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)
| Member | Definition | Class |
|---|---|---|
| aplysiatoxin | The 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 |
| benoxaprofen | A 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 It was used as a non-steroidal anti-inflammatory drug until 1982 when it was withdrawn from the market due to adverse side-effects including liver necrosis, photosensitivity, and carcinogenicity in animals.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 1 | A 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| bryostatin 2 | A member of the class of bryostatins that is bryostatin 1 in which the acetoxy group has been replaced by a hydroxy group. | bryostatin 2 |
| debromoaplysiatoxin | A 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-46 | A 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 |
| flunoxaprofen | A 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 acetate | A 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)
| Timeframe | Studies, Drugs with This Role(%) | All Drugs % |
|---|---|---|
| pre-1990 | 7,792 (25.36) | 18.7374 |
| 1990's | 14,235 (46.33) | 18.2507 |
| 2000's | 6,098 (19.85) | 29.6817 |
| 2010's | 2,331 (7.59) | 24.3611 |
| 2020's | 269 (0.88) | 2.80 |
Study Types
| Publication Type | Studies, Drugs with this Role (%) | All Drugs (%) |
|---|---|---|
| Trials | 108 (0.34%) | 5.53% |
| Reviews | 368 (1.17%) | 6.00% |
| Case Studies | 109 (0.35%) | 4.05% |
| Observational | 4 (0.01%) | 0.25% |
| Other | 30,969 (98.13%) | 84.16% |
Protein Targets (22)
Potency Measurements
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASE | Homo sapiens (human) | Potency | 0.8913 | 1 | 1 |
| Chain A, TYROSYL-DNA PHOSPHODIESTERASE | Homo sapiens (human) | Potency | 63.0957 | 1 | 1 |
| DNA polymerase kappa isoform 1 | Homo sapiens (human) | Potency | 39.8107 | 1 | 1 |
| heat shock 70kDa protein 5 (glucose-regulated protein, 78kDa) | Homo sapiens (human) | Potency | 10.0000 | 1 | 1 |
| Microtubule-associated protein tau | Homo sapiens (human) | Potency | 19.9526 | 1 | 1 |
| nuclear receptor ROR-gamma isoform 1 | Mus musculus (house mouse) | Potency | 10.0000 | 1 | 1 |
Inhibition Measurements
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Beta-1 adrenergic receptor | Rattus norvegicus (Norway rat) | Ki | 0.0018 | 1 | 1 |
| Bile salt export pump | Homo sapiens (human) | IC50 | 139.3500 | 2 | 2 |
| Bile salt export pump | Rattus norvegicus (Norway rat) | IC50 | 99.1000 | 1 | 1 |
| Protein kinase C alpha type | Homo sapiens (human) | Ki | 0.0073 | 4 | 4 |
| Protein kinase C beta type | Homo sapiens (human) | Ki | 0.0018 | 1 | 1 |
| Protein kinase C delta type | Homo sapiens (human) | Ki | 0.0008 | 3 | 3 |
| Protein kinase C epsilon type | Homo sapiens (human) | Ki | 0.0004 | 1 | 1 |
| Protein kinase C gamma type | Homo sapiens (human) | Ki | 0.0049 | 1 | 1 |
Activation Measurements
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Luciferin 4-monooxygenase | Photinus pyralis (common eastern firefly) | EC50 | 0.0100 | 1 | 1 |
| Protein kinase C alpha type | Homo sapiens (human) | EC50 | 850.0048 | 2 | 2 |
| Protein kinase C beta type | Homo sapiens (human) | EC50 | 0.0095 | 1 | 1 |
| Protein kinase C delta type | Homo sapiens (human) | EC50 | 1.8232 | 3 | 3 |
| Protein kinase C epsilon type | Homo sapiens (human) | EC50 | 2.7848 | 2 | 2 |
| Protein kinase C eta type | Homo sapiens (human) | EC50 | 0.0095 | 1 | 1 |
| Protein kinase C gamma type | Homo sapiens (human) | EC50 | 0.0095 | 1 | 1 |
| Protein kinase C iota type | Homo sapiens (human) | EC50 | 0.0095 | 1 | 1 |
| Protein kinase C theta type | Homo sapiens (human) | EC50 | 1.5998 | 2 | 2 |
| Protein kinase C zeta type | Homo sapiens (human) | EC50 | 0.0095 | 1 | 1 |
| Ras guanyl-releasing protein 3 | Homo sapiens (human) | EC50 | 0.0820 | 1 | 1 |
| Serine/threonine-protein kinase D1 | Homo sapiens (human) | EC50 | 0.0095 | 1 | 1 |
| Serine/threonine-protein kinase D3 | Homo sapiens (human) | EC50 | 0.0095 | 1 | 1 |