An EC 3.4.13.* (dipeptidase) inhibitor that interferes with the action of membrane dipeptidase (EC 3.4.13.19).
ChEBI ID: 76926
| Member | Definition | Class |
|---|---|---|
| cilastatin | The thioether resulting from the formal oxidative coupling of the thiol group of L-cysteine with the 7-position of (2Z)-2-({[(1S)-2,2-dimethylcyclopropyl]carbonyl}amino)hept-2-enoic acid. It is an inhibitor of dehydropeptidase I (membrane dipeptidase, 3.4.13.19), an enzyme found in the brush border of renal tubes and responsible for degrading the antibiotic imipenem. Cilastatin is therefore administered (as the sodium salt) with imipenem to prolong the antibacterial effect of the latter by preventing its renal metabolism to inactive and potentially nephrotoxic products. Cilastatin also acts as a leukotriene D4 dipeptidase inhibitor, preventing the metabolism of leukotriene D4 to leukotriene E4. | cilastatin |
| cilastatin sodium | The monosodium salt of cilastatin. It is an inhibitor of dehydropeptidase I (membrane dipeptidase, 3.4.13.19), an enzyme found in the brush border of renal tubes and responsible for degrading the antibiotic imipenem. Cilastatin sodium is therefore administered with imipenem to prolong the antibacterial effect of the latter by preventing its renal metabolism to microbiologically inactive and potentially nephrotoxic products. | cilastatin sodium |
| Timeframe | Studies, Drugs with This Role(%) | All Drugs % |
|---|---|---|
| pre-1990 | 279 (30.23) | 18.7374 |
| 1990's | 325 (35.21) | 18.2507 |
| 2000's | 159 (17.23) | 29.6817 |
| 2010's | 114 (12.35) | 24.3611 |
| 2020's | 46 (4.98) | 2.80 |
| Publication Type | Studies, Drugs with this Role (%) | All Drugs (%) |
|---|---|---|
| Trials | 270 (26.79%) | 5.53% |
| Reviews | 64 (6.35%) | 6.00% |
| Case Studies | 141 (13.99%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 533 (52.88%) | 84.16% |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Cellular tumor antigen p53 | Homo sapiens (human) | Potency | 7.4978 | 1 | 1 |
| Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASE | Homo sapiens (human) | Potency | 75.1930 | 1 | 1 |
| chromobox protein homolog 1 | Homo sapiens (human) | Potency | 100.0000 | 1 | 1 |
| geminin | Homo sapiens (human) | Potency | 16.7185 | 2 | 2 |
| GTP-binding nuclear protein Ran isoform 1 | Homo sapiens (human) | Potency | 6.5131 | 1 | 1 |
| importin subunit beta-1 isoform 1 | Homo sapiens (human) | Potency | 6.5131 | 1 | 1 |
| phosphopantetheinyl transferase | Bacillus subtilis | Potency | 79.4328 | 1 | 1 |
| snurportin-1 | Homo sapiens (human) | Potency | 6.5131 | 1 | 1 |
| thioredoxin glutathione reductase | Schistosoma mansoni | Potency | 0.7943 | 1 | 1 |
| thioredoxin reductase | Rattus norvegicus (Norway rat) | Potency | 70.7946 | 1 | 1 |
| transcriptional regulator ERG isoform 3 | Homo sapiens (human) | Potency | 3.1623 | 1 | 1 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Beta-1 adrenergic receptor | Rattus norvegicus (Norway rat) | Ki | 0.1700 | 1 | 3 |
| Beta-2 adrenergic receptor | Rattus norvegicus (Norway rat) | Ki | 0.1700 | 1 | 3 |
| Beta-3 adrenergic receptor | Rattus norvegicus (Norway rat) | Ki | 0.1700 | 1 | 3 |
| Dipeptidase 1 | Sus scrofa (pig) | Ki | 0.1700 | 1 | 3 |
| Solute carrier family 22 member 6 | Homo sapiens (human) | IC50 | 2,550.0000 | 1 | 1 |
| Solute carrier family 22 member 6 | Rattus norvegicus (Norway rat) | IC50 | 2,387.0000 | 1 | 1 |
| Solute carrier family 22 member 6 | Homo sapiens (human) | Ki | 1,470.0000 | 1 | 1 |
| Solute carrier family 22 member 8 | Homo sapiens (human) | IC50 | 249.0000 | 1 | 1 |
| Solute carrier family 22 member 8 | Rattus norvegicus (Norway rat) | IC50 | 742.0000 | 1 | 1 |
| Solute carrier family 22 member 8 | Homo sapiens (human) | Ki | 231.0000 | 1 | 1 |