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ALK5
Transforming growth factor beta receptor I (activin A receptor type II-like kinase, 53kDa) is a membrane-bound TGF beta receptor protein of the TGF-beta receptor family for the Transforming growth factor beta, TGF beta superfamily of signaling ligands. ''TGFBR1'' is its human gene. Function The protein encoded by this gene forms a heteromeric complex with TGF beta receptor 2, type II TGF-β receptors when bound to TGF-β, transducing the TGF-β signal from the cell surface to the cytoplasm. The encoded protein is a serine/threonine protein kinase. Mutations in this gene have been associated with Loeys–Dietz syndrome, Loeys–Dietz aortic aneurysm syndrome (LDS, LDAS). Interactions TGF beta receptor 1 has been shown to Protein-protein interaction, interact with: * Caveolin 1, * Endoglin, * FKBP1A, * FNTA, * Heat shock protein 90kDa alpha (cytosolic), member A1 * Mothers against decapentaplegic homolog 7, * PPP2R2A, * STRAP, * TGF beta 1, and * TGF beta receptor 2. ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Transforming Growth Factor Beta
Transforming growth factor beta (TGF-β) is a multifunctional cytokine belonging to the transforming growth factor superfamily that includes three different mammalian isoforms (TGF-β 1 to 3, HGNC symbols TGFB1, TGFB2, TGFB3) and many other signaling proteins. TGFB proteins are produced by all white blood cell lineages. Activated TGF-β complexes with other factors to form a serine/threonine kinase complex that binds to TGF-β receptors. TGF-β receptors are composed of both type 1 and type 2 receptor subunits. After the binding of TGF-β, the type 2 receptor kinase phosphorylates and activates the type 1 receptor kinase that activates a signaling cascade. This leads to the activation of different downstream substrates and regulatory proteins, inducing transcription of different target genes that function in differentiation, chemotaxis, proliferation, and activation of many immune cells. TGF-β is secreted by many cell types, including macrophages, in a latent form in which it ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
TGF Beta Receptor
Transforming growth factor beta (TGFβ) receptors are bitopic protein, single pass Receptor protein serine/threonine kinase, serine/threonine kinase receptors that belong to TGFβ superfamily receptor, TGFβ receptor family. They exist in several different isoforms that can be homodimeric, homo- or heterodimeric. (free full text) The number of characterized ligands in the TGFβ superfamily far exceeds the number of known receptors, suggesting the promiscuity that exists between the ligand and receptor interactions. TGFβ is a growth factor and cytokine involved in paracrine signalling and can be found in many different tissue (biology), tissue types, including brain, heart, kidney, liver, bone, and testes. Over-gene expression, expression of TGFβ can induce renal fibrosis, causing kidney disease, as well as diabetes, and ultimately end-stage renal disease. Recent developments have found that, using certain types of protein receptor antagonist, antagonists against TGFβ recepto ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Endoglin
Endoglin (ENG) is a type I membrane glycoprotein located on cell surfaces and is part of the TGF beta receptor complex. It is also commonly referred to as CD105, END, FLJ41744, HHT1, ORW and ORW1. It has a crucial role in angiogenesis, therefore, making it an important protein for tumor growth, survival and metastasis of cancer cells to other locations in the body. Gene and expression The human endoglin gene is located on human chromosome 9 with location of the cytogenic band at 9q34.11. Endoglin glycoprotein is encoded by 39,757 bp and translates into 658 amino acids. The expression of the endoglin gene is usually low in resting endothelial cells. This, however, changes once neoangiogenesis begins and endothelial cells become active in places like tumor vessels, inflamed tissues, skin with psoriasis, vascular injury and during embryogenesis. The expression of the vascular system begins at about 4 weeks and continues after that. Other cells in which endoglin is expressed cons ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
SB-431,542
SB-431542 is a drug candidate developed by GlaxoSmithKline (GSK) as an inhibitor of the activin receptor-like kinase (ALK) receptors, ALK5, ALK4 and ALK7. However, it is ''not'' an inhibitor of anaplastic lymphoma kinase (which are commonly known as ALK inhibitors). In-vitro studies While SB-431542 has not proved directly useful for any clinical application, it is used for several applications in molecular biology. It suppresses the TGF-beta-induced proliferation of osteosarcoma cells in humans. Treatment with SB431542 is a robust, clinically applicable, and efficient system for generating mesenchymal stem/stromal cells (MSCs) from human iPSCs. SB431542 can also be used in combination with LDN193189, CHIR99021 and DAPT to transform astrocytes into neurons. It is also commonly used for immunological studies, for instance as a TGF-β inhibitor to facilitate the generation of dendritic cells from peripheral blood monocytes Monocytes are a type of leukocyte or white blood c ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
TGF-beta Receptor Family
