AnatomyOrganismsChemicals and DrugsPhenomena and Processes
FenclonineTryptophan HydroxylaseTryptophanAmino Acids, DicarboxylicProcollagen-Proline Dioxygenasealpha-MethyltyrosineMethyltyrosinesSerotoninMimosineKynurenine 3-MonooxygenaseRaphe NucleiPhenylalanine HydroxylaseHydroxybenzoatesMixed Function OxygenasesHypoxia-Inducible Factor 1, alpha SubunitHypoxia-Inducible Factor-Proline DioxygenasesSerotonergic NeuronsTyrosine 3-Monooxygenase5-HydroxytryptophanSerotonin Plasma Membrane Transport ProteinsTryptophan OxygenaseSerotonin AgentsSteroid 21-HydroxylaseHydroxyindoleacetic AcidTryptophan SynthasePineal GlandEnzyme InhibitorsEnterochromaffin CellsAromatic-L-Amino-Acid DecarboxylasesRats, Sprague-DawleyTetranitromethane5,7-DihydroxytryptamineCell HypoxiaDopamineReceptor, Serotonin, 5-HT1A5,6-Dihydroxytryptamine
TPH1TelotristatRate-limitiEthylPCPAKynurenine 3-hydroxylaSmall-molecule inhibitorTPH2Tyrosine hydroxylaseOrally bioavailableSerotonin SynthesisSelective serotoninPotentSSRIsPathwayCheckpoint inhibitorEnzyme that catalyzesPeripheralCompoundsVivoSynthesisPARPVemurafenibMiceTargetsBreast cancerMechanisticClinicalTreatmentActivityAcquired resistanceExpressionCellsShowsPatientsPeopleBodyResearch
TPH17
Telotristat2
  • Telotristat (LP-778902) is a potent tryptophan hydroxylase inhibitor with an in vivo IC50 of 0.028 μM. (adooq.com)
  • The TPH inhibitor telotristat ethyl (TE) reduces peripheral serotonin and relieves CS symptoms. (analysisgroup.com)
Rate-limiti3
  • 4-Chloro-DL-phenylalanine is a selective and irreversible inhibitor of tryptophan hydroxylase, a rate-limiting enzyme in the biosynthesis of serotonin (5-HYDROXYTRYPTAMINE). (adooq.com)
  • We investigated the expression of 5-HT and tryptophan hydroxylase (TPH), the rate-limiting enzyme of 5-HT biosynthesis, in the human brain and peripheral tissues. (kaist.ac.kr)
  • These changes were noted in the absence of a significant effect of serotonin antidepressants on the expression of tryptophan hydroxylase (TPH-2), i.e. the rate-limiting enzyme for 5-HT biosynthesis and of SERT at the mRNA level. (tianeptine.com)
Ethyl1
  • Patients with diarrhea that is not controlled with somatostatin analog therapy can be treated with telostristat ethyl, a tryptophan hydroxylase inhibitor. (medscape.com)
PCPA3
  • Depletion of serotonin with the tryptophan hydroxylase inhibitor PCPA (4-chloro-dl-phenylalanine methyl ester hydrochloride) produced similar defects in CO 2 chemoreception and thermoregulation to that seen postictally in DS mice and increased mortality following heat-induced seizures. (jneurosci.org)
  • Early studies used p -chlorophenylalanine (pCPA), an inhibitor of tryptophan hydroxylase to deplete 5-HT from cats, rats, monkeys, and humans (reviewed in Jouvet, 1969 , 1972 ). (aspetjournals.org)
  • In the in vivo evaluation of the pathways of action, the antidepressant potential of ME (50 mg/kg) was reversed by SCH23390 (4 mg/kg intraperitoneally) dopaminergic D1 receptor, Prazosin (1 mg/kg intraperitoneally) α1 adrenergic receptor, and PCPA (4 mg/kg intraperitoneally) tryptophan hydroxylase inhibitor. (bvsalud.org)
Kynurenine 3-hydroxyla1
  • Ro 61-8048 is a potent and competitive kynurenine 3-hydroxylase inhibitor (Ki = 4.8 nM, IC50 = 37 nM). (adooq.com)
Small-molecule inhibitor2
  • Peripartum dietary supplementation of a small-molecule inhibitor of tryptophan hydroxylase 1 compromises infant, but not maternal, bone. (harvard.edu)
  • This presentation will give insights into the discovery of a novel E2/E3 protein-protein interaction small molecule inhibitor that we were able to validate and characterize in a variety of biochemical as well as cell-based assays including primary cell models. (selectbiosciences.com)
TPH21
Tyrosine hydroxylase2
  • Panaxtriol is a tyrosine hydroxylase inducer. (adooq.com)
  • Dopamine is produced from tyrosine by the action of tyrosine hydroxylase (TH) , which uses tetrahydrobiopterin (BH4) as a cofactor. (medscape.com)
Orally bioavailable2
Serotonin Synthesis1
Selective serotonin2
  • SSRIs (selective serotonin reuptake inhibitors) have been shown to help many people with depression. (magnificentworld.com)
  • The aim of the present study was to test a possible effect of the G-protein beta3-subunit (Gbeta3) C825T gene variant on the antidepressant activity of selective serotonin reuptake inhibitors (SSRIs) in a sample of major and bipolar depressives, with or without psychotic features. (neurotransmitter.net)
Potent3
  • LX-1031 is a potent, orally available tryptophan 5-hydroxylase (TPH) inhibitor that reduces serotonin (5-HT) synthesis peripherally. (adooq.com)
  • Osilodrostat (LCI699) is a potent inhibitor of human 11β-hydroxylase and aldosterone synthase with IC50 values of 2.5 and 0.7 nM, respectively. (adooq.com)
  • LX1031 is a potent, orally available tryptophan 5hydroxylase (TPH) inhibitor that reduces serotonin (5HT) synthesis peripherally. (gitelavieenrose.be)
SSRIs1
  • Several 5-HT receptor agonists and selective serotonin receptor uptake inhibitors (SSRIs) have shown beneficial effects on appetite and mood control in clinics. (kaist.ac.kr)
Pathway1
