Page last updated: 2024-10-24

death receptor agonist activity

Definition

Target type: molecularfunction

Interacting with a death receptor such that the proportion of death receptors in an active form is increased. Ligand binding to a death receptor often induces a conformational change to activate the receptor. [GOC:mtg_apoptosis, GOC:pr]

Death receptor agonist activity describes the ability of a molecule to bind to and activate death receptors, transmembrane proteins that initiate a signaling cascade leading to programmed cell death, also known as apoptosis. Death receptors belong to the tumor necrosis factor receptor superfamily (TNFRSF) and are characterized by their cysteine-rich extracellular domain. Upon ligand binding, the receptor trimerizes, bringing together intracellular death domains that recruit adaptor proteins like FADD (Fas-associated protein with death domain) and TRADD (tumor necrosis factor receptor type 1-associated death domain protein). These adaptor proteins, in turn, activate caspase-8, an initiator caspase that sets off a proteolytic cascade leading to the activation of executioner caspases, such as caspase-3 and -7. These executioner caspases cleave specific cellular substrates, leading to the dismantling of the cell and its eventual demise. Death receptor agonists play critical roles in various physiological processes, including immune regulation, development, and the elimination of damaged or infected cells. Dysregulation of death receptor signaling can contribute to various diseases, including cancer, autoimmune disorders, and neurodegenerative diseases. Examples of death receptor agonists include tumor necrosis factor-alpha (TNF-alpha), Fas ligand (FasL), and TRAIL (TNF-related apoptosis-inducing ligand). These ligands can trigger cell death by binding to their respective receptors, TNFR1, Fas, and TRAIL receptors, respectively. Understanding the molecular function of death receptor agonist activity is crucial for developing therapeutic strategies that target apoptosis pathways for treating various diseases.'
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Proteins (2)

ProteinDefinitionTaxonomy
Heat shock 70 kDa protein 1A A heat shock 70 kDa protein 1A that is encoded in the genome of human. [PRO:DAN, UniProtKB:P0DMV8]Homo sapiens (human)
Tumor necrosis factorA tumor necrosis factor that is encoded in the genome of human. [PRO:DNx]Homo sapiens (human)

Compounds (22)

CompoundDefinitionClassesRoles
mesalaminemesalamine : A monohydroxybenzoic acid that is salicylic acid substituted by an amino group at the 5-position.

Mesalamine: An anti-inflammatory agent, structurally related to the SALICYLATES, which is active in INFLAMMATORY BOWEL DISEASE. It is considered to be the active moiety of SULPHASALAZINE. (From Martindale, The Extra Pharmacopoeia, 30th ed)
amino acid;
aromatic amine;
monocarboxylic acid;
monohydroxybenzoic acid;
phenols
non-steroidal anti-inflammatory drug
way 151693
pentoxifyllineoxopurine
4-(3-butoxy-4-methoxybenzyl)-2-imidazolidinone4-(3-Butoxy-4-methoxybenzyl)-2-imidazolidinone: Inhibitor of phosphodiesterases.methoxybenzenes
roliprampyrrolidin-2-onesantidepressant;
EC 3.1.4.* (phosphoric diester hydrolase) inhibitor
sulfasalazinesulfasalazine : An azobenzene consisting of diphenyldiazene having a carboxy substituent at the 4-position, a hydroxy substituent at the 3-position and a 2-pyridylaminosulphonyl substituent at the 4'-position.

Sulfasalazine: A drug that is used in the management of inflammatory bowel diseases. Its activity is generally considered to lie in its metabolic breakdown product, 5-aminosalicylic acid (see MESALAMINE) released in the colon. (From Martindale, The Extra Pharmacopoeia, 30th ed, p907)
adenosine diphosphateAdenosine Diphosphate: Adenosine 5'-(trihydrogen diphosphate). An adenine nucleotide containing two phosphate groups esterified to the sugar moiety at the 5'-position.adenosine 5'-phosphate;
purine ribonucleoside 5'-diphosphate
fundamental metabolite;
human metabolite
adenosinequinquefolan B: isolated from roots of Panax quinquefolium L.; RN not in Chemline 10/87; RN from Toxlitadenosines;
purines D-ribonucleoside
analgesic;
anti-arrhythmia drug;
fundamental metabolite;
human metabolite;
vasodilator agent
bergeninbergenin: RN refers to (2R-(2alpha,3beta,4alpha,4aalpha,10bbeta))-isomer; structuretrihydroxybenzoic acidmetabolite
8-aminoadenosine
marimastatmarimastat : A secondary carboxamide resulting from the foraml condensation of the carboxy group of (2R)-2-[(1S)-1-hydroxy-2-(hydroxyamino)-2-oxoethyl]-4-methylpentanoic acid with the alpha-amino group of N,3-dimethyl-L-valinamide.

marimastat: a matrix metalloproteinase inhibitor active in patients with advanced carcinoma of the pancreas, prostate, or ovary
hydroxamic acid;
secondary carboxamide
antineoplastic agent;
matrix metalloproteinase inhibitor
birb 796aromatic ether;
morpholines;
naphthalenes;
pyrazoles;
ureas
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor;
immunomodulator
ganoderic acid atriterpenoid
ganoderiol fganoderiol F: a ganoderma triterpene from Ganoderma amboinense; structure in first sourcetriterpenoid
1-(phenylmethyl)benzimidazolebenzimidazoles
luteolin-7-glucosideluteolin 7-O-beta-D-glucoside : A glycosyloxyflavone that is luteolin substituted by a beta-D-glucopyranosyl moiety at position 7 via a glycosidic linkage.

luteolin-7-glucoside: has both antiasthmatic and antineoplastic activities; has 3C protease inhibitory activity; isolated from Ligustrum lucidum
beta-D-glucoside;
glycosyloxyflavone;
monosaccharide derivative;
trihydroxyflavone
antioxidant;
plant metabolite
apigetrinapigenin 7-O-beta-D-glucoside : A glycosyloxyflavone that is apigenin substituted by a beta-D-glucopyranosyl moiety at position 7 via a glycosidic linkage.

apigetrin: structure given in first source
beta-D-glucoside;
dihydroxyflavone;
glycosyloxyflavone;
monosaccharide derivative
antibacterial agent;
metabolite;
non-steroidal anti-inflammatory drug
calycosin-7-o-beta-d-glucopyranosidecalycosin-7-O-beta-D-glucoside : A glycosyloxyisoflavone that is calycosin substituted by a beta-D-glucopyranosyl residue at position at 7 via a glycosidic linkage.

calycosin-7-O-beta-D-glucoside: from Radix Astragali
4'-methoxyisoflavones;
7-hydroxyisoflavones 7-O-beta-D-glucoside;
hydroxyisoflavone;
monosaccharide derivative
spd-304SPD-304: structure in first source
ganoderic acid fganoderic acid F: isolated from Ganoderma lucidum; structure in first sourcetriterpenoid
ver 155008VER 155008: structure in first sourcepurine nucleoside
ganoderic acid c2ganoderic acid C2: from the fruiting body of Ganoderma; structure in first sourcetriterpenoid