Compounds > psammaplysene a
Page last updated: 2024-11-12

psammaplysene a

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

Description

psammaplysene A: dimeric bromotyrosine alkaloid; specific inhibitor of FOXO1a nuclear export; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID11434210
CHEMBL ID481437
MeSH IDM0485812

Synonyms (13)

Synonym
bdbm50259870
psammaplysene a
CHEMBL481437 ,
(e)-n-[3-[2,6-dibromo-4-[2-(dimethylamino)ethyl]phenoxy]propyl]-3-[3,5-dibromo-4-[3-(dimethylamino)propoxy]phenyl]prop-2-enamide
850013-02-4
(dimethylamino)ethyl]phenoxy]propyl]-3-[3,5-dibromo-4-
[3-(dimethylamino)propoxy]phenyl]prop-2-enamide
(e)-n-[3-[2,6-dibromo-4-[2-
(e)-n-[3-[2,6-dibromo-4-[2- (dimethylamino)ethyl]phenoxy]propyl]-3-[3,5-dibromo-4- [3-(dimethylamino)propoxy]phenyl]prop-2-enamide
(2e)-n-(3-{2,6-dibromo-4-[2-(dimethylamino)ethyl]phenoxy}propyl)-3-{3,5-dibromo-4-[3-(dimethylamino)propoxy]phenyl}prop-2-enamide
AKOS040749239
CS-0034865
HY-111299
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (1)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Forkhead box protein O1Homo sapiens (human)IC50 (µMol)5.00000.03302.51655.0000AID377823
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (39)

Processvia Protein(s)Taxonomy
negative regulation of transcription by RNA polymerase IIForkhead box protein O1Homo sapiens (human)
blood vessel developmentForkhead box protein O1Homo sapiens (human)
temperature homeostasisForkhead box protein O1Homo sapiens (human)
intracellular glucose homeostasisForkhead box protein O1Homo sapiens (human)
protein acetylationForkhead box protein O1Homo sapiens (human)
autophagyForkhead box protein O1Homo sapiens (human)
apoptotic processForkhead box protein O1Homo sapiens (human)
DNA damage responseForkhead box protein O1Homo sapiens (human)
insulin receptor signaling pathwayForkhead box protein O1Homo sapiens (human)
cellular response to starvationForkhead box protein O1Homo sapiens (human)
gene expressionForkhead box protein O1Homo sapiens (human)
positive regulation of autophagyForkhead box protein O1Homo sapiens (human)
cellular response to insulin stimulusForkhead box protein O1Homo sapiens (human)
negative regulation of stress-activated MAPK cascadeForkhead box protein O1Homo sapiens (human)
positive regulation of smooth muscle cell apoptotic processForkhead box protein O1Homo sapiens (human)
cellular response to oxidative stressForkhead box protein O1Homo sapiens (human)
positive regulation of apoptotic processForkhead box protein O1Homo sapiens (human)
negative regulation of apoptotic processForkhead box protein O1Homo sapiens (human)
fat cell differentiationForkhead box protein O1Homo sapiens (human)
negative regulation of fat cell differentiationForkhead box protein O1Homo sapiens (human)
positive regulation of gluconeogenesisForkhead box protein O1Homo sapiens (human)
positive regulation of protein catabolic processForkhead box protein O1Homo sapiens (human)
negative regulation of DNA-templated transcriptionForkhead box protein O1Homo sapiens (human)
positive regulation of DNA-templated transcriptionForkhead box protein O1Homo sapiens (human)
positive regulation of transcription by RNA polymerase IIForkhead box protein O1Homo sapiens (human)
negative regulation of insulin secretionForkhead box protein O1Homo sapiens (human)
canonical Wnt signaling pathwayForkhead box protein O1Homo sapiens (human)
regulation of transcription initiation by RNA polymerase IIForkhead box protein O1Homo sapiens (human)
cellular response to coldForkhead box protein O1Homo sapiens (human)
response to fatty acidForkhead box protein O1Homo sapiens (human)
cellular response to hyperoxiaForkhead box protein O1Homo sapiens (human)
cellular response to nitric oxideForkhead box protein O1Homo sapiens (human)
negative regulation of canonical Wnt signaling pathwayForkhead box protein O1Homo sapiens (human)
energy homeostasisForkhead box protein O1Homo sapiens (human)
neuronal stem cell population maintenanceForkhead box protein O1Homo sapiens (human)
negative regulation of cardiac muscle hypertrophy in response to stressForkhead box protein O1Homo sapiens (human)
regulation of neural precursor cell proliferationForkhead box protein O1Homo sapiens (human)
regulation of reactive oxygen species metabolic processForkhead box protein O1Homo sapiens (human)
regulation of transcription by RNA polymerase IIForkhead box protein O1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (14)

Processvia Protein(s)Taxonomy
DNA-binding transcription factor activity, RNA polymerase II-specificForkhead box protein O1Homo sapiens (human)
DNA-binding transcription repressor activity, RNA polymerase II-specificForkhead box protein O1Homo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificForkhead box protein O1Homo sapiens (human)
nucleic acid bindingForkhead box protein O1Homo sapiens (human)
chromatin bindingForkhead box protein O1Homo sapiens (human)
DNA-binding transcription factor activityForkhead box protein O1Homo sapiens (human)
protein bindingForkhead box protein O1Homo sapiens (human)
beta-catenin bindingForkhead box protein O1Homo sapiens (human)
chromatin DNA bindingForkhead box protein O1Homo sapiens (human)
ubiquitin protein ligase bindingForkhead box protein O1Homo sapiens (human)
sequence-specific DNA bindingForkhead box protein O1Homo sapiens (human)
protein phosphatase 2A bindingForkhead box protein O1Homo sapiens (human)
promoter-specific chromatin bindingForkhead box protein O1Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingForkhead box protein O1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (6)

