region of the mouse embryo primitive streak referred to as HENSEN'S NODE. It is expressed asymmetrically on the left side in chordates and plays a critical role in the genesis of left-right asymmetry during vertebrate development.
Transforming Growth Factor beta
A factor synthesized in a wide variety of tissues. It acts synergistically with TGF-alpha in inducing phenotypic transformation and can also act as a negative autocrine growth factor. TGF-beta has a potential role in embryonal development, cellular differentiation, hormone secretion, and immune function. TGF-beta is found mostly as homodimer forms of separate gene products TGF-beta1, TGF-beta2 or TGF-beta3. Heterodimers composed of TGF-beta1 and 2 (TGF-beta1.2) or of TGF-beta2 and 3 (TGF-beta2.3) have been isolated. The TGF-beta proteins are synthesized as precursor proteins.
Bone Morphogenetic Proteins
Bone-growth regulatory factors that are members of the transforming growth factor-beta superfamily of proteins. They are synthesized as large precursor molecules which are cleaved by proteolytic enzymes. The active form can consist of a dimer of two identical proteins or a heterodimer of two related bone morphogenetic proteins.
A family of proteins that are involved in the translocation of signals from TGF-BETA RECEPTORS; BONE MORPHOGENETIC PROTEIN RECEPTORS; and other surface receptors to the CELL NUCLEUS. They were originally identified as a class of proteins that are related to the mothers against decapentaplegic protein, Drosophila and sma proteins from CAENORHABDITIS ELEGANS.
The intracellular transfer of information (biological activation/inhibition) through a signal pathway. In each signal transduction system, an activation/inhibition signal from a biologically active molecule (hormone, neurotransmitter) is mediated via the coupling of a receptor/enzyme to a second messenger system or to an ion channel. Signal transduction plays an important role in activating cellular functions, cell differentiation, and cell proliferation. Examples of signal transduction systems are the GAMMA-AMINOBUTYRIC ACID-postsynaptic receptor-calcium ion channel system, the receptor-mediated T-cell activation pathway, and the receptor-mediated activation of phospholipases. Those coupled to membrane depolarization or intracellular release of calcium include the receptor-mediated activation of cytotoxic functions in granulocytes and the synaptic potentiation of protein kinase activation. Some signal transduction pathways may be part of larger signal transduction pathways; for example, protein kinase activation is part of the platelet activation signal pathway.
Growth Differentiation Factors
RNA sequences that serve as templates for protein synthesis. Bacterial mRNAs are generally primary transcripts in that they do not require post-transcriptional processing. Eukaryotic mRNA is synthesized in the nucleus and must be exported to the cytoplasm for translation. Most eukaryotic mRNAs have a sequence of polyadenylic acid at the 3' end, referred to as the poly(A) tail. The function of this tail is not known for certain, but it may play a role in the export of mature mRNA from the nucleus as well as in helping stabilize some mRNA molecules by retarding their degradation in the cytoplasm.
Bone Morphogenetic Protein Receptors, Type I
Gene Expression Regulation, Developmental
In Situ Hybridization
Bone Morphogenetic Protein Receptors, Type II
Supporting cells for the developing female gamete in the OVARY. They are derived from the coelomic epithelial cells of the gonadal ridge. Granulosa cells form a single layer around the OOCYTE in the primordial ovarian follicle and advance to form a multilayered cumulus oophorus surrounding the OVUM in the Graafian follicle. The major functions of granulosa cells include the production of steroids and LH receptors (RECEPTORS, LH).
Molecular Sequence Data
Descriptions of specific amino acid, carbohydrate, or nucleotide sequences which have appeared in the published literature and/or are deposited in and maintained by databanks such as GENBANK, European Molecular Biology Laboratory (EMBL), National Biomedical Research Foundation (NBRF), or other sequence repositories.
The reproductive organ (GONADS) in female animals. In vertebrates, the ovary contains two functional parts: the OVARIAN FOLLICLE for the production of female germ cells (OOGENESIS); and the endocrine cells (GRANULOSA CELLS; THECA CELLS; and LUTEAL CELLS) for the production of ESTROGENS and PROGESTERONE.
Reverse Transcriptase Polymerase Chain Reaction
The processes occurring in early development that direct morphogenesis. They specify the body plan ensuring that cells will proceed to differentiate, grow, and diversify in size and shape at the correct relative positions. Included are axial patterning, segmentation, compartment specification, limb position, organ boundary patterning, blood vessel patterning, etc.
Amino Acid Sequence
Follicle Stimulating Hormone, beta Subunit
Receptors, Cell Surface
Cell surface proteins that bind signalling molecules external to the cell with high affinity and convert this extracellular event into one or more intracellular signals that alter the behavior of the target cell (From Alberts, Molecular Biology of the Cell, 2nd ed, pp693-5). Cell surface receptors, unlike enzymes, do not chemically alter their ligands.
Activin and TGFbeta limit murine primordial germ cell proliferation. (1/240)Mammalian primordial germ cells (PGCs) proliferate as they migrate from their initial location in the extraembryonic mesoderm to the genital ridge, the gonadal anlage. Once in the genital ridge, PGCs cease dividing and differentiate according to their gender. To identify ligands that might limit PGC proliferation, we analyzed growth factor receptors encoded in RNA obtained from purified germ cells shortly after their arrival in the genital ridge. Receptors for two members of the TGFbeta superfamily were found, TGFbeta1 and activin. As the signal-transducing domains of both receptor systems are highly conserved, the effects of both TGFbeta1 and activin on PGCs would be expected to be similar. We found that both ligands limited the accumulation of germ cells in primary PGC cultures. BrdU incorporation assays demonstrated that either ligand inhibits PGC proliferation. These results suggest that these signal transduction pathways are important elements of the mechanism that determines germ cell endowment. (+info)
Expression of inhibin/activin subunits and their receptors and binding proteins in human preimplantation embryos. (2/240)PURPOSE: Our purpose was to study the role of inhibin/activin during embryogenesis. METHODS: Transcripts of inhibin/activin subunits (alpha, beta A, beta B), activin receptors (types I and II), and follistatin were detected by a reverse transcriptase-polymerase chain reaction in human reproductive cells and preembryos cultured alone or co-cultured with human endometrial cells. RESULTS: Transcripts of alpha, beta A, beta B subunits were all detected in granulosa luteal cells, but only beta A units were detected in endometrial stromal and decidualized cells. In human preimplantation embryos, none of these subunits were detected in embryos from the four-cell to the morula stage and only beta A subunits were detectable in blastocyst embryos. Activin receptors were detectable in all of the studied embryos and cells. Transcripts of beta A, activin receptors, and follistatin were differentially expressed in human preimplantation embryos cultured in vitro and their expressions were significantly enhanced with the presence of endometrial stromal cells. CONCLUSIONS: Our data suggest that there is a possible endometrium-embryo interaction via endometrial activins and preimplantation embryo receptors and that the embryonic expressions of these activins, their receptors, and binding proteins are dependent on embryonic stage. (+info)
Assignment of transforming growth factor beta1 and beta3 and a third new ligand to the type I receptor ALK-1. (3/240)Germ line mutations in one of two distinct genes, endoglin or ALK-1, cause hereditary hemorrhagic telangiectasia (HHT), an autosomal dominant disorder of localized angiodysplasia. Both genes encode endothelial cell receptors for the transforming growth factor beta (TGF-beta) ligand superfamily. Endoglin has homology to the type III receptor, betaglycan, although its exact role in TGF-beta signaling is unclear. Activin receptor-like kinase 1 (ALK-1) has homology to the type I receptor family, but its ligand and corresponding type II receptor are unknown. In order to identify the ligand and type II receptor for ALK-1 and to investigate the role of endoglin in ALK-1 signaling, we devised a chimeric receptor signaling assay by exchanging the kinase domain of ALK-1 with either the TGF-beta type I receptor or the activin type IB receptor, both of which can activate an inducible PAI-1 promoter. We show that TGF-beta1 and TGF-beta3, as well as a third unknown ligand present in serum, can activate chimeric ALK-1. HHT-associated missense mutations in the ALK-1 extracellular domain abrogate signaling. The ALK-1/ligand interaction is mediated by the type II TGF-beta receptor for TGF-beta and most likely through the activin type II or type IIB receptors for the serum ligand. Endoglin is a bifunctional receptor partner since it can bind to ALK-1 as well as to type I TGF-beta receptor. These data suggest that HHT pathogenesis involves disruption of a complex network of positive and negative angiogenic factors, involving TGF-beta, a new unknown ligand, and their corresponding receptors. (+info)
Bone morphogenetic proteins regulate the developmental program of human hematopoietic stem cells. (4/240)The identification of molecules that regulate human hematopoietic stem cells has focused mainly on cytokines, of which very few are known to act directly on stem cells. Recent studies in lower organisms and the mouse have suggested that bone morphogenetic proteins (BMPs) may play a critical role in the specification of hematopoietic tissue from the mesodermal germ layer. Here we report that BMPs regulate the proliferation and differentiation of highly purified primitive human hematopoietic cells from adult and neonatal sources. Populations of rare CD34(+)CD38(-)Lin- stem cells were isolated from human hematopoietic tissue and were found to express the BMP type I receptors activin-like kinase (ALK)-3 and ALK-6, and their downstream transducers SMAD-1, -4, and -5. Treatment of isolated stem cell populations with soluble BMP-2, -4, and -7 induced dose-dependent changes in proliferation, clonogenicity, cell surface phenotype, and multilineage repopulation capacity after transplantation in nonobese diabetic/severe combined immunodeficient (NOD/SCID) mice. Similar to transforming growth factor beta, treatment of purified cells with BMP-2 or -7 at high concentrations inhibited proliferation yet maintained the primitive CD34(+)CD38(-) phenotype and repopulation capacity. In contrast, low concentrations of BMP-4 induced proliferation and differentiation of CD34(+) CD38(-)Lin- cells, whereas at higher concentrations BMP-4 extended the length of time that repopulation capacity could be maintained in ex vivo culture, indicating a direct effect on stem cell survival. The discovery that BMPs are capable of regulating repopulating cells provides a new pathway for controlling human stem cell development and a powerful model system for studying the biological mechanism of BMP action using primary human cells. (+info)
