Loading...
  • differentiation
  • Downregulation of topoisomerase IIβ in myeloid leukemia cell lines leads to activation of apoptosis following all-trans retinoicacid-induced differentiation/growth arrest. (springer.com)
  • It binds retinoic acid, the biologically active form of vitamin A which mediates cellular signalling in embryonic morphogenesis, cell growth and differentiation. (wikipedia.org)
  • All-trans retinoic acid (ATRA) triggers a wide range of effects on vertebrate development by regulating cell proliferation, differentiation, and apoptosis. (scirp.org)
  • Genetic knockdown of chemerin or its receptor, CMKLR1 impairs differentiation into adipocytes, and reduces the expression of GLUT4 and adiponectin, while increasing expression of IL-6 and insulin receptor. (wikipedia.org)
  • tretinoin), the acid form of vitamin A. Treatment with ATRA dissociates the NCOR-HDACL complex from RAR and allows DNA transcription and differentiation of the immature leukemic promyelocytes into mature granulocytes by targeting the oncogenic transcription factor and its aberrant action. (wikipedia.org)
  • amino
  • Isoforms 1 and 2 contain 294 and 228 amino acids respectively. (atlasgeneticsoncology.org)
  • Ryan, M.D., King, A.M. and Thomas, G.P. (1991) Cleavage of Foot-and-Mouth Disease Virus Polyprotein Is Mediated by Residues Located within a 19 Amino Acid Sequence. (scirp.org)
  • agonists
  • In 2011, animal studies demonstrated that RARγ agonists, including palovarotene, blocked new bone formation in both an injury-induced mouse model of heterotopic ossification (HO) and a genetically modified biological mouse model of FOP containing a continuously active ACVR1/ALK2 receptor in a dose-dependent manner. (wikipedia.org)
  • ligand
  • On ligand binding, the corepressors dissociate from the receptors and associate with the coactivators leading to transcriptional activation. (abcam.com)
  • The changes elicited by ligand binding (or signal sensing) in a receptor give rise to a signaling cascade, which is a chain of biochemical events along a signaling pathway. (wikipedia.org)
  • Some receptors such as HER2 are capable of ligand-independent activation when overexpressed or mutated. (wikipedia.org)
  • bind
  • Most ligands are soluble molecules from the extracellular medium which bind to cell surface receptors. (wikipedia.org)
  • Components of the extracellular matrix such as fibronectin and hyaluronan can also bind to such receptors (integrins and CD44, respectively). (wikipedia.org)
  • The RORs are somewhat unusual in that they appear to bind as monomers to hormone response elements as opposed to the majority of other nuclear receptors which bind as dimers. (wikipedia.org)
  • lipids
  • Lipid signaling, broadly defined, refers to any biological signaling event involving a lipid messenger that binds a protein target, such as a receptor, kinase or phosphatase, which in turn mediate the effects of these lipids on specific cellular responses. (wikipedia.org)
  • agonist
  • Palovarotene is a highly selective retinoic acid receptor gamma (RAR-γ) agonist that is under investigation as a potential treatment for fibrodysplasia ossificans progressiva (FOP), an ultra-rare and severely disabling genetic disease characterized by extra-skeletal bone formation (heterotopic ossification or HO) in muscle and soft tissues. (wikipedia.org)
  • Palovarotene is a retinoic acid receptor gamma (RARγ) agonist licensed to Clementia Pharmaceuticals from Roche Pharmaceuticals. (wikipedia.org)
  • vitamin
  • Vitamin A crosses the blood-testis barrier in its alcohol form as retinol, where it is stored in the Sertoli cells and converted as needed to its more biologically active form, retinoic acid. (westonaprice.org)
  • Isotretinoin is known to cause birth defects due to in-utero exposure because of the molecule's close resemblance to retinoic acid, a natural vitamin A derivative which controls normal embryonic development. (wikipedia.org)
  • Carotenoid absorption is restricted to the duodenum of the small intestine and dependent on class B scavenger receptor (SR-B1) membrane protein, which are also responsible for the absorption of vitamin E (α-tocopherol). (wikipedia.org)
  • This symmetric cleavage gives two equivalent retinal molecules and each retinal molecule further reacts to give retinol (vitamin A) and retinoic acid. (wikipedia.org)
  • cytokine