Processvia Protein(s)Taxonomy
nucleusForkhead box protein O1Homo sapiens (human)
nucleusForkhead box protein O1Homo sapiens (human)
nucleoplasmForkhead box protein O1Homo sapiens (human)
cytoplasmForkhead box protein O1Homo sapiens (human)
mitochondrionForkhead box protein O1Homo sapiens (human)
cytosolForkhead box protein O1Homo sapiens (human)
chromatinForkhead box protein O1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (1)

Assay IDTitleYearJournalArticle
AID377823Inhibition of FOXO1a nuclear export in PTEN-deficient cells2005Journal of natural products, Apr, Volume: 68, Issue:4
The psammaplysenes, specific inhibitors of FOXO1a nuclear export.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (8)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's5 (62.50)29.6817
2010's2 (25.00)24.3611
2020's1 (12.50)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.20

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 weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index12.20 (24.57)
Research Supply Index2.20 (2.92)
Research Growth Index4.40 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.20)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (12.50%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other7 (87.50%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
carbostyril
Quinolones: A group of derivatives of naphthyridine carboxylic acid, quinoline carboxylic acid, or NALIDIXIC ACID.. quinolin-2(1H)-one : A quinolone that is 1,2-dihydroquinoline substituted by an oxo group at position 2.		3.3510monohydroxyquinoline;
quinolone		bacterial xenobiotic metabolite
tyrosine
Tyrosine: A non-essential amino acid. In animals it is synthesized from PHENYLALANINE. It is also the precursor of EPINEPHRINE; THYROID HORMONES; and melanin.. tyrosine : An alpha-amino acid that is phenylalanine bearing a hydroxy substituent at position 4 on the phenyl ring.		4.6680amino acid zwitterion;
erythrose 4-phosphate/phosphoenolpyruvate family amino acid;
L-alpha-amino acid;
proteinogenic amino acid;
tyrosine		EC 1.3.1.43 (arogenate dehydrogenase) inhibitor;
fundamental metabolite;
micronutrient;
nutraceutical
kainic acid
Kainic Acid: (2S-(2 alpha,3 beta,4 beta))-2-Carboxy-4-(1-methylethenyl)-3-pyrrolidineacetic acid. Ascaricide obtained from the red alga Digenea simplex. It is a potent excitatory amino acid agonist at some types of excitatory amino acid receptors and has been used to discriminate among receptor types. Like many excitatory amino acid agonists it can cause neurotoxicity and has been used experimentally for that purpose.		2.0510dicarboxylic acid;
L-proline derivative;
non-proteinogenic L-alpha-amino acid;
pyrrolidinecarboxylic acid		antinematodal drug;
excitatory amino acid agonist
4-iodophenol
[no description available]		2.0310iodophenol
as 1842856
5-amino-7-(cyclohexylamino)-1-ethyl-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid: inhibits Foxo1 transactivation; inhibits mRNA levels of glucose-6-phosphatase and phosphoenolpyruvate carboxykinase; structure in first source. AS1842856 : A quinolone that is 4-quinolone substituted at positions 1, 3, 5, 6 and 7 by ethyl, carboxy, amino, fluorine, and cyclohexylamino groups, respectively. It can directly bind to and block the transcription activity of the active forkhead box protein O1 (Foxo1), but not the Ser256-phosphorylated form. It induces cell death and growth arrest in Burkitt lymphoma cell lines at low concentrations.		3.3510organofluorine compound;
primary amino compound;
quinolinemonocarboxylic acid;
quinolone;
secondary amino compound;
tertiary amino compound		anti-obesity agent;
antineoplastic agent;
apoptosis inducer;
autophagy inhibitor;
forkhead box protein O1 inhibitor;
hypoglycemic agent
ConditionIndicatedRelationship StrengthStudiesTrials
DDPAC
[description not available]		03.1710
Frontotemporal Dementia
The most common clinical form of FRONTOTEMPORAL LOBAR DEGENERATION, this dementia presents with personality and behavioral changes often associated with disinhibition, apathy, and lack of insight.		03.1710
Cancer of Endometrium
[description not available]		02.0510
Endometrial Neoplasms
Tumors or cancer of ENDOMETRIUM, the mucous lining of the UTERUS. These neoplasms can be benign or malignant. Their classification and grading are based on the various cell types and the percent of undifferentiated cells.		02.0510
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		02.0510
Anterior Horn Cell Disease
[description not available]		02.0510
Motor Neuron Disease
Diseases characterized by a selective degeneration of the motor neurons of the spinal cord, brainstem, or motor cortex. Clinical subtypes are distinguished by the major site of degeneration. In AMYOTROPHIC LATERAL SCLEROSIS there is involvement of upper, lower, and brainstem motor neurons. In progressive muscular atrophy and related syndromes (see MUSCULAR ATROPHY, SPINAL) the motor neurons in the spinal cord are primarily affected. With progressive bulbar palsy (BULBAR PALSY, PROGRESSIVE), the initial degeneration occurs in the brainstem. In primary lateral sclerosis, the cortical neurons are affected in isolation. (Adams et al., Principles of Neurology, 6th ed, p1089)		02.0510
Diffuse Lymphocytic Lymphoma, Poorly-Differentiated
[description not available]		02.0710
Lymphoma, Mantle-Cell
A form of non-Hodgkin lymphoma having a usually diffuse pattern with both small and medium lymphocytes and small cleaved cells. It accounts for about 5% of adult non-Hodgkin lymphomas in the United States and Europe. The majority of mantle-cell lymphomas are associated with a t(11;14) translocation resulting in overexpression of the CYCLIN D1 gene (GENES, BCL-1).		02.0710