A quantitative analysis of signal transduction from activin receptor to nucleus and its relevance to morphogen gradient interpretation. (5/240)Previous work has shown that Xenopus blastula cells sense activin concentration by assessing the absolute number of occupied receptors per cell (100 and 300 molecules of bound activin activate Xbra and Xgsc transcription, respectively; a difference of only 3-fold). We now ask how quantitative differences in the absolute number of occupied receptors lead to the qualitatively distinct gene responses in the nucleus through SMAD2, a transducer of concentration-dependent gene responses to activin. We show that the injection of 0.2 or 0.6 ng of Smad2 mRNA activates Xbra or Xgsc transcription, respectively, involving, again, only a 3-fold difference. Furthermore, Xbra transcription is down-regulated by overexpression of SMAD2 as it is after activin signaling. We have developed a method to isolate nuclei from animal cap cells and subsequently have quantified the amount of nuclear SMAD2 protein. We find that the injection of 0.2 or 0.6 ng of Smad2 mRNA into an egg leads to only a 3-fold difference in the amount of SMAD2 protein in the nuclei of the blastula cells that express Xbra or Xgsc. We conclude that a 3-fold difference in the absolute number of occupied activin receptors can be maintained only as a 3-fold difference in the level of nuclear SMAD2 protein. Therefore, in this example of morphogen action, there appears to be no amplification of a key cytoplasmic transduction response, and a small but developmentally important change in extracellular signal concentration is relayed directly to the nucleus. (+info)
Activin family members in the developing chick retina: expression patterns, protein distribution, and in vitro effects. (6/240)We have investigated whether the activin family of growth factors is involved in the regulation of retinal cell differentiation. Immunocytochemistry and in situ hybridization have shown that activin/inhibin subunits alpha, betaA, and betaB; receptors II and IIB; follistatin; and a follistatin-like gene are expressed in different regions of the chick embryo retina in developmentally regulated patterns. When tested in dissociated retinal cultures, activin did not appear to affect cell survival or proliferation, but it exerted marked inhibitory effects on the differentiation of photoreceptors, while stimulating the differentiation of nonphotoreceptor neurons; both effects were concentration-dependent and follistatin-sensitive. The results are consistent with the possibility that activin family members play significant roles in the regulation of retinal development. (+info)
Smad3 inhibits transforming growth factor-beta and activin signaling by competing with Smad4 for FAST-2 binding. (7/240)Transcriptional regulation by transforming growth factor-beta and activin is mediated by interaction of Smad2 and Smad3 with specific transcription factors and/or DNA elements. However, Smad3 behaves differently from Smad2 in regulating transcription by a winged-helix transcription factor, FAST-2, on an activin-responsive element (ARE) in the Xenopus Mix.2 promoter. Smad3 alone was able to stimulate the ARE through FAST-2, but inhibited the ARE transactivation mediated by Smad2/Smad4 following receptor activation. We characterized the functional domains that are involved in these two activities of Smad3. Deletion of the MH1 domain as well as mutations of four lysine residues in the MH1 domain abrogated the inhibitory activity of Smad3, but did not compromise the self-stimulatory function. In contrast, deletion of the MH2 domain or a point mutation of glycine 379 within this domain obliterated the self-stimulatory activity of Smad3, but not the inhibitory activity. In an electrophoretic mobility shift assay, we found that Smad3 was able to associate with the FAST-2.ARE complex and that this association was dependent on FAST-2. In addition, Smad3 was not able to directly bind the ARE in a DNase I protection assay, in which FAST-2 binds the ARE around a motif (TGTGTATT) previously characterized to associate with the human FAST-1 protein. Interestingly, Smad4 was also able to directly associate with the FAST-2.ARE complex through binding with FAST-2. In a gel shift assay, the association of FAST-2 with Smad4 was mutually exclusive from the association with Smad3. Taken together, these data indicate that Smad3 exerts the inhibitory activity by competitive association with FAST-2. (+info)
Human activin-A is expressed in the atherosclerotic lesion and promotes the contractile phenotype of smooth muscle cells. (8/240)Activin is a member of the transforming growth factor-beta superfamily, and it modulates the proliferation and differentiation of various target cells. In this study, we investigated the role of activin in the initiation and progression of human atherosclerosis. The expression of activin, its physiological inhibitor follistatin, and activin receptors were assayed in human vascular tissue specimens that represented various stages of atherogenesis. In situ hybridization experiments revealed activin mRNA in endothelial cells and macrophages and a strong induction of activin expression in neointimal smooth muscle cells from the early onset of atherogenesis. We developed an "in situ free-activin binding assay" by using biotinylated follistatin, which allowed us to detect bioactive activin at specific sites in atherosclerotic lesions. The mRNAs encoding the activin receptors are expressed similarly in normal and atherosclerotic tissue, which indicates that activin-A signaling in atherogenesis is most likely dependent on changes in growth factor concentrations rather than on receptor levels. In vitro, activin induces the contractile, nonproliferative phenotype in cultured smooth muscle cells, as is reflected by increased expression of smooth muscle-specific markers (SMalpha-actin and SM22alpha). Our data provide evidence that activin induces redifferentiation of neointimal smooth muscle cells, and we hypothesize that activin is involved in plaque stabilization. (+info)
TGF-β 3 superfamily is a group of multifunctional cytokines that affect cell growth, differentiation, apoptosis, and morphogenesis (1, 2, 3) . This family consists of ,40 family members, including TGF-βs, activins, and BMPs. TGF-β superfamily ligands induce heteromeric complex formation of cognate type II and type I serine/threonine kinase receptors. Type II receptor kinases then phosphorylate serine and threonine residues in the GS domain of type I receptors, which results in the activation of type I receptor kinases (4) . Activated type I receptors signal into cytoplasm through phosphorylation of Smad proteins. Thus far, eight mammalian Smad proteins have been identified. Smad1, Smad2, Smad3, Smad5, and Smad8 are R-Smads, which are directly phosphorylated by type I receptors. Smad2 and Smad3 are activated by the TGF-β type I receptor and the activin type IB receptor, whereas Smad1, Smad5, and Smad8 are activated by BMP type I receptors and activin receptor-like kinase 1. Smad4 is a Co-Smad ...
Divergence and convergence of TGF-beta/BMP signaling
The transforming growth factor-beta (TGF-beta) superfamily includes more than 30 members which have a broad array of biological activities. TGF-beta superfamily ligands bind to type II and type I serine/threonine kinase receptors and transduce signals via Smad proteins. Receptor-regulated Smads (R-S …
DANRE:Q9PTF9 - GONUTS
8.0 8.1 Bauer, H et al. (2001) The type I serine/threonine kinase receptor Alk8/Lost-a-fin is required for Bmp2b/7 signal transduction during dorsoventral patterning of the zebrafish embryo. Development 128 849-58 PubMed GONUTS page ...
rat Habrec1 receptor Summary Report | CureHunter
rat Habrec1 receptor: a TGF-beta type I serine/threonine kinase receptor with a partially unique pattern of expression in the developing organism and adult; amino acid sequence given in first source
Human Activin receptor type-2A ELISA Kit
A Sandwich ELISA, Double Antibody ELISA kit for the detection of Homo sapiens, Human, Activin receptor type-2A, Activin receptor type IIA, ACTR-IIA, ACTRIIA, ACVR2A, ACVR2, 126.96.36.199
ACVR2A - Activin receptor type-2A precursor - Bos taurus (Bovine) - ACVR2A gene & protein
On ligand binding, forms a receptor complex consisting of two type II and two type I transmembrane serine/threonine kinases. Type II receptors phosphorylate and activate type I receptors which autophosphorylate, then bind and activate SMAD transcriptional regulators. Receptor for activin A, activin B and inhibin A. Mediates induction of adipogenesis by GDF6.
wen 23072 manual
Find the user manual you need for your tools and more at ManualsOnline. Flooring. Pages: 23072-23076 First Published: 04 September 2020 SiMe 3 and SiEt 3 phenoxy para ‐substituents in Cp*TiCl 2 (O‐2,6‐ i Pr 2 ‐4‐R‐C 6 H 2 ) show remarkable activity in ethylene copolymerizations with 2‐methyl‐1‐pentene, 1‐dodecene, and 9‐decen‐1‐ol. Recruits SMAD7 to ACVR1B which prevents the association of SMAD2 and SMAD3 with the activin receptor complex, thereby blocking the activin signal. Are you having trouble deciding which Wen rotary tool to use, the Wen 2305 vs 2307? Grey literature was not searched as double-reporting could not be ascertained. Contour TV Full TV experience: live & On Demand, voice remote, streaming apps and more! 24 Semiconducting, two-dimensional molybdenum disulfide (MoS2) is considered a promising new material for highly sensitive photodetection, because of its atomically thin profile and favorable bandgap. Pallavi Dubey, Sireesha Reddy, Sharron Manuel, Alok ...
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2h64 - Proteopedia, life in 3D
BACKGROUND: Bone morphogenetic proteins (BMPs) are key regulators in the embryonic development and postnatal tissue homeostasis in all animals. Loss of function or dysregulation of BMPs results in severe diseases or even lethality. Like transforming growth factors beta (TGF-betas), activins, growth and differentiation factors (GDFs) and other members of the TGF-beta superfamily, BMPs signal by assembling two types of serine/threonine-kinase receptor chains to form a hetero-oligomeric ligand-receptor complex. BMP ligand receptor interaction is highly promiscuous, i.e. BMPs bind more than one receptor of each subtype, and a receptor bind various ligands. The activin type II receptors are of particular interest, since they bind a large number of diverse ligands. In addition they act as high-affinity receptors for activins but are also low-affinity receptors for BMPs. ActR-II and ActR-IIB therefore represent an interesting example how affinity and specificity might be generated in a promiscuous ...
Acvrl1 - Serine/threonine-protein kinase receptor R3 precursor - Mus musculus (Mouse) - Acvrl1 gene & protein
Type I receptor for TGF-beta family ligands BMP9/GDF2 and BMP10 and important regulator of normal blood vessel development. On ligand binding, forms a receptor complex consisting of two type II and two type I transmembrane serine/threonine kinases. Type II receptors phosphorylate and activate type I receptors which autophosphorylate, then bind and activate SMAD transcriptional regulators. May bind activin as well.
TRIP Database - BMPR-2 / TRP channels
On ligand binding, forms a receptor complex consisting of two type II and two type I transmembrane serine/threonine kinases. Type II receptors phosphorylate and activate type I receptors which autophosphorylate, then bind and activate SMAD transcriptional regulators. Binds to BMP-7, BMP-2 and, less efficiently, BMP-4. Binding is weak but enhanced by the presence of type I receptors for BMPs ...
Mouse Monoclonal Antibody to BMPR1A - BidScientific.com
Supplier: ProMab Technologies Type of Product: Monoclonal Antibody Description: The bone morphogenetic protein (BMP) receptors are a family of transmembrane serine/threonine kinases that include the type I receptors BMPR1A and BMPR1B and the type II receptor BMPR2. These receptors are also closely related to the activi
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Activin A | Proteintech Group
Proteintechs Humankine Activin A is made from HEK293 human cells, conferring authentic glycosylation and folding in addition to superior stability and activity.
Májové bábätka 2009 - Prežívame to isté - str. 29
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RAP-011, an activin receptor ligand trap, increases hemoglobin concentration in hepcidin transgenic mice<...