  • Regarding in silico studies, ME interacted with dopaminergic D1 and α1 adrenergic pathway receptors and with tryptophan hydroxylase inhibitor. (bvsalud.org)
Checkpoint inhibitor1
  • Launch: In lots of solid and liquid tumors, checkpoint inhibitor immunotherapies (CPIs) can reinvigorate preexisting antitumor immunity to attain durable response prices. (geogise.com)
Enzyme that catalyzes2
Peripheral2
Compounds1
  • In the experiments reported here we studied the effects of three representative compounds, the selective serotonin reuptake inhibitor fluoxetine, the selective serotonin reuptake enhancer tianeptine and the selective norepinephrine reuptake inhibitor desipramine on the structure of central serotonin pathways after a 4-week administration. (tianeptine.com)
Vivo1
  • Serine trap inhibitors provide efficacious inhibition in vitro and in vivo Chemotype, mechanism of action and target confirm this is a promising host-based approach for the treatment of influenza. (selectbiosciences.com)
Synthesis1
  • The long-term decrease in 5-HT concentrations and tryptophan hydroxylase activity produced by MDMA was antagonized by depletion of vesicular monoamines with reserpine or interruption of monoamine synthesis with the decarboxylase inhibitor, monofluoro methyl DOPA (dihydroxyphenylalanine). (erowid.org)
PARP1
  • A randomized phase II study in women with metastatic breast cancer who have mutations in BRCA1 or BRCA2 evaluated the addition of the poly (ADP-ribose) polymerase (PARP) inhibitor veliparib to combination chemotherapy. (ascopost.com)
Vemurafenib1
  • In patients with metastatic colorectal cancer who have mutations in BRAF V600, the addition of the BRAF inhibitor vemurafenib (Zelboraf) to cetuximab -(Erbitux) and irinotecan significantly improved progression-free survival, results of the phase II Southwest Oncology Group (SWOG) 1406 trial have. (ascopost.com)
Mice1
Targets1
  • the final decade greater knowledge of the pathophysiology of diarrhea-predominant irritable bowel syndrome (IBS-D) has led to exploration of newer treatment targets including tryptophan hydroxylase inhibitor (LX-1031) newer M3 muscarinic antagonists (otilonium darifenacin solifenacin) oral carbon adsorbents (AST-120) mast cell stabilizers (disodium cromoglycate ketotifen) and proteins (glutamine)1. (biotech-angels.com)
Breast cancer1
  • Clinical trials of Irosustat validate this approach and new data show efficacy in early breast cancer and that aromatase inhibitor combination adds clinical benefit. (selectbiosciences.com)
Mechanistic1
  • in character generates considerable desire for both understanding the mechanistic basis of resistance to inactivation and developing effective inhibitors (6). (radarcon2008.org)
Clinical1
  • More importantly, we can show that this first-in-class inhibitor is highly effective in a pre-clinical autoimmune mouse model for Rheumatoid Arthritis. (selectbiosciences.com)
Treatment2
  • The aim of this study was to assess the mental state and gastrointestinal complaints of patients with small intestinal bacterial overgrowth (SIBO) in relation to tryptophan metabolism and rifaximin treatment. (biomedcentral.com)
  • Rifaximin treatment of SIBO patients ameliorated their mood disorders and gastrointestinal aliments underlined by changes in tryptophan metabolism. (biomedcentral.com)
Activity2
  • Metyrapone is an inhibitor of cytochrome P450-mediated ω/ω-1 hydroxylase activity and CYP11B1. (adooq.com)
  • In addition, we performed checkerboard assays to obtain more information about the activity of riparins as potential inhibitors of MepA efflux and also analyzed the ability of riparins to act on the permeability of the bacterial membrane of S. aureus by the fluorescence method with SYTOX Green. (bvsalud.org)
Acquired resistance1
  • Single molecule dual aromatase-sulfatase inhibitors should facilitate multi-targeted intervention and address acquired resistance mechanisms. (selectbiosciences.com)
Expression2
Cells1
  • The dysfunctional immune system state cannot end up being reversed by anti-PD-1 monotherapy unless Treg cells had been depleted (anti-CTLA-4) or destabilized (EZH2 inhibitor). (geogise.com)
Shows1
  • This graph shows the total number of publications written about "Tryptophan Hydroxylase" by people in Harvard Catalyst Profiles by year, and whether "Tryptophan Hydroxylase" was a major or minor topic of these publication. (harvard.edu)
Patients1
  • The mental state of patients was assessed using the Hamilton Anxiety Rating Scale (HAM-A), and the Hamilton Depression Rating Scale (HAM-D). L-tryptophan (TRP) and its metabolites: 5-hydroxyindoleacetic acid (5-HIAA), kynurenine (KYN), xanthurenic acid (XA) and quinolinic acid (QA) were measured in urine by liquid-chromatography-tandem mass spectrometry and related to creatinine level. (biomedcentral.com)
People1
  • Below are the most recent publications written about "Tryptophan Hydroxylase" by people in Profiles. (harvard.edu)
Body1
Research1
  • This presentation will introduce the newly created Alzheimer's Research UK Drug Discovery Institutes and then illustrate how new inhibitors of the bromodomain of the BRPF family are being used to explore the fundamental biology and possible disease association of these proteins. (selectbiosciences.com)