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Last updated January 31, 2026
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Stapled peptide macrocyclization chemistry: MerckRecent Research Landscape

Rapid proteolytic degradation of linear peptides limits therapeutic half-life and receptor binding affinity. Hydrocarbon stapling constrains the alpha-helical conformation to enhance metabolic stability and dual-agonist potency.

What technical problems is Merck addressing in Stapled peptide macrocyclization chemistry?

Poor cellular uptake efficiency

(7)evidences

Standard insulin therapy lacks autonomous regulation based on real-time blood sugar levels. Solving this prevents life-threatening hypoglycemic episodes and chronic hyperglycemic damage.

Peptide metabolic instability

(1)evidences

Rapid proteolytic degradation and poor pharmacokinetic profiles of native peptide hormones. Improving structural integrity extends therapeutic half-life and potency.

Inadequate glycemic control

(1)evidences

Rapid enzymatic degradation and short half-life of linear peptides in systemic circulation. Enhancing proteolytic resistance enables sustained therapeutic efficacy for chronic conditions.