Target intelligence / Profile preview

Proinsulin C-peptide (C-peptide)

Target
C-peptide
Molecular classification
Peptide hormone precursor fragment, Other (not an enzyme, receptor, transporter, ion channel)
01

Overview

Proinsulin C-peptide ("connecting peptide") is a 31-amino-acid polypeptide that connects the A-chain to the B-chain within human proinsulin during its biosynthesis in pancreatic beta cells. Upon proteolytic cleavage by specific convertases within secretory granules, equimolar amounts of mature insulin and free C-peptide are released into circulation. While originally considered biologically inert beyond its role in facilitating proper folding/processing of insulin precursors, recent studies suggest possible regulatory roles affecting vascular health—though these findings have yet to translate into clinical therapies. Clinically, measurement of circulating C-peptide serves primarily as an indicator of endogenous insulin production capacity rather than being targeted by drugs itself.

Other names
Connecting peptideInsulin C-peptideProinsulin connecting peptideHuman c-peptide
02

Mechanism of action

Not applicable as a drug target. When administered experimentally (as recombinant human C-peptide), proposed mechanisms include modulation of microvascular blood flow or cellular signaling pathways in diabetic complications—these remain unproven clinically.

03

Biological functions

Facilitates correct folding and processing of proinsulin into mature insulin by linking A-chain and B-chain during biosynthesisMarker of endogenous insulin secretion; used clinically to assess pancreatic beta cell function in diabetes diagnosis/monitoringPossible bioactive effects on microvascular blood flow and tissue health have been reported but remain under investigation
04

Disease associations

Diabetes mellitus (Type 1 & Type 2): Used diagnostically to distinguish between types of diabetes or causes of hypoglycemia based on endogenous insulin productionDiabetic complications: Investigated for potential therapeutic effects in diabetic kidney disease and neuropathy but with inconclusive results so far
05

Safety considerations

No major safety concerns identified when measured diagnostically; when administered therapeutically in trials, no significant adverse events were reported compared to placebo—but efficacy was also lacking.
06

Interacting drugs

None established. No approved drugs directly target proinsulin C-peptide itself; it has been tested as an investigational agent rather than as a molecular target for other drugs.
07

Biomarkers

C-peptide levels are widely used as biomarkers for assessing pancreatic beta cell function/endogenous insulin secretion in patients with diabetes or suspected hypoglycemia.

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