Page last updated: 2024-11-13

apelin-13 peptide

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

apelin-13 peptide: amino acid sequence in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

apelin-13 : A 13 amino acid oligopeptide which is the ligand for the apelin receptor (also known as the APJ receptor). It exhibits hypotensive and neuroprotective effects, and may be a potential prognostic biomarker for acute ischemic stroke and multiple sclerosis. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID25078060
CHEMBL ID414173
CHEBI ID80131
MeSH IDM0479465

Synonyms (24)

Synonym
[125i]apelin-13
gtpl605
gtpl602
gln-arg-pro-arg-leu-ser-his-lys-gly-pro-met-pro-phe
apelin-13
CHEMBL414173 ,
217082-58-1
bdbm50014620
apelin 13
J-014247
apelin-13 (human, bovine, mouse, rat) (h-gln-arg-pro-arg-leu-ser-his-lys-gly-pro-met-pro-phe-oh)
mfcd02094627
XXCCRHIAIBQDPX-PEWBXTNBSA-N
apelin-13, human, bovine
Q27074480
EX-A7483
CS-0095059
HY-P1944
l-gln-l-arg-l-pro-l-arg-l-leu-l-ser-l-his-l-lys-l-gly-l-pro-l-met-l-pro-l-phe
apelin-13 peptide
CHEBI:80131
qrprlshkgpmpf
q-r-p-r-l-s-h-k-g-p-m-p-f
l-glutaminyl-l-arginyl-l-prolyl-l-arginyl-l-leucyl-l-seryl-l-histidyl-l-lysylglycyl-l-prolyl-l-methionyl-l-prolyl-l-phenylalanine

Research Excerpts

Toxicity

ExcerptReferenceRelevance
"The ototoxic side effect of cisplatin is a main cause of sensorineural hearing loss."( Apelin-13 protects against cisplatin-induced ototoxicity by inhibiting apoptosis and regulating STAT1 and STAT3.
Guo, Y; Sun, Y; Wang, F; Ya, B; Yang, Q; Yin, H; Zhang, L; Zhang, W; Zhao, H, 2023
)
0.91

Bioavailability

ExcerptReferenceRelevance
" We concluded that this engineered nanocarrier system can serve as a delivery platform for treating heart injuries through sustained bioavailability of cardioprotective therapeutics."( [Pyr1]-Apelin-13 delivery via nano-liposomal encapsulation attenuates pressure overload-induced cardiac dysfunction.
Bernstein, D; Huang, X; Inayathullah, M; Mahmoudi, M; Malkovskiy, AV; Metzler, S; Rajadas, J; Ruiz-Lozano, P; Serpooshan, V; Sivanesan, S; Wagh, D; Wu, JC; Zhang, XJ; Zhao, M, 2015
)
0.42

Dosage Studied

ExcerptRelevanceReference
" Chronic oral dosing in a rat myocardial infarction model reduced myocardial collagen content and improved diastolic function to a similar extent as losartan, a RAS antagonist standard-of-care therapy, but lacked additivity with coadministration."( Cardiovascular response to small-molecule APJ activation.
Ason, B; Boden, A; Chan, J; Chen, R; Chen, Y; Chintalgattu, V; Chui, RW; Dransfield, P; Fielden, M; Gao, B; Guo, Q; Hoagland, KM; Houze, J; Hu, LA; Khakoo, AY; Li, N; Li, X; Liu, D; Ma, J; Ma, X; Mihardja, S; Nguyen, K; Pattaropong, V; Qu, Y; Rajamani, S; Sun, Y; Sutherland, W; Swaminath, G; Turk, JR; Vargas, HM; VĂ©niant, MM; Wang, J; Wong, J; Zhang, Y, 2020
)
0.56
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (5)

RoleDescription
antihypertensive agentAny drug used in the treatment of acute or chronic vascular hypertension regardless of pharmacological mechanism.
biomarkerA substance used as an indicator of a biological state.
autophagy inhibitorAny compound that inhibits the process of autophagy (the self-digestion of one or more components of a cell through the action of enzymes originating within the same cell).
neuroprotective agentAny compound that can be used for the treatment of neurodegenerative disorders.
human metaboliteAny mammalian metabolite produced during a metabolic reaction in humans (Homo sapiens).
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (1)