TY - JOUR. T1 - RAP-011, an activin receptor ligand trap, increases hemoglobin concentration in hepcidin transgenic mice. AU - Langdon, Jacqueline M.. AU - Barkataki, Sangjucta. AU - Berger, Alan E.. AU - Cheadle, Chris. AU - Xue, Qian Li. AU - Sung, Victoria. AU - Roy, Cindy N.. PY - 2015/1/1. Y1 - 2015/1/1. N2 - Over expression of hepcidin antimicrobial peptide is a common feature of iron-restricted anemia in humans. We investigated the erythroid response to either erythropoietin or RAP-011, a murinized ortholog of sotatercept, in C57BL/6 mice and in hepcidin antimicrobial peptide 1 over expressing mice. Sotatercept, a soluble, activin receptor type IIA ligand trap, is currently being evaluated for the treatment of anemias associated with chronic renal disease, myelodysplastic syndrome, β-thalassemia, and Diamond Blackfan anemia and acts by inhibiting signaling downstream of activin and other Transforming Growth Factor-β superfamily members. We found that erythropoietin and RAP-011 ...
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Activin Receptor Type IIA兔多克隆抗体(ab124072)可与小鼠样本反应并经WB实验严格验证。所有产品均提供质保服务，中国75%以上现货。
Recombinant Human Activin Receptor Type IIA protein (ab114449) References
References for Abcams Recombinant Human Activin Receptor Type IIA protein (ab114449). Please let us know if you have used this product in your publication
Activin C antagonizes activin A in vitro and overexpression leads to pathologies in vivo<...
TY - JOUR. T1 - Activin C antagonizes activin A in vitro and overexpression leads to pathologies in vivo. AU - Gold, Elspeth Joan. AU - Jetly, Niti. AU - OBryan, Moira Kathleen. AU - Meachem, Sarah J. AU - Srinivasan, Deepa. AU - Behuria, Supreeti. AU - Sanchez-Partida, Luis Gabriel. AU - Woodruff, Teresa K. AU - Hedwards, Shelley Lee. AU - Wang, Hong. AU - McDougall, Helen. AU - Casey, Victoria. AU - Niranjan, Birunthi. AU - Patella, Shane. AU - Risbridger, Gail Petuna. PY - 2009. Y1 - 2009. N2 - Activin A is a potent growth and differentiation factor whose synthesis and bioactivity are tightly regulated. Both follistatin binding and inhibin subunit heterodimerization block access to the activin receptor and/or receptor activation. We postulated that the activin-beta(C) subunit provides another mechanism regulating activin bioactivity. To test our hypothesis, we examined the biological effects of activin C and produced mice that overexpress activin-beta(C). Activin C reduced activin A ...
Activin receptor type 1C / ACVR1C antibody | acris-antibodies.com
Activins are dimeric growth and differentiation factors which belong to the transforming growth factor-beta (TGF-beta) superfamily of structurally…
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Lagna G et al. (1996), Partnership between DPC4 and SMAD proteins in T... - Paper
The TGF-beta/activin/BMP superfamily of growth factors signals through heteromeric receptor complexes of type I and type II serine/threonine kinase receptors. The signal originated by TGF-beta-like molecules appears to be transduced by a set of evolutionarily conserved proteins known as SMADs, which upon activation directly translocate to the nucleus where they may activate transcription. Five SMAD proteins have so far been characterized in vertebrates. These factors are related to the mediator of decapentaplegic (dpp) signalling, mothers against dpp (Mad), in Drosophila and to the Sma genes from Caenorhabditis elegans. Smad1 and Smad2 have been shown to mimic the effects of BMP and activin, respectively, both in Xenopus and in mammalian cells, whereas Smad3 (a close homologue of Smad2) and the related protein DPC4, a tumour-suppressor gene product, mediate TGF-beta actions. We report here that DPC4 is essential for the function of Smad1 and Smad2 in pathways that signal mesoderm induction and ...
JCI - Biological basis for efficacy of activin receptor ligand traps in myelodysplastic syndromes
Signaling by the TGF-β superfamily is important in the regulation of hematopoiesis and is dysregulated in myelodysplastic syndromes (MDSs), contributing to ineffective hematopoiesis and clinical cytopenias. TGF-β, activins, and growth differentiation factors exert inhibitory effects on red cell formation by activating canonical SMAD2/3 pathway signaling. In this Review, we summarize evidence that overactivation of SMAD2/3 signaling pathways in MDSs causes anemia due to impaired erythroid maturation. We also describe the basis for biological activity of activin receptor ligand traps, novel fusion proteins such as luspatercept that are promising as erythroid maturation agents to alleviate anemia and related comorbidities in MDSs and other conditions characterized by impaired erythroid maturation.. ...
JCI - Biological basis for efficacy of activin receptor ligand traps in myelodysplastic syndromes
Signaling by the TGF-β superfamily is important in the regulation of hematopoiesis and is dysregulated in myelodysplastic syndromes (MDSs), contributing to ineffective hematopoiesis and clinical cytopenias. TGF-β, activins, and growth differentiation factors exert inhibitory effects on red cell formation by activating canonical SMAD2/3 pathway signaling. In this Review, we summarize evidence that overactivation of SMAD2/3 signaling pathways in MDSs causes anemia due to impaired erythroid maturation. We also describe the basis for biological activity of activin receptor ligand traps, novel fusion proteins such as luspatercept that are promising as erythroid maturation agents to alleviate anemia and related comorbidities in MDSs and other conditions characterized by impaired erythroid maturation.. ...
Cancers | Free Full-Text | Intertwining of Activin A and TGFβ Signaling: Dual Roles in Cancer Progression and Cancer Cell...
In recent years, a significant amount of research has examined the controversial role of activin A in cancer. Activin A, a member of the transforming growth factor β (TGFβ) superfamily, is best characterized for its function during embryogenesis in mesoderm cell fate differentiation and reproduction. During embryogenesis, TGFβ superfamily ligands, TGFβ, bone morphogenic proteins (BMPs) and activins, act as potent morphogens. Similar to TGFβs and BMPs, activin A is a protein that is highly systemically expressed during early embryogenesis; however, post-natal expression is overall reduced and remains under strict spatiotemporal regulation. Of importance, normal post-natal expression of activin A has been implicated in the migration and invasive properties of various immune cell types, as well as endometrial cells. Aberrant activin A signaling during development results in significant morphological defects and premature mortality. Interestingly, activin A has been found to have both oncogenic and
Gene Expression Literature Summary - MGI
J:22651 Manova K, De Leon V, Angeles M, Kalantry S, Giarre M, Attisano L, Wrana J, Bachvarova RF, mRNAs for activin receptors II and IIB are expressed in mouse oocytes and in the epiblast of pregastrula and gastrula stage mouse embryos. Mech Dev. 1995 Jan;49(1-2):3-11 ...
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Cripto - Wikipedia
Cripto is an EGF-CFC or epidermal growth factor-CFC, which is encoded by the Cryptic family 1 gene. Cryptic family protein 1B is a protein that in humans is encoded by the CFC1B gene. Cryptic family protein 1B acts as a receptor for the TGF beta signaling pathway. It has been associated with the translation of an extracellular protein for this pathway. The extracellular protein which Cripto encodes plays a crucial role in the development of left and right division of symmetry. Mutations of it could cause congenital heart disease. Crypto is a glycosylphosphatidylinositol-anchored co-receptor that binds nodal and the activin type I ActRIB (ALK)-4 receptor (ALK4). Cripto is composed of two adjacent cysteine-rich motifs: the EGF-like and the CFC of an N-terminal signal peptide and of a C-terminal hydrophobic region attached by a GPI anchor, which makes it a potentially essential element in the signaling pathway directing vertebrate embryo development. NMR data confirm that the CFC domain has a ...
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Pages 283-306 - David Foster Wallace Wiki : Infinite Jest
The book length of a punt is not the same as its physical distance. Hal kicked the baptismal competitive punt 90 yards in the air, but was only credited with a 40-yard punt. Because the line of scrimmage was Syracuses 40, and Hal kicked the ball through the end zone, the punt is recorded as 40 yards (the distance from the line of scrimmage to the end zone). The ball would be placed at Syracuses 20, so the net on the punt would only have been 20 yards. 90-yard punt ...
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Activin A is a TGF-β family member that exhibits a wide range of biological activities, including regulation of cellular proliferation
activin AB | Ligand page | IUPHAR/BPS Guide to PHARMACOLOGY
The IUPHAR/BPS Guide to Pharmacology. activin AB ligand page. Quantitative data and detailed annnotation of the targets of licensed and experimental drugs.
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Left-right axis malformations associated with mutations in ACVR2B, the gene for human activin receptor type IIB<...
TY - JOUR. T1 - Left-right axis malformations associated with mutations in ACVR2B, the gene for human activin receptor type IIB. AU - Kosaki, Rika. AU - Gebbia, Marinella. AU - Kosaki, Kenjiro. AU - Lewin, Mark. AU - Bowers, Peter. AU - Towbin, Jeffry A.. AU - Casey, Brett. PY - 1999/1/1. Y1 - 1999/1/1. N2 - Targeted disruption of the mouse activin receptor type IIB gene (Acvr2b) results in abnormal left-right (LR) axis development among Acvr2b(-/-) homozygotes [Oh and Li, 1997: Genes Dev 11:1812,1826]. The resulting malformations include atrial and ventricular septal defects, right-sided morphology of the left atrium and left lung, and spleen hypoplasia. Based on these results, we hypothesized that mutations in the type IIB activin receptor gene are associated with some cases of LR axis malformations in humans. We report here characterization of the ACVR2B genomic structure, analysis of ACVR2B splice variants, and screening for ACVR2B mutations among 112 sporadic and 14 familial cases of LR ...
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Loss of Heterozygosity and Mutational Analyses of the ACTRII Gene Locus in Human Colorectal Tumors<...
TY - JOUR. T1 - Loss of Heterozygosity and Mutational Analyses of the ACTRII Gene Locus in Human Colorectal Tumors. AU - Olaru, Andreea. AU - Mori, Yuriko. AU - Yin, Jing. AU - Wang, Suna. AU - Kimos, Martha C.. AU - Perry, Kellie. AU - Xu, Yan. AU - Sato, Fumiaki. AU - Selaru, Florin M.. AU - Deacu, Elena. AU - Sterian, Anca. AU - Shibata, David. AU - Abraham, John M.. AU - Meltzer, Stephen J.. N1 - Funding Information: This work was supported in part by United States Public Health Service Grants DK47717, CA95323, CA85069 and CA63670, and CA77057. Address reprint requests to: Dr. S. J. Meltzer, University of Maryland School of Medicine, 22 S. Greene St., Room N3W62, Baltimore, MD 21201. E-mail: [email protected] PY - 2003/12. Y1 - 2003/12. N2 - The activin type II receptor gene (ACTRII) is mutated in 58.1% of microsatellite-unstable (MSI-H) colorectal cancers and is a close relative of the TGFβ-1 type II receptor, which is known to be involved in both MSI-H and non-MSI-H ...
