Drug intelligence / Profile preview

[lys15-octanoate]-esculentin-2cha(1-30)

Development stage
Unknown
Lead developer
Ulster University
Modality
Peptides
Administration
Intraperitoneal
01

Overview

[Lys15-octanoate]-esculentin-2CHa(1-30) is a modified analogue of esculentin-2CHa(1-30), designed to improve plasma enzyme resistance and enhance biological activity. This peptide is derived from the antimicrobial peptide esculentin-2CHa, originally isolated from the skin secretions of the Chiricahua leopard frog (*Lithobates chiricahuensis*). The modification involves the attachment of a fatty acid (l-octanoate) to lysine at position 15 of the truncated esculentin-2CHa(1-30) peptide. This fatty acid acylation confers enhanced plasma stability while preserving insulin-releasing activity[3]. The peptide demonstrates anti-diabetic effects through multiple mechanisms including membrane depolarization, increased intracellular calcium levels, and insulin secretion via a KATP channel-independent pathway[3][6]. It also exhibits antimicrobial properties and has shown efficacy in improving glucose tolerance, insulin sensitivity, reducing body weight, and decreasing fat mass in high-fat diet-fed mice[5]. The acylated analogue specifically showed beneficial effects on LDL cholesterol reduction compared to the parent peptide[5].

Other names
Lys15-octanoate-esculentin-2CHa(1-30)[Lys15-octanoate]-esculentin-2CHa(1-30)
02

Targets

KATP channel (ATP-sensitive potassium channel)PLC (Phospholipase C family)PKC (Protein kinase C family)CaV (Voltage-gated calcium channel protein complex)

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