The transforming growth factor beta (TGFβ) receptors are a family of serine/threonine kinase receptors involved in TGF beta signaling pathway. These receptors bind growth factor and cytokine signaling proteins in the TGF-beta family such as TGFβs ( TGFβ1, TGFβ2, TGFβ3), bone morphogenetic proteins (BMPs), growth differentiation factors (GDFs), activin and inhibin, myostatin, anti-Müllerian hormone (AMH), and NODAL. TGFβ family receptors TGFβ family receptors are grouped into three types, type I, type II, and type III. There are seven type I receptors, termed the activin-like receptors (ALK1–7), five type II receptors, and one type III receptor, for a total of 13 TGFβ superfamily receptors. In the transduction pathway, ligand-bound type II receptors activate type I receptors by phosphorylation, which then autophosphorylate and bind SMAD. The Type I receptors have a glycine-serine (GS, or TTSGSGSG) repeat motif of around 30 AA, a target of type II activity. At leas ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
STRAP
A strap, sometimes also called strop, is an elongated wikt:flap, flap or ribbon, usually of leather or other flexible materials. Thin straps are used as part of clothing or baggage, or bedding such as a sleeping bag. See for example spaghetti strap, shoulder strap. A strap differs from a belt (clothing), belt mainly in that a strap is usually integral to the item of clothing; either can be used in combination with buckles. Straps are also used as fasteners to attach, secure, carry, or bind items, to objects, animals (for example a saddle on a horse) and people (for example a watch on a wrist), or even to tie down people and animals, as on an apparatus for corporal punishment. Occasionally a strap is specified after what it binds or holds, e.g. chin strap. Webbing is a particular type of strap that is a strong fabric woven as a flat strip or tube that is also often used in place of rope. Modern webbing is typically made from exceptionally high-strength material and is used in aut ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Knock-in
In molecular cloning and biology, a gene knock-in (abbreviation: KI) refers to a genetic engineering method that involves the one-for-one substitution of DNA sequence information in a genetic locus or the insertion of sequence information not found within the locus. Typically, this is done in mice since the technology for this process is more refined and there is a high degree of shared sequence complexity between mice and humans. The difference between knock-in technology and traditional transgenic techniques is that a knock-in involves a gene inserted into a specific locus, and is thus a "targeted" insertion. It is the opposite of gene knockout. A common use of knock-in technology is for the creation of disease models. It is a technique by which scientific investigators may study the function of the regulatory machinery (e.g. promoters) that governs the expression of the natural gene being replaced. This is accomplished by observing the new phenotype of the organism in question. T ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Gene Knock-out
A gene knockout (abbreviation: KO) is a genetic technique in which one of an organism's genes is made inoperative ("knocked out" of the organism). However, KO can also refer to the gene that is knocked out or the organism that carries the gene knockout. Knockout organisms or simply knockouts are used to study gene function, usually by investigating the effect of gene loss. Researchers draw inferences from the difference between the knockout organism and normal individuals. The KO technique is essentially the opposite of a gene knock-in. Knocking out two genes simultaneously in an organism is known as a double knockout (DKO). Similarly the terms triple knockout (TKO) and quadruple knockouts (QKO) are used to describe three or four knocked out genes, respectively. However, one needs to distinguish between heterozygous and homozygous KOs. In the former, only one of two gene copies (alleles) is knocked out, in the latter both are knocked out. Methods Knockouts are accomplished throu ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Galunisertib
Galunisertib (LY2157299) is a small molecular experimental cancer drug previously in development by Eli Lilly. It is a TGF-b inhibitor. Development of galunisertib by Eli Lilly was discontinued in January 2020. Galunisertib was investigated in a phase II trial for treatment of hepatocellular carcinoma. Pre-clinically, combination of galunisertib with PD-L1 Programmed death-ligand 1 (PD-L1) also known as cluster of differentiation 274 (CD274) or B7 homolog 1 (B7-H1) is a protein that in humans is encoded by the ''CD274'' gene. Programmed death-ligand 1 (PD-L1) is a 40kDa type 1 transmembrane protei ... blockade resulted in improved tumor growth inhibition. References {{reflist Experimental cancer drugs ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
LY-2109761
LY-2109761 is a synthetic compound which acts as a potent and selective inhibitor for the growth factor receptor TGF beta receptor 1. It is used for research into conditions such as pulmonary fibrosis and cancer. See also * Galunisertib * GW788388 GW 788388 is a synthetic compound which acts as a potent and selective inhibitor for TGF beta receptor 1. It has applications in research into various disorders such as liver, kidney and heart disease (especially associated with Chagas disease), ... References Kinase inhibitors {{pharm-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