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Fig. 4. Hypertrophy response as measured via (A) body weight, (B) muscle weight change from sham group, after 4-wk treatment with ActRIIA-specific Ab, ActRIIB-specific Ab, combination thereof, and bimagrumab in SCID mice (n = 12 per group). Mice were untreated, sham group (white), or treated with weekly s.c. injection of isotype control antibody (20 mg/kg/wk) or of anti-ActRIIA Ab (CSJ089, blue, 6 or 20 mg/kg), an anti-ActRIIB Ab (CQI876, orange, 6 or 20 mg/kg), a combination of CSJ089 and CQI876 (black, 6 or 20 mg/kg of each Ab), or bimagrumab (green, 6 or 20 mg/kg). (C) Invasive muscle contractile function determination in gastrocnemius muscle of sham (white) and bimagrumab (green, 6 and 20 mg/kg)-treated groups, average of three stimulations. Hypertrophy response was measured through gastrocnemius and quadriceps muscle weight changes in SCID mice, (D) after 2-wk treatment with the same antibodies as in A, all dosed at 20 mg/kg, with CQI876 being also dosed at 100 mg/kg (orange crosses), (E) ...
NODAL - Wikipedia
Nodal is a secretory protein that in humans is encoded by the NODAL gene which is located on chromosome 10q22.1. It belongs to the Transforming Growth Factor (TGF-β) superfamily. Like many other members of this superfamily it is involved in cell differentiation in early embryogenesis, playing a key role in signal transfer from the node, in the anterior primitive streak, to lateral plate mesoderm (LPM). Nodal signaling is important very early in development for mesoderm and endoderm formation and subsequent organization of left-right axial structures. In addition, Nodal seems to have important functions in neural patterning, stem cell maintenance and many other developmental processes, including left/right handedness. Nodal can bind type I and type II Serine/Threonine kinase receptors, with Cripto-1 acting as its co-receptor. Signaling through SMAD 2/3 and subsequent translocation of SMAD 4 to the nucleus promotes the expression of genes involved in proliferation and differentiation. Nodal also ...
Researchers identify brain pathway linked with cocaine addiction | Addiction Professional Magazine
University at Buffalo researchers have identified a neural pathway that could hold a key to preventing relapse in individuals recovering from cocaine addiction. Their study focused on the activity of Activin receptors in the brain that are located in regions involved in pleasure and reward.. Published online June 1 in Nature Neuroscience, the study authored by Amy Gancarz, PhD, found that the Activin pathway controls the ability of cocaine to alter the connections between various neurons. By manipulating the activity of Activin receptors, researchers were able to change cocaine-taking behavior in animal models.. Understanding this critical pathway will help us pursue new directions in potential pharmacological and gene therapies to prevent drug relapses, senior author David Dietz, PhD, assistant professor at the university medical schools Department of Pharmacology and Toxicology, said in a June 18 news release.. ...
Structural basis for the inhibition of activin signalling by follistatin | The EMBO Journal
Previous structures of activin in complex with type II receptor domains showed the growth factor in two very different interprotomer conformations when compared to each other and to the canonical TGF‐β family members (Thompson et al, 2003; Greenwald et al, 2004). The structures presented here further emphasise the flexibility of activin A (Figure 7C). While the uncomplexed activin A is very similar to the activin A in the type II receptor complex structure by Greenwald et al (2004), in the Fs12 complex, the growth factor exhibits a more closed structure. Here, the fingers rotate away from the other protomer, pulling with them the interfacial α‐helix. β‐strands 1 and 2, which show the largest displacement compared to free activin, move by more than 20 Å at the tip of the fingers.. With four independent crystal structures of activin now available, it is likely that the observed conformational divergence from the canonical TGF‐β structures is a reflection of true structural plasticity ...
Acvr2b MGI Mouse Gene Detail - MGI:87912 - activin receptor IIB
View mouse Acvr2b Chr9:119402118-119434995 with: phenotypes, sequences, polymorphisms, proteins, references, function, expression
4213 Transforming growth factor-? (TGF-?) is a multifunctional cytokine which signals to the nucleus through cell surface transmembrane serine/threonine kinase receptors and cytoplasmic effectors, including Smad2, Smad3 and Smad4 proteins. The role of TGF-? in carcinogenesis is complex with tumor suppressor activities in early stages of disease and pro-oncogenic activities in advanced stages of invasive, metastatic disease. We recently identified a novel modulator of this pathway, TLP (TRAP-1-like protein), which associates with TGF-? receptors constitutively and with the common-mediator Smad4 upon ligand binding. We have shown that TLP regulates formation of Smad3/4 complexes and Smad3-dependent transcriptional responses. Since no inactivating mutations in Smad3 have been observed in human tumors, we hypothesized that proteins that regulate Smad3 function, such as TLP, rather than Smad3 itself might be direct targets of oncogenic change. To assess whether the expression of TLP might be ...
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Umair Z et al. (2020), Dusp1 modulates activin/smad2 mediated germ lay... - Paper
Activin, a member of the transforming growth factor (TGF-β) superfamily, induces mesoderm, endoderm and neuro-ectoderm formation in Xenopus embryos. Despite several previous studies, the complicated gene regulatory network and genes involved in this induction await more elaboration. We identified expression of various fibroblast growth factor (FGF) genes in activin/smad2 treated animal cap explants (AC) of Xenopus embryos. Activin/smad2 increased fgf3/8 expression, which was reduced by co-injection of dominant negative activin receptor (DNAR) and dominant negative Fgf receptor (DNFR). Interestingly, activin/smad2 also increased expression of dual specificity phosphatase 1 (dusp1) which has been known to inhibit Fgf signaling. Dusp1 overexpression in dorsal marginal zone caused gastrulation defect and decreased Jnk/Erk phosphorylation as well as Smad1 linker region phosphorylation. Dusp1 decreased neural and organizer gene expression with increasing of endodermal and ventral gene expression in ...
ACVR1B Protein, activin A receptor, type 1B - Creative BioMart
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 hete
FGF signaling is very important to the forming of mesoderm in - bcl-2 family members and the mitochondria in apoptosis
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Computational methods for designing potential inhibitors for activin type IIb (ActRIIB) receptor for treatment of anaemia |...
Anaemia is a clinical syndrome of blood characterized by decrease in the haemoglobin content in the red blood cells resulting in the marked reduction ..
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Activin type 2 receptors
The activin type 2 receptors belong to a larger TGF-beta receptor family and modulate signals for transforming growth factor ... inhibin/activin betaA and betaB and the activin type II and inhibin beta-glycan receptors in the developing human testis". ... A ligand binds to a type 2 receptor, which recruits and trans-phosphorylates a type I receptor. The type I receptor recruits a ... There are two activin type two receptors: ACVR2A and ACVR2B. Despite the large amount of processes that these ligands regulate ...
Activin type 1 receptors
There are three type I Activin receptors: ACVR1, ACVR1B, and ACVR1C. Each bind to a specific type II receptor-ligand complex. ... A ligand binds to a Type two receptor, which recruits and trans-phosphorylate a type I receptor. The type I receptor recruits a ... The Activin type I receptors transduce signals for a variety of members of the Transforming growth factor beta superfamily of ... This family of cytokines and hormones include activin, Anti-müllerian hormone (AMH), bone morphogenetic proteins (BMPs), and ...
An Activin receptor is a receptor which binds activin. Types include: Activin type 1 receptors Activin type 2 receptors These ... Activin+receptors at the US National Library of Medicine Medical Subject Headings (MeSH) This article incorporates text from ... Wrana JL, Attisano L, Wieser R, Ventura F, Massague J (1994). "Mechanism of activation of the TGF-beta receptor". Nature. 370 ( ... Massague J, Weis-Garcia F (1996). "Serine/threonine kinase receptors: mediators of transforming growth factor beta family ...
... is a receptor in the TGF beta signaling pathway. It is also known as activin receptor-like kinase 1, or ALK1. This gene ... "Activin receptor-like kinases: a novel subclass of cell-surface receptors with predicted serine/threonine kinase activity". ... "Identification of human activin and TGF beta type I receptors that form heteromeric kinase complexes with type II receptors". ... "Entrez Gene: ACVRL1 activin A receptor type II-like 1". Olivieri C, Mira E, Delù G, Pagella F, Zambelli A, Malvezzi L, ...
Activin receptor type-2B is a protein that in humans is encoded by the ACVR2B gene. ACVR2B is an activin type 2 receptor. ... This gene encodes activin A type IIB receptor, which displays a 3- to 4-fold higher affinity for the ligand than activin A type ... Schneider-Kolsky ME, Manuelpillai U, Waldron K, Dole A, Wallace EM (2002). "The distribution of activin and activin receptors ... II activin receptor genes during differentiation of human K562 cells and cDNA cloning of the human type IIB activin receptor". ...
... is an activin type 2 receptor. This gene encodes activin A type II receptor. Activins are dimeric growth and ... "Inhibin interferes with activin signaling at the level of the activin receptor complex in Chinese hamster ovary cells". ... "Variations in activin receptor, inhibin/activin subunit and follistatin mRNAs in human prostate tumour tissues". Br. J. Cancer ... "Truncated activin type II receptors inhibit bioactivity by the formation of heteromeric complexes with activin type I. ...
Activin A receptor type 2A (ACVR2A) is a transmembrane receptor that is involved in ligand-binding and mediates the functions ... "ACVR2A activin A receptor type 2A [Homo sapiens (human)] - Gene - NCBI". Gene. Bock, J B; Klumperman, J; Davanger, S; Scheller ... Bone morphogenetic protein receptor type 1A(BMPR1A) is expressed almost exclusively in skeletal muscle and is a transcriptional ... Fibroblast growth factor receptor 2 (FGFR2) plays an essential role in the regulation of osteoblast differentiation, ...
"Characterization of type I receptors for transforming growth factor-beta and activin". Science. 264 (5155): 101-4. Bibcode: ... kinase receptors: type I receptors of about 50-55 kD and type II receptors of about 70-80 kD. Type II receptors bind ligands in ... whereas type I receptors require their respective type II receptors for ligand binding. The BMPR1B receptor plays a role in the ... Receptors, Transmembrane receptors, S/T domain, EC 2.7.11). ... Bone morphogenetic protein receptor type-1B also known as ...
These receptors are also closely related to the activin receptors, ACVR1 and ACVR2. The ligands of these receptors are members ... kinase receptors: type I receptors of about 50-55 kD and type II receptors of about 70-80 kD. Type II receptors bind ligands in ... "Activin receptor-like kinases: a novel subclass of cell-surface receptors with predicted serine/threonine kinase activity". ... the absence of type I receptors, but they require their respective type I receptors for signaling, whereas type I receptors ...