ClassDescription
oligopeptideA peptide containing a relatively small number of amino acids.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (1)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Apelin receptorHomo sapiens (human)Ki0.00070.00020.00070.0010AID1749755
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Apelin receptorHomo sapiens (human)EC50 (µMol)0.01700.00000.01290.0600AID1141245; AID1749756; AID1749757; AID1749758; AID1847790
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (25)

Processvia Protein(s)Taxonomy
negative regulation of gene expressionApelin receptorHomo sapiens (human)
regulation of gap junction assemblyApelin receptorHomo sapiens (human)
angiogenesisApelin receptorHomo sapiens (human)
vasculogenesisApelin receptorHomo sapiens (human)
vasculature developmentApelin receptorHomo sapiens (human)
heart loopingApelin receptorHomo sapiens (human)
atrioventricular valve developmentApelin receptorHomo sapiens (human)
endocardial cushion formationApelin receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayApelin receptorHomo sapiens (human)
gastrulationApelin receptorHomo sapiens (human)
heart developmentApelin receptorHomo sapiens (human)
adult heart developmentApelin receptorHomo sapiens (human)
regulation of gene expressionApelin receptorHomo sapiens (human)
vascular associated smooth muscle cell differentiationApelin receptorHomo sapiens (human)
aorta developmentApelin receptorHomo sapiens (human)
negative regulation of cAMP-mediated signalingApelin receptorHomo sapiens (human)
positive regulation of angiogenesisApelin receptorHomo sapiens (human)
regulation of body fluid levelsApelin receptorHomo sapiens (human)
positive regulation of release of sequestered calcium ion into cytosolApelin receptorHomo sapiens (human)
ventricular septum morphogenesisApelin receptorHomo sapiens (human)
venous blood vessel developmentApelin receptorHomo sapiens (human)
coronary vasculature developmentApelin receptorHomo sapiens (human)
positive regulation of blood vessel endothelial cell proliferation involved in sprouting angiogenesisApelin receptorHomo sapiens (human)
positive regulation of inhibitory G protein-coupled receptor phosphorylationApelin receptorHomo sapiens (human)
blood vessel developmentApelin receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (4)

Processvia Protein(s)Taxonomy
G protein-coupled receptor activityApelin receptorHomo sapiens (human)
protein bindingApelin receptorHomo sapiens (human)
signaling receptor activityApelin receptorHomo sapiens (human)
apelin receptor activityApelin receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (1)

Processvia Protein(s)Taxonomy
plasma membraneApelin receptorHomo sapiens (human)
plasma membraneApelin receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (15)

