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Identification of Subtype Selective SST5 Receptor Agonist Peptide HTL0030310 using Structure-Based Drug Design

By Miles Congreve | Mar 29, 2022

Miles Congreve, CSO at Sosei Heptares presented a poster at the American Chemical Society (ACS) Spring 2022 meeting, describing the SBDD based identification of HTL0030310, a novel selective SST5 agonist. 

 

Abstract

Somatostatin is a peptide hormone that plays a physiological role in inhibiting growth hormone (GH) release from the pituitary gland and in controlling glucose homeostasis by inhibiting the release of glucagon and insulin from the pancreas. We set out to design a subtype selective SST5 agonist to explore the hypothesis that activation of SST5 would lead to a hyperglycaemic profile without effects on GH secretion. Such an agent in clinical practice might be suitable for treatment of hypoglycaemic disorders, such as congenital hyperinsulinism (CHI) and post-bariatric surgery hypoglycaemia (PBSH).

 

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