2020 scientists reported that suppressing activin type 2 receptors-signalling proteins myostatin and activin A via activin A/ ... A two-week treatment of normal mice with soluble activin type IIB receptor, a molecule that is normally attached to cells and ... Myostatin binds to the activin type II receptor, resulting in a recruitment of either coreceptor Alk-3 or Alk-4. This ... Treating progeric mice with soluble activin receptor type IIB before the onset of premature ageing signs appear to protects ...
... resulting in phosphorylation of type I receptors by type II receptors. This gene encodes activin A type I receptor which ... Activin A receptor, type I (ACVR1) is a protein which in humans is encoded by the ACVR1 gene; also known as ALK-2 (activin ... "Activin receptor-like kinases: a novel subclass of cell-surface receptors with predicted serine/threonine kinase activity". ... and type II receptors are required for binding ligands and for expression of type I receptors. Type I and II receptors form a ...
Nuclear receptor 4A1
Engelse MA, Arkenbout EK, Pannekoek H, de Vries CJ (November 2003). "Activin and TR3 orphan receptor: two 'atheroprotective' ... The other two members are Nuclear receptor 4A2 (NR4A2) and Nuclear receptor 4A3 (NR4A3). Nuclear receptor 4A1 has a high degree ... The nuclear receptor 4A1 (NR4A1 for "nuclear receptor subfamily 4 group A member 1") also known as Nur77, TR3, and NGFI-B is a ... Nuclear receptor 4A1 has the systematic HUGO gene symbol NR4A1. It belongs to a group of three closely related orphan receptors ...
"Identification and characterization of a PDZ protein that interacts with activin type II receptors". J Biol Chem. 275 (8): 5485 ... 2003). "PKC regulates the delta2 glutamate receptor interaction with S-SCAM/MAGI-2 protein". Biochem. Biophys. Res. Commun. 301 ... 2001). "beta 1-adrenergic receptor association with the synaptic scaffolding protein membrane-associated guanylate kinase ... inverted-2 (MAGI-2). Differential regulation of receptor internalization by MAGI-2 and PSD-95". J. Biol. Chem. 276 (44): 41310- ...
2003). "Inhibin, activin, follistatin, activin receptors and beta-glycan gene expression in the placental tissue of patients ... Mathews LS, Vale WW (1991). "Expression cloning of an activin receptor, a predicted transmembrane serine kinase". Cell. 65 (6 ... 2003). "Activin betaC-subunit heterodimers provide a new mechanism of regulating activin levels in the prostate". Endocrinology ... 2001). "Localization of activin beta(A)-, beta(B)-, and beta(C)-subunits in humanprostate and evidence for formation of new ...
Fibrodysplasia ossificans progressiva
ACVR1 encodes activin receptor type-1, a BMP type-1 receptor. The mutation causes substitution of codon 206 from arginine to ... Normally, the ACVR1 gene encodes the activin receptor type-1 transmembrane kinase that bind BMP receptors (Type I BMPR and Type ... Regeneron announced new insight into the mechanism of disease involving the activation of the ACVR1 receptor by activin A. In ... "ACVR1 R206H receptor mutation causes fibrodysplasia ossificans progressiva by imparting responsiveness to activin A". Science ...
Mothers against decapentaplegic homolog 2
This protein can also be phosphorylated by activin type 1 receptor kinase, and mediates the signal from the activin. ... Lebrun JJ, Takabe K, Chen Y, Vale W (January 1999). "Roles of pathway-specific and inhibitory Smads in activin receptor ... This protein is recruited to the TGF-beta receptors through its interaction with the SMAD anchor for receptor activation (SARA ... O'Neill TJ, Zhu Y, Gustafson TA (April 1997). "Interaction of MAD2 with the carboxyl terminus of the insulin receptor but not ...
Mothers against decapentaplegic homolog 7
It is a TGFβ type 1 receptor antagonist. It blocks TGFβ1 and activin associating with the receptor, blocking access to SMAD2. ... By occupying type I receptors for Activin and bone morphogenetic protein (BMP), it also plays a role in negative feedback of ... Lebrun JJ, Takabe K, Chen Y, Vale W (January 1999). "Roles of pathway-specific and inhibitory Smads in activin receptor ... "Smurf1 interacts with transforming growth factor-beta type I receptor through Smad7 and induces receptor degradation". J. Biol ...
1997). "Inhibin interferes with activin signaling at the level of the activin receptor complex in Chinese hamster ovary cells ... Mathews LS, Vale WW (1991). "Expression cloning of an activin receptor, a predicted transmembrane serine kinase". Cell. 65 (6 ... From these receptors betaglycan (the TGF-β type III receptor) and InhBP/p120 (a membrane-tethered proteoglycan) were identified ... 2001). "Localization of activin beta(A)-, beta(B)-, and beta(C)-subunits in humanprostate and evidence for formation of new ...
Tan SM, Zhang Y, Connelly KA, Gilbert RE, Kelly DJ (May 2010). "Targeted inhibition of activin receptor-like kinase 5 signaling ... Lho Y, Do JY, Heo JY, Kim AY, Kim SW, Kang SH (April 2021). "Effects of TGF-β1 Receptor Inhibitor GW788388 on the Epithelial to ... GW 788388 is a synthetic compound which acts as a potent and selective inhibitor for TGF beta receptor 1. It has applications ... McMillin M, Grant S, Frampton G, Petrescu AD, Williams E, Jefferson B, DeMorrow S (May 2019). "The TGFβ1 Receptor Antagonist ...
"The Interpretation of Position in a Morphogen Gradient as Revealed by Occupancy of Activin Receptors". Cell. 93 (4): 557-568. ... The low receptor occupancy permits increases in receptor occupancy which alter the cell fate, but the high receptor affinity ... Receptors which initiate cell fate transduction cascades, in early embryo development, exhibit a ratchet effect in response to ...
2001). "The orphan receptor ALK7 and the Activin receptor ALK4 mediate signaling by Nodal proteins during vertebrate ... The activin A receptor also known as ACVR1C or ALK-7 is a protein that in humans is encoded by the ACVR1C gene. ACVR1C is a ... 2006). "Activin receptor-like kinase 7 induces apoptosis through up-regulation of Bax and down-regulation of Xiap in normal and ... 2004). "Activin receptor-like kinase-7 induces apoptosis through activation of MAPKs in a Smad3-dependent mechanism in hepatoma ...
Mir-24 microRNA precursor family
January 2008). "MicroRNA miR-24 inhibits erythropoiesis by targeting activin type I receptor ALK4". Blood. 111 (2): 588-95. doi ...
TGF beta 1
"Determination of type I receptor specificity by the type II receptors for TGF-beta or activin". Science. 262 (5135): 900-2. ... Oh SP, Seki T, Goss KA, Imamura T, Yi Y, Donahoe PK, Li L, Miyazono K, ten Dijke P, Kim S, Li E (March 2000). "Activin receptor ... It can also decrease the expression levels of cytokine receptors, such as the IL-2 receptor to down-regulate the activity of ... Chen W, Wahl SM (2002). "TGF-β: Receptors, Signaling Pathways and Autoimmunity". TGF-beta: receptors, signaling pathways and ...
TGF beta receptor 1
... activin A receptor type II-like kinase, 53kDa) is a membrane-bound TGF beta receptor protein of the TGF-beta receptor family ... "Entrez Gene: TGFBR1 transforming growth factor, beta receptor I (activin A receptor type II-like kinase, 53kDa)". Razani B, ... "Determination of type I receptor specificity by the type II receptors for TGF-beta or activin". Science. 262 (5135): 900-2. ... Oh SP, Seki T, Goss KA, Imamura T, Yi Y, Donahoe PK, Li L, Miyazono K, ten Dijke P, Kim S, Li E (March 2000). "Activin receptor ...
BMP influences AV node development through Alk3 receptor (Activin receptor-like kinase 3). Abnormalities seen in BMP and Alk3 ... and Morphology in the Atrioventricular Node of Mice With Atrioventricular Canal-Targeted Deletion of Alk3/Bmpr1a Receptor". ...
Rodgers, B.; Ward, C. (2022). "Myostatin/Activin Receptor Ligands In Muscle And The Development Status Of Attenuating Drugs". ... GDF11 can bind type I TGF-beta superfamily receptors ACVR1B (ALK4), TGFBR1 (ALK5) and ACVR1C (ALK7), but predominantly uses ... This cytokine also inhibits the proliferation of olfactory receptor neural progenitors to regulate the number of neurons in the ... Schneyer AL, Sidis Y, Gulati A, Sun JL, Keutmann H, Krasney PA (September 2008). "Differential antagonism of activin, myostatin ...
Lambert-Messerlian G, Eklund E, Pinar H, Tantravahi U, Schneyer AL (2007). "Activin subunit and receptor expression in normal ... Walsh S, Metter EJ, Ferrucci L, Roth SM (June 2007). "Activin-type II receptor B (ACVR2B) and follistatin haplotype ... activin complex reveals antagonism of both type I and type II receptor binding". Developmental Cell. 9 (4): 535-543. doi: ... In the blood, activin and follistatin are both known to be involved in the inflammatory response following tissue injury or ...
Nodal signaling pathway
In the cell surface Dapper2 tightly binds to the active form of the activin type 1 receptors and targets the receptor for ... Activation of the Nodal pathway involves nodal binding to activin and activin-like receptors which leads to phosphorylation of ... The binding of Nodal proteins to activin or activin-like serine/threonine kinase receptors results in the phosphorylation of ... Somehow the reduction of activin receptors would lead to the decrease in activity of different TGFb pathways. Smad proteins are ...
... and activin type II receptors balance BMP9 signals mediated by activin receptor-like kinase-1 in human pulmonary artery ... The physiological receptor of GDF2 is activin receptor-like kinase 1, ALK1 (also called ACVRL1), an endothelial-specific type I ... also known has Activin A receptor, type I (ACVR1), and the other type II receptors BMPRII and ActRIIA. GDF2 and BMP10 are the ... Endoglin, a type I membrane glycoprotein that forms the TGF-beta receptor complex, is a co-receptor of ALK1 for GDF2/BMP-9 ...
Bone morphogenetic protein 4
Feijen A, Goumans MJ, van den Eijnden-van Raaij AJ (December 1994). "Expression of activin subunits, activin receptors and ... Feijen A, Goumans MJ, van den Eijnden-van Raaij AJ (December 1994). "Expression of activin subunits, activin receptors and ... TGF-β family receptors most commonly use the Smad signaling pathway to tranduce signals. Type 2 receptors are responsible for ... TGF-β receptors induce the MAPK signaling pathways of ERK, JNK and p38. BMP4 is also known to activate the ERK, JNK and p38 ...
The downstream effectors of TGF-β are the Smad receptors (also known as receptor-activated Smads). Smad2 and Smad3 are ... and activin are involved in regulating important cellular functions such as proliferation, differentiation, apoptosis, and ... HSCs secrete angiopoietin, and its receptor molecule Tie2 has been implicated in angiogenesis of tumors in both humans and mice ... the presence of EVI1 in cancer has not been linked to aberrant production of any hormones or hormone receptors. It is likely ...
