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Target intelligence / Profile preview
Renal dehydropeptidase-1 (DPEP1)
- Target
- DPEP1
- Molecular classification
- Enzyme, Metalloenzyme, Hydrolase
01
Overview
Renal dehydropeptidase-1 (DPEP1) is a membrane-bound glycoprotein enzyme primarily expressed in the kidney. It hydrolyzes dipeptides and certain β-lactam antibiotics, notably imipenem. DPEP1 is anchored to the brush border of renal tubular epithelial cells via a glycosylphosphatidylinositol (GPI) anchor. It contains binuclear zinc ions at its active site and exists as a disulfide-linked homodimer. Clinically, cilastatin is co-administered with imipenem to inhibit DPEP1, preventing imipenem degradation and prolonging its antibiotic efficacy. DPEP1 may also be implicated in cancer progression and inflammatory responses.
- Other names
- Dipeptidase 1
02
Mechanism of action
Cilastatin inhibits renal dehydropeptidase-I activity, preventing the degradation of imipenem and increasing its bioavailability and efficacy.
03
Biological functions
Hydrolysis of dipeptidesβ-lactam antibiotic metabolismRegulation of peptide metabolismModulation of inflammatory responsesCell proliferation regulationTumor progression regulation
04
Disease associations
CancerInflammationAcute respiratory distress syndrome (ARDS)Multiple organ dysfunction syndrome (MODS)
05
Safety considerations
The primary safety concern revolves around the potential for reduced efficacy of carbapenem antibiotics like imipenem if DPEP1 is not adequately inhibited by cilastatin.
06
Interacting drugs
Imipenem
1 more in the full profile.
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