  • An immunocytokine of the human monoclonal antibody fragment F16 (scFv) against the extra-domain A1 of tenascin-C fused, via a short 5-amino acid linker, to a recombinant form of the human cytokine interleukin-2 (IL-2) with potential immunostimulating and antineoplastic activities. (newyorkoncology.com)
  • expression
  • There are strong indications that ERβ functions as a tumor suppressor in breast, prostate and colon cancer because clinical investigations show that expression of the receptor is lost during progression of these cancers. (uh.edu)
  • More specifically, ligand binding to a nuclear receptor results in a conformational change in the receptor, which, in turn, activates the receptor, resulting in up- or down-regulation of gene expression. (wikipedia.org)
  • modulation
  • Some of these proposed pathways include inappropriate modulation of nuclear receptor function which therefore allows the compounds to be classified as endocrine disrupting chemicals that act to mimic hormones in the body, altering the normal homeostasis maintained by the endocrine system. (wikipedia.org)
  • dependent
  • In 2011, animal studies demonstrated that RARγ agonists, including palovarotene, blocked new bone formation in both an injury-induced mouse model of heterotopic ossification (HO) and a genetically modified biological mouse model of FOP containing a continuously active ACVR1/ALK2 receptor in a dose-dependent manner. (wikipedia.org)
  • cancers
  • it has also been proposed to be involved in regulating the growth of various types of human cancers (see 20-Hydroxyeicosatetraenoic acid#cancer). (wikipedia.org)
  • PPAR
  • The RXR receptor itself is the second major target of obesogens next to the PPAR receptors. (wikipedia.org)
  • The PPARα receptor, when complexed with RXR and activated by the binding of a lipid, promotes peroxisome proliferation leading to increased fatty acid β-oxidation. (wikipedia.org)
  • In addition, fatty acid oxidation stimulated by PPARα requires continuous stimulation while only a single activation event of PPARγ is required to permanently increase adipocyte differentiation and number. (wikipedia.org)
  • function
  • A second project is focusing on variants of ERβ1 the ERβ2, ERβ4 and ERβ5 which have a truncated c-terminal domain preventing normal receptor function (see figure 2). (uh.edu)
  • tumor
  • Radiolableled amino acid-based agents are useful in PET brain tumor imaging because F-18 fluoro-deoxyglucose (F-18 FDG), commonly used in PET tumor imaging, is relatively insensitive for detecting tumors in the brain due the high levels of glycolytic metabolism in the normal cortex and to a lesser extent in white matter. (newyorkoncology.com)
  • Another study demonstrated a causal role of BRG1 in the control of retinoic acid and glucocorticoid-induced cell differentiation in lung cancer and in other tumor types. (wikipedia.org)
  • Humans
  • In humans, an interstitial chromosomal deletion of about 800 kilobases at 4q12 deletes the CHIC2 gene (i.e.cysteine rich hydrophobic domain 2 gene) to create an in-frame fusion of the FIP1L1 gene with the platelet-derived growth factor receptor alpha gene (PGDFRA) gene. (wikipedia.org)
  • whereas
  • Ca 2+ release from the SR via the ryanodine receptor initiates muscle contraction, whereas Ca 2+ reuptake into the lumen of the SR leads to muscle relaxation. (ahajournals.org)
  • ERα is the dominating receptor in breast tumors whereas ERβ is the dominating ER in normal breast, colon and prostate. (uh.edu)
  • cell
  • Retinoic acid early inducible 1 (RAE-1) family of murine cell surface glycoproteins is composed of at least five members (RAE-1α-ε). (wikipedia.org)
  • sequence
  • Due to the amino acid sequence and the periodicity of the helices, the leucine side chains are arranged along one face of the α helix and form a hydrophobic surface that modulates dimerization. (wikipedia.org)
  • metabolize
  • Both variants localize on the endoplasmic reticulum and metabolize leukotriene B4 and very likely 5-hydroxyeicosatetraenoic acid, 5-oxo-eicosatetraenoic acid, and 12-hydroxyeicosatetraenoic acid by an omega oxidation reaction, i.e. by adding a hydroxyl residue to their terminal (i.e. (wikipedia.org)
  • effects
  • Most common adverse effects include: Nausea (22%) Drowsiness (19%) Dizziness (12%) Vomiting (12%) Weakness (10%) Serious adverse effects include: Bleeding Low blood platelets Encephalopathy Suicidal behavior and thoughts Low body temperature Valproic acid has a black box warning for hepatotoxicity, pancreatitis, and fetal abnormalities. (wikipedia.org)