FSH enhances the production of androgen-binding protein by the Sertoli cells of the testes by binding to FSH receptors on their ... and enhanced by activin. FSH regulates the development, growth, pubertal maturation and reproductive processes of the human ... This presents possible use of FSH and FSH-receptor antagonists as an anti-tumor angiogenesis therapy (cf. avastin for current ... Eventually, the FSH level becomes so high that downregulation of FSH receptors occurs and by postmenopause any remaining small ...
October 2005). "Modulation of androgen receptor transactivation by FoxH1. A newly identified androgen receptor corepressor". ... Zhou S, Zawel L, Lengauer C, Kinzler KW, Vogelstein B (July 1998). "Characterization of human FAST-1, a TGF beta and activin ... FOXH1 encodes a human homolog of Xenopus forkhead activin signal transducer-1. FOXH1 protein binds SMAD2 and activates an ... "Smad4 and FAST-1 in the assembly of activin-responsive factor". Nature. 389 (6646): 85-89. Bibcode:1997Natur.389...85C. doi: ...
... has been shown to interact with its receptors corticotropin-releasing hormone receptor 1 (CRFR1 ... and activin A". Steroids. 68 (10-13): 801-807. doi:10.1016/S0039-128X(03)00137-5. PMID 14667971. S2CID 20953018. Vamvakopoulos ... "Localization of ligand-binding domains of human corticotropin-releasing factor receptor: a chimeric receptor approach". ... A CRH1 receptor antagonist developed by Pfizer, CP-154,526 is under investigation for the potential treatment of alcoholism. ...
Activin and Nodal ligands bind to their receptors and activate Smads that bind to DNA and promote gene transcription. Activin ... Therefore, there are four main transmembrane receptor types: G protein coupled receptors (GPCRs), tyrosine kinase receptors ( ... PAR1 and PAR4 receptors), platelet-derived thromboxane A2 (TxA2) (TP receptor) and ADP (P2Y1 and P2Y12 receptors) that is ... So, ZP3 can activate G protein coupled receptors and tyrosine kinase receptors, that leads to production of PLC. PLC cleaves ...
... such as the activin type 2 receptor; and bone morphogenetic protein receptor, type IA. Other LU domain proteins are small ... "Three-finger toxin fold for the extracellular ligand-binding domain of the type II activin receptor serine kinase". Nature ... Other receptors with LU domains include members of the transforming growth factor beta receptor (TGF-beta) superfamily, ... such as the nicotinic acetylcholine receptors, muscarinic acetylcholine receptors, and acetylcholinesterase. Another large ...
... such as the activin type 2 receptor; and bone morphogenetic protein receptor, type IA. Other LU domain proteins are small ... Besides uPAR, other receptors with LU domains include members of the transforming growth factor beta receptor (TGF-beta) ... "Three-finger toxin fold for the extracellular ligand-binding domain of the type II activin receptor serine kinase". Nature ... Behrendt N, Ploug M, Patthy L, Houen G, Blasi F, Danø K (April 1991). "The ligand-binding domain of the cell surface receptor ...
... is a recombinant fusion protein derived from human activin receptor type IIb (ActRIIb) linked to a protein derived ...
Lee, JH; Park, JW; Kim, SW; Park, J; Park, TS (15 December 2017). "C-X-C chemokine receptor type 4 (CXCR4) is a key receptor ... that are cultured for two days in the presence of FGF and Activin-A to adopt an epiblast-like state. These cells are then ... the PGCs express two CXCR4 transmembrane receptor proteins. The signaling system involving this protein and its ligand, Sdf1, ...
Teratocarcinoma-derived growth factor 1
2001). "The orphan receptor ALK7 and the Activin receptor ALK4 mediate signaling by Nodal proteins during vertebrate ...
... has been shown to interact with TGF beta receptor 1. GRCh38: Ensembl release 89: ENSG00000168522 - Ensembl, May 2017 ... 1996). "The p21(RAS) farnesyltransferase alpha subunit in TGF-beta and activin signaling". Science. 271 (5252): 1120-2. Bibcode ... 1996). "Interaction of the transforming growth factor-beta type I receptor with farnesyl-protein transferase-alpha". J. Biol. ... "Interaction of the transforming growth factor-beta type I receptor with farnesyl-protein transferase-alpha". J. Biol. Chem. ...
Genes such as activin ß-A, which encodes a subunit of activin A, are up-regulated during early stage LTP. The activin molecule ... In a dynamic process that is maintained in equilibrium, N-methyl D-aspartate receptor (NMDA receptor) and AMPA receptors are ... Insertion or removal of post-synaptic AMPA receptors. Phosphorylation and de-phosphorylation inducing a change in AMPA receptor ... These activated protein kinases serve to phosphorylate post-synaptic excitatory receptors (e.g. AMPA receptors), improving ...
NK2 homeobox 1
NKX2.1 can be induced by activin A via SMAD2 signaling in a human embryonic stem cell differentiation model. NKX2.1 is key to ... Yan C, Naltner A, Conkright J, Ghaffari M (June 2001). "Protein-protein interaction of retinoic acid receptor alpha and thyroid ... Naltner A, Wert S, Whitsett JA, Yan C (December 2000). "Temporal/spatial expression of nuclear receptor coactivators in the ...
AMH binds to its Type 2 receptor AMHR2, which phosphorylates a type I receptor under the TGF beta signaling pathway. In male ... and activin A in follicular fluid in IVF/ICSI patients for assessing the maturation and developmental potential of oocytes". ... anti-Müllerian hormone receptors). The best-known and most specific effect, mediated through the AMH type II receptors, ... Functional AMH receptors have also been found to be expressed in neurons in the brains of embryonic mice, and are thought to ...
TNF receptor superfamily (TNFRs), T-cell receptor (TCR), Epidermal growth factor receptor (EGFR), and TGF beta receptor (TGFβR ... September 2003). "A role for MEK kinase 1 in TGF-beta/activin-induced epithelium movement and embryonic eyelid closure". The ... April 1998). "hUBC9 associates with MEKK1 and type I TNF-alpha receptor and stimulates NFkappaB activity". FEBS Letters. 425 (3 ... September 2006). "Key function for the Ubc13 E2 ubiquitin-conjugating enzyme in immune receptor signaling". Nature Immunology. ...
The drug is a synthetic androgen and anabolic steroid and hence is an agonist of the androgen receptor (AR), the biological ... NPP is or has been marketed under a variety of brand names including Durabolin, Fenobolin, Activin, Deca-Durabolin, Evabolin, ... As such, it is an androgen and anabolic steroid, or an agonist of the androgen receptor, the biological target of androgens ... 25-. ISBN 978-1-59259-388-0. Gao W, Bohl CE, Dalton JT (2005). "Chemistry and structural biology of androgen receptor". Chem. ...
BMP and activin membrane-bound inhibitor homolog (Xenopus laevis), also known as BAMBI, is a protein which in humans is encoded ... This gene encodes a transmembrane glycoprotein related to the type I receptors of the transforming growth factor-beta (TGF beta ... "Entrez Gene: BMP and activin membrane-bound inhibitor homolog (Xenopus laevis)". Degen WG, Weterman MA, van Groningen JJ, ... 2008). "The pseudoreceptor BMP and activin membrane-bound inhibitor positively modulates Wnt/beta-catenin signaling". J. Biol. ...
TGF beta signaling pathway
In mammals there are seven known type I receptors and five type II receptors. There are three activins: Activin A, Activin B ... It can then either form a receptor complex with activin A receptor, type IB (ACVR1B) or with activin A receptor, type IC ( ... They bind to TGF-beta receptor type-2 (TGFBR2). Nodal binds to activin A receptor, type IIB ACVR2B. ... The type II receptor is a serine/threonine receptor kinase, which catalyzes the phosphorylation of the Type I receptor. Each ...
Mir-367 microRNA precursor family
Tsai ZY, Singh S, Yu SL, Kao LP, Chen BZ, Ho BC, Yang PC, Li SS (Jan 2010). "Identification of microRNAs regulated by activin A ... "Functional SNP in the microRNA-367 binding site in the 3'UTR of the calcium channel ryanodine receptor gene 3 (RYR3) affects ...
Crypto is a glycosylphosphatidylinositol-anchored co-receptor that binds nodal and the activin type I ActRIB (ALK)-4 receptor ( ... In the Nodal signaling pathway of embryonic development, Cripto has been shown to have dual function as a co-receptor as well ... Cryptic family protein 1B acts as a receptor for the TGF beta signaling pathway. It has been associated with the translation of ... EGF-CFC proteins' composition as a receptor complex is further solidified by the GPI linkage, making the cell membrane ...
The cause of the disease was traced to a single mutation in the activin A receptor, type I gene. Once the cause of the disease ... "A recurrent mutation in the BMP type I receptor ACVR1 causes inherited and sporadic fibrodysplasia ossificans progressiva". ... "A recurrent mutation in the BMP type I receptor ACVR1 causes inherited and sporadic fibrodysplasia ossificans progressiva". ... "A recurrent mutation in the BMP type I receptor ACVR1 causes inherited and sporadic fibrodysplasia ossificans progressiva". ...
ACVR2B activin A receptor type 2B [Homo sapiens (human)] - Gene - NCBI
Activin Type IIB Receptor. pfam01064. Location:41 → 110. Activin_recp; Activin types I and II receptor domain. ... Activin Type IIB Receptor. pfam01064. Location:47 → 116. Activin_recp; Activin types I and II receptor domain. ... Activin Type IIB Receptor. pfam01064. Location:48 → 138. Activin_recp; Activin types I and II receptor domain. ... activin receptor type-2B. Names. activin A receptor, type IIB. NP_001097.2. *EC 188.8.131.52 ...
Activin Receptors, Type I | Profiles RNS
One of the two types of ACTIVIN RECEPTORS or activin receptor-like kinases (ALKS). There are several type I activin receptors ... "Activin Receptors, Type I" by people in this website by year, and whether "Activin Receptors, Type I" was a major or minor ... Receptors, Transforming Growth Factor beta [D12.776.543.750.750.400.820]. *Activin Receptors [D12.776.543.750.750.400.820.500] ... In the absence of type III receptor, the transforming growth factor (TGF)-beta type II-B receptor requires the type I receptor ...
Inhibition of the Activin Receptor Type-2B Pathway Restores Regenerative Capacity in Satellite Cell-Depleted Skeletal Muscle -...
RePub, Erasmus University Repository: Activin receptor-like kinase 1 ligand trap reduces microvascular density and improves...
BioCryst Pharmaceuticals Inc - Research and Markets - Page 5
The role of activin type I receptors in activin A-induced growth arrest and apoptosis in mouse B-cell hybridoma cells<...
