【摘 要】
：
Many peptide ligands adopt a reverse turn secondary structure at the residues that form critical binding interactions with G-protein coupled receptors (GPCR
【机 构】
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Mimetica Pty Ltd Australia
【出 处】
：
中国上海第七届国际新药发明科技年会
论文部分内容阅读
Many peptide ligands adopt a reverse turn secondary structure at the residues that form critical binding interactions with G-protein coupled receptors (GPCRs).Mimetica has developed a series of drug-like non-peptide scaffolds that mimic the shape of a reverse turn,and which can be readily synthesized with a high degree of diversity and stereocontrol.We have employed these scaffolds to mimic α-melanocyte stimulating hormone (α-MSH),producing compounds active at the melanocortin family of receptors.Good selectivity for the melanocortin-5 receptor (MC5R),which controls the production of sebum and is therefore a novel acne therapeutic target,has been achieved.The development of this MC5R antagonist lead series and its optimization for drug-like properties will be described.
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