Page last updated: 2024-08-05 15:34:45

protein kinase C agonist

An agonist that selectively binds to and activates a protein kinase C receptor

ChEBI ID: 64018

Members (8)

MemberDefinitionClass
aplysiatoxinThe parent member of the class of aplysiatoxins. It is a cyanotoxin produced by several species of freshwater and marine cyanobacteria, as well as algae and molluscs.aplysiatoxin
benoxaprofenA monocarboxylic acid that is propionic acid substituted at position 2 by a 2-(4-chlorophenyl)-1,3-benzoxazol-5-yl group. It was used as a non-steroidal anti-inflammatory drug until 1982 when it was withdrawn from the market due to adverse side-effects including liver necrosis, photosensitivity, and carcinogenicity in animals.benoxaprofen
bryostatin 1A member of the class of bryostatins that is (17E)-2-oxooxacyclohexacos-17-ene which is substituted by hydroxy groups at positions 4, 10, and 20; an acetoxy group at position 8; methyl groups at positions 9, 9, 18, and 19; 2-methoxy-2-oxoethylidene groups at positions 14 and 24; an (E,E)-octa-2,4-dienoyloxy group at position 21; and with oxygen bridges linking positions 6 to 10, 12 to 16, and 20 to 24. It is one of the most abundant member of the class of bryostatins.bryostatin 1
bryostatin 2A member of the class of bryostatins that is bryostatin 1 in which the acetoxy group has been replaced by a hydroxy group.bryostatin 2
debromoaplysiatoxinA member of the class of aplysiatoxins that has the structure of the parent aplysiatoxin, but is lacking the bromo substituent on the benzene ring at the position para to the phenolic hydroxy group. It is a cyanotoxin produced by several species of freshwater and marine cyanobacteria, as well as algae and molluscs.debromoaplysiatoxin
ebc-46A diterpenoid natural product isolated from the kernels of the Australian blushwood tree (Fontainea picrosperma). It is approved as a veterinary pharmaceutical for the treatment of non-metastatic and non-resectable canine mast cell tumours.tigilanol tiglate
flunoxaprofenA monocarboxylic acid that is propionic acid substituted at position 2 by a 2-(4-chlorophenyl)-1,3-benzoxazol-5-yl group (the S-enantiomer). Although it was shown to be effective in treatment of rheumatoid arthritis and osteoarthritis, the clinical use of flunoxaprofen was discontinued due to possible hepatotoxic side-effects.flunoxaprofen
tetradecanoylphorbol acetateA phorbol ester that is phorbol in which the hydroxy groups at the cyclopropane ring juction (position 13) and the adjacent carbon (position 12) have been converted into the corresponding acetate and myristate esters. It is a major active constituent of the seed oil of Croton tiglium. It has been used as a tumour promoting agent for skin carcinogenesis in rodents and is associated with increased cell proliferation of malignant cells. However its function is controversial since a decrease in cell proliferation has also been observed in several cancer cell types.phorbol 13-acetate 12-myristate

Research

Studies (30,725)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-19907,792 (25.36)18.7374
1990's14,235 (46.33)18.2507
2000's6,098 (19.85)29.6817
2010's2,331 (7.59)24.3611
2020's269 (0.88)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials108 (0.34%)5.53%
Reviews368 (1.17%)6.00%
Case Studies109 (0.35%)4.05%
Observational4 (0.01%)0.25%
Other30,969 (98.13%)84.16%

Protein Targets (22)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency0.891311
Chain A, TYROSYL-DNA PHOSPHODIESTERASEHomo sapiens (human)Potency63.095711
DNA polymerase kappa isoform 1Homo sapiens (human)Potency39.810711
heat shock 70kDa protein 5 (glucose-regulated protein, 78kDa)Homo sapiens (human)Potency10.000011
Microtubule-associated protein tauHomo sapiens (human)Potency19.952611
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency10.000011

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Beta-1 adrenergic receptorRattus norvegicus (Norway rat)Ki0.001811
Bile salt export pumpHomo sapiens (human)IC50139.350022
Bile salt export pumpRattus norvegicus (Norway rat)IC5099.100011
Protein kinase C alpha typeHomo sapiens (human)Ki0.007344
Protein kinase C beta typeHomo sapiens (human)Ki0.001811
Protein kinase C delta typeHomo sapiens (human)Ki0.000833
Protein kinase C epsilon typeHomo sapiens (human)Ki0.000411
Protein kinase C gamma typeHomo sapiens (human)Ki0.004911

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Luciferin 4-monooxygenasePhotinus pyralis (common eastern firefly)EC500.010011
Protein kinase C alpha typeHomo sapiens (human)EC50850.004822
Protein kinase C beta typeHomo sapiens (human)EC500.009511
Protein kinase C delta typeHomo sapiens (human)EC501.823233
Protein kinase C epsilon typeHomo sapiens (human)EC502.784822
Protein kinase C eta typeHomo sapiens (human)EC500.009511
Protein kinase C gamma typeHomo sapiens (human)EC500.009511
Protein kinase C iota typeHomo sapiens (human)EC500.009511
Protein kinase C theta typeHomo sapiens (human)EC501.599822
Protein kinase C zeta typeHomo sapiens (human)EC500.009511
Ras guanyl-releasing protein 3Homo sapiens (human)EC500.082011
Serine/threonine-protein kinase D1Homo sapiens (human)EC500.009511
Serine/threonine-protein kinase D3Homo sapiens (human)EC500.009511