Activins transduce their signals by binding to activin type I receptors and activin type II receptors, both of which contain a ... N2 - Activins transduce their signals by binding to activin type I receptors and activin type II receptors, both of which ... AB - Activins transduce their signals by binding to activin type I receptors and activin type II receptors, both of which ... abstract = "Activins transduce their signals by binding to activin type I receptors and activin type II receptors, both of ...
Osler-Weber-Rendu Disease (Hereditary Hemorrhagic Telangiectasia) Workup: Approach Considerations, Laboratory Studies, Oximetry
Mutations in the activin receptor-like kinase 1 gene in hereditary haemorrhagic telangiectasia type 2. Nat Genet. 1996 Jun. 13 ... Identification of BMP9 and BMP10 as functional activators of the orphan activin receptor-like kinase 1 (ALK1) in endothelial ... found on chromosome 9 and the activin receptorlike kinase type I (ALK-1) gene (ALK1) found on chromosome 12. These tests should ...
Identification of a novel mutation in activin receptor type 1 (ACVR1) in a fibrodysplasia ossificans progressiva (FOP) patient ...
Fibrodysplasia Ossificans Progressiva: Practice Essentials, Pathophysiology, Epidemiology
An Activin Receptor IA/Activin-Like Kinase-2 (R206H) Mutation in Fibrodysplasia Ossificans Progressiva. Case Rep Genet. 2013. ... A novel mutation in the activin A type 1 receptor gene was described in one patient.  Analysis showed that the patient was ... which encodes a type I BMP transmembrane receptor. A recurrent mutation in the BMP type I receptor ACVR1 causes inherited and ... A recurrent mutation in the BMP type I receptor ACVR1 causes inherited and sporadic fibrodysplasia ossificans progressiva. Nat ...
Besides "de novo protein design" are we doing also a lot of benchmarks?
activin receptor, tgfr... If I look for a PDP structure of these proteins, I always found the crystal structure of them. If you ... activin receptor, tgfr... If I look for a PDP structure of these proteins, I always found the crystal structure of them (and ... Sctructures of tgfbR2 and activin_receptorII are already known so I suppose the second one is being designed de novo (probably ...
Publications | Crick
β-Thalassemia | Genetics in Medicine
A modified activin type IIB receptor inhibiting signaling induced by some members of the TGF-β superfamily promotes maturation ... Modified activin receptor IIB ligand trap mitigates ineffective erythropoiesis and disease complications in murine β- ... Activins, members of TGF-β family signaling, are key regulators of human hematopoiesis and modulate various cellular responses ...
lung small cell carcinoma - Ontology Report - Rat Genome Database
activin A receptor type 1B. ISO. RGD. PMID:33880365. RGD:151665493. NCBI chr 7:132,286,266...132,329,679 Ensembl chr 7: ... Eph receptor A7. ISO. CTD Direct Evidence: marker/mechanism. CTD. PMID:22941188. NCBI chr 5:42,975,353...43,128,703 Ensembl chr ... glutamate ionotropic receptor kainate type subunit 3. ISO. CTD Direct Evidence: marker/mechanism. CTD. PMID:22941189. NCBI chr ... KIT proto-oncogene receptor tyrosine kinase. ISO. CTD Direct Evidence: marker/mechanism. CTD. PMID:15499612. NCBI chr14: ...
Cell line - CECR2 - The Human Protein Atlas
Esophageal squamous cell carcinoma invasion is inhibited by Activin A in ACVRIB-positive cells | BMC Cancer | Full Text
... the Activin type I receptor. We found that overexpression of stromal-derived Activin A inhibited invasion of esophageal ... The objective of this study was to investigate the role of Activin A signaling in ESCC. To investigate the role Activin A plays ... in the context of fibroblast-secreted Activin A, to identify the effects of Activin A on cell invasion and determine protein ... In recent years, the ligand Activin A has been implicated as a player in the progression of a number of cancers. ...
Rogers CD et al. (2009), Xenopus Sox3 activates sox2 and geminin and ind... - Paper
Dorsomorphin: Uses, Interactions, Mechanism of Action | DrugBank Online
UActivin receptor type-1. Not Available. Humans. UPeptidyl-prolyl cis-trans isomerase FKBP1A. Not Available. Humans. ... Type II receptors phosphorylate and activate type I receptors which auto.... Gene Name. ACVR1. Uniprot ID. Q04771. Uniprot Name ... Transmembrane receptor protein serine/threonine kinase activity. Specific Function. On ligand binding, forms a receptor complex ... Keeps in an inactive conformation TGFBR1, the TGF-beta type I serine/threonine kinase receptor, preventing TGF-beta receptor ...
The Prohibited List | World Anti Doping Agency
Activin receptor IIB competitors such as: *Decoy activin receptors (e.g. ACE-031) ... Anti-activin receptor IIB antibodies (e.g. bimagrumab). *Myostatin inhibitors such as: *Agents reducing or ablating myostatin ... Peroxisome proliferator-activated receptor delta (PPARδ) agonists, e.g. 2-(2-methyl-4-((4-methyl-2-(4-(trifluoromethyl)phenyl) ... Selective androgen receptor modulators [SARMs, e.g. andarine, LGD-4033 (ligan- drol)enobosarm (ostarine) and RAD140] ...
Cancers | Free Full-Text | Differentially Expressed MicroRNAs in Meningiomas Grades I and II Suggest Shared Biomarkers with...
SMART: STYKc domain annotation
Crystal structure of Activin receptor type II kinase domain from human. 2rio. Structure of the dual enzyme Ire1 reveals the ... TGF-beta Receptor type 1 in complex with SB431542. 3uim. Structural basis for the impact of phosphorylation on plant receptor- ... Crystal structure of Activin receptor type-IIA (ACVR2A) kinase domain in complex with a beta-carboline inhibitor. ... Crystal structure of Activin receptor type-IIA (ACVR2A) kinase domain in complex with a quinazolin. ...
NIOSHTIC-2 Search Results - Full View
... activin receptor-like kinase 5 (ALK5) receptor] and TGF-Beta/Smad signaling pathway in CNT-induced collagen production in human ... In this study, we investigated the activation of transforming growth factor-beta receptor-1 [TGF-Beta R1; i.e., ... Identification of TGF-beta receptor-1 as a key regulator of carbon nanotube-induced fibrogenesis. ...
Mutation Detection in Activin A Receptor, Type I (ACVR1) Gene in Fibrodysplasia Ossificans Progressiva in An Iranian Family ... The mutation c.617G,A in the Activin A receptor, type I (ACVR1) gene was found in all previously reported patients with FOP. ... An agonist of this receptor (GCS) decreases the cytotoxcity of MDMA, while the antagonist of this receptor (SCH) increases its ... The peroxisome proliferator-activated receptors (PPARs) are a group of nu- clear receptor proteins whose functions as ...
Momelotinib dosing, indications, interactions, adverse effects, and more
Results for 'Excretory system development' | Abcam: antibodies, proteins, kits...
Staff Profile - Faculty of Medical Sciences - Newcastle University
BNIP similar (Cytokines & Cells Encyclopedia - COPE)
Characterization and differential expression of microRNAs in the ovaries of pregnant and non-pregnant goats (Capra hircus) |...
... and let-7b may target the Activin receptor I and Smad 2/3 genes in the TGF-beta signaling pathway. The expression level of 5 ... Further analysis showed that miR-143 was predicted to bind to the target sequences of Frizzled-6 and -3 receptor genes in the ... C, D) Activin receptor I (AR type I) and Smad 2/3 were predicted as potential targets of let-7b. ... may target the Activin receptor I and Smad 2/3 genes in the TGF-beta signaling pathway (Figure 6C and D), and affect mammalian ...
- Activins transduce their signals by binding to activin type I receptors and activin type II receptors, both of which contain a serine/threonine kinase domain. (elsevier.com)
- Over-expression of ActRI suppressed activin A-induced cell-cycle arrest in the G1 phase caused by inhibition of retinoblastoma protein phosphorylation through induction of p21(CIP1/WAF1), a cyclin-dependent kinase inhibitor, and subsequent apoptosis. (elsevier.com)
- At specific centers and laboratories, genetic tests are available for various mutations in the endoglin gene ( ENG ) found on chromosome 9 and the activin receptorlike kinase type I (ALK-1) gene ( ALK1 ) found on chromosome 12. (medscape.com)
- Structure of the FGF receptor tyrosine kinase domain reveals a novel autoinhibitory mechanism. (embl-heidelberg.de)
- The crystal structure of the tyrosine kinase domain of fibroblast growth factor receptor 1 (FGFR1K) has been determined in its unliganded form to 2.0 angstroms resolution and in complex with with an ATP analog to 2.3 angstrosms A resolution. (embl-heidelberg.de)
- Several features distinguish the structure of FGFR1K from that of the tyrosine kinase domain of the insulin receptor. (embl-heidelberg.de)
- Finally, the structure provides a basis for rationalizing the effects of kinase mutations in FGF receptors that lead to developmental disorders in nematodes and humans. (embl-heidelberg.de)
- In mammals, they bind to the GDNF family receptor α (Gfrα) and signal through the Ret receptor tyrosine kinase. (sdbonline.org)
- Therefore, a mouse model was developed with a genetics-based approach that conditionally deleted the causative activin receptor-like kinase 1 ( Acvrl1 or Alk1 ) gene. (thejns.org)
- i.e., activin receptor-like kinase 5 (ALK5) receptor] and TGF-Beta/Smad signaling pathway in CNT-induced collagen production in human lung fibroblasts. (cdc.gov)
- Taken from the article 'Targeting tumour vasculature by inhibiting activing receptor-like kinase (ALK)1 function' by de Vinuesa et al. (portlandpress.com)
- Bone morphogenetic protein (BMP)9 and BMP10 are high affinity ligands for activin receptor-like kinase 1 (ALK1), a type I BMP receptor mainly expressed on vascular endothelial cells (ECs). (portlandpress.com)
- M4K2163 is a potent and selective activin receptor-like kinase 2 (ALK2) inhibitor (IC 50 values are 19 nM in vivo and 98 nM in vitro ). (tocris.com)
- Activins initiate cellular signal transduction by first binding to the type II receptors (ACTIVIN RECEPTORS, TYPE II ) which then recruit and phosphorylate the type I receptors (ACTIVIN RECEPTORS, TYPE I ) with subsequent activation of the type I kinase activity. (bvsalud.org)
- Further analysis showed that miR-143 was predicted to bind to the target sequences of Frizzled-6 and -3 receptor genes in the Wnt/beta-catenin signaling pathway, and let-7b may target the Activin receptor I and Smad 2/3 genes in the TGF-beta signaling pathway. (biomedcentral.com)
- A schematic representation of TGF-β and BMP9 signalling in endothelial cells via their serine/threonine type I and type II receptors, co-receptor endoglin and downstream Smad intracellular proteins. (portlandpress.com)
- A study by deKruijf and colleagues [ 8 ] showed that high levels of TGF-β receptor expression in conjunction with Smad expression conferred an unfavorable prognosis after breast cancer diagnosis. (cdc.gov)
- One study has shown that BMP-Smad activation is involved in the progression of estrogen receptor positive (ER+) breast cancers specifically [ 13 ]. (cdc.gov)