Assay IDTitleYearJournalArticle
AID1749758Agonist activity at human APJ receptor expressed in HEK293 cells co-expressing Rlucll-beta-arrestin2 assessed as induction of beta-arrestin2 recruitment to receptor incubated for 30 mins by BRET assay2021Journal of medicinal chemistry, 05-13, Volume: 64, Issue:9
Constraining the Side Chain of C-Terminal Amino Acids in Apelin-13 Greatly Increases Affinity, Modulates Signaling, and Improves the Pharmacokinetic Profile.
AID1749755Displacement of [125I] [NIe75,Tyr77]Pyr-apelin-13 from YFP-tagged human APJ receptor expressed in HEK293 cells incubated for 1 hr by gamma counting analysis2021Journal of medicinal chemistry, 05-13, Volume: 64, Issue:9
Constraining the Side Chain of C-Terminal Amino Acids in Apelin-13 Greatly Increases Affinity, Modulates Signaling, and Improves the Pharmacokinetic Profile.
AID1749756Agonist activity at human APJ receptor expressed in HEK293T cells co-expressing Galphai1 RlucII assessed as dissociation of Galphai1 from Gbetta/gamma subunit measured using coelenterazine luciferase substrate incubated for 5 mins by BRET assay2021Journal of medicinal chemistry, 05-13, Volume: 64, Issue:9
Constraining the Side Chain of C-Terminal Amino Acids in Apelin-13 Greatly Increases Affinity, Modulates Signaling, and Improves the Pharmacokinetic Profile.
AID1749761AUCtot in Sprague-Dawley rat plasma at 3 mg/kg, iv bolus injection measured up to 240 mins by LC-MS/MS analysis2021Journal of medicinal chemistry, 05-13, Volume: 64, Issue:9
Constraining the Side Chain of C-Terminal Amino Acids in Apelin-13 Greatly Increases Affinity, Modulates Signaling, and Improves the Pharmacokinetic Profile.
AID1749762Half life in Sprague-Dawley rat plasma at 3 mg/kg, iv bolus injection measured up to 240 mins by LC-MS/MS analysis2021Journal of medicinal chemistry, 05-13, Volume: 64, Issue:9
Constraining the Side Chain of C-Terminal Amino Acids in Apelin-13 Greatly Increases Affinity, Modulates Signaling, and Improves the Pharmacokinetic Profile.
AID1749757Agonist activity at human APJ receptor expressed in HEK293T cells co-expressing PDZ-Rho-Gef-RLucll and rGFP-CAAX assessed as induction of recruitment of Galpha12 to cell membrane using coelenterazine luciferase substrate incubated for 5 mins by BRET assay2021Journal of medicinal chemistry, 05-13, Volume: 64, Issue:9
Constraining the Side Chain of C-Terminal Amino Acids in Apelin-13 Greatly Increases Affinity, Modulates Signaling, and Improves the Pharmacokinetic Profile.
AID1847790Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysis2021Journal of medicinal chemistry, 12-23, Volume: 64, Issue:24
Identification of a Hydroxypyrimidinone Compound (
AID1141246Agonist activity at APJ receptor (unknown origin) expressed in CHO cells co-expressing with Calphaq16 assessed as calcium mobilization relative to pyr-apelin-132014Bioorganic & medicinal chemistry, Jun-01, Volume: 22, Issue:11
Identifying structural determinants of potency for analogs of apelin-13: integration of C-terminal truncation with structure-activity.
AID1749763Clearance in Sprague-Dawley rat plasma at 3 mg/kg, iv bolus injection measured up to 240 mins by LC-MS/MS analysis2021Journal of medicinal chemistry, 05-13, Volume: 64, Issue:9
Constraining the Side Chain of C-Terminal Amino Acids in Apelin-13 Greatly Increases Affinity, Modulates Signaling, and Improves the Pharmacokinetic Profile.
AID1749759Stability in Sprague-Dawley rat plasma assessed as half life measured up to 24 hrs by UPLC-MS analysis2021Journal of medicinal chemistry, 05-13, Volume: 64, Issue:9
Constraining the Side Chain of C-Terminal Amino Acids in Apelin-13 Greatly Increases Affinity, Modulates Signaling, and Improves the Pharmacokinetic Profile.
AID331173Ratio of Kcat to Km for ACE22008Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
Development of potent and selective phosphinic peptide inhibitors of angiotensin-converting enzyme 2.
AID1141245Agonist activity at APJ receptor (unknown origin) expressed in CHO cells co-expressing with Calphaq16 assessed as calcium mobilization2014Bioorganic & medicinal chemistry, Jun-01, Volume: 22, Issue:11
Identifying structural determinants of potency for analogs of apelin-13: integration of C-terminal truncation with structure-activity.
AID1346467Human apelin receptor (Apelin receptor)2000The Journal of biological chemistry, Jul-14, Volume: 275, Issue:28
Molecular and functional characteristics of APJ. Tissue distribution of mRNA and interaction with the endogenous ligand apelin.
AID1346467Human apelin receptor (Apelin receptor)2003Journal of neurochemistry, Mar, Volume: 84, Issue:5
Pharmacological and immunohistochemical characterization of the APJ receptor and its endogenous ligand apelin.
AID1346467Human apelin receptor (Apelin receptor)2003Biochemistry, Sep-02, Volume: 42, Issue:34
Structural and functional study of the apelin-13 peptide, an endogenous ligand of the HIV-1 coreceptor, APJ.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (273)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's31 (11.36)29.6817
2010's170 (62.27)24.3611
2020's72 (26.37)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 31.65

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index31.65 (24.57)
Research Supply Index5.65 (2.92)
Research Growth Index6.64 (4.65)
Search Engine Demand Index38.91 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (31.65)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials3 (1.07%)5.53%
Reviews5 (1.79%)6.00%
Case Studies0 (0.00%)4.05%
Observational1 (0.36%)0.25%
Other271 (96.79%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]