DPP-4 (Dipeptidyl Peptidase-4)
Definition
The enzyme that inactivates native GLP-1 and GIP within a couple of minutes of their release by clipping two residues off the N-terminus. Long-acting incretin analogues are engineered to resist it, which is what turns a minutes-long hormone into a weekly one.
Terms used in this definition
Other entries this definition refers to.
What this means for research sourcing
Mechanistic terms like this describe how research compounds behave in vitro. See the mechanism overviews for compounds Volta stocks.
Related Terms in Pharmacology
Receptor Agonist
A molecule that binds a receptor and switches it on, producing the kind of response the endogenous signal produces. Most peptide drugs are agonists at a receptor their parent hormone already occupies.
Receptor Antagonist
A molecule that occupies a receptor without activating it, so the natural ligand cannot bind. The effect is to suppress a pathway rather than drive it.
Partial Agonist
An agonist that cannot produce the full response however much of it is present, because it activates the receptor less completely than the natural ligand does. Against a full agonist it can behave as a brake.
Dual Agonist
One molecule that activates two receptors. Tirzepatide is a GLP-1 and GIP agonist; survodutide combines GLP-1 with glucagon-receptor activity. The pairing is a design decision about which pathways to engage at once.
Triple Agonist
One molecule that activates three receptors. Retatrutide acts at the GLP-1, GIP and glucagon receptors, and it is the compound that put the class into clinical development.
Binding Affinity
How tightly a molecule holds its receptor, reported as a dissociation constant where a lower number means tighter binding. Affinity alone does not predict the size of a response: that also depends on how well the bound molecule activates the receptor.
EC50
The concentration producing half of a compound's maximum effect in a given assay. It is a potency measure and is only comparable between compounds tested in the same system, which is why cross-paper EC50 comparisons mislead so often.
Potency
How little of a compound is needed to produce a given effect. A more potent molecule works at a lower concentration, which says nothing about whether its maximum achievable effect is larger.