- These receptors are all transmembrane proteins, composed of a ligand-binding extracellular domain with cysteine-rich region, a transmembrane domain, and a cytoplasmic domain with predicted serine/threonine specificity. (nih.gov)
- Type I and II receptors form a stable complex after ligand binding, resulting in phosphorylation of type I receptors by type II receptors. (nih.gov)
- This gene encodes activin A type IIB receptor, which displays a 3- to 4-fold higher affinity for the ligand than activin A type II receptor. (nih.gov)
- In recent years, the ligand Activin A has been implicated as a player in the progression of a number of cancers. (biomedcentral.com)
- Predicated on series homology, ligand framework or receptor function, GPCRs are categorized into several hundred subfamilies. (mdm2-inhibitors.com)
Type I receptor3
- In the absence of type III receptor, the transforming growth factor (TGF)-beta type II-B receptor requires the type I receptor to bind TGF-beta2. (umassmed.edu)
- A recurrent mutation in the BMP type I receptor ACVR1 causes inherited and sporadic fibrodysplasia ossificans progressiva. (medscape.com)
- Analysis of ESCC patient samples indicated that patients with high stromal Activin A expression had low epithelial ACVRIB, the Activin type I receptor. (biomedcentral.com)
- Activin A and Acvr2b mRNA from Umbilical Cord Blood Are Not Reliable Markers of Mild or Moderate Neonatal Hypoxic-Ischemic Encephalopathy. (nih.gov)
- Treatment of these mice with an Activin receptor type-2B (AcvR2B) pathway blocker reverses muscle fiber atrophy as expected, but also restores regenerative potential of the remaining satellite cells. (pasteur.fr)
- The BMPR2 gene provides instructions for making a protein called bone morphogenetic protein receptor type 2. (medlineplus.gov)
- The genetic cause of fibrodysplasia ossificans progressiva lies within the ACVR1 gene, which encodes a type I BMP transmembrane receptor. (medscape.com)
- A novel mutation in the activin A type 1 receptor gene was described in one patient. (medscape.com)
- Genetic association of the activin A receptor gene (ACVR2A) and pre-eclampsia. (cdc.gov)
- Activins signal through a heteromeric complex of receptor serine kinases which include at least two type I (I and IB) and two type II (II and IIB) receptors. (nih.gov)
- Type II receptors are considered to be constitutively active kinases. (nih.gov)
- One of the two types of ACTIVIN RECEPTORS or activin receptor-like kinases (ALK'S). (umassmed.edu)
- Residues in the activation loop of FGFR1K appear to interfere with substrate peptide binding but not with ATP binding, revealing a second and perhaps more general autoinhibitory mechanism for receptor tyrosine kinases. (embl-heidelberg.de)
- Receptors for ACTIVINS are membrane protein kinases belonging to the family of PROTEIN-SERINE-THREONINE KINASES, thus also named activin receptor-like kinases (ALK's). (bvsalud.org)
- As those transmembrane receptors of the TGF-beta superfamily (RECEPTORS, TRANSFORMING GROWTH FACTOR BETA), ALK's consist of two different but related protein kinases, Type I and Type II. (bvsalud.org)
- Activins are dimeric growth and differentiation factors which belong to the transforming growth factor-beta (TGF-beta) superfamily of structurally related signaling proteins. (nih.gov)
- Furthermore, inhibition of TGF-β I receptor activity by SB431542 or inhibition of Smad3 phosphorylation by SIS3 blocked TGF-β2 stimulated ECM expression as well as activation of downstream canonical pathway signaling molecules. (molvis.org)
- Several genetic mutations in the genes encoding the ligands and receptors of this pathway have been reported in two cardiovascular diseases, pulmonary arterial hypertension (PAH) and hereditary haemorrhagic telangiectasia (HHT). (portlandpress.com)
- ACVR2A promoter polymorphism rs1424954 in the Activin-A signaling pathway in trophoblasts. (cdc.gov)
- Bone morphogenetic protein receptor type 2 spans the cell membrane, so that one end of the protein is on the outer surface of the cell and the other end remains inside the cell. (medlineplus.gov)
- About half of the mutations involved in this condition disrupt the assembly of bone morphogenetic protein receptor type 2, reducing the amount of this protein in cells. (medlineplus.gov)
- Other mutations prevent bone morphogenetic protein receptor type 2 from reaching the cell surface or alter its structure so it cannot receive or transmit signals. (medlineplus.gov)
- We utilized three-dimensional organotypic reconstruct cultures of dysplastic and esophageal squamous tumor cells lines, in the context of fibroblast-secreted Activin A, to identify the effects of Activin A on cell invasion and determine protein expression and localization in epithelial and stromal compartments by immunofluorescence. (biomedcentral.com)
- Sotatercept is a recombinant fusion protein consisting of the extracellular domain of the human activin receptor type IIA linked to the Fc piece of human IgG1. (clinicaltrials.gov)
- Researchers from the University of Jyväskylä in Finland have found that continued treatment of muscle wasting with a soluble growth factor receptor protein, produced at the University of Helsinki, improved survival in a pre-clinical cancer model without affecting the tumor size. (news-medical.net)
- Intestine farnesoid X receptor agonist and the gut microbiota activate G-protein bile acid receptor-1 signaling to improve metabolism. (omeka.net)
- Bile acids activate farnesoid X receptor (FXR) and G protein-coupled bile acid receptor-1 (aka Takeda G protein-coupled receptor-5 [TGR5]) to regulate bile acid metabolism and glucose and insulin sensitivity. (omeka.net)
- Introduction G-protein combined receptors (GPCRs), known as seven-transmembrane (7TM) site receptors also, although diverse functionally, constitute the biggest integral membrane proteins family members in the human being genome C. (mdm2-inhibitors.com)
- Activin B, like certain other members of the TGF-β family, signals through the ActRII receptor (Activin Receptor type II). (sbhsciences.com)
- These receptors are essential in human beings physiologically, taking part in the rules of all of our physiological activities such as for example neurotransmission, enzyme launch, inflammation or chemotaxis, aswell as our feeling of vision, taste and smell, by sensing endogenous or environmental stimuli through binding suitable ligands and AZD-3965 IC50 transducing related sign into cells typically through combined heterotrimeric G proteins. (mdm2-inhibitors.com)
- In this study, we established stable transfectants expressing two types of activin receptors, ActRI and ActRIB, to clarify the role of these receptors in activin signalling for growth inhibition in HS-72 mouse B-cell hybridoma cells. (elsevier.com)
- It seems that circulating pro-inflammatory cytokines, physical activity, or hepatic and splenic physiology, which were all altered in cancer, may not be determining factors for improved survival with the soluble growth factor receptor, more specifically soluble activin receptor 2B. (news-medical.net)
- Blockade of VEGF function via soluble decoy receptors suppressed tumor development, inhibited tumor angiogenesis, and blocked tumor cell proliferation. (perkinelmer.com)
- Activin Receptors, Type I" is a descriptor in the National Library of Medicine's controlled vocabulary thesaurus, MeSH (Medical Subject Headings) . (umassmed.edu)
- Human Activin B is a 26.0 kDa disulfide-linked homodimer consisting of two βB chains, each containing 115 amino acid residues. (sbhsciences.com)
- In contrast, HS-72 clones that over-expressed ActRIB significantly facilitated activin A-induced apoptosis. (elsevier.com)
- Endothelial tube formation was disrupted in the presence of conditioned media from fibroblasts overexpressing Activin A. Interestingly, ACVRIB-negative TE-11 cells did not show the prior observed effects in the context of Activin A overexpression, indicating a dependence on the presence of ACVRIB. (biomedcentral.com)
- Formyl peptide receptors (FPRs) comprise a functionally specific GPCR subfamily involved with leukocyte chemotaxis and activation. (mdm2-inhibitors.com)
- In addition, a dimeric form of FGFR1K observed in the crystal structure may provide insights into the molecular mechanisms by which FGF receptors are activated. (embl-heidelberg.de)
- Activin receptors also bind TRANSFORMING GROWTH FACTOR BETA . (bvsalud.org)
- Activin-B is a TGF-beta family member that exhibits a wide range of biological activities including regulation of embryogenesis, osteogenesis, hematopoiesis, reproductive physiology and hormone secretion from the hypothalamic, pituitary and gonadal glands. (sbhsciences.com)
- To identify the functional consequences of stromal-derived Activin A on angiogenesis, we performed endothelial tube formation assays. (biomedcentral.com)
- We describe the first observation of an inhibitory role for Activin A in ESCC progression that is dependent on the expression of ACVRIB. (biomedcentral.com)
- We found that overexpression of stromal-derived Activin A inhibited invasion of esophageal dysplastic squamous cells, ECdnT, and TE-2 ESCC cells, both positive for ACVRIB. (biomedcentral.com)
- Furthermore, human being FPR expression continues to be observed in several distinct cells and cell types (C and sources therein), indicating a much broad distribution of the receptors and their significant role in vivo physiologically. (mdm2-inhibitors.com)
- Expression of the PDGF-alpha-receptor 1.5 kb transcript, OCT4, and c-KIT in human normal and malignant tissues. (eur.nl)
- Reconstituted Human Activin-B should be stored in working aliquots at -80 0 C. (sbhsciences.com)
- These receptors could also impact the function and manifestation of CCR5 and CXCR4 on human being monocytes, two main GPCR chemokine coreceptors of human being immunodeficiency pathogen type 1 (HIV-1) , . (mdm2-inhibitors.com)
- however, similar to TGFβ, Activin A can act as a tumor promoter or suppressor in different contexts. (biomedcentral.com)
- The objective of this study was to investigate the role of Activin A signaling in ESCC. (biomedcentral.com)
- To investigate the role Activin A plays in ESCC biology, tissue microarrays containing 200 cores from 120 ESCC patients were analyzed upon immunofluorescence staining. (biomedcentral.com)
- The fertility defects that were describe in DmGfrl null flies suggest that GDNF receptor-like has an evolutionarily ancient role in regulating male fertility and a previously unrecognized role in regulating oogenesis. (sdbonline.org)
- The GIP receptor in the central nervous system plays a crucial role in the regulation of body weight and food intake. (brightsurf.com)
- Are thyroid hormone receptors good or bad for you? (endocrine-abstracts.org)
- and type II receptors are required for binding ligands and for expression of type I receptors. (nih.gov)
- Moreover, high serum levels and high levels of expression of TGF-β and its receptors have been linked to breast cancer prognosis [ 9 ] and presence of phosphorylated-Smad2 has been associated with positive node status [ 10 ]. (cdc.gov)