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.