Page last updated: 2024-10-24

signaling receptor inhibitor activity

Definition

Target type: molecularfunction

Binds to and modulates the activity of a signaling receptor. [GOC:ceb]

Signaling receptor inhibitor activity describes the ability of a molecule to modulate the activity of signaling receptors. Signaling receptors are proteins embedded in the cell membrane that receive signals from the outside environment and transmit them to the inside of the cell. These signals can be chemical, such as hormones or neurotransmitters, or physical, such as light or mechanical stress. Once activated, signaling receptors trigger a series of events that lead to changes in the cell's behavior, such as growth, differentiation, or apoptosis.

Signaling receptor inhibitors work by blocking or reducing the activity of signaling receptors. This can be achieved through a variety of mechanisms, including:

* Binding to the receptor and preventing the signal from reaching the intracellular domain.
* Interfering with the receptor's ability to bind to its ligand.
* Inhibiting the downstream signaling pathways activated by the receptor.

Signaling receptor inhibitors are used in a variety of therapeutic applications, including:

* **Cancer treatment:** Many cancer drugs target signaling receptors involved in cancer cell growth and proliferation.
* **Autoimmune disease treatment:** Signaling receptor inhibitors can suppress the immune response in autoimmune diseases, such as rheumatoid arthritis and lupus.
* **Inflammation treatment:** Signaling receptor inhibitors can reduce inflammation by blocking the activity of receptors that promote inflammation.
* **Cardiovascular disease treatment:** Signaling receptor inhibitors can regulate blood pressure and heart rate by modulating the activity of receptors involved in these processes.

Overall, signaling receptor inhibitors play a crucial role in modulating cellular signaling pathways, offering therapeutic potential in various diseases.'
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Proteins (2)

ProteinDefinitionTaxonomy
Proprotein convertase subtilisin/kexin type 9A proprotein convertase subtilisin/kexin type 9 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q8NBP7]Homo sapiens (human)
Peptidyl-prolyl cis-trans isomerase FKBP1AA peptidyl-prolyl cis-trans isomerase FKBP1A that is encoded in the genome of human. [PRO:DNx, UniProtKB:P62942]Homo sapiens (human)

Compounds (13)

CompoundDefinitionClassesRoles
thiabendazoleTresaderm: dermatologic soln containing dexamethasone, thiabendazole & neomycin sulfate1,3-thiazoles;
benzimidazole fungicide;
benzimidazoles
antifungal agrochemical;
antinematodal drug
cycloheximidecycloheximide : A dicarboximide that is 4-(2-hydroxyethyl)piperidine-2,6-dione in which one of the hydrogens attached to the carbon bearing the hydroxy group is replaced by a 3,5-dimethyl-2-oxocyclohexyl group. It is an antibiotic produced by the bacterium Streptomyces griseus.

Cycloheximide: Antibiotic substance isolated from streptomycin-producing strains of Streptomyces griseus. It acts by inhibiting elongation during protein synthesis.
antibiotic fungicide;
cyclic ketone;
dicarboximide;
piperidine antibiotic;
piperidones;
secondary alcohol
anticoronaviral agent;
bacterial metabolite;
ferroptosis inhibitor;
neuroprotective agent;
protein synthesis inhibitor
3-(3-pyridyl)-1-propyl-(2s)-1-(3,3-dimethyl-1,2-dioxopentyl)-2-pyrrolidinecarboxylate
tacrolimustacrolimus (anhydrous) : A macrolide lactam containing a 23-membered lactone ring, originally isolated from the fermentation broth of a Japanese soil sample that contained the bacteria Streptomyces tsukubaensis.

Tacrolimus: A macrolide isolated from the culture broth of a strain of Streptomyces tsukubaensis that has strong immunosuppressive activity in vivo and prevents the activation of T-lymphocytes in response to antigenic or mitogenic stimulation in vitro.
macrolide lactambacterial metabolite;
immunosuppressive agent
s 1033(trifluoromethyl)benzenes;
imidazoles;
pyridines;
pyrimidines;
secondary amino compound;
secondary carboxamide
anticoronaviral agent;
antineoplastic agent;
tyrosine kinase inhibitor
N-(2-fluorophenyl)-2-[2-(4-thiazolyl)-1-benzimidazolyl]acetamidebenzimidazoles
biricodarbiricodar: a non-macrocyclic ligand for FKBP12; structure in first sourcealpha-amino acid ester
l 683590immunomycin: from Streptomyces hygroscopicus; structure given in first sourceether;
lactol;
macrolide;
secondary alcohol
antifungal agent;
bacterial metabolite;
immunosuppressive agent
cyclosporineramihyphin A: one of the metabolites produced by Fusarium sp. S-435; RN given refers to cpd with unknown MFhomodetic cyclic peptideanti-asthmatic drug;
anticoronaviral agent;
antifungal agent;
antirheumatic drug;
carcinogenic agent;
dermatologic drug;
EC 3.1.3.16 (phosphoprotein phosphatase) inhibitor;
geroprotector;
immunosuppressive agent;
metabolite
sirolimussirolimus : A macrolide lactam isolated from Streptomyces hygroscopicus consisting of a 29-membered ring containing 4 trans double bonds, three of which are conjugated. It is an antibiotic, immunosupressive and antineoplastic agent.

Sirolimus: A macrolide compound obtained from Streptomyces hygroscopicus that acts by selectively blocking the transcriptional activation of cytokines thereby inhibiting cytokine production. It is bioactive only when bound to IMMUNOPHILINS. Sirolimus is a potent immunosuppressant and possesses both antifungal and antineoplastic properties.
antibiotic antifungal drug;
cyclic acetal;
cyclic ketone;
ether;
macrolide lactam;
organic heterotricyclic compound;
secondary alcohol
antibacterial drug;
anticoronaviral agent;
antineoplastic agent;
bacterial metabolite;
geroprotector;
immunosuppressive agent;
mTOR inhibitor
bastadin 5
timcodartimcodar: a mutlidrug resistance inhibitor; structure in first source
PF-06446846PF-06446846 : A triazolopyridine that is 3H-[1,2,3]triazolo[4,5-b]pyridine substituted by a 4-{(3-chloropyridin-2-yl)[(3R)-piperidin-3-yl]carbamoyl}phenyl group at position 3. It is a potent inhibitor of PCSK9.

PF-06446846: inhibits translation of PCSK9 ;structure in first source
benzamides;
monochloropyridine;
piperidines;
tertiary carboxamide;
triazolopyridine
antilipemic drug;
EC 3.4.21.61 (kexin) inhibitor